Study of an injectable in situ forming gel for sustained-release of Ivermectin in vitro and in vivo

被引：14

作者：

Geng, Zhixia ^{[1
,2
]}

Luo, Xiaoqing ^{[1
]}

Zhang, Zhenrui ^{[1
]}

Li, Huimin ^{[1
]}

Tian, Jing ^{[1
]}

Yu, Zugong ^{[1
]}

机构：

[1] Nanjing Agr Univ, Coll Vet Med, Lab Vet Pharmacol & Toxicol, Nanjing 210095, Jiangsu, Peoples R China

[2] HeBei Yuanzheng Pharmaceut Co Ltd, Qual & Technol Dept, Shijiazhuang 050041, Hebei Province, Peoples R China

来源：

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES | 2016年 / 85卷

关键词：

Ivermectin; In situ forming gel; Sustained-release; Pharmacokinetic; Dog; DRUG-DELIVERY SYSTEM; PLGA-PEG-PLGA; COLLOIDAL GELS; MOLECULAR-WEIGHT; BURST RELEASE; STEM-CELLS; FORMULATION; IMPLANTS; DEPOT; HYDROXYAPATITE;

D O I：

10.1016/j.ijbiomac.2015.12.028

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The purpose of this study was to develop an in situ forming gel based on SAIB-PLA composite matrix depot for sustained release of Ivermectin. The burst release and cumulative release were significantly reduced with the increased content of solvents and the minimum burst release and cumulative release were found in formulations with NMP. With the addition of PLA in the NMP based gel, burst release and cumulative release were reduced. When concentration of IVM raised from 1% to 2% and 4%, cumulative release was 2.4-2.9 and 3.1-3.7 times that of 1%. The optimal prescription displayed a slow in vitro release rate with 10.46% burst release and 80% cumulative release in 80 days. Pharmacokinetic results indicate that the effective blood concentration of the gel could be maintained up to 110-120 days, t(1/2 lambda z) of the gels was (24.37 +/- 1.71) days and MRT was (32.86 +/- 0.91) days. (C) 2016 Published by Elsevier B.V.

引用

页码：271 / 276

页数：6

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