Abstract: COMPOSITION FOR SKIN BENEFITS AND METHODS THEREOF The present disclosure discloses a composition comprising: xylan and mandelic acid, wherein xylan and mandelic acid has a combined weight percentage in a range of 0.005%-0.02% with respect to the composition, and xylan to mandelic acid weight ratio is in a range of 1:0.05 to 1:0.3. The composition inhibits breakdown of collagen in the skin. Also, method for preparing the composition is provided.
FIELD OF INVENTION
[001] The present disclosure broadly relates to field of cosmetics and particularly relates to a composition comprising xylan and mandelic acid for skin benefits.
BACKGROUND OF INVENTION
[002] Skin is the largest organ of human body and is made up of multiple types of cells which perform specific functions to maintain the integrity of skin. Three layers namely epidermis, dermis and hypodermis make up the skin. The dermis comprises majorly collagen made by fibroblasts. Collagen is an insoluble protein which is found throughout the body that provides a structural framework to the skin. During the ageing process, skin undergoes a drastic change with respect to the framework leading to a loss in elasticity and structure of the skin. There are typically two types of ageing namely, intrinsic ageing and extrinsic ageing. While the extrinsic ageing is due to the environmental process, the intrinsic ageing is due to three main features: (a) atrophy of dermis due to loss of collagen; (b) degeneration in fiber network; and (c) loss of hydration.
[003] Matrix metalloprotease are zinc-containing endopeptidases which mediate the degradation of the different components of the extracellular matrix (ECM) secretions of the cells. Matrix metalloprotease 1 (MMP1), also known as interstitial collagenase, is the protease involved in the breakdown of collagen, the predominant protein of the ECM. These proteases are secreted by keratinocytes and dermal fibroblasts in response to multiple stimuli such as aging, oxidative stress, UV radiation, and cytokines. Upon the onset of skin aging the formation of fine lines and wrinkles appear on the facial skin and other parts of the body due to fragmented collagen, which are obtained as a result of the up regulated MMP1 levels. The decrease in the density of the collagen protein in the ECM results in the loss of the skin's mechanical properties as a result of which skin loses its firmness and elasticity.
[004] US20070202203A1 discloses a composition containing, in a physiologically acceptable medium, at least: hyaluronic acid and/or one of its salts;
at least one extract of soybean proteins; and at least one compound of formula (I)
as described herein. This composition is useful for preventing and/or decreasing the
signs of skin ageing, in particular the loss of firmness and/or of elasticity of the
skin.
[005] WO2008136676A3 discloses an anti ageing skin care composition, more in
particular a cosmetic anti aging skin care composition. The anti ageing skin care
composition of the invention comprise, in a physiologically acceptable medium, (i)
at least one peptide from Laminin-1 that is able to promote synthesis of Laminin-5;
(ii) at least one peptide capable of at least partially inhibiting neuronal exocytosis;
and (iii) at least one tripeptide producing a rapid and strong stimulation of collagen
synthesis.
[006] Although there are several anti-ageing compositions that exist, but
compositions that target crucial molecular mechanisms are lacking and needs to be
worked upon.
SUMMARY OF THE INVENTION
[007] In an aspect of the present invention, there is provided a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.005% - 0.02% with respect to the composition, and wherein xylan to mandelic acid weight ratio is in a range of 1:0.05 to 1:0.3.
[008] In an aspect of the present invention, there is provided a process for preparing the composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.005% -0.02% with respect to the composition, and wherein xylan to mandelic acid weight ratio is in a range of 1:0.05 to 1:0.3, said process comprising: (i) obtaining xylan; (ii) obtaining mandelic acid; and (iii) contacting xylan and mandelic acid, to obtain the composition.
[009] 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 ACCOMPANYING DRAWINGS
[0010] The following drawings form a part of the present specification and are
included to further illustrate aspects of the present disclosure. The disclosure may be
better understood by reference to the drawings in combination with the detailed
description of the specific embodiments presented herein.
[0011] Figure 1 illustrates cytotoxicity data for different concentrations of xylan, in
accordance with an embodiment of the present disclosure.
[0012] Figure 2 illustrates cytotoxicity data for different concentrations of
mandelic acid, in accordance with an embodiment of the present disclosure.
[0013] Figure 3 illustrates the effect of a combination of 0.01% xylan and 0.001%
mandelic acid on MMP-1 protein production, in accordance with an embodiment of
the present disclosure.
