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Microemulsions vs chitosan derivative-coated microemulsions for dermal delivery of 8-methoxypsoralen

Authors Wu JY, Li YJ, Liu TT, Ou G, Hu XB, Tang TT, Wang JM, Liu XY, Xiang DX

Received 23 October 2018

Accepted for publication 3 February 2019

Published 1 April 2019 Volume 2019:14 Pages 2327—2340


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Dr Lei Yang

Jun-Yong Wu,1–3,* Yong-Jiang Li,1–3,* Ting-Ting Liu,1–3 Ge Ou,1–3 Xiong-Bin Hu,1–3 Tian-Tian Tang,1–3 Jie-Min Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–3

1Department of Pharmacy, Second Xiangya Hospital, Central South University, Changsha, Hunan 410011, People’s Republic of China; 2Institute of Clinical Pharmacy, Central South University, Changsha, Hunan 410011, People’s Republic of China; 3Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drugs, Changsha, Hunan, People’s Republic of China

*These authors contributed equally to this work

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.

Keywords: 8-methoxypsoralen, microemulsion, chitosan-coated microemulsion, ex vivo permeation, microdialysis, pharmacokinetics

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