[Preparation and in vitro and in vivo evaluations of topically applied capsaicin transfersomes].
OBJECTIVE
To prepare capsaicin transfersomes and evaluate them in vitro and in vivo.


METHODS
Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated by entrapment efficiency, release rate, in vitro skin permeation and distribution in different tissues in vivo.


RESULTS
Capsaicin transfersomes were composed of single unilamellar vesicles with an average diameter of 150.6 nm. Capsaicin entrapment efficiency increased distinctly with increasing of concentration of lecithin and entrapment efficiency is 96.7% while concentration of lecithin to 8%. Cumulative release amount of capsaicin is in direct proportion to the ethanol concentration in the receptor medium. In vitro capsaicin cumulative penetration amount showed higher levels in transfersomes than cream and suspension in rat abdominal skin. Abdominal skin cumulative penetration amount in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men. In the same way, abdominal skin epidermal membrane cumulative penetration amount in vitro of capsaicin transfersomes was significantly higher than that from derma and full skin in human abdominal skin. The capsaicin tissue distribution of capsaicin injection by multiple celiac injections in rats is different: bone > plasma > skin > muscle. There is a similar result by multiple thigh topical application of capsaicin transfersomes: bone > skin > plasma > muscle.


CONCLUSIONS
Entrapment efficiency of capsaicin transfersomes reached the criterion of China Pharmacopoeia (> 80%) and capsaicin skin penetration can be increased by capsaicin transfersomes. It should be noted that the diverse characters and levels of skin may probably affect the permeating capability of capsaicin. Capsaicin tissue distribution in bone and muscle is similar and is different in plasma and skin by multiple injections and topical skin apply.
Xiao-Ying
Long
L
Southern Medical University, Guangzhou 510515, China. longxy3156@163.com
Luo
Jia-Bo
JB
Yan
Zhi-Hong
ZH
Rong
Hui-Si
HS
Huang
Wei-Min
WM
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002211:Capsaicin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D006801:Humans; D054709:Lecithins / Q000737:chemistry; D008297:Male; D051379:Mice; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D020358:Sodium Cholate / Q000737:chemistry; D014018:Tissue Distribution
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D054709:Lecithins; D020358:Sodium Cholate; D002211:Capsaicin