TECHNICAL FIELD
[001] The subject matter described herein in general relates to the field of cosmetic and health care products, and in particular to the field of delivery system for increasing bio-availability.
BACKGROUND OF INVENTION
[002] Herbal formulations have been explored for ages for medicinal purposes, since they provide distinct advantages, i) such formulations typically have increased bio-compatibility, and ii) also such formulations have minimum side-effects. However, many important bio-active molecules have very poor aqueous-solubility. An example, would be chrysin (5',7-dihydroxyflavone), a naturally-occurring flavone, present in several plants.
[003] Various recent reports including in-vitro and in-vivo studies confirms that chrysin (CH) has many health benefits including anti-inflammatory, anti-ageing, anti-oxidant, anti-diabetic, anti-allergic, anti-bacterial and anti-cancer activities (Lee. B. K. et al, Int. J. Mol. Sci. 2017, 18, 1424; Eman M. Mantawy et al., Scientific Reports. 2017, 7, 4795). For a desired effect biological benefit, actives should hold a stable structure, low molecular weight and the ability to readily solubilize and pass through cell membrane. But, unfortunately, CH has poor solubility in aqueous solution, that results in low absorption, low physicochemical stability, rapid intestinal and hepatic metabolism, and low cellular bioavailability (Farideh Mohammadian et al, Asian Pac J Cancer Prev, 2015 16 (18), 8259-8263). Therefore, it is essential to improve the solubility of CH in order to increase its utilization in various fields including health, food and personal care industry. [004] Till today, various methods have been reported to enhance the solubility and dissolution rate of many hydrophobic actives including, physical and chemical modifications, particle size reduction, crystal engineering, inclusion complex, use of surfactant, and so forth (Savjani K.T. et al. ISRN Pharm. 2012; 2012: 195727). Above all, micellar encapsulation method seems to be one of the most promising approach that permits sustained, controlled release, and higher loading capacity for poor water-soluble actives with enhanced bioavailability and reduced degradation.

Encapsulation in polymeric matrix is a convenient method for ensuring increased bio-activity. EP128664A2 reveals novel polymeric micelles which are pH and/or temperature sensitive for increasing potency of therapeutic agents. EP20151998A1 reveals polymeric micellar clusters formed from amphiphillic carbohydrate polymers and their uses in formulating drugs.
SUMMARY OF THE INVENTION
[005] In an aspect of the present invention, there is provided a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5.
[006] In another aspect of the present invention, there is provided a formulation comprising: i) the polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer; and ii) at least one excipient selected from the group consisting of diluent, chelating agent, humectant, moisturizer, thickening agent, emollient, emulsion stabilizer, emulsifying agent, photo stabilizer, neutralizer, preservative, feel enhancer, perfume, and combinations thereof, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5.
[007] In another aspect of the present invention, there is provided a process for preparing a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, said process comprising the steps of: a) obtaining at least one active; b) obtaining at least one polymer; c) obtaining at least one drug penetration enhancer; and d) contacting the at least one active, the at least one polymer and the at least one drug penetration enhancer to obtain the polymeric micellar composition, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5.

[008] These and other features, aspects, and advantages of the present subject matter will be better understood with reference to the following description and appended claims. This summary is provided to introduce a selection of concepts in a simplified form. This summary is not intended to identify key features or essential features of the claimed subject matter, nor is it intended to be used to limit the scope of the claimed subject matter.
BRIEF DESCRIPTION OF THE DRAWINGS
[009] The detailed description is described with reference to the accompanying
figures. The same numbers are used throughout the drawings to reference like
features and components.
[0010] Figure 1A and 1B illustrates confocal microscopic images of the polymeric
micellar composition, in accordance with an implementation of the present subject
matter.
[0011] Figure 2 illustrates stability of polymeric micellar composition, in
accordance with an implementation of the present subject matter.
[0012] Figure 3 illustrates cellular uptake of polymeric micellar composition in
Caco-2 cells, in accordance with an implementation of the present subject matter.
[0013] Figure 4 illustrates quantification of fluorescence intensity obtained through
confocal laser scanning microscopy, in accordance with an implementation of the
present subject matter.
DETAILED DESCRIPTION OF THE INVENTION
[0014] Those skilled in the art will be aware that the present disclosure is subject to
variations and modifications other than those specifically described. It is to be
understood that the present disclosure includes all such variations and
modifications. The disclosure also includes all such steps, features, compositions,
and compounds referred to or indicated in this specification, individually or
collectively, and any and all combinations of any or more of such steps or features.
Definitions
[0015] For convenience, before further description of the present disclosure,
certain terms employed in the specification, and examples are delineated here.
These definitions should be read in the light of the remainder of the disclosure and

understood as by a person of skill in the art. The terms used herein have the
meanings recognized and known to those of skill in the art, however, for
convenience and completeness, particular terms and their meanings are set forth
below.
[0016] The articles “a”, “an” and “the” are used to refer to one or to more than one
(i.e., to at least one) of the grammatical object of the article.
[0017] The terms “comprise” and “comprising” are used in the inclusive, open
sense, meaning that additional elements may be included. It is not intended to be
construed as “consists of only”.
[0018] Throughout this specification, unless the context requires otherwise the
word “comprise”, and variations such as “comprises” and “comprising”, will be
understood to imply the inclusion of a stated element or step or group of element or
steps but not the exclusion of any other element or step or group of element or
steps.
[0019] The term “including” is used to mean “including but not limited to”.
“Including” and “including but not limited to” are used interchangeably.
[0020] Ratios, concentrations, amounts, and other numerical data may be presented
herein in a range format. It is to be understood that such range format is used
merely for convenience and brevity and should be interpreted flexibly to include
not only the numerical values explicitly recited as the limits of the range, but also
to include all the individual numerical values or sub-ranges encompassed within
that range as if each numerical value and sub-range is explicitly recited. For
example, a temperature range of about 30-35 ℃ should be interpreted to include not
only the explicitly recited limits of about 22 ℃ to about 28 ℃, but also to include
sub-ranges, such as 32-35 ℃, 30-32 ℃, and so forth, as well as individual amounts,
including fractional amounts, within the specified ranges, such as 32.2 ℃, and 32.5
℃, for example.
[0021] The term “at least one” is used to mean one or more and thus includes
individual components as well as mixtures/combinations.
[0022] Unless defined otherwise, all technical and scientific terms used herein have
the same meaning as commonly understood by one of ordinary skill in the art to

