Abstract

Skin is an attractive site for drug administration partly because of its easy accessibility and favorable properties (e.g., less invasiveness and high patient compliance) over some other common routes of administration. Despite this, the efficiency in transdermal drug delivery has been largely limited by poor skin permeation. To address this problem, this study reports the generation of oleic acid-containing vesicles, which can enhance the drug delivery efficiency while showing good stability and limited skin disruption. Upon being loaded into a complex gel, along with the incorporation of the polymer blending technique, a delivery system exhibiting tunable transdermal flux of 2,3,5,4′-tetrahydroxystilbene 2-O-β-D-glucoside is reported. Taking the good biocompatibility and tunable delivery performance into account, our system warrants further development and optimization for future applications in the treatment of skin diseases.

Highlights

  • Skin makes an attractive site for drug delivery partly because of its easy accessibility and favorable properties over other common routes of administration

  • This study reports the generation of oleic acid-containing vesicles, which can enhance the drug delivery efficiency while showing good stability and limited skin disruption

  • We take advantage of the close relationship between the composition and swelling/erosion behavior of our gel and integrate the gel with the vesicles to generate a biocompatible system which enables the transdermal flux of 2,3,5,4 -tetrahydroxystilbene 2-O-β-D-glucoside (THSG) to be manipulated

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Summary

Introduction

Skin makes an attractive site for drug delivery partly because of its easy accessibility and favorable properties over other common routes of administration. Transdermal drug delivery, has yet to fully achieve its potential as a drug administration method alternative to hypodermic injection at the moment. This is true for hydrophilic drugs, in which the efficiency in transdermal drug delivery is largely affected by their inability to enter the skin at a therapeutically useful rate [1]. We have adopted a polymer blending technique to generate a gel system for controlled co-delivery of multiple drugs, with the release rate of each of the co-delivered drugs being able to be fine-tuned to meet the practical needs of a therapeutic regimen [7,8]. THSG is, a drug candidate that shows potential to be further developed into a transdermal formulation for real applications

Materials
Synthesis of Oleic Acid-Containing Vesicles
Determination of Size Distribution
Generation of a Vesicle-Loaded Complex Gel
Mechanical Strength and Rheological Measurement
Determination of the Swelling and Erosion Behavior
Cytotoxicity Assay
Skin Preparation
2.10. Skin Permeation Analysis
Characterization of Oleic Acid-Containing Vesicles as Transdermal Carriers
Properties of the Complex Gels for Sustained Vesicle Release
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