[Preparation and in vitro evaluations of topically applied capsaicin transfersomes].
OBJECTIVE
Capsaicin transfersomes were prepared and its quality specifications were evaluated.


METHODS
Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated on the entrapment efficiency, drugs release rate and in vitro skin permeation.


RESULTS
Capsaicin transfersomes is composed of single unilamellar vesicles, with average size of 150.6 nm. Capsaicin entrapment efficiency achieved 96.7% while concentration of lecithin used was 8%. cumulative release amount of capsaicin was in direct proportion to the ethanol concentration in the medium. The in vitro rate cumulative penetration rate of capsaicin was higher in transfersomes than in cream and suspension in rats. Adomen skin cumulative penetration rate in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men. In the same way,cumulative penetration rate in vitro of capsaicin transfersomes through abdomen skin epidermal membrance was significantly higher than that with derma and full skin in men.


CONCLUSIONS
Entrapment efficiency of capsaicin transfersomes reached 96.7%, meeting the criterion of China pharmacopia( > 80%), skin penetration of capsaicin was enhanced by a capsaicin transfersomes preparation and was affected by diverse characters and levels of skin.
Long
Xiao-ying
XY
Southern Medical University, Guangzhou 510515, China. longxy3156@163.com
Luo
Jia-bo
JB
Li
Li-ren
LR
Lin
Dan
D
Rong
Hui-si
HS
Huang
Wei-min
WM
D000279:Administration, Cutaneous; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D002211:Capsaicin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D010316:Particle Size; D010713:Phosphatidylcholines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects
D018712:Analgesics, Non-Narcotic; D004337:Drug Carriers; D010713:Phosphatidylcholines; D002211:Capsaicin