Abstract: The present invention deals with composition for oral drink as beauty enhancement therapy. The composition consists of various vitamins, minerals, Coenzyme Q-1 0, P-carotene, collagen and hyaluronic acidas beauty therapy. In addition, it may also contain pharmaceutically acceptable additives like surfactant, sweetner, flavour, pH modifiersand preservative/s. The composition consists of ingredients which has properties like prevention from sun induced skin damage, oxidation, wrinkles, transepidermal water loss (TEWL) and discoloration and acts like cushion to connective tissues in skin. The invention shall deal therapeutically or prophylactically to cure skin ageing.
Present invention deals with nutritional composition, more ·particularly it consist of Vitamins
like Thiamine (Vitamin 81 ), Riboflavin (Vitamin 82), Pyridoxine (Vitamin 86), ascorbic
acid (Vitamin C), a-Tocopherol (Vitamin E), minerals, coenzyme Q-1 0, P-carotene, collagen
and hyaluronic acidin oral drink for enhanced skin beauty. The composition may further
contain surfactant, sweetners, pH modifiers, preservative/s and flavors for enhanced
palatability and appearance of the beauty drink. These ingredients are useful in preventing
sun light induced skin damage, oxidation, wrinkles, TEWL and discoloration and acts as an
aid to cushion connective tissues in skin.
Background of the invention:
Like all other organs skin suffers a progressive deterioration with age. However, due to
various extrinsic factors like UV light, tobacco, smoking etc may lead to premature ageing of
skin. As the skin ages the lipid barrier decreases due to decreased cholesterol synthesis and
reduction of lipids in stratum corneum, there is altered immune response which leads to
increased susceptibility of skin to mechanical trauma and infection, the vascular orientation
gets disturbed in photodamaged skin along with connective tissues. The sebaceous glands in
photoaged skin are damaged causing loss of lubrication produced by sebum. The visual
effects of skin ageing include wrinkles, pigmentation, sagging, atropy, elastosis and
telangiectasis. It leads to low self-esteem of an individual. Many nutrients when taken in adequate amount helps in prevention of premature ageing of
skin. Of utmost importance are known to be Vitamin E, C and ~-carotene. They scanvenge
reactive oxygen species (ROS) and prevent skin oxidation and UV -light induced skin
erythema. Hydrolyzed collagen helps to maintain the decreased amount of collagen in skin
during ageing. Studies have reported that 1 0 g of daily collagen intake decreases skin
wrinkles and improves skin properties. Skin hydration is vital for maintaining healthy skin. In
ageing skin, levels of hyaluronic acid (HA) are drastically reduced causing loss of moisture
leading to dry and scaly skin. Ageing skin also has decreased level of natural skin antioxidant
called coenzyme Q-1 0. Thus, a supplement containing HAand coenzyme Q-1 0 would
reduce skin ageing process. Deficiency of Vitamin B 1 causes decreased neolipidogenesis
leading to skin thinning, vitamin B2 causes fissured and dry lips and seborrheic dermatitis
like condition while vitamin B6 deficiency may lead to skin inflammatory changes. A
supplement consisting of Vitamin B 1, B2 and B6 may help prevent skin ageing. Thus,
present invention consists of a combined composition of essential ingredients to prevent
agemg and maintain skin health. The invention is specifically designed for oral
administration because by this route the nutrients will be metabolized in blood stream into
their active form and then get distributed to all the parts of skin like epidermis, dermis and
subcutaneous site. These skin layers are continuously replenished by fresh nutrient in its
active form.
