IP Library Granted Patent US 9,801,807
Granted Patent B2
US 9,801,807 · App. 14/104,074 · Granted Oct 31, 2017

Topical formulations for increasing the dermal concentration of hyaluronic acid

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Quick Facts
Patent No.
US 9,801,807
App. No.
14/104,074
Granted
Oct 31, 2017
Kind
B2
Abstract

Described herein are methods and compositions for increasing dermal concentrations of glycosaminoglycans (GAG), including hyaluronic acid. Exemplary methods involve a one-step protocol and a three-step protocol. Either method can be used over a 90-day treatment period.

Claims (220)

1. A method of increasing the hyaluronic acid concentration in an area of skin of a subject, comprising the steps of:

applying to the area of skin a therapeutically-effective amount of a first formulation, wherein the first formulation comprises

water, in a quantity from about 25% to about 65% by weight;

denatured alcohol, in a quantity from about 12% to about 36% by weight;

a plurality of keratolytic agents in a quantity from about 6% to about 18% by weight; and

a plurality of moisturizers, emollients, humectants, or skin soothing agents in a quantity from about 5% to about 15% by weight;

applying to the area of skin a therapeutically-effective amount of a second formulation, wherein the second formulation comprises

a) water;

b) glycerin;

c) dimethicone;

d) pentylene glycol;

e) water, purified;

f) dimethicone/divinyl-dimethicone/silsesquioxane crosspolymer;

g) Helianthus annuus (sunflower) seed oil;

h) panthenol;

i) ethylhexyl stearate;

j) dimethiconol;

k) tetrahexyldecyl ascorbate;

l) betaine;

m) tocopherol;

n) acrylates/c10-30 alkyl acrylate crosspolymer;

o) Rubus occidentalis (black raspberry) seed oil;

p) Vaccinium macrocarpon (cranberry) seed oil;

q) Punica granatum (pomegranate) seed oil;

r) urea;

s) Rubus idaeus (raspberry) seed oil;

t) superoxide dismutase;

u) allantoin;

v) chlorphenesin;

w) sodium hydroxide;

x) potassium lactate;

y) sodium lauroyl lactylate;

z) xanthan gum;

aa) sodium benzoate;

bb) ethyl hexylglycerin;

cc) sodium isostearate;

dd) sodium hyaluronate crosspolymer;

ee) polyglyceryl-4 diisostearate/polyhydroxystearate/sebacate;

ff) potassium sorbate;

gg) hydrolyzed hyaluronic acid;

hh) zinc citrate;

ii) (ii) disodium EDTA;

jj) sodium butyroyl/formoyl hyaluronate;

kk) hydrolyzed sclerotium gum;

ll) polyglutamic acid;

mm) caprylyl glycol;

nn) lecithin;

oo) tetradecyl aminobutyroylvalyl-aminobutyric urea trifluoro-acetate;

pp) palmitoyl tripeptide-5;

qq) ceramide 3;

rr) phytosphingosine;

ss) cholesterol;

tt) ceramide 6 II;

uu) methylisothiazolinone;

vv) Micrococcus lysate;

ww) Arabidopsis thaliana extract;

xx) plankton extract;

yy) carbomer;

zz) palmitoyl dipeptide-5diaminohydroxybutyrate;

aaa) palmitoyl dipeptide-5diamino-butyroyl hydroxy threonine;

bbb) magnesium chloride;

ccc) acetyl octapeptide-3;

ddd) pentapeptide-3;

eee) ceramide 1; and

fff) fragrance; and

applying to the area of skin a therapeutically-effective amount of a third formulation, wherein the third formulation comprises

water, in about 25% to about 75% by weight;

a plurality of moisturizers, emollients, humectants, or skin soothing agents in a quantity from about 15% to about 45% by weight; and

a plurality of plant extracts or fruit seed oils.

2. The method of claim 1 , wherein the method represents a 90-day treatment regimen.

3. The method of claim 1 , wherein the first formulation is applied once daily.

4. The method of claim 2 , wherein the first formulation is applied once daily on days 1-5, 31-35, and 61-65 of the 90-day treatment regimen.

