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Development of an Auraptene-Loaded Transdermal Formulation Using Non-ionic Sugar Ester Surfactants
Kathrine Anne Flores1,2, Akie Okada1, Florencio Arce2,3
1Graduate School of Pharmaceutical Sciences, Josai University.
Chemical & Pharmaceutical Bulletin
|March 20, 2024
Summary
Sugar esters enhance the transdermal delivery of auraptene (Aur), a therapeutic compound with low skin penetration. Dispersion-type formulations, particularly with sucrose palmitate, improved Aur skin permeation and retention.
Area of Science:
- Pharmacology
- Materials Science
- Dermatology
Background:
- Auraptene (Aur) is a natural compound with therapeutic benefits but poor skin penetration, limiting its topical application.
- Transdermal drug delivery systems are sought to overcome Aur's low lipophilicity and skin barrier challenges.
- Non-ionic sugar esters (SEs) are biocompatible excipients with potential for enhancing the delivery of challenging molecules.
Purpose of the Study:
- To investigate the efficacy of novel sugar esters (SEs) in improving the transdermal permeation and skin distribution of auraptene (Aur).
- To develop and characterize gel- and dispersion-type formulations for Aur delivery using various SEs.
- To evaluate the skin permeation and retention profiles of Aur delivered via SE-based formulations.
Main Methods:
- Preparation of gel- and dispersion-type formulations containing Aur and different SEs.
- Quantification of Aur entrapment efficiency within the formulations.
- Assessment of Aur skin permeation and deposition using Franz diffusion cells with rat skin.
- Comparison of SE-based formulations against a control formulation.
Main Results:
- Dispersion-type formulations demonstrated higher Aur entrapment efficiency compared to gel-type formulations.
- SE-based dispersion formulations significantly enhanced Aur skin permeation and retention over 8 hours.
- The formulation containing sucrose palmitate (sSP) showed the highest Aur skin permeation.
- Increased Aur concentration in full-thickness skin was observed with the dispersion-type formulation.
Conclusions:
- Sugar esters, particularly in dispersion-type formulations, are effective in enhancing the transdermal delivery of auraptene (Aur).
- Sucrose palmitate shows promise as an excipient for improving Aur's skin permeation and retention.
- The developed SE-based formulations hold potential for pharmaceutical and cosmetic applications requiring effective transdermal Aur delivery.
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