Summary of the invention:
Current invention deals with oral nutraceutical nanoformulation with unit pack of 50 mi. It
deals with water soluble vitamins like Thiamine or Thiamine hydrochloride NL T 0.0099%
w/v, Riboflavin or Riboflavin-5 '- sodium monophosphate NL T 0.01 05% w/v, Pyridoxine or
Pyridoxine hydrochloride NLT 0.010% w/v and L-ascorbic acid NLT 0.6% w/v and/or oil
soluble vitamins like a-Tocopherol acetateNLT 0.09% v/v and Coenzyme Q 10
(Ubidecarenone) NL T 0.02% w/v. Further, the invention includes other beauty enhancing
ingredients like collagen from marine source (Type I) NL T 26% w/v and hyaluronic acid
NLT 0.02% w/v. It involves purified water between 50% v/v- 60% v/v as vehicle for
hydrophilic ingredients and lipophilic ingredients were solubilized in natural or synthetic oils
including but·not restricted to linoleic acid, linolenic acid and arachidonic acid derived from
safflower oil, sunflower oil, olive oil, corn oil, jojoba oil and rapseed oil etc. fatty acid esters
like ethyl oleate, caprylocaprylate, ethyl linoleate etc., medium chain triglycerides like
Isopropyl myristate, isopropyl palmitate, caproic acid, caprylic acid, lauric acid etc. Current invention deals with 0%-0.91% vdv of isopropyl myristate as vehicle of lipophilic
ingredients. The lipophilic and hydrophilic phases are stabilized by means of suitable anionic,
cationic or non-ionic emulsifier in HLB range of 1-20, more specifically 2-6 and 8-17.
Suitable emulsifiers include but not limited to, non-ionic surfactant such as polyalcohol ether
derivatives such as aliphatic or cycloaliphatic alcohols, saturated fatty acids and alkylphenols,
water-soluble polyethyleneoxy adducts onto polypropylene glycol and alkyl polypropylene
glycol, nonylphenol polyethoxyethanols, castor oil polyglycol ethers, polypropylene/
polyethylene oxide adducts, tributylphenoxy-polyethoxyethanol, polyethylene glycol,
octylphenoxy-polyethoxyethanol, lanolin alcohol, polyoxyethoxylated (POE) alkyl phenols,
POE fatty amides, POE fatty alcohol ethers, POE fatty amines, POE fatty esters, poloxamer
(7-19), POE glycol monoethers (3-16), polysorbates (15-17) and sorbitan esters (bracketed
values depict the HLB value of the emulsifier). Specifically, polysorbate 80 in 0% w/v -8.2%
w/v. Current composition deals with pH modifiers to maintain the pH of nanoformulation
between 1-6, preferably 4-5 to maintain ascorbic acid and hyaluronic acid in protonated,
uncharged form. As an illustration, it may include citric acid, tartaric acid, phosphoric acid,
lactic acid, glycolic acid etc. Specifically, it involves lactic acid in 0%-1% w/v. The invention
further involves mono-, di- and tri- polysaccharide either alone or in combination or their
oligomer thereof in syrup form or in solid form. As an illustration, it may consist of invert
sugar, sucrose, fructose, maltose, dextrose, poly dextrose, polydextrin, glucose (corn syrup),
maltodextrin (corn syrup solid) while illustration for solid form may include saccharin,
aspartame, asulfame, sucralose, sorbitol, mannitol, maltitol, xylitol as well as other
commercial sweetners like dihydrochalcone compounds, glycyrrhizin, stevioside and
hydrogenated starch hydrolysates etc. Of these, glucose syrup (corn syrup) is preferred for the
said nanoformulation in 0%w/v -20% w/v in order to achieve desired sweet taste and flavour
along with consistency. Preservatives which elicit their action in acidic pH like sorbic acid,
thiomersal, quaternary ammonium salts, benzyl alcohol, benzoic acid, chlorhexidine
gluconate, potassium sorbate and phenyl ethanol etc. and antioxidants like sodium bisulfite,
sodium metabisulfite, butylated hydroxyanisole, butylated hydroxytoluene etc may be
included in nanoformulation but not restricted to the illustrations. Current invention deals
with potassium sorbate in NL T 0%w/v-0.18% w/v. lt further involves synthetic fruit flavours
to mask the bitter taste of the formulation. Various flavouring agent can be added from