5. The method of claim 1 , wherein the second formulation is applied twice daily.

6. The method of claim 1 , wherein the third formulation is applied twice daily.

7. The method of claim 1 , wherein the third formulation is applied twice daily on days 1-5, 31-35, and 61-65 of the 90-day treatment regimen.

8. The method of claim 1 , wherein the subject is human.

9. The method of claim 1 , wherein the second formulation comprises

a) water from about 25% to about 90% by weight of the second formulation;

b) glycerin from about 3% to about 9% by weight of the second formulation;

c) dimethicone from about 3% to about 9% by weight of the second formulation;

d) pentylene glycol from about 2% to about 8% by weight of the second formulation;

e) water, purified from about 1% to about 5% by weight of the second formulation;

f) dimethicone/divinyl-dimethicone/silsesquioxane crosspolymer from about 1% to about 5% by weight of the second formulation;

g) Helianthus annuus (sunflowerj seed oil from about 1% to about 3% by weight of the second formulation;

h) panthenol from about 0.5% to about 2.5% by weight of the second formulation;

(i) ethyihexyl stearate from about 0.5% to about 2.5% by weight of the second formulation;

j) dirnethiconol from about 0.5% to about 1.5% by weight of the second formulation;

k) tetrahexyldecyl ascorbate from about 0.5% to about 1.5% by weight of the second formulation;

l) betaine from about 0.5% to about 1.5% by weight of the second formulation;

m) tocopherol from about 0.5% to about 1.5% by weight of the second formulation;

n) acrylates/c10-30 alkyl acrylate crosspolynier from about 0.5% to about 1.5% by weight of the second formulation;

o) Rubus occidentalis (black raspberry) seed oil from about 0.2% to 0.8% by weight of the second formulation;

p) Vaccinium macrocarpon (cranberry) seed oil from about 0.2% to 0.8% by weight of the second formulation;

q) Punica granaturn (pomegranate) seed oil from about 0.2% to 0.8% by weight of the second formulation;

r) urea from about 0.2% to 0.8% by weight of the second formulation;

s) Rubus idaeus (raspberry) seed oil from about 0.2% to 0.8% by weight of the second formulation;

t) superoxide dismutase from about 0.2% to 0.8% by weight of the second formulation;

u) allantoin from about 0.2% to 0.6% by weight of the second formulation;

v) chlorphenesin from about 0.1% to about 0.5% by weight of the second formulation;

w) sodium hydroxide from about 0.1% to about 0.5% by weight of the second formulation;

x) potassium lactate from about 0.1% to about 0.4% by weight of the second formulation;

y) sodium lauroyl lactylate from about 0.1% to about 0.4% by weight of the second formulation;

z) xanthan gum from about 0.1% to about 0.3% by weight of the second formulation;

aa) sodium benzoate from about 0.1% to about 0.3% by weight of the second formulation;

bb) ethyl hexylglycerin from about 0.1% to about 0.3% by weight of the second formulation;

cc) sodium isostearate from about 0.1% to about 0.3% by weight of the second formulation:

dd) sodium hyaluronate crosspoiymer from about 0.1% to about 0.3% by weight of the second formulation;

ee) polyglyceryl-4 diisostearate/polyhydroxystearate/sebacate from about 0.1% to about 0.3% by weight of the second formulation;

ff) potassium sorbate from about 0.07% to about 0.25% by weight of the second formulation;

gg) hydrolyzed hyaiuronic acid from about 0.5% to about 0.15% by weight of the second formulation;

hh) zinc citrate from about 0.5% to about 0.15% by weight of the second formulation;

ii) disodiurn EDTA from about 0.5% to about 0.15% by weight of the second formulation;

jj) sodium butyroyl/formoyl hyaluronate from about 0.5% to about 0.15% by weight of the second formulation;

kk) hydrolyzed sclerotium gum from about 0.03% to about 0.10% by weight of the second formulation;

ll) polyglutamic acid from about 0.03% to about 0.10% by weight of the second formulation;

mm) caprylyl glycol from about 0.02% to about 0.08% by weight of the second formulation;