[0014] Figure 4 illustrates the effect of a combination of 0.1% xylan and 0.01%
mandelic acid on MMP-1 protein production, in accordance with an embodiment of
the present disclosure.
[0015] Figure 5 illustrates the effect of a combination of 0.001% xylan and
0.0001% mandelic acid on MMP-1 protein production, in accordance with an
embodiment of the present disclosure.
DETAILED DESCRIPTION OF THE INVENTION
[0016] 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
[0017] 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.
[0018] 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.
[0019] 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".
[0020] 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.
[0021] The term "including" is used to mean "including but not limited to".
"Including" and "including but not limited to" are used interchangeably.
[0022] 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.
[0023] Xylans are a diverse group of polysaccharides formed from xylose residues
linked by (3-(l,4) glycosidic bonds and bearing side chains of 4-O-methyl
glucuronic acid. They are widely found in cell wall of plants and in some algae.
[0024] Mandelic acid is an aromatic a hydroxy acid with the molecular formula
C6H5CH(OH)C02H. It is derived from hydrolysis of an extract of bitter almonds
[0025] An excipient is an inactive substance that serves as the vehicle or medium
for a drug or other active substance. Excipients include colouring agents,
humectants, diluting agent, preservatives, emollients, other known cosmetically
suitable additives, and combinations thereof.
[0026] For the purposes of the present disclosure, the composition of xylan and
mandelic acid which comprises the formulation of the present disclosure is only the
partial solution for skin anti-ageing mechanism.
[0027] To address the problem of skin ageing, an effective solution would be to
intervene the process of ageing at the molecular level. As was discussed in the
background section, it can be inferred that MMP-1 is a crucial enzyme that
degrades collagen present in the skin. There are also previous reports available
(Pittayapruek P et al, 2016. Int. Mol Sci. 17(6); Xia et al, 2013. Aging Cell;
12(4):661-71) that relates to inhibition of MMP-1 synthesis as a solution to
decrease manifestation of skin ageing. The present disclosure aims to contravene
the process of MMP-1 synthesis to provide a solution to the problem of collagen
degradation.
[0028] The present disclosure provides a composition comprising xylan and
mandelic acid and combined weight percentage of xylan and mandelic acid is in a
range of 0.01%-0.012% with respect to the composition. The weight ratio of xylan
to mandelic acid is 1:0.1. The composition is shown to be effective in inhibiting
MMP-1 synthesis in human dermal fibroblast cells. Also provided is a method to
prepare the composition as disclosed herein.
[0029] 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.
[0030] 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. [0031] In an embodiment of the present disclosure, there is provided a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.005% - 0.02% with respect to the composition, and wherein xylan to mandelic acid weight ratio is in a range of 1:0.05 to 1:0.3. In another embodiment of the present disclosure, xylan and mandelic acid has a combined weight percentage is in the range of 0.007% -0.015% with respect to the composition, and xylan to mandelic acid weight ratio is in a range of 1:0.07 to 1:0.2. In yet another embodiment of the present disclosure, xylan to mandelic acid weight ratio is in a range of 1:0.09 to 1:0.15. [0032] In an embodiment of the present disclosure, there is provided a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1. In another embodiment of the present disclosure, xylan and mandelic acid has a combined weight percentage is in the range of 0.01% - 0.011% with respect to the composition.
[0033] In an embodiment of the present disclosure, there is provided a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, and the composition inhibits expression of matrix metalloprotease 1 (MMP1). In another embodiment of the present disclosure, the composition inhibits breakdown of collagen. In yet another embodiment of the present disclosure, the composition is beneficial for retarding skin-ageing.
[0034] In an embodiment of the present disclosure, there is provided a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, and xylan
has a weight percentage of 0.01% with respect to the composition and mandelic acid has a weight percentage of 0.001% with respect to the composition. [0035] In an embodiment of the present disclosure, there is provided a formulation comprising: (i) a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.005% - 0.02% with respect to the composition, and wherein xylan to mandelic acid weight ratio is in a range of 1:0.05 to 1:0.3; and (ii) at least one excipient. [0036] In an embodiment of the present disclosure, there is provided a formulation comprising: (i) a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1; and (ii) at least one excipient.