natural or synthetic source these include but not restricted to volatile oils, synthetic flavouring
oils, flavouring aromatics, oils, liquids, powders, oleoresins or extracts derived from plants or
parts of plants. As an illustration, citrus flavour from lemon, orange, grape, lime or grapefruit, while other fruit flavours derived from mango, apple, strawberry, pear, peach, grape,
raspberry, cherry, plum, pineapple, apricot etc. Various class of flavouring agents include but
not restricted to aldehydes and esters such as benzaldehyde from almond and cherry, alpha
citra) from lemon and lime, beta-citra) from lemon, lime, decanal from orange or lime,
aldehyde Cs,C9, C12 from citrus fruit, tolyl aldehyde from cherry and almond, 2,6
dimethyloctanal from green fruit, dodecanal from citrus and mandarin. Flavours may also
include chocolate, vanilla and cream from natural or synthetic source. They can be utilized as
such or combination thereof.Fiavours can be added into the oral nutraceutical
nanoformulation in 0-0.3% w/v.A skilled artisan may utilize various derivatives like
mononitrate, hydrochloride, phosphate, alkali metal, amine and alcohol of Thiamine,
Riboflavin, Pyridoxine and ascorbic acid and Ceramide from skin or spinal marrow of any
other animal, wheat, rice, soy and spinach.
Detailed description of the invention:
a- Tocopherol (Vitamin E)
Vitamin E is an essential vitamin which cannot be synthesized by the body but whose need
can be fulfilled by replenishing vitamin E from various sources like food and vegetables. ·
However, the Vitamin E content depletes by 50% upon exposure to UV -A radiation at dose
lesser than the ones causing mild redness of the skin. Oral or topical Vitamin E has antitumorogenic,
photoprotective and skin barrier stabilizing properties. On exposure to UV -light
there is increase in matrix metalloproteinase-I (MMP) enzymes. This enzyme degrade
collagen and other extracellular matrix proteins present in dermal connective tissues of the
skin leading to premature photoageing. Vitamin E is a known antioxidant which prevents
formation of MMP-1 enzymes in the skin. Further, it inhibits protein kinase C which reduces
age dependant synthesis of collagenase and prevents sunburned cell formation in the skin.
Clinical trials has proven the effectiveness of Vitamin E in combination with ascorbic acid in
UVA/ UV-B induced skin erythema. Vitamin E is an inhibitor of lipid peroxidation during
which Tocopherol gets converted to Tocopheroxyl radical. Ascorbate converts this radical
into Tocopherol, which contributes to synergistic action of both on photodamaged skin. It is
known to control rhytides, skin roughness, length of facial lines and depth of wrinkles. It
increases stratum corneum hydration and depth of water-binding capacity. Oral Vitamin E
supplements can be an excellent source in treatment of atopic dermatitis. It is generally used in concentration range of 0.0001% to 20 %. It can be utilized as such or as its derivatives like
succinate, acetate, phosphate etc.
Ascorbic acid (Vitamin C):
Vitamin C is well-known skin antioxidant known to reduce UV -B induced skin inflammation
and pigmentation. It acts by neutralizing the reactive oxygen species formed in aqueous
compartment of the cell leading to stable ascorbate ion. After donation of second electron it
leads to the formation of dehydroascorbic acid which can be converted to L-ascorbic acid in
body. 1t regenerates lipid soluble anti-oxidant vitamin E. It is a cofactor of lysyl and prolyl
hydroxylase which are enzymes responsible for stabilizing and crosslinking collagen. It can
also activate collagen synthesis by activating its transcription and stabilizing procollagen
messenger RNA. Further it inhibits elastin which is responsible for photoaging of the skin. It
also has anti-inflammatory effect on the skin due to its TNF-a and NF-KP cells suppressing
ability. Vitamin C also helps improve skin conditions with acne and acne scarring.It can be
utilized as such or as its alkali metal derivatives.