which this disclosure belongs. Although any methods and materials similar or
equivalent to those described herein can be used in the practice or testing of the
disclosure, the preferred methods, and materials are now described. All
publications mentioned herein are incorporated herein by reference.
[0023] The present disclosure is not to be limited in scope by the specific
embodiments described herein, which are intended for the purposes of
exemplification only. Functionally-equivalent products, compositions, and methods
are clearly within the scope of the disclosure, as described herein.
[0024] As mentioned previously, various actives such as chrysin suffer from poor
bio-availability. The present disclosure attempts to solve the said problem by using
a making a polymeric micellar composition which encapsulates chrysin and allows
effective delivery of said active.
[0025] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) at least one active; and b) at least one
polymer; and c) at least one drug penetration enhancer, wherein the at least one
active to the at least one polymer to the at least one drug penetration enhancer
weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5. In another embodiment of the
present disclosure, the at least one active to the at least one polymer to the at least
one drug penetration enhancer weight ratio is in a range of 1:2.2:2.5 to 1:25:2.5. In
yet another embodiment of the present disclosure, the at least one active to the at
least one polymer to the at least one drug penetration enhancer weight ratio is in a
range of 1:2.0:2.5 to 1:22:2.5.
[0026] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition as described herein, wherein the at least one active is a
flavone.
[0027] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition as described herein, wherein the at least one active is a
flavone is selected from the group consisting of chrysin (5',7-dihydroxyflavone),
4',7-dihydroxyflavone, 4'-dimethylamino-7,8-dihydroxyflavone, 6-hydroxyflavone,
7,8,3'-trihydroxyflavone, 7,8-dihydroxyflavone, acacetin, alnetin, amentoflavone,
ansoxetine, apigenin, apigenin trimethyl ether, arcapillin, baicalein-7-methylether,

baicalein, casticin, catechins, chrysin dimethylether, chrysoeriol, delphinidin, diosmetin, epicatechin, epigallacatechin gallate, eucalyptin, eupatorin, eupatorin-5-methyl ether, fisetin, gardenin, enkwanin, hesperetin, hinokiflavone, hispidulin, hypolaetin, isoscutellarein, kaempferol, luteolin, luteolin tetramethyl ether, malvidin, morin, naringin, norartocarpetin, norwogonin, oochnaflavone, pectolinarigenin, pectolinarin, peonidin, petunidin, prato, primuletin, quercetin, sciadopitysin, scutellarein, scutellarein tetramethyl ether, sinensetin, tangeritin, tricetin, velutin, veronicastroside, wogonin, and combinations thereof. In another embodiment of the present disclosure, the at least one active is chrysin. [0028] In an embodiment of the present disclosure, there is provided a polymeric micellar composition as described herein, wherein the at least one polymer is a copolymer of ethylene oxide and propylene oxide. The said polymer may be defined as a poloxamer comprising a tri-block copolymer of two hydrophilic chains of ethylene oxide chains (PEO) that is sandwiched between one hydrophobic propylene oxide chain (PPO). The varying length of polymer blocks give rise to different polymers identified as 124, 188, 237, and 338. The at least one polymer may be selected from these and other known poloxamers.
[0029] In an embodiment of the present disclosure, there is provided a polymeric micellar composition as described herein, wherein the at least one drug penetration enhancer is selected from the group consisting of sodium deoxycholate, acyl carnites, acyl choline, caprylic acid, dioctyl sodium sulfosuccinate, lauric acids, nonylphenoxypolyoxetyylenes, oleic acid, polysorbitate, sodium caprate, sodium caprylate, sodium dihydrofusidate, sodium dodecylsulphate, sodium glycholate, sodium glycodihdro fusidate, sodium glycolate, sodium lauryl sulphate, sodium taurocholate, tween80, and combinations thereof. In another embodiment of the present disclosure, the at least one drug penetration enhancer is sodium deoxycholate.
[0030] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer

weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5 and the at least one active is
chrysin.
[0031] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) at least one active; and b) at least one
polymer; and c) at least one drug penetration enhancer, wherein the at least one
active to the at least one polymer to the at least one drug penetration enhancer
weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5 and the at least one polymer is a
copolymer of ethylene oxide and propylene oxide.
[0032] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) at least one active; and b) at least one
polymer; and c) at least one drug penetration enhancer, wherein the at least one
active to the at least one polymer to the at least one drug penetration enhancer
weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5 and the at least one drug
penetration enhancer is sodium deoxycholate.
[0033] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide
and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the
copolymer of ethylene oxide and propylene oxide to sodium deoxycholate weight
ratio is in a range of 1:2.0:2.5 to 1:25:2.5.
[0034] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition as described herein, wherein the at least one active to the at
least one polymer to the at least one drug penetration enhancer weight ratio is in
range of 1:2.5:2.5.
[0035] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) at least one active; and b) at least one
polymer; and c) at least one drug penetration enhancer, wherein the at least one
active to the at least one polymer to the at least one drug penetration enhancer
weight ratio is 1:2.5:2.5.
[0036] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide
and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the

copolymer of ethylene oxide and propylene oxide to sodium deoxycholate weight
ratio is 1:2.5:2.5.
[0037] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition as described herein, wherein the at least one active to the at
least one polymer to the at least one drug penetration enhancer is 1:5:2.5.
[0038] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) at least one active; and b) at least one
polymer; and c) at least one drug penetration enhancer, wherein the at least one
active to the at least one polymer to the at least one drug penetration enhancer is
1:5:2.5.
[0039] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide
and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the
copolymer of ethylene oxide and propylene oxide to sodium deoxycholate weight
ratio is 1:5:2.5.
[0040] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition as described herein, wherein the least one active to the at
least one polymer to the at least one drug penetration enhancer is 1:10:2.5.
[0041] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) at least one active; and b) at least one
polymer; and c) at least one drug penetration enhancer, wherein the least one active
to the at least one polymer to the at least one drug penetration enhancer is 1:10:2.5.
[0042] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide
and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the
copolymer of ethylene oxide and propylene oxide to sodium deoxycholate weight
ratio is 1:10:2.5.
[0043] In an embodiment of the present disclosure, there is provided a polymeric
micellar composition as described herein, wherein the least one active to the at
least one polymer to the at least one drug penetration enhancer is 1:20:2.5.