[0037] In an embodiment of the present disclosure, there is provided a formulation comprising: (i) a composition comprising: (a) xylan having a weight percentage of 0.01% with respect to the composition; and (b) mandelic acid having a weight percentage of 0.001% with respect to the composition, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1; and (ii) at least one excipient.
[0038] In an embodiment of the present disclosure, there is provided a formulation comprising: (i) a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1; and (ii) at least one excipient, and the formulation inhibits breakdown of collagen by inhibiting expression of matrix metalloprotease 1 (MMP1).
[0039] In an embodiment of the present disclosure, there is provided a process for preparing the composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.005% -0.02% with respect to the composition, and wherein xylan to mandelic acid weight ratio is in a range of 1:0.05 to 1:0.3, said process comprising: (i) obtaining xylan;
(ii) obtaining mandelic acid; and (iii) contacting xylan and mandelic acid, to obtain the composition.
[0040] In an embodiment of the present disclosure, there is provided a process for preparing the composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said process comprising: (i) obtaining xylan; (ii) obtaining mandelic acid; and (iii) contacting xylan and mandelic acid, to obtain the composition.
[0041] In an embodiment of the present disclosure, there is provided a process for preparing the composition comprising: (a) xylan having a weight percentage of 0.01% with respect to the composition; and (b) mandelic acid having a weight percentage of 0.001% with respect to the composition, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said process comprising: (i) obtaining xylan; (ii) obtaining mandelic acid; and (iii) contacting xylan and mandelic acid, to obtain the composition. [0042] In an embodiment of the present disclosure, there is provided a process for preparing the formulation comprising: (i) a composition comprising: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1; and (ii) at least one excipient, said process comprising: (1) obtaining xylan; (2) obtaining mandelic acid; (3) obtaining the at least one excipient; and (4) contacting xylan, mandelic acid, and the at least one excipient, to obtain the formulation.
[0043] In an embodiment of the present disclosure, there is provided a process for preparing the formulation comprising: (i) a composition comprising: (a) xylan having a weight percentage of 0.01% with respect to the composition; and (b) mandelic acid having a weight percentage of 0.001% with respect to the composition, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to
mandelic acid weight ratio is 1:0.1; and (ii) at least one excipient, said process comprising: (1) obtaining xylan; (2) obtaining mandelic acid; (3) obtaining the at least one excipient; and (4) contacting xylan, mandelic acid, and the at least one excipient, to obtain the formulation.
[0044] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan; and (ii) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition.
[0045] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan having a weight percentage of 0.01% with respect to the composition; and (ii) mandelic acid having a weight percentage of 0.001% with respect to the composition, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition.
[0046] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan; and (ii) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition, and wherein the solution B is prepared in an organic solvent.
[0047] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan; and (ii)mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -
0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition, and wherein the solution A is prepared in an inorganic solvent.
[0048] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan; and (ii) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition, and wherein the solution A and the solution B is prepared in an organic solvent.
[0049] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan; and (ii) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition, and wherein the solution A and the solution B is prepared in an inorganic solvent.
[0050] In an embodiment of the present disclosure, there is provided a method for preparing a composition comprising: (i) xylan; and (ii) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% -0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; and (c) contacting solution A and solution B to obtain said composition, and wherein the solution A and the solution B is prepared in dimethyl sulfoxide (DMSO).
[0051] In an embodiment of the present disclosure, there is provided a method for preparing a formulation comprising: (i) xylan; and (ii) mandelic acid; and (iii) at
least one excipient, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1, said method comprising: (a) obtaining a solution A of xylan; (b) obtaining a solution B of mandelic acid; (c) obtaining a solution C of the at least one excipient; and (d) contacting solution A, solution B, and solution C to obtain said composition.
[0052] In an embodiment of the present disclosure, there is provided a process to inhibit breakdown of collagen in skin, said process comprising: (a) obtaining the composition comprising: (i) xylan; and (ii) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1; and (b) contacting the composition of step (a) with skin, to inhibit the breakdown of collagen.
[0053] In an embodiment of the present disclosure, there is provided a process to inhibit breakdown of collagen in skin, said process comprising: (a) obtaining the composition comprising: (i) xylan having a weight percentage of 0.01% with respect to the composition; and (ii) mandelic acid having a weight percentage of 0.001% with respect to the composition, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1; and (b) contacting the composition of step (a) with skin, to inhibit the breakdown of collagen.