Marine/Fish collagen:
Collagen can be obtained from regular diet like fish, meat and offal. If collagen obtained
from food is insufficient to meet the body needs, collagen supplement is required. There is
decrease in collagen content of skin by 1% per year which further initiates the need for
collagen supplement. Porcine, bovine and marine collagen are generally used as source of
collagen. Specifically, marine collagen also known as Type 1 is preferred due to their smaller
molecular weight and particle size causing better absorption (1.5 times compared to bovine
and porcine collagen) and bioavailability. 1t consist of almost 97% protein with no fats, sugar
and carbohydrate. It's also source of ions like Iron, Calcium, Sodium and Potassium.
In humans, 25% of body proteins are made up of collagen, specifically type I collagen which
helps to maintain the flexibility and mechanical strength of skin, hair and bones. It consist of
high concentration of amino acids like proline, hydroxyproline and glycine. Hydroxyproline
activates the cells in skin, bones and hair and stimulates production of collagen in these
tissues through cell activation and growth. Due to ageing there is decrease in collagen
synthesis by the body leading to increased demand of collagen by skin, hair and bone tissue
which can be replenished by collagen supplement. Studies have reported 59% decline of
collagen content in irradiated skin. Clinical studies have reported I 0 g of daily intake of
collagen can improve skin property like smoothness, moisture retention ability, increase suppleness and reduce skin '"'rinkles. Due to the vitality of collagen many collagen drinks
from various countries like USA, Japan & China are available as elixirs while DXN
cobeaute' Collagen Powder Drink is available as premix powder form produced by DXN
marketing Sdn. Bhd., Selangor, Malaysia.
Hyaluronic acid:
It is an endogenous polysaccharide found in skin and connective tissue. It can be obtained
from various sources like meat, vegetables, seeds, nuts and fruits. In skin, it binds water
forming a viscous substance which helps in hydration of skin and turgor. Hydration helps
skin to maintain its volume. It also stimulates fibroblast in dermis causing de novo synthesis
of collagen, interact with CD44 receptor and help in keratinocyte differentiation and stratum
corneum (SC) lipid formation required for SC structure and lipid barrierand reduces
transforming growth factor-~ I cells which are responsible for increased scar formation. It is
therefore useful in ageing and photodamaged skin which suffers from dehydration, wrinkles,
scars and reduced keratinocyte differentiation.
Ubidecarenone (Coenzyme Q-1 0):
It is known as vitamin like substance useful in prevention of external and chronological
ageing process. It is known to prevent 60-70% DNA damage caused by UV -A radiation. It
also suppresses collagenase m-RNA in photodamaged skin. It acts as antioxidant preventing
oxidation ofUV-damaged skin and helps replenish the natural skin anti-oxidant ofthe skin.
Vitamin B-complex:
Thiamine (vitamin B 1) helps keep collagen rich connective tissues and is involved in
neolipidogenesis. Riboflavin (vitamin B2) is involved in overall growth of skin, hair and
nails. lt helps in antibody production and red blood cell formation. Pyridoxine (vitamin B6)
plays a vital role of stimulation of nucleic acid synthesis which in turn stimulates antibody
formation. It also plays a role in curing skin inflammation. Ageing skin is deficient in vitamin
B-complex, more specifically vitamin B I, B2 and B6. They can be utilized as such or their
derivatives thereof.
Inactive Ingredients:
Purified water can be considered as a suitable vehicle for hydrophilic actives involved in the
said oral nutraceutical nanoformulation. Lipophilic actives like Coenzyme Q-1 0 and vitamin E can be solubilized or can be made miscible with the aid of natural or synthetic oils
including but not restricted to linoleic acid, linolenic acid and arachidonic acid derived from
safflower oil, sunflower oil, olive oil, corn oil, jojoba oil and rapseed oil etc. fatty acid esters
like .ethyl oleate, caprylocaprylate, ethyl linoleate etc., medium chain triglycerides like
isopropyl myristate, isopropyl palmitate, caproic acid, caprylic acid, lauric acid etc.
