Methods for topical delivery of prostaglandins to subcutaneous fat
Inventors
Singer, Michael S. • Kalayoglu, Murat V.
Assignees
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Publication Number
US-9849179-B2
Publication Date
2017-12-26
Expiration Date
Abstract
Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid ester (e.g., isopropyl myristate), optionally comprising an ointment base such as a hydrocarbon base (e.g., petroleum jelly) and/or an organic alcohol (e.g., propylene glycol), that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound to subcutaneous fat under the skin, and methods of preparation. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject.
Core Innovation
The invention provides topical compositions and methods for delivering a prostaglandin FP receptor agonist to subcutaneous fat and for reducing body fat in a subject. The composition includes a prostaglandin FP receptor agonist and a fatty acid ester carrier, with petroleum jelly used as an ointment base. Exemplary compounds include latanoprost and tafluprost, and related compounds such as bimatoprost and travoprost are described.
The invention addresses local reduction of body fat by administering the topical composition to a site that includes subcutaneous fat. The described sites include the face, periorbital region, eyelids, and other body regions, and the document references steatoblepharon. The formulation is described as achieving efficient skin-to-fat delivery using the fatty acid ester carrier with petroleum jelly, while being non-irritating and well-tolerated.
The disclosure also provides a broad chemical-structure framework for compounds according to Formulas (I-a)–(I-f), Formula I-n, Formula II, and related formula variants, with substituents such as R1, R2, Z, X, L, A, B, Y, (Y)n, x, y, and heteroatom linkage group G. The framework includes pharmaceutically acceptable salts and derivatives, stereochemical definitions, and relative stereochemistry, including cis and trans double bonds and whether a double bond is endocyclic or exocyclic.
Claims Coverage
The provided independent claim set contains 1 independent claim. The inventive features focus on a method for reducing body fat via administering a topical composition that contains latanoprost, isopropyl myristate, and petroleum jelly, with dependent claims refining formulation scope, preservative selection, administration frequency, and local reduction of body fat.
Topical body-fat reduction composition for a subject
A method for reducing body fat in a subject, the method comprising administering to the subject a composition comprising latanoprost, isopropyl myristate, and petroleum jelly.
Multi-component w/w composition concentration ranges
The method further specifies formulation concentrations (w/w) for latanoprost, isopropyl myristate, and petroleum jelly within defined ranges.
Composition essentially consisting of specified ingredients
The method is further limited such that the composition essentially consists of latanoprost, isopropyl myristate, and petroleum jelly.
Specific preservative selection
The method is characterized in that the preservative used is chlorobutanol.
About once per day administration
The method is performed by administering the treatment about once per day.
Local reduction of body fat
The method further includes locally reducing body fat in a subject.
Overall, the claim coverage centers on a method of reducing body fat in a subject by administering a topical composition containing latanoprost combined with isopropyl myristate and petroleum jelly, with dependent claims refining ingredient scope, w/w concentration ranges, preservative selection, and administration frequency and target as local body fat.
Stated Advantages
Efficient skin-to-fat delivery.
Surprising performance versus multiple alternative vehicles.
Non-irritating and well-tolerated.
Aesthetic properties.
Stability.
Suitability for sterile ophthalmic-compatible manufacture, including sterile and endotoxin-free processing concepts.
Documented Applications
Topical administration to reduce excess subcutaneous fat at sites including face, periorbital region, and eyelids.
Treatment of steatoblepharon.
Topical administration to reduce local body fat at other body regions.
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