[0054] In an embodiment of the present disclosure, there is provided a process to inhibit breakdown of collagen in skin, said process comprising: (a) obtaining the formulation as described herein; and (b) contacting the composition of step (a) with skin, to inhibit the breakdown of collagen.
[0055] In an embodiment of the present disclosure, there is provided an anti-wrinkle formulation comprising a composition, wherein the composition comprises: (a) xylan; and (b) mandelic acid, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1.
[0056] In an embodiment of the present disclosure, there is provided an anti-wrinkle formulation comprising a composition, wherein the composition comprises: (a) xylan having a weight percentage of 0.01% with respect to the composition; and (b) mandelic acid having a weight percentage of 0.001% with respect to the composition, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1.
[0057] In an embodiment of the present disclosure, there is provided a composition described herein, wherein said composition inhibits skin aging by inhibiting collagen degrading enzymes. In another embodiment of the present disclosure, said composition inhibits skin aging by inhibiting MMP-1 enzyme production. [0058] In an embodiment of the present disclosure, there is provided a formulation as described herein, wherein said composition can be for topical application. [0059] In an embodiment of the present disclosure, there is provided a formulation as described herein, wherein said composition can be in the form of an aerosol. [0060] In an embodiment of the present disclosure, there is provided a formulation as described herein, wherein said composition can be in the form of a lotion. [0061] In an embodiment of the present disclosure, there is provided a formulation as described herein, wherein said composition can be in form of an oil. [0062] In an embodiment of the present disclosure, there is provided a formulation as described herein, wherein said composition can be in the form of a serum. [0063] Although the subject matter has been described in considerable detail with reference to certain examples and implementations thereof, other implementations are possible.
EXAMPLES
[0064] The disclosure will now be illustrated with working examples, which is intended to illustrate the working of disclosure and not intended to take restrictively to imply any limitations on the scope of the present disclosure. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood to one of ordinary skill in the art to which this
disclosure belongs. Although methods and materials similar or equivalent to those described herein can be used in the practice of the disclosed methods and compositions, the exemplary methods, devices and materials are described herein. It is to be understood that this disclosure is not limited to particular methods, and experimental conditions described, as such methods and conditions may apply. [0065] The working and non-working examples of the composition comprising xylan and mandelic acid will provide support to the weight percentage range and weight ratio as claimed in the present disclosure. Dose response to the individual component of either xylan or mandelic acid will provide exemplary support to the synergistic effect of the composition as described herein.
Material and Methods
[0066] Xylan from Beech wood was procured from SIGMA (CAS NO. 9014-63-5), Mandelic acid was procured from SIGMA (CAS NO. 90-64-2), Pierce BCA protein assay kit from Thermo Fisher Scientific, and Human MMP1 Elisa kit from SIGMA.
Protocol of experiment performed
[0067] Human dermal fibroblasts were seeded in 12- well plates (Costar) in
Fibroblast basal media (LONZA). The culture was incubated in 5% CO2 incubator
and was allowed to reach 100% confluency. Then, the fully confluent fibroblast
cells were treated with actives (xylan or mandelic acid, or combinations) and
incubated in 5% CO2 incubator. Spent medium was harvested after 48 hrs and total
protein was estimated with Pierce BCA protein assay kit.
[0068] MMP1 ELISA was performed as per manufacturer's protocol to estimate
secreted MMP1.
[0069] Cytotoxicity assay: The assay was performed by the following steps:
1. Human dermal fibroblast cells were seeded at 5 x 104 seeding density in 96 well
microliter plates.
2. After 24 hrs, cells were treated with actives at different concentrations in a final volume of 100 ul/well culture medium in a humidified atmosphere (37°C 5% C02) for 24 hrs.
3. After the incubation period, 10 ul/well Premix WST-1 reagent was added and incubated for lhr.
4. The absorbance of the samples was measured in a spectrophotometer at 440nm against the appropriate controls.
Example 1
Cytotoxicity data for xylan and mandelic acid
[0070] The cytotoxicity assay was performed with actives to assess the
concentration which can be regarded as safe for the human fibroblast cells.
[0071] As can be inferred from Figure 1, xylan up to a concentration of 0.1% does
not affect cell viability in a significant manner. Xylan at a concentration of 0.5%
proves to be slightly toxic to the cells with the data from Figure 1 revealing a cell
viability of 75% at this particular concentration.
