Biodegradable microdepot delivery system for topical delivery
Inventors
XU, Jinjie • TONG, Ho Wang • KWOK, Sau Kuen Connie • HUEN, Ngar Yee
Assignees
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Publication Number
US-9833405-B2
Publication Date
2017-12-05
Expiration Date
Abstract
The present invention provides a biodegradable microdepot delivery system for topical delivery of active ingredients through the skin surface of a subject. The configuration, dimension, and chemical composition of the microdepots allow a relatively short dissolution time of less than 5 minutes while insertion ratio of the microdepots can reach more than 60%, some of which can even reach about 97%, under exertion of a relatively low pressing force. The present invention also provides a method for fabricating the biodegradable microdepot delivery system and a polymeric solution for forming the same.
Core Innovation
The invention provides a polymeric solution for forming an array of microdepots of a biodegradable microdepot delivery system. The polymeric solution comprises one or more biodegradable polymers, a glycosaminoglycan, and a polysaccharide, with the weight ratio of glycosaminoglycan:polysaccharide:biodegradable polymer being 9-11:10-8:1 and the total concentration of Povidone K90, dextran 70 and hyaluronic acid being 50% by volume of the polymeric solution.
In the biodegradable microdepot delivery system for topical application, the array of microdepots is formed from the polymeric solution and is supported by a base. The microdepots are described with cone-shaped, pyramid-shaped, and bevel-angled shapes, together with specified geometry, dimensions, and tip-to-tip distance constraints.
The system is configured for rapid dissolution and skin interaction, with degradation of the microdepot array within 60 minutes on exposure to a skin surface. The array is operable under a force of 0.3 N or less with an insertion efficiency above 60%, and the polymeric formulation can be combined with Niacinamide, Pal-KTTKS, and GHK-Cu.
Claims Coverage
The independent claim is directed to the polymeric solution that forms an array of microdepots, defining three main inventive formulation features together with explicit weight-ratio and total concentration constraints. Dependent claims further add optional active ingredients and define microdepot and system characteristics, including geometry, tip-to-tip distance, degradation, insertion efficiency, and fabrication details.
Polymeric solution with specified HA/dextran 70/Povidone K90 weight ratio
A polymeric solution comprising one or more biodegradable polymers, a glycosaminoglycan, and a polysaccharide, wherein the weight ratio of glycosaminoglycan:polysaccharide:biodegradable polymer is 9-11:10-8:1.
Povidone K90 as biodegradable polymer with specified total concentration
The polymeric solution wherein the one or more biodegradable polymers is Povidone K90, the polysaccharide is dextran 70, the glycosaminoglycan is hyaluronic acid, and the total concentration of Povidone K90, dextran 70 and hyaluronic acid is 50% by volume of the polymeric solution.
Biodegradable microdepot delivery system with microdepot array supported by a base
A biodegradable microdepot delivery system for topical application having an array of microdepots formed from the polymeric solution, supported by a base, wherein the microdepot geometry and dimensions fall within specified aseptic ratio, height, and base width ranges and are formed as one of cone-shaped, pyramid-shaped, or bevel-angled shapes.
Microdepot array degradation and insertion efficiency under low force
A biodegradable microdepot delivery system wherein the array degrades within 60 minutes on exposure to a skin surface under a force of 0.3 N or less with an insertion efficiency above 60%.
Active ingredients comprising Niacinamide, Pal-KTTKS, and GHK-Cu
The at least one active ingredient comprises Niacinamide, Pal-KTTKS, and GHK-Cu.
Microdepot tip-to-tip distance constraint
The system includes two microdepots whose tip-to-tip distance is between 500 and 600 μm.
Across the independent claim and its refinements, the claim coverage centers on a polymeric solution defined by hyaluronic acid, dextran 70, and Povidone K90 with explicit weight-ratio and 50% by volume total concentration constraints. Dependent claims then specify microdepot-array and system geometries, degradation and insertion behavior on skin under low force, and named active ingredients.
Stated Advantages
Rapid dissolution/degradation behavior of the microdepot array on exposure to a skin surface.
High skin insertion efficiency, with insertion efficiency above 60% and up to about 97% reported in the provided description.
Operability under low pressing force, described as 0.3 N or less.
Compatibility with topical delivery of active ingredients including Niacinamide, Pal-KTTKS, and GHK-Cu.
Documented Applications
Topical application of a biodegradable microdepot delivery system for delivering active ingredients.
Use of the microdepot array on exposure to a skin surface to achieve microdepot insertion, as evaluated by skin insertion testing described in the provided content.
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