[Transdermal and lymph targeting transfersomes of vincristine].
Vincristine (VCR) is mainly used to treat acute lymphocytic leukemia, Hodgkin and non-Hodgkin lymphoma in clinic with definite therapeutic effect. But the obvious neurotoxicity and local stimulation of which limit its clinic use. In order to increase the lymph targeting to enhance the curative effect and to lower the adverse reaction of VCR, the VCR loaded transfersomes (VCR-T) were prepared with dry-film and ultrasonic dispersing methods, and the corresponding pharmaceutical properties, pharmacokinetical characteristics and the targeting ability were studied. The average particle size of VCR-T prepared was 63 nm with an entrapment ratio of 59%. The in vitro transdermal research with modified Franz cell showed that VCR-T permeated through the skin in accordance with polynomial equation, and with an accumulation permeation percentage of 67.4% up to 12 h. An HPLC method was utilized to determine the pharmacokinetics and tissue distribution of VCR. Compared with the iv injection of VCR solution, the retention time of VCR in blood was extended by 12 times with VCR-T, and the targeting index in rat lymph was increased by 2.75 times. As a result, transfersomes could penetrate the skin and enter into the systemic circulation carrying VCR with good lymph targeting ability, which makes it probably a new lymphtic targeting drug delivery system.
Lu
Yi
Y
West China School of Pharmacy, Sichuan University, Chengdu 610041, China. toluyi@163.com
Hou
Shi-xiang
SX
Zhang
Liang-ke
LK
Li
Ye
Y
He
Jun-yao
JY
Guo
Dan-dan
DD
D000279:Administration, Cutaneous; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D019540:Area Under Curve; D016503:Drug Delivery Systems; D008081:Liposomes / Q000737:chemistry; D008198:Lymph Nodes / Q000378:metabolism*; D008297:Male; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D013154:Spleen / Q000378:metabolism; D013501:Surface-Active Agents / Q000737:chemistry; D014018:Tissue Distribution; D014750:Vincristine / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics
D000972:Antineoplastic Agents, Phytogenic; D008081:Liposomes; D013501:Surface-Active Agents; D014750:Vincristine