Preparation and characteristic of vinorelbine bitartrate-loaded solid lipid nanoparticles.
A hydrophilic and temperature-induced degradation drug, vinorelbine bitartrate (VB)-loaded solid lipid nanoparticles (SLNs) were prepared by a cold homogenization technique. The physicochemical properties of the SLNs, with various lipid composition, drug content and altered homogenizing times, were investigated. The mean particle size of the SLNs ranged from 150 to 350 nm. The enhancement of lecithin content in lipid matrix resulted in smaller particle of SLNs. The atomic force microscopy (AFM) images displayed that the shape of the SLNs was irregular sphere with smooth surface. The drug entrapment efficiency (EE) could be improved with the increasing of lecithin or oleic acid content in lipid matrix, and reduced with the added amount of drug. The highest EE and drug loading capacity (DL) could reach up to 80 and 6.6%, respectively. The studies of drug release showed that the drug release could last for 48 h, and the rate was delayed by the addition of lecithin or oleic acid in the formulations. The physical stability experiment indicated that the SLNs were stable for 2 months under room temperature. Moreover, the cellular cytotoxicity of VB against MCF-7 cells could be improved by the entrapment of SLNs.
You
Jian
J
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China. youjiandoc@zju.edu.cn
Wan
Feng
F
de Cui
Fu
F
Sun
Yu
Y
Du
Yong-Zhong
YZ
Hu
Fu Qiang
FQ
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D006801:Humans; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D013499:Surface Properties; D014747:Vinblastine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D000077235:Vinorelbine
D000972:Antineoplastic Agents, Phytogenic; D008055:Lipids; D014747:Vinblastine; D000077235:Vinorelbine