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Microemulsions vs chitosan derivative-coated microemulsions for dermal delivery of 8-methoxypsoralen
Jun-Yong Wu1,2,3, Yong-Jiang Li1,2,3, Ting-Ting Liu1,2,3
1Department of Pharmacy, Second Xiangya Hospital, Central South University, Changsha, Hunan 410011, People's Republic of China, xiangdaxiong@csu.edu.cn.
Background:
8-methoxypsoralen (8-MOP) is one of the most commonly utilized drugs in psoralen-ultraviolet A therapy for treatment of vitiligo. However, poor skin retention and systemic side effects limit the clinical application of 8-MOP.
Methods:
Microemulsions (MEs) and chitosan derivative-coated 8-MOP MEs were developed and compared for dermal delivery of 8-MOP. Ex vivo skin retention/permeation study was performed to select the ME formulation with the highest retention:permeation ratio. Four different chitosan-coated MEs were prepared and compared with the ME formulation for their ability to distribute 8-MOP in the skin.
Results:
Among various ME formulations developed, a formulation containing 2.9% ethyl oleate, 17.2% Cromophor EL35, 8.6% ethanol and 71.3% water showed the highest ex vivo skin retention:permeation ratio (1.98). Of four chitosan-coated MEs prepared, carboxymethyl chitosan-coated MEs (CC-MEs) and hydroxypropyl chitosan-coated MEs (HC-MEs) showed higher ex vivo skin retention:permeation ratio (1.46 and 1.84). and were selected for in vivo pharmacokinetic study. AUCskin (0-12 h) for 8-MOP MEs (4578.56 h·ng·mL-1) was higher than HC-MEs (3422.47 h·ng·mL-1), CC-MEs (2808.51 h·ng·mL-1) and tincture (1500.16 h·ng·mL-1). Also, AUCplasma (0-12 h) for MEs (39.35±13.90 h·ng·mL-1) was significantly lower than HC-MEs (66.32 h·ng·mL-1), CC-MEs (59.70 h·ng·mL-1) and tincture (73.02 h·ng·mL-1).
Conclusion:
These combined results suggested that the MEs developed could be a promising and safe alternative for targeted skin delivery of 8-MOP.
Insights
Microemulsions (MEs) enhance skin delivery of 8-methoxypsoralen (8-MOP) for vitiligo treatment. Chitosan-coated MEs improve retention and reduce systemic exposure, offering a safer alternative for targeted dermal delivery.
Area of Science:
- Pharmaceutical Sciences
- Dermatology
- Nanotechnology
Background:
- 8-methoxypsoralen (8-MOP) is a key drug in psoralen-ultraviolet A therapy for vitiligo.
- Poor skin retention and systemic side effects of 8-MOP limit its clinical use.
Purpose of the Study:
- To develop and evaluate microemulsions (MEs) for enhanced dermal delivery of 8-MOP.
- To compare the efficacy of chitosan derivative-coated MEs against conventional MEs and tincture for skin retention and permeation.
Main Methods:
- Formulation of various microemulsions (MEs) with different compositions.
- Preparation and characterization of chitosan-coated 8-MOP MEs (CC-MEs and HC-MEs).
- Ex vivo skin retention/permeation studies and in vivo pharmacokinetic analysis.
Main Results:
- A specific ME formulation showed the highest ex vivo skin retention:permeation ratio.
- Carboxymethyl chitosan-coated MEs (CC-MEs) and hydroxypropyl chitosan-coated MEs (HC-MEs) demonstrated superior skin retention compared to plain MEs.
- Plain MEs exhibited higher skin drug concentration (AUCskin) and significantly lower plasma concentration (AUCplasma) than chitosan-coated MEs and tincture.
Conclusions:
- Microemulsions (MEs) show potential for targeted skin delivery of 8-MOP.
- Chitosan-coated MEs offer improved skin retention and reduced systemic absorption.
- Developed MEs represent a promising and safer alternative for vitiligo treatment.
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