Methods and formulations for transdermal administration

• US 20160235851A1
• Filed: 12/23/2015
• Published: 08/18/2016
• Est. Priority Date: 02/17/2015
• Status: Abandoned Application

• Current Assignee: Dyve Biosciences, Inc.
• Original Assignee: Intellectual Property Associates, LLC
• Inventors: Beal, Ryan R., Burnham, Philippe H., Sand, Bruce J.
• Application Number:
  US14/757,703
• Publication Number:
  US 20160235851A1
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61F 13/00063 comprising medicaments or additives, e.g. odor control, PH control, debriding, antimicrobic drug delivery dressings A61K9/70; chemical aspect of the additives A61L15/00
• CPC Class Codes: A61F 13/02 Adhesive bandages or dressings
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 31/196 the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
• CPC Class Codes: A61K 31/197 the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid carnitine A61K31/205
• CPC Class Codes: A61K 31/205 Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• CPC Class Codes: A61K 31/245 Amino benzoic acid types, e.g. procaine, novocaine salicylic acid esters A61K31/60
• CPC Class Codes: A61K 31/454 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/7004 Monosaccharides having only carbon, hydrogen and oxygen atoms
• CPC Class Codes: A61K 31/7076 containing purines, e.g. adenosine, adenylic acid
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61K 38/06 Tripeptides
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 47/24 : containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 47/28 : Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
• CPC Class Codes: A61K 8/0291 : Micelles
• CPC Class Codes: A61K 8/042 : Gels
• CPC Class Codes: A61K 8/34 : Alcohols
• CPC Class Codes: A61K 8/36 : Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 8/37 : Esters of carboxylic acids
• CPC Class Codes: A61K 8/42 : Amides
• CPC Class Codes: A61K 8/4953 : containing pyrimidine ring derivatives, e.g. minoxidil
• CPC Class Codes: A61K 8/553 : Phospholipids, e.g. lecithin
• CPC Class Codes: A61K 8/86 : Polyethers
• CPC Class Codes: A61K 9/0014 : Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/06 : Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/1075 : Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 21/00 : Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 3/00 : Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61Q 19/08 : Anti-ageing preparations
• CPC Class Codes: A61Q 7/00 : Preparations for affecting hair growth

Abstract

Improved formulations for topical treatment that ensure at least localized transdermal or systemic delivery of an active agent through skin, nails or hair follicles are disclosed.

Claims

1. A formulation for transdermal delivery of an active agent through the skin, nail or hair follicle of a subject, which formulation comprises at least one active agent in an amount effective for treatment of a condition in said subject and

benzyl alcohol—

0.5-20% w/w of said formulation; and

lecithin organogel—

25-70% w/w of said formulation.

2. The formulation of claim 1 wherein the lecithin organogel is present at 30%-60% w/w.

3. The formulation of claim 1 wherein the lecithin organogel is a combination of soy lecithin with isopropyl palmitate.

4. The formulation of claim 1 which further comprises

nonionic surfactant—

2-25% w/w of said formulation; and

polar solvent at least in an amount in molar excess of the nonionic surfactant.

5. The formulation of claim 4 wherein the polar solvent completes the formulation.

6. The formulation of claim 4 wherein the nonionic surfactant is a poloxamer and the polar solvent is water.

7. The formulation of claim 1 which is essentially anhydrous and further comprises nonionic surfactant and bile salt wherein the bile salt is present at 1-15% w/w and the surfactant is provided in powdered form at 20-60% w/w.

8. The formulation of claim 1 which further contains an antioxidant.

9. The formulation of claim 1 wherein at least two active agents are included in said formulation.

10. The formulation of claim 1 wherein the formulation comprises micelles.

11. The formulation of claim 1 wherein the formulation has a pH of 9-11.

12. The formulation of claim 1 wherein an active ingredient is an anesthetic, a fat-dissolving agent, a nutrient or nutrient combination, a tissue volume enhancer, a vaccine component, a hair growth modulator, an antifungal agent, an agent to promote smoking cessation, and/or a cannabinoid.

13. The formulation of claim 1, which comprises an active agent in an amount effective for treatment of a condition in said subject;

and

benzyl alcohol—

0.5-20% w/w of said formulation;

lecithin organogel—

30-60% w/w of said formulation; and

the remainder of the formulation a 20%-40% w/w nonionic detergent in a polar solvent.

14. The formulation of claim 1, which comprises an active agent in an amount effective for treatment of a condition in said subject;

and

benzyl alcohol—

0.5-20% w/w of said formulation;

lecithin organogel—

30-60% w/w of said formulation;

bile salt—

5-15% w/w of said formulation; and

the remainder of the formulation a nonionic detergent.

15. A method to effect transdermal delivery of an active ingredient, which method comprises applying to the skin, nails or hair follicles of a subject an effective amount of the formulation of claim 1.

19. The method of claim 15 wherein said treating is of skin and which further includes, following said treating, applying a composition comprising linoleic acid to the area of treatment.

21. A penetrant composition which comprises sufficient lecithin organogel, benzyl alcohol, surfactant, polar solvent and/or bile salt to result, when mixed with active agent, the formulation of claim 1.

16. A method to dissolve localized fat in a subject which comprises treating the skin proximal to the localized fat with a formulation comprising benzyl alcohol in the range of 0.5% w/w-20% w/w, lecithin organogel in the range of 0.5% w/w-70% w/w, and bile salt in the range of 5-15% w/w.

17. The method of claim 16 wherein said formulation further comprises an effective amount of anesthetic.

20. The method of claim 16 which further includes, following said treating, applying a composition comprising linoleic acid to the area of treatment.

18. A method to alleviate pain associated with dissolving localized fat in a subject which method comprises, along with said dissolving, applying to the area wherein said dissolving is performed a formulation comprising benzyl alcohol in the range of 0.5% w/w-20% w/w, lecithin organogel in the range of 0.5% w/w-70% w/w and an effective amount of anesthetic.

22. A formulation for transdermal delivery of an active agent through the skin, nail or hair follicle of a subject, which formulation comprises at least one active agent in an amount effective for treatment of a condition in said subject and

benzyl alcohol—

0.5-20% w/w of said formulation;

lecithin organogel—

0.5-70% w/w of said formulation;

bile salt—

1-15% w/w of said formulation; and

surfactant—

20-60% w/w of said formulation.