[0044] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, wherein the least one active to the at least one polymer to the at least one drug penetration enhancer is 1:20:2.5. [0045] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the copolymer of ethylene oxide and propylene oxide to sodium deoxycholate weight ratio is 1:20:2.5.
[0046] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active having a weight percentage in a range of 0.01- 80 % with respect to the composition; and b) at least one polymer having weight percentage in a range of 1 - 90 % with respect to the composition; and c) at least one drug penetration enhancer having weight percentage in a range of 1 - 20 % with respect to the composition, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5. In another embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active having weight percentage in a range of 0.1- 80 % with respect to the composition; and b) at least one polymer having weight percentage in a range of 5 - 90 % with respect to the composition; and c) at least one drug penetration enhancer having weight percentage in a range of 2 - 20 % with respect to the composition. In yet another embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active having weight percentage in a range of 10 - 70 % with respect to the composition; and b) at least one polymer having weight percentage in a range of 15 - 80 % with respect to the composition; and c) at least one drug penetration enhancer having weight percentage in a range of 5 - 18 % with respect to the composition.
[0047] In an embodiment of the present disclosure, there is provided a polymeric micellar composition as described herein, wherein the composition has an

encapsulation efficiency in a range of 15 – 75 %. In another embodiment of the present disclosure, the composition has an encapsulation efficiency in a range of 18 – 75 %. In yet another embodiment of the present disclosure, the composition has an encapsulation efficiency in a range of 18 – 72 %.
[0048] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in range of 1:2.0:2.5 to 1:25:2.5 and encapsulation efficiency in range of 15 – 75 %.
[0049] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the copolymer of ethylene oxide and propylene oxide to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5 and encapsulation efficiency in range of 15 – 75 %.
[0050] In an embodiment of the present disclosure, there is provided a polymeric micellar composition as described herein, wherein the composition has an active loading in a range of 0.2 to 6.5%. In another embodiment of the present disclosure, the composition has an active loading in a range of 0.22 to 6.4%.
[0051] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5 and the composition has an active loading in range of 0.2 to 6.5%.
[0052] In an embodiment of the present disclosure, there is provided a polymeric micellar composition comprising: a) chrysin; and b) copolymer of ethylene oxide and propylene oxide; and c) sodium deoxycholate, wherein chrysin to the copolymer of ethylene oxide and propylene oxide to the at least one drug

penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5 and the composition has an active loading in a range of 0.2 to 6.5%.
[0053] In an embodiment of the present disclosure, there is provided a formulation comprising: i) the polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer; and ii) at least one excipient selected from the group consisting of diluent, chelating agent, humectant, moisturizer, thickening agent, emollient, emulsion stabilizer, emulsifying agent, photo stabilizer, neutralizer, preservative, feel enhancer, perfume, and combinations thereof, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5.
[0054] In an embodiment of the present disclosure, there is provided a formulation
as described herein, wherein the diluent is water; the chelating agent is a
combination of first chelating agent and second chelating agent, wherein the first
chelating agent and the second cheating agent is independently selected from the
group consisting of disodium ethylenediamminetetraacetic acid (EDTA), citric acid
monohydrate, diethylenetriaminepentaacetic acid (DTPA), deferoxamine,
deferiprone, pyridoxal isonicotinoyl hydrazone, rhodotorulic acid, picolinic acid,
nicotinic acid, neoaspergillic acid, methionine, lactic acid, N,N-ethylene bis[N-
phosphonomethyl]glycine, tetraethylenepentaamine heptaacetic acid (TPHA), tri(2-
aminoethyl)aminehexaacetic acid (TAAHA), triethylenetetraaminehexaacetic acid
(TTHA), oxybis(ethylenenitrilo)tetraacetic acid (BAETA), trans-1,2-
cyclohexaneediaminetetraacetic acid, salicyclic acid, tartaric acid, 2,3-dihydroxybenzoic acid, penicillamine, etidronic acid (1-hydroxyethan-1,1-diyl)bis(phosphonic acid), dimercaptosuccinic acid, dimercapto-propane sulfonate, and dimercaprol, desferrithiocin (DFT), polycarboxylates, hydroxamates, catecholates, hydroxypyridonates, terathalamides and combinations and derivatives thereof; the humectant is selected from the group consisting of glycerine, sorbitol, hyaluronic acid, butylene glycol, sodium PCA, propylene glycol, allantoin, glycerol alpha hydroxy acids, panthenol, carboxylic acid, sodium hyaluronate, sodium ammonium lactate, sodium pyrrolidine, urea, propylene glycol, gelatin,