The lipophilic and hydrophilic phases are stabilized by means of suitable emulsifier. Suitable
emulsifiers include but not limited to, anionic surfactants such as alcohol ether sulfates, alkyl
sulfates (30-40), soaps (12-20) and sulfosuccinates; cationic surfactants like quaternary
ammonium compounds, zv·litterionic derivatives like alkyl betaine derivatives, amphoteric
such as fatty amine sulfates, difattyalkyltriethanolamine derivatives (16-17); and non-ionic
surfactant such as polyalcohol ether derivatives such as aliphatic or cycloaliphatic alcohols,
saturated fatty acids and alkylphenols, water-soluble polyethyleneoxyaducts onto
polypropylene glycol and alkyl polypropylene glycol, nonylphenol polyethoxyethanols,
castor oil polyglycol ethers, polypropylene/ polyethylene oxide adducts, tributylphenoxypolyethoxyethanol,
polyethylene glycol, octylphenoxy-polyethoxethanol, lanolin alcohol,
polyoxyethoxylated (POE) alkyl phenols, POE fatty amides, POE fatty alcohol ethers, POE
fatty amines, POE fatty esters, poloxamer (7 -19), POE glycol monoethers (3-16),
polysorbates (15-23) and sorbitan esters.
Current composition deals with nanoformulation m pHrange of 1-6, preferably 4-5 to
maintain ascorbic acid and hyaluronic acid in protonated, uncharged form. Therefore, the
composition involves but not restricted to pH modifiers like weak acids. As an illustration, it
may include citric acid, phosphoric acid, lactic acid, glycolic acid etc.
The formulation properties like soothing effect, sweet taste and flavour, viscosity can be
enhanced by addition of syrup base or solid sweetners which may involve mono-, di- and tripolysaccharide
either alone or in combination or their oligomers thereof. As an illustration, it
may consist of invert sugar, sucrose, fructose, maltose, dextrose, polydextrose, polydextrin,
glucose (corn syrup), maltodextrin (corn syrup solid) while illustration for solid form may
include but not restricted to saccharin, aspartame, asulfame, sucralose, sorbitol, mannitol,
maltitol, xylitol as well as other commercial sweetners like dihydrochalcone compounds,
glycyrrhizin, stevioside and hydrogenated starch hydrolysates etc.
Preservatives which elicit their action in acidic pH like sorbic acid, potassium sorbate,
thiomersal, quaternary ammonium salts, benzyl alcohol, benzoic acid, chlorhexidine gluconate and phenyl ethanol etc.may be included in ·nanoformulation but not restricted to the
illustrations.
To enhance the taste of nanoformulation with natural fruit flavours various flavouring agent
can be added from natural or synthetic source these include but not restricted to volatile oils,
synthetic flavouring oils, flavouring aromatics, oils, liquids, powders, oleoresins or extracts
derived from plants or parts of plants. As an illustration, citrus flavour from lemon, orange,
grape, lime or grapefruit, while other fruit flavours derived from mango, apple, strawberry,
pear, peach, grape, raspberry, cherry, plum, pineapple, apricot etc. Various flavouring agent
chemical class may include but not restricted to, aldehydes and esters such as benzaldehyde
from almond and cherry, alpha citra) from lemon and lime, beta-citra) from lemon, lime,
decanal from orange or lime, aldehyde Cs,C9, C12 from citrus fruit, tolyl aldehyde from cherry
and almond, 2,6 dimethyloctanal from green fruit, dodecanal from citrus and mandarin.
Flavours may also include chocolate and vanilla from natural or synthetic source. They can
be utilized as such or combination thereof .