nn) lecithin from about 0.01% to about 0.05% by weight of the second formulation;

oo) tetradecyl aminobutyroylvalyl-aminobutyric urea, trifluoro-acetate from about 0.01% to about 0.04% by weight of the second formulation;

pp) palmitoyl tripeptide-5 from about 0.01% to about 0.04% by weight of the second formulation;

qq) ceramide 3 from about 0.01% to about 0.04% by weight of the second formulation;

rr) phytosphingosine from about 0.01% to about 0.04% by weight of the second formulation;

ss) cholesterol from about 0.01% to about 0.04% by weight of the second formulation;

tt) ceramide 6 II from about 0.01% to about 0.04% by weight of the second formulation;

uu) methylisothiazolinone from about 0.005% to about 0.015% by weight of the second formulation;

vv) Micrococcus lysate from about 0.005% to about 0.015% by weight of the second formulation;

ww) Arabidopsis thafiana extract from about 0.005% to about 0.015% by weight of the second formulation;

xx) plankton extract from about 0.005% to about 0.015% by weight of the second formulation;

yy) carbomer from about 0.003% to about 0.01% by weight of the second formulation;

zz) palmitoyl dipeptide-5diaminohydroxybutyrate from about 0.002% to about 0.008% by weight of the second formulation;

aaa) palmitoyl dipeptide-5diamino-butyroyl hydroxy threonine from about 0.002% to about 0.008% by weight of the second formulation;

bbb) magnesium chloride from about 0.001% to about 0.004% by weight of the second formulation;

ccc) acetyl octapeptide-3 from about 0.001% to about 0.004% by weight of the second formulation;

ddd) pentapeptide-3 from about 0.001% to about 0.004% by weight of the second formulation;

eee) ceramide 1 from about 0.00001% to about 0.00004% by weight of the second formulation; and

fff) fragrance from about 0.3% to about 1.0% by weight of the second formulation.

10. The method of claim 9 , wherein the second formulation further comprises niacinamide from about 0.5% to about 2.5% by weight of the second formulation.

11. The method of claim 1 , wherein the second formulation further comprises

(ggg) dipeptide diaminobutyroyl benzylamide diacetate;

(hhh) caprylic/capric triglyceride;

(iii) hydrolyzed rice bran protein;

(jjj) steareth-20;

(kkk) N-hydroxy succinimide;

(lll) chrysin;

(mmm) glycine soja (soybean) protein;

(nnn) chlorella vulgaris extract;

(ooo) oxido reductases;

(ppp) geranylgeranylisopropanol;

(qqq) palmitoyl tetrapeptide-7; and

(rrr) palmitoyl oligopeptides.

12. The method of claim 1 , wherein the second formulation comprises

a) water from about 25% to about 75% by weight of the second formulation;

b) glycerin from about 5% to about 15% by weight of the second formulation;

c) dimethicone from about 3% to about 9% by weight of the second formulation;

d) pentylene glycol from about 2% to about 8% by weight of the second formulation;

e) water, purified from about 1% to about 5% by weight of the second formulation;

f) dimethicone/divinyl-dimethicone/silsesquioxane crosspolymer from about 1% to about 5% by weight of the second formulation;

g) Helianthus annuus (sunflower) seed oil from about 1% to about 3% by weight of the second formulation;

h) panthenol from about 0.5% to about 2.5% by weight of the second formulation;

i) ethylhexyl stearate from about 0.6% to about 2.0% by weight of the second formulation;

j) dimethiconol from about 0.5% to about 1.5% by weight of the second formulation;

k) tetrahexyldecyl ascorbate from about 0.5% to about 1.5% by weight of the second formulation;

l) betaine from about 0.5% to about 1.5% by weight of the second formulation;

m) tocopherol from about 0.5% to about 1.5% by weight of the second formulation;

n) acrylates/c10-30 alkyl acrylate crosspolymer from about 0.5% to about 1.5% by weight of the second formulation;

o) Rubus occidentalis (black raspberry) seed oil from about 0.2% to about 0.8% by weight of the second formulation;