honey, and combinations thereof; the moisturizer is selected from the group
consisting of propylene glycol, glycerin, sodium hyaluronate, shea butter, and
combinations thereof; the thickening agent is selected from the group consisting of
carbomer, acrylate cross polymer, xanthan gum, methyl cellulose, bee wax, and
combinations thereof; the emollient is selected from the group consisting of
caprylic triglyceride, polypropylene glycol (PPG) steryl ether, isopropyl palmitate,
ethylhexyl palmitate, ethylhexyl stearate, hexyl laurate, dibutyl adipate, coco-
caprylate, coco-caprylate/caprate, dicaprylyl carbonate, oleyl erucate, dicaprylyl
ether, diethylhexylcyclohexane, propylheptyl caprylate, cetearyl isononanoate,
octyldodecanol, hexyldecanol, hexyldecyl stearate, isopropyl myristate,
cocoglycerides, myristyl myristate, cetyl palmitate, and combinations thereof; the
emulsion stabilizer is selected from the group consisting of cetyl alcohol, glyceryl
monostearate, PEG 7 glyceryl cocoate, glycol stearate, lecithin, sodium cocoyl
glycinate, 12-hydroxy stearic acid, ceto stearyl alcohol, lauric acid, myristic acid,
palmitic acid, oleic acid, and combinations thereof; the emulsifying agent is
selected from the group consisting of glyceryl stearate, polyethylene glycol (PEG)
stearate, cetearyl alcohol (and) ceteareth-20, borax with beeswax, BTMS 25%,
carbomer, emulsifying wax-NF, lecithin, PEG-20 stearate, propylene glycol, silky
emulsifying wax, stearyl alcohol NF, polysorbate 80, and combinations thereof; the
photo stabilizer is selected from the group consisting of diethylhexyl syringylidene
malonate, octocrylene, diethylhexyl 2,6-naphthalate, butyloctyl salicylate,
undecylcrylene dimethicone, terephthalylidene dicamphor sulfonic acid, 4-
methylbenzylidene camphor, polysilicone-15, polyester-8, polyester-25, ethylhexyl
methoxycrylene, methylene bis-benzotriazolyl tetramethylbutylphenol, bis-
ethylhexyloxyphenol methoxyphenyl triazine, and combinations thereof; the
neutralizer is selected from the group consisting of triethanolamine, aminomethyl
propanol, arginine, acrylate polymer, and combinations thereof; the preservative is
selected from the group consisting of 2-phenoxyethanol, methyl paraben,
propylparaben, imidiazolidinyl urea, DMDM hydantoin, methyl paraben, propyl
paraben, butyl paraben, ethyl paraben, benzalkonium chloride,
chloromethylisothiazolinone, isothiazolinone, methylisothiazolinone,

methylchloroisothiazolinone, butylated hydroxytoluene (BHT), butylated
hudroxyanisole (BHA), tea tree essential oil, thyme essential oil, grapefruit seed
extract, bitter orange extract, and combinations thereof; the feel enhancer is
selected from the group consisting of cylcopentasiloxane (and) dimethicone cross
polymer, cyclopentasiloxane, dimethiconol, dimethicone cross polymer,
phenyltrimethicone blend, cyclopentasiloxane (and) polysilicone-22,
cyclohexasiloxane (and) dimethiconol, cyclopentasiloxane (and) dimethicone/vinyl
dimethicone crosspolymer, cyclotetrasiloxane (and) cyclopentasiloxane (and)
dimethiconol, cyclopentasiloxane (and) dimethiconol (and) propoxytetramethyl
piperidinyl dimethicone, cyclotetrasiloxane (and) dimethicone, dimethicone (and)
dimethicone/vinyl dimethicone crosspolymer, and combinations thereof; and the
perfume is selected from fragrances well-known in the art. In another embodiment
of the present disclosure, there is provided a formulation as described herein,
wherein the diluent is water; the first chelating agent is disodium
ethylenediamminetetraacetic acid (EDTA) and the second chelating agent is citric
acid monohydrate; the humectant is a combination of glycerine and sorbitol;
moisturizer is propylene glycol; the thickening agent is a combination of carbomer,
acrylate cross polymer, and xanthan gum; emollient is a combination of caprylic
triglyceride, polypropylene glycol (PPG) steryl ether, and isopropyl palmitate; the
emulsion stabilizer is cetyl alcohol; the emulsifying agent is a combination of
glyceryl stearate, polyethylene glycol (PEG) stearate, and cetearyl alcohol (and)
ceteareth-20; the photo stabilizer is diethylhexyl syringylidene malonate;
neutralizer is triethanolamine; the preservative is a combination of 2-
phenoxyethanol, methyl paraben, and propylparaben; the feel enhancer is a
combination of cylcopentasiloxane (and) dimethicone cross polymer,
cyclopentasiloxane, dimethiconol, dimethicone cross polymer, and
phenyltrimethicone blend.
[0055] In an embodiment of the present disclosure, there is provided a process for preparation of a polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer, said process comprising the steps of: a) obtaining the at least one active; b) obtaining

the at least one polymer; c) obtaining the at least one drug penetration enhancer; and d) contacting the at least one active, the at least one polymer and the at least one drug penetration enhancer to obtain the polymeric micellar composition, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5.
[0056] In an embodiment of the present disclosure, there is provided a process for preparation of a formulation comprising: i) the polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer; and ii) at least one excipient selected from the group consisting of diluent, chelating agent, humectant, moisturizer, thickening agent, emollient, emulsion stabilizer, emulsifying agent, photo stabilizer, neutralizer, preservative, feel enhancer, perfume, and combinations thereof, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in range of 1:2.0:2.5 to 1:25:2.5, said process comprising the steps of: a) contacting the first chelating agent, the humectant, the moisturizer, and the thickening agent with the diluent to obtain a first mixture; b) contacting the first mixture with the emollient, the emulsion stabilizer, the emulsifying agent, and the photo stabilizer to obtain a second mixture; c) obtaining the polymeric micellar composition; d) contacting the polymeric micellar composition with the second mixture to obtain a third mixture; e) contacting the third mixture with the neutralizer to obtain a fourth mixture; f) contacting the fourth mixture with the preservative to obtain a fifth mixture; g) contacting the fifth mixture with the second chelating agent to obtain a sixth mixture; h) contacting the sixth mixture with the feel enhancer to obtain a seventh mixture; and i) contacting seventh mixture with perfume to obtain the formulation.
[0057] In an embodiment of the present disclosure, there is provided a process for preparation of a formulation comprising: i) the polymeric micellar composition comprising: a) at least one active; and b) at least one polymer; and c) at least one drug penetration enhancer; and ii) at least one excipient selected from the group consisting of diluent, chelating agent, humectant, moisturizer, thickening agent, emollient, emulsion stabilizer, emulsifying agent, photo stabilizer, neutralizer,

