摘要
目的:研究一种由羧甲基壳聚糖修饰的pH敏感阿霉素纳米脂质体,并考察羧甲基壳聚糖的分子参数对其敏感性的影响。方法:采用逆相蒸发-pH梯度法制备羧甲基壳聚糖修饰的阿霉素脂质体;用反透析-UV分光光度法测定包封率;用TEM和激光粒度仪分别考察脂质体形态与粒径分布;由药物渗漏实验考察pH敏感性。并研究羧甲基壳聚糖取代度、相对分子质量和质量分数对脂质体pH敏感性的影响。结果:所制纳米脂质体的包封率达87%,形态圆整,粒径分布为(74.7±11.5)nm;羧甲基壳聚糖的羧甲基取代度、相对分子质量、质量分数对修饰的纳米脂质体药物渗漏有不同程度的影响。结论:逆相蒸发-pH梯度法可成功制备羧甲基壳聚糖修饰pH敏阿霉素纳米脂质体;调变羧甲基壳聚糖的取代度、相对分子质量和质量分数均可实现羧甲基壳聚糖修饰阿霉素纳米脂质体的pH敏智能控释。
Aim： To prepare a pH-sensitive doxorubicin （DXR） nanoliposomes modified by carboxymethyl chitosan （CMCT）, and to investigate the effects of molecular parameters of the CMCT on the pH-sensitivity. Methods： CMCT-modified DXR liposomes were prepared by pH-gradient plus reverse-phase evaporation method. The encapsulation efficiency, morphology, particle size distribution, pH-sensitivity and the effects on pH sensitivity of CMCT substitution degree, molecular weight and concentration were investigated. Results： It was shown that the eneapsulation effieiency of CMCT-modified DXR nanoliposomes was above 87%. The liposomes were spherical with particle size distribution （74. 7 ± 11.5） nm; CMCT substitution degree, molecular weight and concentration had different effects on the pH-sensitivity of DXR nanoliposomes. Conclusion： The reverse-phase evaporation-pH gradient method has the potential in the preparation of CMCT-modified pH-sensitive nanoliposomes. CMCT substitution degree, molecular weight and concentration can be adjusted to obtain CMCT- modified DXR nanoliposomes with the characteristics of an intelligent pH-sensitive controlled-release.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2008年第3期209-213,共5页
Journal of China Pharmaceutical University
基金
上海市重点学科建设项目
上海市纳米科技专项资助项目(No0652nm027)
