IP Library › Granted Patent US 9,895,393

Granted Patent B2

US 9,895,393 · App. 15/372,652 · Granted Feb 20, 2018

Topical formulations for increasing the dermal concentration of hyaluronic acid

Inventors: Mark W. Trumbore (Westford, MA); Drake D. Stimson (Terrace Park, OH); Ronald M. Gurge (Franklin, MA)

Assignee: SHAMROC, INC.

A61K31/728 A61K8/64 A61K8/735 A61K8/97 A61K9/0014 A61K36/00 A61K38/00 A61Q19/00

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Quick Facts

Patent No.: US 9,895,393
App. No.: 15/372,652
Granted: Feb 20, 2018
Kind: B2

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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 (206)

1. A method of increasing the hyaluronic acid concentration in an area of skin of a subject, comprising applying to the area of skin a therapeutically-effective amount of a formulation comprising:

(a) water;

(b) glycerin;

(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) 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-5 diaminohydroxybutyrate;

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

(bbb) magnesium chloride;

(ccc) acetyl octapeptide-3;

(ddd) pentapeptide-3;

(eee) ceramide 1; and

(fff) fragrance.

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

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

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

5. The method of claim 1 , wherein the formulation comprises

(a) water from 25% to 90% by weight of the composition;

(b) glycerin from 3% to 9% by weight of the composition;

(d) pentylene glycol from 2% to 8% by weight of the composition;

(e) water, purified from 1% to 5% by weight of the composition;

(f) dimethicone/divinyl-dimethicone/silsesquioxane crosspolymer from 1% to 5% by weight of the composition;

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

(h) panthenol from 0.5% to 2.5% by weight of the composition;

(i) ethylhexyl stearate from 0.5% to 2.5% by weight of the composition;

(j) dimethiconol from 0.5% to 1.5% by weight of the composition;

(k) tetrahexyldecyl ascorbate from 0.5% to 1.5% by weight of the composition;

(l) betaine from 0.5% to 1.5% by weight of the composition;

(m) tocopherol from 0.5% to 1.5% by weight of the composition;

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

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

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

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

(r) urea from 0.2% to 0.8% by weight of the composition;

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

(t) superoxide dismutase from 0.2% to 0.8% by weight of the composition;

(u) allantoin from 0.2% to 0.6% by weight of the composition;

(v) chlorphenesin from 0.1% to 0.5% by weight of the composition;

(w) sodium hydroxide from 0.1% to 0.5% by weight of the composition;

(x) potassium lactate from 0.1% to 0.4% by weight of the composition;

(y) sodium lauroyl lactylate from 0.1% to 0.4% by weight of the composition;

(z) xanthan gum from 0.1% to 0.3% by weight of the composition;

(aa) sodium benzoate from 0.1% to 0.3% by weight of the composition;

(bb) ethyl hexylglycerin from 0.1% to 0.3% by weight of the composition;

(cc) sodium isostearate from 0.1% to 0.3% by weight of the composition;

(dd) sodium hyaluronate crosspolymer from 0.1% to 0.3% by weight of the composition;

(ee) polyglyceryl-4 diisostearate/polyhydroxystearate/sebacate from 0.1% to 0.3% by weight of the composition;

(ff) potassium sorbate from 0.07% to 0.25% by weight of the composition;

(gg) hydrolyzed hyaluronic acid from 0.05% to 0.15% by weight of the composition;

(hh) zinc citrate from 0.05% to 0.15% by weight of the composition;

(ii) disodium EDTA from 0.05% to 0.15% by weight of the composition;

(jj) sodium butyroyl/formoyl hyaluronate from 0.05% to 0.15% by weight of the composition;

(kk) hydrolyzed sclerotium gum from 0.03% to 0.10% by weight of the composition;

(ll) polyglutamic acid from 0.03% to 0.10% by weight of the composition;

(mm) caprylyl glycol from 0.02% to 0.08% by weight of the composition;

(nn) lecithin from 0.01% to 0.05% by weight of the composition;

(oo) tetradecyl aminobutyroylvalyl-aminobutyric urea trifluoro-acetate from 0.01% to 0.04% by weight of the composition;

(pp) palmitoyl tripeptide-5 from 0.01% to 0.04% by weight of the composition;

(qq) ceramide 3 from 0.01% to 0.04% by weight of the composition;

(rr) phytosphingosine from 0.01% to 0.04% by weight of the composition;

(ss) cholesterol from 0.01% to 0.04% by weight of the composition;

(tt) ceramide 6 II from 0.01% to 0.04% by weight of the composition;

(uu) methylisothiazolinone from 0.005% to 0.015% by weight of the composition;

(vv) Micrococcus lysate from 0.005% to 0.015% by weight of the composition;

(ww) Arabidopsis thaliana extract from 0.005% to 0.015% by weight of the composition;

(xx) plankton extract from 0.005% to 0.015% by weight of the composition;

(yy) carbomer from 0.003% to 0.01% by weight of the composition;

(zz) palmitoyl dipeptide-5diaminohydroxybutyrate from 0.002% to 0.008% by weight of the composition;

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

(bbb) magnesium chloride from 0.001% to 0.004% by weight of the composition;

(ccc) acetyl octapeptide-3 from 0.001% to 0.004% by weight of the composition;

(ddd) pentapeptide-3 from 0.001% to 0.004% by weight of the composition;

(eee) ceramide 1 from 0.00001% to 0.00004% by weight of the composition; and

(fff) fragrance from 0.3% to 1.0% by weight of the composition.

6. The method of claim 5 , wherein the formulation further comprises niacinamide from 0.5% to 2.5% by weight of the formulation.

7. The method of claim 1 , wherein the 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.

8. The use method of claim 1 , wherein the formulation comprises

(a) water from 25% to 75% by weight of the composition;

(b) glycerin from 5% to 15% by weight of the composition;