preservative, feel enhancer, perfume, and combinations thereof, wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in range of 1:2.0:2.5 to 1:25:2.5, said process comprising the steps of: a) contacting the first chelating agent, the humectant, the moisturizer, and the thickening agent with the diluent is carried out a temperature in the range of 70 – 90 ℃ for a period in the range of 25 -35 min under a stirring in the range of 600 -800 rpm to obtain the first mixture; b) contacting the first mixture with the emollient, the emulsion stabilizer, the emulsifying agent, and the photo stabilizer is carried out a temperature in the range of 70 – 90 ℃ for a period in the range of 25 -35 min under a stirring in the range of 1500 -1700 rpm to obtain the second mixture; c) obtaining the polymeric micellar composition; d) contacting the polymeric micellar composition with the second mixture is carried out a temperature in the range of 50 -60 ℃ for a period in the range of 25 -35 min under a stirring in the range of 800 -1000 rpm to obtain a third mixture; e) contacting the third mixture with the neutralizer is carried out a temperature in the range of 50 – 60 ℃ for a period in the range of 25 -35 min under a stirring in the range of 800 -1000 rpm to obtain the fourth mixture; f) contacting the fourth mixture with the preservative is carried out a temperature in the range of 35 – 45 ℃ for a period in the range of 25 -35 min under a stirring in the range of 800 -1000 rpm to obtain the fifth mixture; g) contacting the fifth mixture with the second chelating agent is carried out a temperature in the range of 35 – 45
[0058] The prepared solid CH/copolymer/salt matrix were dissolved in Milli Q water to form CH-loaded micelles. Thus, obtained CH polymeric micelles solution was stored at room temperature for further use.
Table 1: Concentration of actives, polymer and drug penetration enhancer (or salt) used for the micellar preparation.



Example 2: Morphology analysis
[0059] Subsequent to synthesis as mentioned in Example 1, the micelles were
suitably investigated for morphological analysis. A Zeiss LSM 710 confocal laser
scanning microscopy (CLSM) was used to investigate the structure and
morphology of the micelles. All confocal fluorescence pictures were obtained using
40x objective oil immersion, laser line 543 nm, Laser power 2%, Grain 915, image
size 1024x1024 (8bit), Zoom 1, pinhole 36 µN, filter MBS 458/543. The software
used for the CLSM imaging was Zeiss 2010.
[0060] The structural morphology of CH loaded polymeric micelles were
examined by CLSM (Table 2 below). Visualization of CH loaded micellar
preparation using confocal laser scanning microscopy 40x magnification is

presented in Figure 1A. Mixed shape (tubes and spherical, Experiment code J of Table 1) is shown in Figure 1B. Tubular structure as observed in Figure 1B is loaded with chrysin. Some preparations showed mixed structures including irregular spherical and small tube-like structures (Figure 1A). On the other hand, some preparations surprisingly showed tubular structure loaded with chrysin (red florescence) which may be formed after reaching the second critical concentration of micellisation and forming a three-dimensional network as shown in Figure 1B. Examination of the literature shows that the concentration of the monomers present in the solutions increases after the CMC and there is a possibility of a second marked aggregation, known as second CMC. These, undoubtedly, reflect change in size, shape, polydispersity and degree of concentration binding to the micelle and also change rate of hydration. Furthermore, the tubular morphology is a surprising finding and though the structure-activity relationship has not been explored, the tubular morphology may also be influential in providing increased stability of the micelles. Furthermore, regularity in structure is preferred as the irregular structure seen in Figure 1A may lead to irregular activity.
Table 2- Morphological analysis of CH (chrysin) loaded micellar preparation using confocal laser scanning microscopy.



Example 3: Stability
[0061] Appropriate amount of CH (chrysin) loaded micelles were dissolved in Milli Q water and stored at room temperature and monitored periodically (once a week; for 2 months) for any changes in appearance. Once the hydrophobic drugs are completely solubilized in the core of the micelle, no precipitation will be observed. Therefore, any change in the appearance of the solution indicates instability.
[0062] The observations have been shown in Figure 2. Appearance of free CH dissolved in DMSO (left; CH), CH micelles prepared by hydration method dissolved in water. 1A CH – Vehicle control, 2B- CH – ratios of active to copolymer to salt 1:2.5:2.5 (K from Table 2), 3C- CH – ratios of active to copolymer to salt 1:5:2.5 (L from Table 2), 4D- CH – ratios of active to copolymer to salt 1:10:2.5 (M from Table 2) and 5E- CH – ratios of active to copolymer to salt 1:20:2.5 (N from Table 2). No change was observed in the appearance of the aqueous solution even after 2 months, which clearly indicates that CH loaded were retained inside the micelles without disruption at room temperature.
Example 4: Determination of drug loading entrapment efficiency
[0063] Drug loading (DL %) and encapsulation efficiency % (EE) of the CH
micelles were estimated using high performance liquid chromatography (HPLC;

Agilent 1200 with PDA Detector). Briefly, an appropriate amount of lyophilized CH micelles was dissolved in required volume of methanol to form a mixture. 20uL of the mixture was chromatographed in to HPLC consisting of an auto sampler using the mobile phase of Methanol(A) and 10mM Phosphoric acid(B) in the ratio 80:20. The flow rate was set at 1 mL/min with Inertsil ODS 3V, 250*4.6mm, 5µm column. The detection wave-length for CH was set at 280 nm, and the elution time for CH was 6.2 min under chromatographic conditions described above.
[0064] Drug loading (DL %) and encapsulation efficiency (EE %) of the CH micelles were calculated using the equation (a) and (b) below
������ - ������� (��%) = ������ ∗ 100 (�)
������������� - ���������� (��%)
= ������������ ������ �������
�ℎ��������� ������ ������� ∗ 100 (�)
[0065] DL% and EE % of the CH-loaded polymeric tube-like micelles were summarized in Table 3 below. CH loaded micelles prepared by thin-film hydration method, showed maximum DL% (6.64 %.) and EE % (70.22%) when compared to other ratios. Table 3- Summary of chrysin loading parameter into polymeric micelles.

