Cyclodextrin-Based Microemulsions, and Dermatological Uses Thereof

a technology of cyclodextrin and microemulsion, which is applied in the direction of biocide, drug composition, aerosol delivery, etc., can solve the problems of skin dryness, volatile lower alcohol composition, extremely flammable volatile lower alcohol microemulsion, etc., and achieve uneven skin tone and increase pore size

Inactive Publication Date: 2013-09-26
PRECISION DERMATOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015]In certain embodiments, the invention relates to any one of the aforementioned methods, wherein the treatment or prevention o...

Problems solved by technology

However, topical application of volatile lower alcohols has a drying effect on the skin.
Additionally, volatile lower alcohols and compositions containing them are extremely flammable.
For these reasons, volatile lower alcohol-containing microemulsions for topical application have seen limited commercial use.
Developing a formulation for a water-immiscible drug that displays d...

Method used

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  • Cyclodextrin-Based Microemulsions, and Dermatological Uses Thereof
  • Cyclodextrin-Based Microemulsions, and Dermatological Uses Thereof
  • Cyclodextrin-Based Microemulsions, and Dermatological Uses Thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Spontaneous Microemulsion Formation by Mixtures of a Caprylocaproyl Polyethylene Glycol-Based Surfactant and Cyclodextrin in Aqueous Media

[0936]Microemulsion preparation: Any two components (examples: Labrasol®-water, HPXCD-water, or Labrasol®-HPXCD) were mixed (in different ratios) in different scintillation vials and then the third component was titrated to each vial until a clear-to-turbid or turbid-to-clear transition occurred (in simple situations). Finally wt % percentages data for each component (Labrasol®, water, and cyclodextrin) were plotted to construct the ternary phase diagram. See FIG. 2.

[0937]In FIG. 3, the “water” phase (above) was replaced with an “aqueous” phase. An example of an aqueous phase is shown in FIG. 5.

example 2

Solubility / Dispersibility of Retinol in the Labrasol®-HPGCD-Water Systems and in Labrasol®, HPGCD, and Water, Individually

[0938]Materials

[0939]Drug used: 1. Solid Retinol (98%) from Sigma, 2. Retistar (5% Retinol, caprylic / capric triglyceride, sodium ascorbate, Tocopherol) from BASF, 3. Retinol 50C (50% retinol, ethoxylated sorbitan monolaurate (Tween 20), butylated hydroxytoluene (BHT), 2-(1,1-dimethylethyl)-4-methoxy-phenol) from BASF.

[0940]Cyclodextrin used: hydroxypropyl-X-cyclodextrin (X=alpha, beta, or gamma).

[0941]Methods

[0942]Vial L from FIG. 4(a) shows the formation of a novel microemulsion (clear transparent system) as well as complete miscibility of Retistar (final retinol concentration: 0.06%) in Labrasol®-HPGCD-water microemulsion system (Note: capric / caprylic triglycerides coming from the Retistar are also contributing to the microemulsion system). The miscibility of retinol may be attributed to the drug incorporation in the cyclodextrin system as well as the micro emu...

example 3

Encapsulation of Pharmaceutical / Cosmetic Ingredients in CD-Stabilized Microemulsions

[0946]Materials

[0947]Retinol used: 1. Solid retinol (98%) from Sigma, 2. Retistar (5% retinol, caprylic / capric triglyceride, sodium ascorbate, tocopherol) from BASF, 3. Retinol 50C (50% retinol, ethoxylated sorbitan monolaurate, BHT, 2-(1,1-dimethylethyl)-4-methoxy-phenol from BASF

[0948]Methods

[0949]Microemulsion Preparation:

[0950]Any two components (examples: Labrasol®-water, cyclodextrin-water, or Labrasol®-HPBCD) were mixed (in different ratios) in different scintillation vials and then the third component was titrated to each vial until a clear-to-turbid or turbid-to-clear transition occurred (in simple situations). Finally wt % percentages data for each component (Labrosol, water, and cyclodextrin) were plotted to construct the ternary phase diagram.

[0951]Incorporation of Drug:

[0952]Drug can be dissolved in the individual components or any of the two-component combination systems, followed by mi...

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Abstract

Described herein are cyclodextrin-stabilized microemulsion systems useful for increasing the solubility, stability, bioavailability, or safety of an active agent for delivery to the skin. The microemulsions may reduce the occurrence of skin irritation or odor upon application. In certain embodiments, the active agent is substantially insoluble in water. The microemulsions may be formulated as semi-solids, for example creams, or as aerosol or non-aerosol foams. Also described are methods of treating skin disorders, comprising the step of applying to an affected area of a subject in need thereof a therapeutically-effective amount of an inventive microemulsion.

Description

RELATED APPLICATIONS[0001]This application claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 61 / 614,177, filed Mar. 22, 2012, the contents of which are hereby incorporated by reference.BACKGROUND[0002]Microemulsions are thermodynamically-stable, optically-clear emulsions having submicron-sized droplets suspended in a continuous phase. These emulsions form spontaneously, and typically consist of an aqueous phase, an organic phase, and a surfactant / co-surfactant component.[0003]Previous data suggest that volatile lower alcohols, such as ethanol, are required to maintain stable oil-in-water microemulsions. However, topical application of volatile lower alcohols has a drying effect on the skin. Additionally, volatile lower alcohols and compositions containing them are extremely flammable. For these reasons, volatile lower alcohol-containing microemulsions for topical application have seen limited commercial use.[0004]Developing a formulation for a water-immi...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K8/67A61K31/07A61K8/73A61Q19/08
CPCA61K31/455A61K8/39A61K8/068A61K47/40A61K9/1075A61Q19/08A61K31/07A61K8/671A61K9/0014A61K8/738A61K2300/00A61P17/00A61P17/16A61K33/08A61K47/14A61K8/92
Inventor MAJHI, PINAKI RANJANTRUMBORE, MARK W.
Owner PRECISION DERMATOLOGY
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