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Topical gel compositions including polycaprolactone polymer and methods for enhancing the topical application of a benefit agent

Inactive Publication Date: 2015-06-25
JOHNSON & JOHNSON CONSUMER COPANIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention provides a topical product made of polycaprolactone polymer, lower alcohol, and co-solvent. This product can be used in personal care and helps to enhance the application of benefit agents.

Problems solved by technology

Although effective, these compositions can be difficult to manufacture and the cost of the products are relatively high.
However, PCL has not been shown as a skin permeation enhancing component in a topical composition to enhance a topical applied drug to penetrate into the intact skin.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0069]Polycaprolactone diol was purchased from Polysciences, Inc. (Warrington, Pa.). One sample was 1,250 Daltons; the other sample was molecular weight 2,000 Daltons.

[0070]A gel was made with the ingredients in Table 1 and following the procedure below:

TABLE 1Chemical NameFormula AFormula BFormula CEthyl Alcohol20.0020.0020.00Pentylene Glycol4.004.004.00Glycerin12.0012.0012.00Lactic Acid3.203.203.20Minoxidil5.005.005.00Butylated0.100.100.10HydroxytolueneWater52.2049.249.2Steareth-101.501.51.5Steareth-22.002.002.00Polycaprolactone diol0.03.00.0(Mwt = 1250)Polycaprolactone diol0.00.03.0(Mwt = 2000)Total100.00100.00100.00

[0071]Step 1—20 parts of ethyl alcohol, 4 parts of pentylene glycol, 12 parts of glycerin, 3.2 parts of lactic acid, 0.10 parts of butylated hydroxytoluene, and 5 parts of minoxidil were added to a glass container and mixed until the solution is clear at room temperature.

[0072]Step 2—In a separate glass container, 49.2 parts of water, 3 parts of polycaprolactone diol ...

example 2

In Vitro Skin Permeation of 5% Minoxidil Compositions Through Human Cadaver Skin

[0074]A skin penetration study evaluated the penetration of minoxidil into different skin layers for the inventive samples (Formulas B and C) prepared as disclosed in Example 1 vs. a test sample without the PCL polymer (Formula A). A well-known Franz diffusion cell method (as taught in US20020006418 A1, which is hereby incorporated by reference) was used. Franz cells had a diameter of 0.5 cm2 and a volume of liquid receptor of 5 ml. A magnetic stirrer bar was added in the donor compartment. The liquid receptor was filled with Phosphate-buffered saline (PBS) solution. Air bubbles in the donor compartment were removed. The system was thermostated at 37° C. above a magnetic stirrer to ensure the homogeneity of the liquid receptor during the experiment. A cadaver skin sample from a commercial tissue bank (Ohio Valley Tissue and Skin Center, Cincinnati, Ohio, dermatomed to approximately 0.4 mm) was cut to fit...

example 3

[0077]Polycaprolactone diol was purchased from Polysciences, Inc. (Warrington, Pa.). One sample was 1,250 Daltons; the other sample was molecular weight 2,000 Daltons.

[0078]Gels were made with the ingredients in Table 4 and following the procedure below:

TABLE 4Chemical NameFormula DFormula EEthyl Alcohol, USP20.0020.00(95%)Pentylene Glycol4.004.00Glycerin12.0012.00Sodium Hydroxide1.001.00Ibuprofen5.005.00Butylated0.100.10HydroxytolueneWater51.4051.40Steareth-101.501.50Steareth-22.002.00Polycaprolactone diol1.00.0(Mwt = 1250)Polycaprolactone diol0.01.0(Mwt = 2000)Sodium Hydroxide (20%Adjust theAdjust thein water)aqueousaqueousphase tophase topH 6pH 6WaterAdd To 100Add To 100Hydroxypropylcellulose1.001.00(KLUCEL, HF Pharm)Total101.00101.00

[0079]Step 1—20 parts of ethyl alcohol, 4 parts of pentylene glycol, 12 parts of glycerin, 0.10 parts of butylated hydroxytoluene, 5 parts of ibuprofen, and 30 parts of purified water were added to a glass container. The pH was adjusted to pH 6 using...

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Abstract

A composition comprising: a benefit agent; at least one polymer including a polycaprolactone polymer; at least one lower alcohol; and at least one co-solvent; and a method for enhancing topical delivery of a benefit agent is disclosed.

Description

[0001]The present invention relates to compositions and methods for enhancing the topical application of a benefit agent. The compositions may be gels including a benefit agent, at least one polymer including a polycaprolactone polymer, at least one lower alcohol, and at least one co-solvent. The compositions are useful in topically applied personal care applications.BACKGROUND OF THE INVENTION[0002]Liquid compositions for delivering benefit agents are well known. Typical formulations include solutions, emulsions, suspensions and gels. The viscosity may vary based on intended area for application, intended use (leave on or rinse off), or consumer preference. Liquids are typically easy to dispense and spread out. There is a continuing need for improved liquid compositions.[0003]There is also a need for compositions that improve skin penetration of benefit agents. U.S. Pat. No. 6,419,913 teaches micellar compositions that enhance skin penetration. Although effective, these composition...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K31/506A61K47/10
CPCA61K47/34A61K31/506A61K47/10A61K8/345A61Q19/00A61K9/0014A61K8/34A61Q19/02A61Q19/08A61K8/85A61K31/192A61P17/00A61P17/10A61P17/14A61P25/04A61P29/00A61P31/04A61P31/12A61P43/00A61K8/4953A61Q7/00A61K8/042A61K2800/591
Inventor SUN, YINGGOSIEWSKA, ANNAJAMIOLKOWSKI, DENNISWU, JEFFREY M.
Owner JOHNSON & JOHNSON CONSUMER COPANIES
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