[0072] In case of mandelic acid, it can be appreciated from Figure 2 that up to a
concentration of 0.01% cell viability is not affected. The cell viability is
significantly affected at the concentrations of 0.05%, 0.1%, and 0.5%.
[0073] Thus, it can be inferred from the present example that xylan up to a
concentration of 0.1% may be regarded as safe and mandelic acid up to a
concentration of 0.01% may be regarded as non-toxic to the fibroblast cells.
Example 2
Working Example of a combination of xylan and mandelic acid
[0074] The present example depicts a working example of a combination of xylan and mandelic acid in a specific weight ratio and specific weight percentage that synergistically inhibits the production of MMP-1 protein.
[0075] Figure 3 depicts a percentage expression of MMP-1 protein in response to the composition as described herein. Vehicle control signifies the presence of only solvent used in the composition. The solvent used in the composition is DMSO.
Referring to Figure 3, in presence of 0.01% xylan alone, the production of MMP-1 protein is not inhibited. Similarly, in the presence of 0.001% mandelic acid, the production of mandelic acid does not decrease. Surprisingly, at a combination of 0.01% xylan and 0.001% mandelic acid significant decrease of about 21% is observed (79% production of MMP-1 protein). Thus, it can be inferred that the composition comprising 0.01% xylan and 0.001% mandelic acid synergistically inhibit the production of MMP-1 protein. Therefore, the present combination can be used to prevent collagen breakdown in skin.
Example 3
Non-Working combination of xylan and mandelic acid
[0076] The present non-working examples have been depicted to assert the experimentation that assisted to arrive at the particular composition. Non-Working Example A
[0077] Non-Working Example A illustrates the combination of 0.1% xylan and 0.01% mandelic acid. Figure 4 depicts the percentage production of MMP-1 protein in presence of the above-mentioned combination. Referring to Figure 4, it can be observed that neither 0.1% xylan alone, 0.01% mandelic acid alone and nor a combination of 0.1% xylan and 0.01% mandelic acid is able to inhibit the production of MMP-1 protein. In spite of the presence of xylan and mandelic acid in a weight ratio of 1:0.1 in the present combination, the composition is unable to exhibit inhibition. It can be correlated with the range of combined weight percentage as the combined weight percentage in the present example is more than 0.1% which is beyond the disclosed range of 0.01%-0.012%. Thus, a mere combination of both the actives in a weight ratio of 1:0.1 does not give the desired result and significant experimentation is involved at arriving at the composition. Non-Working Example B
[0078] Non-Working Example B illustrates the combination of 0.001% xylan and 0.0001% mandelic acid. Figure 5 depicts the percentage production of MMP-1 protein in presence of the above-mentioned combination, the w/w ratio of the present combination is 1:0.1 (xylan: mandelic acid). Referring to Figure 5,
independently 0.001% xylan and 0.0001% mandelic acid is not able to show any inhibition in MMP-1 production. The composition combining 0.001% xylan and 0.0001% mandelic acid is also not showing any inhibition in MMP-1 levels. It has been revealed in the present disclosure that xylan and mandelic acid combined weight percentage is in the range of 0.01% - 0.012% with respect to the composition. Thus, the present example asserts the importance of combined weight percentage of both the components, simply mixing the components in any weight percentage does not address the present problem.
[0079] Overall, it can be inferred that the composition comprising xylan and mandelic acid in a w/w ratio of 1:0.1 and having a combined weight percentage of 0.011% is displaying a synergistic inhibition of MMP-1 protein production.
Advantages of the present disclosure
[0080] The present disclosure discloses a composition comprising xylan and mandelic acid in a specific weight ratio and a specific combined weight percentage that synergistically inhibit the production of MMP-1. Since, MMP-1 protein is a collagenase and is involved in active breakdown of collagen, thus inhibiting the production of MMP-1 in turn will slow down the rate of collagen breakdown. Inhibiting the breakdown of collagen will prove beneficial in terms of maintaining the tensile strength of skin. Therefore, the present composition will help in reducing facial wrinkles and lines that develop due to ageing process and will also assist in maintaining the tensile strength of skin thereby, maintaining the overall health of skin. Thus, the present composition can be a part of a formulation that can be used for improving skin health.
