中国药房2018，Vol.29Issue(5)：611-614,4.DOI:10.6039/j.issn.1001-0408.2018.05.09
麦胚凝集素修饰的长春瑞滨阳离子脂质体的处方优选及细胞毒性试验
Optimization of Wheat Germ Agglutinin Modified Vinorelbine Cationic Liposomes Formulation and Cytotoxicity Test
摘要
Abstract
OBJECTIVE: To prepare Wheat germ agglutinin (WGA) modified vinorelbine (VRB) cationic liposomes (WGA-VRB cationic liposomes), and to optimize the formulation and conduct cytotoxicity test.METHODS: Thin-film diffusion and ammonium sulfate gradient method were used to prepare WGA-VRB cationic liposomes using phospholipid and cholesterol as excipient, 3β-[N-(N' -N' -dimethyl aminoethane) -carbamoyl] cholesterol hydrochloride (DC-Chol) as cationic material, distearoyl phosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) as long cycle chain. Using encapsulation rate as index, central composite design-response surface methodology was used to optimize the amount of DC-Chol, cholesterol and VRB. The contents of VRB in VRB liposomes and WGA-VRB cationic liposomes were determined. The effects of them and blank cationic liposomes on survival rates of human breast cancer cell MCF-7 and human non-small cell lung cancer cells A549 were compared. RESULTS: The optimal formulation of 5 mL WGA-VRB cationic liposomes was as follows as phospholipid 22 mg, cholesterol 12 mg, DC-Chol 8 mg, VRB 0. 5 mg. Encapsulation rate of the liposomes was (92. 24 ± 1. 21)％ (n=3), relative error of which to predicted value was 5. 3％. The contents of VRB in VRB liposomes and WGA-VRB cationic liposomes were (96. 01 ± 3. 26), (93. 39 ± 1. 59) μg/mL(n=3). Compared with blank cationic liposomes and VRB liposomes, WGA-VRB cationic liposomes could significantly reduce survival rate of MCF-7 and A549. CONCLUSIONS: WGA-VRB cationic liposomes are prepared successfully. Inhibitory effect of WGA-VRB cationic liposomes on MCF-7 and A549 cell survival is stronger than that of VRB liposomes.关键词
麦胚凝集素/长春瑞滨/阳离子脂质体/处方优选/星点设计-响应面法/含量测定Key words
Wheat germ agglutinin/Vinorelbine/Cationic liposomes/Formulation optimization/Central composite design-response surface methodology/Content determination分类
医药卫生引用本文复制引用
肖瑶,王鑫,符敏,刘晶晶,李学涛,程岚..麦胚凝集素修饰的长春瑞滨阳离子脂质体的处方优选及细胞毒性试验[J].中国药房,2018,29(5):611-614,4.基金项目
国家自然科学基金资助项目(No.81541081 （）
81673603) （）