We Claim
I. An oral nanoformulation of active ingredients, wherein the active ingredients
comprise of collagen peptide from marine source (type- I), coenzyme Q I 0 and
vitamins like riboflavin, pyridoxine, ascorbic acid, tocopherol, thiamine and their
salt/s thereof in effective amount.
2. Nanoformulation according to claim I further comprises of inactive ingredients,
wherein inactive ingredient comprised of atleast one surfactant, atleast one sugar,
atleast one preservative, atleast one flavor, atleast one organic acid and mixture
thereof.
3. Nanoformulation according to claim 2 wherein the surfactant concentration range.s
from 1-8.2% w/v and is chosen from among anionic, non-ionic, cationic and
amphoteric surfactants. The preferred surfactants being dioctylsulfosuccinate sodium,
sodium Iaury! sulphate, polyoxyethylene-polyoxypropylene block co-polymers,
polyoxyethylene sorbitan fatty acid esters, tween 80 or combinations thereof.
4. Nanoformulation according to claim 2 wherein the sugar may be sucrose, corn syrup
or any source of fructose and sorbitol used between 1-45% w/v concentration in said
nanoformulation.
5. Nanoformulation according to claim 2 wherein the organic acid is lactic acid used
upto I% w/v concentration in said nanoformulation.
6. Nanoformulation according to claim 2 wherein the preservative concentration is NMT
0.2% w/v and is chosen from among parabens, phenols, benzoates and sorbates. The
preferable preservative for said nanoformulation being potassium sorbate.
7. Nanoformulation according to claim 2 wherein the flavour is chosen from natural
flavours. The preferred flavor being vanilla, mixed fruit, strawberry, mango, banana
or combinations thereof.
8. Nanoformulation according to claim 2 wherein pH of the nanoformulation should be
maintained acidic in the range of 1-6, preferably 4-5.
9. Nanoformulation according to claim I wherein the amount of active ingredient
comprises of NLT 26% w/v of collagen peptide, NL T 0.02%w/v coenzyme Q-1 0,
NLT 0.0105% w/v riboflavin and 0.01% w/v pyridoxine, NLT 0.6% w/v ascorbic
acid, NL T 0.09% w/v tocopherol and NL T 0.0099% w/v thiamine.
I 0. Nanoformulation according to claim 2 wherein particle size of the formulation 200-
500 nm with specific gravity from 1-1.3 and total energy content from 173-400
Kcal/1 00 ml
| # | Name | Date |
|---|---|---|
| 1 | 202011006771-Form-18-260923.pdf | 2023-11-03 |
| 1 | 202011006771-Other Patent Document-170220.pdf | 2021-10-18 |
| 2 | 202011006771-FORM28-170220.pdf | 2021-10-18 |
| 2 | 202011006771-Other Patent Document-260923.pdf | 2023-11-03 |
| 3 | 202011006771-Form 1-170220.pdf | 2021-10-18 |
| 3 | 202011006771-Form 5-170220.pdf | 2021-10-18 |
| 4 | 202011006771-Form 2(Title Page)-170220.pdf | 2021-10-18 |
| 4 | 202011006771-Form 3-170220.pdf | 2021-10-18 |
| 5 | 202011006771-Form 26-170220.pdf | 2021-10-18 |
| 6 | 202011006771-Form 2(Title Page)-170220.pdf | 2021-10-18 |
| 6 | 202011006771-Form 3-170220.pdf | 2021-10-18 |
| 7 | 202011006771-Form 1-170220.pdf | 2021-10-18 |
| 7 | 202011006771-Form 5-170220.pdf | 2021-10-18 |
| 8 | 202011006771-FORM28-170220.pdf | 2021-10-18 |
| 8 | 202011006771-Other Patent Document-260923.pdf | 2023-11-03 |
| 9 | 202011006771-Form-18-260923.pdf | 2023-11-03 |
| 9 | 202011006771-Other Patent Document-170220.pdf | 2021-10-18 |