p) Vaccinium macrocarpon (cranberry) seed oil from about 0.2% to about 0.8% by weight of the second formulation;

q) Punica granatum ( pomegranate) seed oil from about 0.2% to about 0.8% by weight of the second formulation;

r) urea from about 0.2% to about 0.8% by weight of the second formulation;

s) Rubus idaeus (raspberry) seed oil from about 0.2% to about 0.8% by weight of the second formulation;

t) superoxide dismutase from about 0.2% to about 0.8% by weight of the second formulation;

u) allantoin from about 0.2% to about 0.6% by weight of the second formulation;

v) chlorphenesin from about 0.1% to about 0.5% by weight of the second formulation;

w) sodium hydroxide from about 0.1% to 0.5% of the formulation;

x) potassium lactate from about 0.1% to about 0.4% by weight of the second formulation;

y) sodium lauroyl lactylate from about 0.1% to about 0.4% by weight of the second formulation;

z) xanthan gum from about 0.1% to about 0.3% by weight of the second formulation;

aa) sodium benzoate from about 0.1% to about 0.3% by weight of the second formulation;

bb) ethyl hexylglycerin from about 0.1% to about 0.3% by weight of the second formulation;

cc) sodium isostearate from about 0.1% to about 0.3% by weight of the second formulation;

dd) sodium hyaluronate crosspolymer from about 0.1% to about 0.3% by weight of the second formulation;

ee) polyglyceryl-4 diisostearate/polyhydroxystearate/sebacate from about 0.1% to about 0.3% by weight of the second formulation;

ff) potassium sorbate from about 0.07% to about 0.22% by weight of the second formulation;

gg) hydrolyzed hyaluronic acid from about 0.1% to about 0.3% by weight of the second formulation;

hh) zinc citrate from about 0.05% to about 0.15% by weight of the second formulation;

ii) disodium EDTA from about 0.05% to about 0.15% by weight of the second formulation;

jj) sodium butyroyl/formoyl hyaluronate from about 0.05% to about 0.15% by weight of the second formulation;

kk) hydrolyzed sclerotium gum from about 0.03% to about 1.1% by weight of the second formulation;

ll) polyglutamic acid from about 0.03% to about 1.1% by weight of the second formulation;

mm) caprylyl glycol from about 0.03% to about 1.1% by weight of the second formulation;

nn) lecithin from about 0.02% to about 0.8% by weight of the second formulation;

oo) tetradecyl aminobutyroylvalyl-aminobutyric urea trifluoro-acetate from about 0.01% to about 0.04% by weight of the second formulation;

pp) palmitoyl tripeptide-5 from about 0.01% to about 0.04% by weight of the second formulation;

qq) ceramide 3 from about 0.01% to about 0.04% by weight of the second formulation;

rr) phytosphingosine from about 0.005% to about 0.02% by weight of the second formulation;

ss) cholesterol from about 0.005% to about 0.015% by weight of the second formulation;

tt) ceramide 6 II from about 0.005% to about 0.02% by weight of the second formulation;

uu) methylisothiazolinone from about 0.005% to about 0.015% by weight of the second formulation;

vv) Micrococcus lysate from about 0.01% to about 0.03% by weight of the second formulation;

ww) Arabidopsis thaliana extract from about 0.01% to about 0.03% by weight of the second formulation;

xx) plankton extract from about 0.01% to about 0.03% by weight of the second formulation;

yy) carbomer from about 0.003% to about 0.01% by weight of the second formulation;

zz) palmitoyl dipeptide-5 diaminohydroxybutyrate from about 0.002% to about 0.008% by weight of the second formulation;

aaa) palmitoyl dipeptide-5 diamino-butyroyl hydroxy threonine from about 0.002% to about 0.008% by weight of the second formulation;

bbb) magnesium chloride from about 0.001% to about 0.004% by weight of the second formulation;

ccc) acetyl octapeptide-3 from about 0.002% to about 0.008% by weight of the second formulation;

ddd) pentapeptide-3 from about 0.001% to about 0.004% by weight of the second formulation;