I/We Claim;
1. A composition comprising:
a. xylan; and
b. mandelic acid,
wherein xylan and mandelic acid combined weight percentage is in the range of 0.005% - 0.02% with respect to the composition, and wherein xylan to mandelic acid weight ratio is in a range of 1:0.05-l :0.3.
2. The composition as claimed in claim 1, wherein xylan and mandelic acid combined weight percentage is in the range of 0.01%-0.012% with respect to the composition, and wherein xylan to mandelic acid weight ratio is 1:0.1.
3. The composition as claimed in claim 1, wherein the composition inhibits expression of matrix metalloprotease 1 (MMP1).
4. The composition as claimed in claim 3, wherein the composition inhibits breakdown of collagen.
5. The composition as claimed in claim 1, said composition comprising:
a. xylan having a weight percentage of 0.01% with respect to the
composition; and
b. mandelic acid having a weight percentage of 0.001 % with respect to
the composition.
6. A formulation comprising: (a) the composition as claimed in any of the claims 1-5; and (b) at least one excipient.
7. The formulation as claimed in claim 6, wherein the formulation inhibits breakdown of collagen by inhibiting expression of matrix metalloprotease 1 (MMP1).
8. A process for preparing the composition as claimed in any of the claims 1-5, said process comprising:
a. obtaining xylan;
b. obtaining mandelic acid; and
c. contacting xylan and mandelic acid, to obtain the composition.
9. A process for preparing the formulation as claimed in any of the claims 6-7,
said process comprising:
a. obtaining xylan;
b. obtaining mandelic acid;
c. obtaining the at least one excipient; and
d. contacting xylan, mandelic acid, and the at least one excipient to
obtain the formulation.
10. A process to inhibit breakdown of collagen in skin, said process
comprising:
a. obtaining the composition as claimed in any of the claims 1-5; and
b. contacting the composition of step (a) with skin, to inhibit the
breakdown of collagen.
11. The formulation as claimed in claim 6, wherein the formulation provides
anti-wrinkle properties.
| # | Name | Date |
|---|---|---|
| 1 | 201841008869-FER.pdf | 2022-01-19 |
| 1 | 201841008869-STATEMENT OF UNDERTAKING (FORM 3) [09-03-2018(online)].pdf | 2018-03-09 |
| 2 | 201841008869-FORM 1 [09-03-2018(online)].pdf | 2018-03-09 |
| 2 | 201841008869-FORM 18 [17-12-2021(online)].pdf | 2021-12-17 |
| 3 | 201841008869-DRAWINGS [09-03-2018(online)].pdf | 2018-03-09 |
| 3 | Correspondence by Agent_Form1_Power of Attorney_17-04-2018.pdf | 2018-04-17 |
| 4 | 201841008869-DECLARATION OF INVENTORSHIP (FORM 5) [09-03-2018(online)].pdf | 2018-03-09 |
| 4 | 201841008869-FORM-26 [13-04-2018(online)].pdf | 2018-04-13 |
| 5 | 201841008869-Proof of Right (MANDATORY) [13-04-2018(online)].pdf | 2018-04-13 |
| 5 | 201841008869-COMPLETE SPECIFICATION [09-03-2018(online)].pdf | 2018-03-09 |
| 6 | 201841008869-COMPLETE SPECIFICATION [09-03-2018(online)].pdf | 2018-03-09 |
| 6 | 201841008869-Proof of Right (MANDATORY) [13-04-2018(online)].pdf | 2018-04-13 |
| 7 | 201841008869-DECLARATION OF INVENTORSHIP (FORM 5) [09-03-2018(online)].pdf | 2018-03-09 |
| 7 | 201841008869-FORM-26 [13-04-2018(online)].pdf | 2018-04-13 |
| 8 | 201841008869-DRAWINGS [09-03-2018(online)].pdf | 2018-03-09 |
| 8 | Correspondence by Agent_Form1_Power of Attorney_17-04-2018.pdf | 2018-04-17 |
| 9 | 201841008869-FORM 1 [09-03-2018(online)].pdf | 2018-03-09 |
| 9 | 201841008869-FORM 18 [17-12-2021(online)].pdf | 2021-12-17 |
| 10 | 201841008869-STATEMENT OF UNDERTAKING (FORM 3) [09-03-2018(online)].pdf | 2018-03-09 |
| 10 | 201841008869-FER.pdf | 2022-01-19 |
| 1 | SearchHistory-321-convertedE_18-01-2022.pdf |