摘要
目的对阿霉素纳米囊(adriamyc in nanocapsu les,ADM-NC)的制备工艺进行研究,优化最佳制备工艺,并对ADM-NC进行了急性毒性试验。方法以可生物降解的聚氰基丙烯酸正丁酯(polybutylcyanoacrylate,PBCA)为囊材,采用乳化聚合法(emu lsion polym erization m ethod)制备ADM-NC;以NC粒度和包封率为评价指标,通过正交试验设计(orthogonal design)优化制备工艺。以小鼠尾静脉注射方式分别测定空白纳米囊及载药纳米囊的半数致死量LD50。结果优化制备工艺后ADM-NC冻干前后的粒径分别为110nm和130nm;Zeta电位为114.6mV;以凝胶色谱法测得ADM-NC中药物的包封率达53.5%;测得空白纳米囊的LD50为(238.1±40.0)mg/kg,载药纳米囊ADM-NC的LD50为(36.6±6.2)mg/kg。结论利用乳化聚合法可制备具有较高包封率的ADM-NC;与ADM普通制剂的LD50(8.7±0.3)mg/kg相比,ADM-NC的毒性明显降低。
OBJECTIVE To find the best preparation method of adriamycin nanocapsules, and to investigate the toxicity of adriamycin nanocapsules. METHODS Adriamycin nanocapsules（ADM-NC） were prepared by emulsion polymerization method with polybutylcyanoacrylate（PBCA） as carrier material. The preparation procedure was optimized using orthogonal design according to the parameters of ADM-NC size and encapsulation efficiency. LD50 in mice of free nanocapsules and ADM-NC were also determined. RESULTS Under this optimum condition, the mean diameters of the ADM-NC prior to or posterior to be dry-frozen were 110nm and 130nm,respectively. The encapsulation efficiency and Zeta potential of ADM-NC were 53.5% and 114.6mV,respectively. LD50 of free nanocapsules and ADM-NC in mice were 238.1±40.0mg/kg and 36.6±6.2mg/kg, respectively. CONCLUSION ADM-NC with high encapsulation efficiency can be obtained through optimized emulsion polymerization method. Compared to the LD50 of ADM common formulation（8.7 0.3mg/kg） ,we drew the conclusion that the toxicity of ADM can be decreased significantly through NC preparation.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2006年第6期474-477,共4页
Chinese Journal of Modern Applied Pharmacy
关键词
阿霉素
纳米囊
聚氰基丙烯酸正丁酯
乳化聚合法
adriamycin
nanocapsule
polybutylcyanoacrylate
emulsion polymerization method