eee) ceramide 1 from about 0.00001% to about 0.00004% by weight of the second formulation;

fff) fragrance from about 0.1% to about 0.3% by weight of the second formulation;

ggg) dipeptide diaminobutyroyl benzylamide diacate from about 0.01% to about 0.03% by weight of the second formulation;

hhh) caprylic/capric triglyceride from about 1% to about 3% by weight of the second formulation;

iii) hydrolyzed rice bran protein from about 0.2% to about 0.6% by weight of the second formulation;

jjj) steareth-20 from about 0.1% to about 0.3% by weight of the second formulation;

kkk) N-hydroxy succinimide from about 0.0.3% to about 0.09% by weight of the second formulation;

lll) chrysin from about 0.03% to about 0.09% by weight of the second formulation;

mmm) glycine soja (soybean) protein from about 0.02% to about 0.08% by weight of the second formulation;

nnn) chlorella vulgaris extract from about 0.02% to about 0.08% by weight of the second formulation;

ooo) oxido reductases from about 0.02% to about 0.06% by weight of the second formulation;

ppp) geranylgeranylisopropanol from about 0.02% to about 0.06% by weight of the second formulation;

qqq) palmitoyl tetrapeptide-7 from about 0.02% to about 0.06% by weight of the second formulation; and

rrr) palmitoyl oligopeptides from about 0.02% to about 0.06% by weight of the second formulation.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Apr 8, 2025
From: BARCLAYS BANK PLC, AS COLLATERAL AGENT
To: SOLTA MEDICAL, INC.; PRECISION DERMATOLOGY, INC.; BAUSCH HEALTH IRELAND LIMITED (F/K/A/ VALEANT PHARMACEUTICALS IRELAND LIMITED); SALIX PHARMACEUTICALS, INC.; SALIX PHARMACEUTICALS, LTD; SANTARUS, INC.; MEDICIS PHARMACEUTICAL CORPORATION; HUMAX PHARMACEUTICAL S.A.; SOLTA MEDICAL IRELAND LIMITED; BAUSCH & LOMB MEXICO, S.A. DE C.V.; BAUSCH+LOMB OPS B.V.; BAUSCH HEALTH AMERICAS, INC.; BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH HOLDCO LIMITED; BAUSCH HEALTH MAGYARORSZAG KFT (A/K/A BAUSCH HEALTH HUNGARY LLC); BAUSCH HEALTH POLAND SPOLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA (F/K/A VALEANT PHARMA POLAND SPOLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA); BAUSCH HEALTH US, LLC; BAUSCH HEALTH, CANADA INC. / SANTE BAUSCH, CANADA INC.; ICN POLFA RZESZOW SPOLKA AKCYJNA (A/K/A ICN POLFA RZESZOW S.A.); ORAPHARMA, INC.; PRZEDSIEBIORSTWO FARMACEUTYCZNE JELFA SPOLKA AKCYJNA (A/K/A PRZEDSIEBIORSTWO FARMACEUTYCZNE JELFA S.A.); SOLTA MEDICAL DUTCH HOLDINGS B.V.; V-BAC HOLDING CORP.; VRX HOLDCO LLC; 1261229 B.C. LTD.; 1530065 B.C. LTD.
Reel/Frame 070778/0199 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 22, 2016
From: PRECISION DERMATOLOGY, INC.
To: SHAMROC, INC.
Reel/Frame 037562/0479 →
RELEASE OF SECURITY INTEREST Recorded Dec 28, 2015
From: BARCLAYS BANK PLC
To: PRECISION DERMATOLOGY, INC.
Reel/Frame 037365/0438 →
SECURITY AGREEMENT Recorded Jul 6, 2015
From: ECR PHARMACEUTICALS CO., INC.; PRECISION DERMATOLOGY, INC.
To: BARCLAYS BANK PLC, AS COLLATERAL AGENT
Reel/Frame 036091/0257 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 28, 2014
From: TRUMBORE, MARK W.; STIMSON, DRAKE D.; GURGE, RONALD M.
To: PRECISION DERMATOLOGY, INC.
Reel/Frame 032059/0323 →