Transfersomes - A novel vesicular carrier for enhanced transdermal delivery: Development, characterization, and performance evaluation

被引:305
作者
Jain, S [1 ]
Jain, P [1 ]
Umamaheshwari, RB [1 ]
Jain, NK [1 ]
机构
[1] Dr Hari Singh Gour Vishwavidyalaya, Dept Pharmaceut Sci, Pharmaceut Res Lab, Sagar 470003, Madhya Pradesh, India
关键词
deformable liposomes; transdermal; delivery; dexamethasone;
D O I
10.1081/DDC-120025458
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This work describes the use of a novel vesicular drug carrier system called transfersomes, which is composed of phospholipid, surfactant, and water for enhanced transdermal delivery. The transfersomal system was much more efficient at delivering a low and high molecular weight drug to the skin in terms of quantity and depth. In the present study transfersomes and liposomes were prepared by using, dexamethasone as a model drug. The system was evaluated in vitro for vesicle shape and size, entrapment efficiency, degree of deformability, number of vesicles per cubic turn, and drug diffusion across the artificial membrane and rat skin. The effects of surfactant type, composition, charge, and concentration of surfactant were studied. The in vivo performance of selected formulation was evaluated by using a carrageenan-induced rat paw edema model. Fluorescence microscopy by using rhodamine-123 and 6-carboxyfluorescein as fluorescence probe was performed. The stability study was performed at 4degreesC and 37degreesC. An in vitro drug release study has shown a nearly zero order release of drug and no lag phase. The absence of lag phase in comparison to liposomes and ointment is attributed to the greater deformability, which may account for better skin permeability of transfersomes. In vivo studies of transfersomes showed better antiedema activity in comparison to liposomes and ointment, indicating better permeation through the penetration barrier of the skin. This was further confirmed through a fluorescence microscopy study. Finally, it may be concluded from the study that complex lipid molecules, transfersomes, can increase the transdermal flux, prolong the release, and improve the site specificity of bioactive molecules.
引用
收藏
页码:1013 / 1026
页数:14
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