首页|鬼臼毒素脂质体的制备及其质量评价

鬼臼毒素脂质体的制备及其质量评价

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目的 优化鬼臼毒素脂质体(POD-Lps)处方工艺并进行质量评价.方法 采用乙醇注入法制备POD-Lps,建立HPLC法测定脂质体中鬼臼毒素的含量及包封率.以包封率为指标,通过Box-Behnken响应面分析法对处方和工艺进行优化.观察其微观形态,测定其粒径、Zeta电位,并考察体外释放过程.结果 POD-Lps最优处方为:胆固醇和磷脂质量比为1∶14.49,药物和磷脂质量比为1∶32.36,磷酸盐缓冲液pH值5.82,水浴温度55℃.所得的POD-Lps包封率为(87.43±1.8)%,平均粒径为(139.12±9.81)nm,多分散系数(PDI)为(0.21±0.04),Zeta电位为(-26.37±0.36)mV.体外释放研究表明,POD-Lps具有明显的缓释效果.POD-Lps的稳定性较好,4℃条件下放置1个月后,各项指标均没有明显变化.结论 乙醇注入法简单、稳定,可用于POD-Lps的制备.
Preparation optimization and quality evaluation of podophyllotoxin liposomes
Objective To optimize podophyllotoxin liposomes(POD-Lps)and evaluate its quality.Methods POD-Lps were prepared by ethanol injection method.HPLC method was used to determine the content and encapsulation efficiency of POD-Lps.The formulation and process of POD-Lps were optimized by Box-Behnken response surface method.The micromorphology of liposomes was observed by transmission electron microscopy.The particle size,Zeta potential,and in vitro release were determined.Results The optimum technological parameters of POD-Lps were as follows:the ratio of cholesterol to phosphorus was 1∶14.49,the ratio of drug to lipid was 1∶32.36,the pH value of phosphate buffer was 5.82,and the temperature of dissolved lipid solution was 55 ℃.The encapsulation efficiency of POD-Lps was(87.43±1.8)%,the particle size was(139.12±9.81)nm,the polydispersity index was(0.21±0.04),and the Zeta potential was(-26.37±0.36)mV.The in vitro release study showed that POD-Lps had an obvious sustained release effect.POD-Lps had good stability.No obvious change was found in each index of POD-Lps after storing at 4 ℃ for 30 days.Conclusion The ethanol injection method for POD-Lps is rapid,simple and reliable.

podophyllotoxinliposomeethanol injection methodBox-Behnken response surface methodencapsulation efficiency

张朗朗、戴粤湘、张涵、郭波红、索绪斌

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广东药科大学药学院,广州 510006

广东药科大学中药学院,广州 510006

鬼臼毒素 脂质体 乙醇注入法 Box-Behnken响应面法 包封率

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(1)
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