Lidocaine-loaded biodegradable nanospheres.: I.: Optimization of the drug incorporation into the polymer matrix
Lidocaine-loaded biodegradable nanospheres.: I.: Optimization of the drug incorporation into the polymer matrix
复制标题
DOI：
10.1016/s0168-3659(98)00121-7
复制
发表时间：
1999-02-22
影响因子：
10.8
通讯作者：
Dellacherie, E
中科院分区：
文献类型：
--
作者：
Görner, T;Gref, R;Dellacherie, E
设计了粒径可控的聚D， l -乳酸球形纳米药物载体。局部麻醉剂利多卡因，一种小疏水分子，加入到核心中，负载从约7%到32% （w/w）不等，并随着颗粒大小而增加。制备的颗粒粒径在250 ~ 820 nm之间，多分散性低，重现性好；聚合物的浓度（表面活性剂浓度恒定时）决定了颗粒的大小。在体外条件下，高载药量的大颗粒（约30%）在24-30小时内缓释，中等大小的载体（约13%）在15小时内释放药物，而小载药量的小颗粒（约7%）在几个小时内快速释放。药物释放速率似乎与药物掺入聚合物基质的状态（结晶或分散）有关。(C) 1999 Elsevier Science B.V.版权所有
Spherical nanoparticulate drug carriers made of poly(D,L-lactic acid) with controlled size were designed. A local anesthetic, lidocaine, a small hydrophobic molecule, was incorporated in the core with loadings varying from about 7 to 32% (w/w) and increasing with the particle size. Particles with sizes from about 250 to 820 nm and low polydispersity were prepared with good reproducibility; the polymer concentration (at constant surfactant concentration) governed the particle size. The large particles with a high loading (similar to 30%) showed under in vitro conditions a slow release over 24-30 h, the medium sized carriers (loading of similar to 13%) released the drug over about 15 h, whereas the small particles with small loading (similar to 7%) exhibited a rapid release over a couple of hours. It seems that the drug release rate is related to the state (crystallized or dispersed) of the drug incorporated in the polymer matrix. (C) 1999 Elsevier Science B.V. All rights reserved.