Example 5: Cellular uptake of micelles

[0066] Cellular uptake of CH micelles by Caco-2 cells were quantitatively measured using confocal laser scanning microscopy (CLSM). Briefly, Caco-2 cells were plated in 6 well plate (5 × 105 cells per well) containing complete DMEM medium supplemented with 1% non-essential amino acids, 1% of penicillin-streptomycin, 10% FBS and incubated overnight. The medium was changed every alternate day. Cellular uptake studies were carried out with cell monolayers that were 21 days old. CaCo-2 cells were then washed and treated with an equivalent dose (10μg/ml) of free CH and aqueous CH loaded micelles. After 8 hours, the cells were washed thrice with 1X PBS for 5 mins and imaged immediately using Zeiss LSM 710 confocal microscope with 543 nm laser and 40x objective. The cellular fluorescence intensity of CH micelles was also quantitatively measured using Zeiss 2010 software. All the experiments were performed in triplicates. [0067] The cellular uptake of free CH and CH loaded tube-like micelles prepared by thin-film hydration methods were evaluated using CLSM. (Figure 3). Cells were incubated with 10μg/ml of CH-loaded micelles diluted in FBS-free medium in 6-well plates at 37°C for 18 h. Fluorescence of CH was subsequently examined at 543 nm using confocal laser scanning microscopy (CLSM). Red color shows the fluorescence of CH. Panel A: free CH; panel B, C, D, and E shows the cells exposed to CH micelles prepared using various ratios of copolymer to salt (1:2.5:2.5; 1:5:2.5; 1:10:2.5; 1:20:2.5 respectively) by hydration method. The white line represents 20 µm. Panel A shows the CLSM images of Caco-2 cells treated with free CH and panel B, C, D and E shows the cells exposed to CH loaded tube-like micelles prepared using various ratios of copolymer to salt (1:2.5:2.5; 1:5:2.5;1:10:2.5; 1:20:2.5 respectively) by hydration method. Medium without CH micelles are regarded as control group (Not shown). After 8 h, very less/moderate level of fluorescence intensity (red color) can be observed in Caco-2 cells that are exposed with free CH (Panel A). On the other hand, the Caco-2 cells treated with CH polymeric micelles (hydration method; Panel B, C, D, E) shows increased level of fluorescence intensity.
[0068] Furthermore, the mean fluorescence intensity of Caco-2 cells treated with free CH and CH micelles were measured and illustrated in Figure 4. The

fluorescence intensity of CH present inside the Caco-2 cells were analyzed using the CLSM images captured earlier (Figure 3; red). B refers to ratios of active to copolymer to salt 1:2.5:2.5; C- ratios of active to copolymer to salt 1:5:2.5; D-ratios of active to copolymer to salt 1:10:2.5; E- ratios of active to copolymer to salt 1:20:2.5. The mean fluorescence intensity was determined using Zeiss 2010 software. The increased level of mean fluorescence intensity can be observed in cells treated with CH micelles prepared by hydration method using various ratios of copolymer to salt (B-1:2.5:2.5 – 32.63%; C-1:5:2.5-85.62%; D-1:10:2.5-97.12%; E-1:20:2.5- 73.78%) when compared to free CH (data not shown). The increase level of fluorescence inside the cytoplasm confirms that micelles prepared by hydration method facilitate the diffusion of CH across the cellular membrane and increases the cellular bioavailability.
Example 6: Formulation comprising the polymeric micellar composition [0069] The disclosure has been illustrated with a working example, which is intended to explain the working template for the commercial application of the polymeric micellar composition used in the present disclosure (enlisted in Table 4 below). However, this working example does not imply any limitations on the scope of the present disclosure.
Table 4- Ingredients used in formulation comprising the polymeric micellar composition along with the process parameters.

[0070] Process for preparation of the formulation comprises the following steps: a) the first chelating agent, the humectant, the moisturizer, and the thickening agent was contacted with the diluent at a temperature in the range of 70 – 90 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 600 - 800 rpm to obtain the first mixture; b) the first mixture was contacted with the emollient, the emulsion stabilizer, the emulsifying agent, and the photo stabilizer at a temperature in the range of 70 – 90 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 1500 - 1700 rpm to obtain the second mixture; c) the polymeric micellar composition was obtained by the process as mentioned in Example 1; d) the polymeric micellar composition was contacted with the second mixture at a temperature in the range of 50 - 60 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain a third mixture; e) the third mixture was contacted with the neutralizer at a temperature in the range of 50 – 60 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 -1000 rpm to obtain the fourth mixture; f) the fourth mixture was contacted with the preservative at a temperature in the range of 35 – 45 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain the fifth mixture; g) the fifth mixture was contacted with the second chelating agent at a temperature in the range of 35 – 45 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain a sixth mixture; h) the sixth mixture was contacted with the feel enhancer at a temperature in the range of 30 – 40 ℃ for a period in the range of X -Y min under a stirring in the range of 25 - 35 rpm to obtain a seventh mixture; and i) contacting seventh mixture with perfume is carried out a temperature in the range of 28 – 38 ℃ for a period in the range of 25 -35 min under a stirring in the range of 800 - 1000 rpm to obtain the formulation.
Advantages of the present disclosure:
[0071] The present disclosure reveals a polymeric micellar composition capable of increasing bioavailability of aqueous-insoluble natural compounds such as flavone. The enhancement of bio-availability has been revealed using chrysin, a naturally

occurring medicinally-important flavone. The surprising tubular morphology of the micellar composition was found to assist enhanced bio-uptake. The composition was found to be stable over a period of 2 months and was found to allow an encapsulation efficiency of up to 70.22%. The treatment of Caco-2 cells with said micellar composition revealed an enhancement in bio-uptake of the active (chrysin) of up to 97.12% versus the chrysin without any encapsulation. The polymeric micellar composition is capable of being processed easily using known methods in the art and can also be further adapted to commercially useful formulations.

