Multivesicular liposome formulation for the sustained delivery of breviscapine.
Breviscapine, a well-known bioactive flavonoid ingredient extracted from the traditional Chinese medicine, has been extensively used in clinic to treat ischemic cerebrovascular and cardiovascular diseases in China. In order to prolong the duration of the drug in the circulation, reduce the frequency of injection administration and subsequently afford patient compliance, multivesicular liposome (MVL, namely DepoFoam) was utilized as a sustained-delivery system for breviscapine. In vitro release and in vivo pharmacokinetics of MVLs containing breviscapine (bre-MVLs) following intramuscular injection to rats were investigated compared with those of traditional liposomes containing breviscapine (bre-TLs). The drug durations both in vitro and in vivo were significantly prolonged for the bre-MVL, and that the drug release in vitro and the absorption in vivo showed a good linear correlation (R=0.9834), which provided an evidence for the suitability to select human plasma as the medium of drug release from MVLs in vitro. Drug release from bre-MVLs (triolein/tricaprylin, 10/0) in vitro extended a long period of 5-6 days, while the bre-TLs released 80% within only 4h. The mean residence time (MRT) obtained from the pharmacokinetics study of bre-MVL was about 16.6- and 5.04-fold longer than those of breviscapine solution (BS) and bre-TL, respectively. A duration in vivo for a period of 4-5 days was fulfilled for bre-MVL. In conclusion, MVL can be successfully used as a sustained delivery system of breviscapine.
Zhong
Haijun
H
Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, P.O. Box 52, No. 103 Wenhua Road, Shenyang City, Liaoning Province 110016, PR China. effzhj@sina.com
Deng
Yingjie
Y
Wang
Xiumin
X
Yang
Binghua
B
D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D047310:Apigenin / Q000737:chemistry; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005079:Excipients; D005260:Female; D005419:Flavonoids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005965:Glucuronates / Q000737:chemistry; D007273:Injections, Intramuscular; D008081:Liposomes; D008297:Male; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar
D000925:Anticoagulants; D003692:Delayed-Action Preparations; D005079:Excipients; D005419:Flavonoids; D005965:Glucuronates; D008081:Liposomes; C061097:breviscapine; C484876:scutellarin; D047310:Apigenin