Preparation and Pharmacokinetics in Rats of Cabazitaxel Liposomes by Film Dispersion Method
文献类型：期刊论文
| 作者 | Zhang Li2; Li Yaping2 ; Chen Lingli1
|
| 刊名 | Chinese Journal of Pharmaceuticals
 |
| 出版日期 | 2017 |
| 卷号 | 48期号:6页码:874-878 |
| 关键词 | cabazitaxel liposome film dispersion-high pressure homogenization method in vitro release pharmacokinetics |
| ISSN号 | 1001-8255 |
| 其他题名 | 卡巴他赛脂质体的制备及其大鼠药动学 |
| 文献子类 | Article |
| 英文摘要 | Liposomes can be aggregated through the enhanced permeability and retention (EPR) effect in the target site, enhance the accumulation of drugs, so as to improve efficacy and reduce the side effects. Hydroxylated soybean phosphatidylcholine (HSPC), cholesterol and distearoyl phosphatidylglycerol (DSPG) were used as raw materials to prepare the liposomes by film dispersion-high pressure homogenization method. The morphology of the liposomes was observed by transmission electron microscopy. The particle size and distribution were determined by laser scattering method. The encapsulation efficiency was determined by dextran gel column chromatography. The in vitro release behavior of liposomes was determined by dialysis method. The results showed that the average particle size, polydispersion index, zeta potential and entrapment efficiency of the liposomes were (68.041.73)nm, 0.2130.015, (-57.71.2)mV and (86.71.5)%, respectively. The obtained negatively charged liposomes were able to avoid aggregation. In 0.05% Tween-80 solution, the cumulative amount at 48 h of cabazitaxel liposomes was 74%, while for its injection was 80% at 20 h. It demonstrated that the release rate of cabazitaxel liposomes was slower than that of its injection. Furthermore, the pharmacokinetic behaviors of the above two preparations were compared with male SD rats as the animal models. The results showed that the AUC_(0 ) values for cabazitaxel injection group and cabazitaxel liposome group were (696.890.16) and (4 210.070.19)ng·ml~(-1)·h, and t_(1/2) were (5.850.32) and (7.280.40)h, suggesting that liposomes had a role in delaying drug release. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:6005149 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269203]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Chen Lingli |
| 作者单位 | 1.Center for Formulations System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. 2.School of Pharmacy, Jiangsu University, Zhenjiang, Jiangsu 212013, China.; |
| 推荐引用方式 GB/T 7714 | Zhang Li,Li Yaping,Chen Lingli. Preparation and Pharmacokinetics in Rats of Cabazitaxel Liposomes by Film Dispersion Method[J]. Chinese Journal of Pharmaceuticals,2017,48(6):874-878. |
| APA | Zhang Li,Li Yaping,&Chen Lingli.(2017).Preparation and Pharmacokinetics in Rats of Cabazitaxel Liposomes by Film Dispersion Method.Chinese Journal of Pharmaceuticals,48(6),874-878. |
| MLA | Zhang Li,et al."Preparation and Pharmacokinetics in Rats of Cabazitaxel Liposomes by Film Dispersion Method".Chinese Journal of Pharmaceuticals 48.6(2017):874-878. |
入库方式： OAI收割
来源：上海药物研究所
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