I/We Claim:
1. A polymeric micellar composition comprising:
a) at least one active;
b) at least one polymer; and
c) at least one drug penetration enhancer,
wherein the at least one active to the at least one polymer to the at least one drug penetration enhancer weight ratio is in a range of 1:2.0:2.5 to 1:25:2.5.
2. The polymeric micellar composition as claimed in claim 1, wherein the at least one active is a flavone.
3. The polymeric micellar composition as claimed in claim 2, wherein the flavone is selected from the group consisting of chrysin (5',7-dihydroxyflavone), 4',7-dihydroxyflavone, 4'-dimethylamino-7,8-dihydroxyflavone, 6-hydroxyflavone, 7,8,3'-trihydroxyflavone, 7,8-dihydroxyflavone, acacetin, alnetin, amentoflavone, ansoxetine, apigenin, apigenin trimethyl ether, arcapillin, baicalein-7-methylether, baicalein, casticin, catechins, chrysin dimethylether, chrysoeriol, delphinidin, diosmetin, epicatechin, epigallacatechin gallate, eucalyptin, eupatorin, eupatorin-5-methyl ether, fisetin, gardenin, enkwanin, hesperetin, hinokiflavone, hispidulin, hypolaetin, isoscutellarein, kaempferol, luteolin, luteolin tetramethyl ether, malvidin, morin, naringin, norartocarpetin, norwogonin, oochnaflavone, pectolinarigenin, pectolinarin, peonidin, petunidin, prato, primuletin, quercetin, sciadopitysin, scutellarein, scutellarein tetramethyl ether, sinensetin, tangeritin, tricetin, velutin, veronicastroside, wogonin, and combinations thereof.
4. The polymeric micellar composition as claimed in claim 1, wherein the at least one polymer is a copolymer of ethylene oxide and propylene oxide.
5. The polymeric micellar composition as claimed in claim 1, wherein the at least one drug penetration enhancer is selected from the group consisting of sodium deoxycholate, acyl carnites, acyl choline, caprylic acid, dioctyl

sodium sulfosuccinate, lauric acids, nonylphenoxypolyoxetyylenes, oleic acid, polysorbitate, sodium caprate, sodium caprylate, sodium dihydrofusidate, sodium dodecylsulphate, sodium glycholate, sodium glycodihdro fusidate, sodium glycolate, sodium lauryl sulphate, sodium taurocholate, tween80, and combinations thereof.
6. The polymeric micellar composition as claimed in claim 1, wherein the at
least one active to the at least one polymer to the at least one drug
penetration enhancer weight ratio is in a range of 1:2.5:2.5.
7. The polymeric micellar composition as claimed in claim 1, wherein the at
least one active to the at least one polymer to the at least one drug
penetration enhancer is in a range of 1:5:2.5.
8. The polymeric micellar composition as claimed in claim 1, wherein the least one active to the at least one polymer to the at least one drug penetration enhancer is in a range of 1:10:2.5.
9. The polymeric micellar composition as claimed in claim 1, wherein the least one active to the at least one polymer to the at least one drug penetration enhancer is in a range of 1:20:2.5.
10. The polymeric micellar composition as claimed in any one of the claims 1-9, the composition comprising:

a) at least one active having weight percentage in a range of 0.01- 80 % with respect to the composition;
b) at least one polymer having weight percentage in a range of 1 - 90 % with respect to the composition; and
c) at least one drug penetration enhancer having weight percentage in a range of 1 - 20 % with respect to the composition.

11. The polymeric micellar composition as claimed in any one of the claims 1-10, wherein the composition has an encapsulation efficiency in a range of 15 – 75 %.
12. The polymeric micellar composition as claimed in any one of the claims 1-10, wherein the composition has an active loading in a range of 0.2 to 6.5%.

13. A formulation comprising: (a) the polymeric micellar composition as claimed in any one of the claims 1-12; (b) at least one excipient selected from the group consisting of diluent, chelating agent, humectant, moisturizer, thickening agent, emollient, emulsion stabilizer, emulsifying agent, photo stabilizer, neutralizer, preservative, feel enhancer, perfume, and combinations thereof.
14. The formulation as claimed in claim 13, wherein the diluent is water and combinations thereof; the chelating agent is a combination of a first chelating agent and a second chelating agent, wherein the first chelating agent and the second chelating agent is independently selected from the group consisting of disodium ethylenediamminetetraacetic acid (EDTA), citric acid monohydrate, diethylenetriaminepentaacetic acid (DTPA), deferoxamine, deferiprone, pyridoxal isonicotinoyl hydrazone, rhodotorulic acid, picolinic acid, nicotinic acid, neoaspergillic acid, methionine, lactic acid, N,N-ethylene bis[N-phosphonomethyl]glycine, tetraethylenepentaamine heptaacetic acid (TPHA), tri(2-aminoethyl)aminehexaacetic acid (TAAHA), triethylenetetraaminehexaacetic acid (TTHA), oxybis(ethylenenitrilo)tetraacetic acid (BAETA), trans-1,2-cyclohexaneediaminetetraacetic acid, salicyclic acid, tartaric acid, 2,3-dihydroxybenzoic acid, penicillamine, etidronic acid (1-hydroxyethan-1,1-diyl)bis(phosphonic acid), dimercaptosuccinic acid, dimercapto-propane sulfonate, and dimercaprol, desferrithiocin (DFT), polycarboxylates, hydroxamates, catecholates, hydroxypyridonates, terathalamides, and combinations thereof; the humectant is selected from the group consisting of glycerine, sorbitol, hyaluronic acid, butylene glycol, sodium PCA, propylene glycol, allantoin, glycerol alpha hydroxy acids, panthenol, carboxylic acid, sodium hyaluronate, sodium ammonium lactate, sodium pyrrolidine, urea, propylene glycol, gelatin, honey, and combinations thereof; the moisturizer is selected from the group consisting of propylene glycol, glycerin, sodium hyaluronate, shea butter, and combinations

