The manufacture of stable paclitaxel-loaded poly(n-butyl cyanoacrylate) (PBCA) nanoparticles containing high loading and encapsulation efficiency simultaneously were achieved in the presence of pluronic F127 via miniemulsion. It was found that both drug loading and encapsulation efficiencies of PBCA nanoparticles prepared by miniemulsion were higher (approximately three times) than those obtained by emulsion with similar paclitaxel content in the feed monomer (1%, w/w). Furthermore, the loading and encapsulation efficiencies increased concurrently (to a maximum of 4 and 80%, respectively) with increasing paclitaxel content and these nanoparticles were spherical in shape and with size near 100 nm. XRD patterns revealed that paclitaxel in particles was distributed in the molecular or amorphous state or in the form of small crystals. The in vitro drug release profile of drug-loaded PBCA nanoparticles prepared from miniemulsion exhibited a gradual release; more than 80% (w/w) of the paclitaxel was released after 96 h.

译文

:在普卢尼克F127的存在下,通过细乳液实现了稳定的负载紫杉醇的聚氰基丙烯酸正丁酯(PBCA)纳米粒子的制备,该纳米粒子同时具有高负载和包封效率。发现通过细乳液制备的PBCA纳米颗粒的载药量和包封效率均比通过进料单体中紫杉醇含量相似(1%,w / w)的乳液获得的载药量和包封效率更高(约三倍)。此外,随着紫杉醇含量的增加,加载和包封效率同时提高(分别达到最大4%和80%),并且这些纳米颗粒呈球形,尺寸接近100 nm。 XRD图谱表明,紫杉醇在颗粒中以分子或非晶态或小晶体形式分布。由细乳液制备的载有药物的PBCA纳米颗粒的体外药物释放曲线显示出逐渐释放; 96小时后释放出超过80%(w / w)的紫杉醇。

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