thereof; the thickening agent is selected from the group consisting of
carbomer, acrylate cross polymer, xanthan gum, methyl cellulose, bee
wax, and combinations thereof; the emollient is selected from the group
consisting of caprylic triglyceride, polypropylene glycol (PPG) steryl
ether, isopropyl palmitate, ethylhexyl palmitate, ethylhexyl stearate, hexyl
laurate, dibutyl adipate, coco-caprylate, coco-caprylate/caprate, dicaprylyl
carbonate, oleyl erucate, dicaprylyl ether, diethylhexylcyclohexane,
propylheptyl caprylate, cetearyl isononanoate, octyldodecanol,
hexyldecanol, hexyldecyl stearate, isopropyl myristate, cocoglycerides,
myristyl myristate, cetyl palmitate, and combinations thereof; the
emulsion stabilizer is selected from the group consisting of cetyl alcohol,
glyceryl monostearate, PEG 7 glyceryl cocoate, glycol stearate, lecithin,
sodium cocoyl glycinate, 12-hydroxy stearic acid, ceto stearyl alcohol,
lauric acid, myristic acid, palmitic acid, oleic acid, and combinations
thereof; the emulsifying agent is selected from the group consisting of
glyceryl stearate, polyethylene glycol (PEG) stearate, cetearyl alcohol
(and) ceteareth-20, borax with beeswax, BTMS 25%, carbomer,
emulsifying wax-NF, lecithin, PEG-20 stearate, propylene glycol, silky
emulsifying wax, stearyl alcohol NF, polysorbate 80, and combinations
thereof; the photo stabilizer is selected from the group consisting of
diethylhexyl syringylidene malonate, octocrylene, diethylhexyl 2,6-
naphthalate, butyloctyl salicylate, undecylcrylene dimethicone,
terephthalylidene dicamphor sulfonic acid, 4-methylbenzylidene camphor,
polysilicone-15, polyester-8, polyester-25, ethylhexyl methoxycrylene,
methylene bis-benzotriazolyl tetramethylbutylphenol, bis-
ethylhexyloxyphenol methoxyphenyl triazine, and combinations thereof;
the neutralizer is selected from the group consisting of triethanolamine,
aminomethyl propanol, arginine, acrylate polymer, and combinations
thereof; the preservative is selected from the group consisting of 2-
phenoxyethanol, methyl paraben, propylparaben, imidiazolidinyl urea,
DMDM hydantoin, methyl paraben, propyl paraben, butyl paraben, ethyl

paraben, benzalkonium chloride, chloromethylisothiazolinone,
isothiazolinone, methylisothiazolinone, methylchloroisothiazolinone,
butylated hydroxytoluene (BHT), butylated hudroxyanisole (BHA), tea
tree essential oil, thyme essential oil, grapefruit seed extract, bitter orange
extract, and combinations thereof; the feel enhancer is selected from the
group consisting of cylcopentasiloxane (and) dimethicone cross polymer,
cyclopentasiloxane, dimethiconol, dimethicone cross polymer,
phenyltrimethicone blend, cyclopentasiloxane (and) polysilicone-22,
cyclohexasiloxane (and) dimethiconol, cyclopentasiloxane (and)
dimethicone/vinyl dimethicone crosspolymer, cyclotetrasiloxane (and)
cyclopentasiloxane (and) dimethiconol, cyclopentasiloxane (and)
dimethiconol (and) propoxytetramethyl piperidinyl dimethicone,
cyclotetrasiloxane (and) dimethicone, dimethicone (and)
dimethicone/vinyl dimethicone crosspolymer, and combinations thereof.
. A process for preparation of the polymeric micellar composition as claimed in any one of the claims 1-12, the process comprising the steps of: a) obtaining at least one active; b) obtaining at least one polymer; c) obtaining at least one drug penetration enhancer; and d) contacting the at least one active, the at least one polymer and the at least one drug penetration enhancer to obtain the polymeric micellar composition.
. A process for preparation of the formulation as claimed in claim 13, the process comprising the steps of: a) contacting the first chelating agent, the humectant, the moisturizer, and the thickening agent with the diluent to obtain a first mixture; b) contacting the first mixture with the emollient, the emulsion stabilizer, the emulsifying agent, and the photo stabilizer to obtain a second mixture; c) obtaining the polymeric micellar composition by the process as claimed in claim 15; d) contacting the polymeric micellar composition with the second mixture to obtain a third mixture; e) contacting the third mixture with the neutralizer to obtain a fourth mixture; f) contacting the fourth mixture with the preservative to obtain a fifth mixture; g) contacting the fifth mixture with the second chelating agent to

obtain a sixth mixture; h) contacting the sixth mixture with the feel enhancer to obtain a seventh mixture; and i) contacting the seventh mixture with the perfume to obtain the formulation. 17. The process as claimed in claim 16, the process comprising the steps of: a) contacting the first chelating agent, the humectant, the moisturizer, and the thickening agent with the diluent is carried out a temperature in the range of 70 – 90 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 600 - 800 rpm to obtain the first mixture; b) contacting the first mixture with the emollient, the emulsion stabilizer, the emulsifying agent, and the photo stabilizer is carried out a temperature in the range of 70 – 90 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 1500 - 1700 rpm to obtain the second mixture; c) obtaining the polymeric micellar composition by the process as claimed in claim 15; d) contacting the polymeric micellar composition with the second mixture is carried out a temperature in the range of 50 - 60 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain a third mixture; e) contacting the third mixture with the neutralizer is carried out a temperature in the range of 50 – 60 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain the fourth mixture; f) contacting the fourth mixture with the preservative is carried out a temperature in the range of 35 – 45 ℃ for a period in the range of 25 -35 min under a stirring in the range of 8000 - 1000 rpm to obtain the fifth mixture; g) contacting the fifth mixture with the second chelating agent is carried out a temperature in the range of 35 – 45 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain a sixth mixture; h) contacting the sixth mixture with the feel enhancer is carried out a temperature in the range of 30 – 40 ℃ for a period in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain a seventh mixture; and i) contacting seventh mixture with perfume is carried out a temperature in the range of 28 – 38 ℃ for a period

in the range of 25 - 35 min under a stirring in the range of 800 - 1000 rpm to obtain the formulation.