The effect of additives on naltrexone hydrochloride release and solvent removal rate from an injectable in situ forming PLGA implant
The effect of additives on naltrexone hydrochloride release and solvent removal rate from an injectable in situ forming PLGA implant
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DOI：
10.1002/pat.717
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发表时间：
2006-05-01
影响因子：
3.4
通讯作者：
Khakpour, Mazyar
中科院分区：
文献类型：
--
作者：
Bakhshi, Raheleh;Vasheghani-Farahani, Ebrahim;Khakpour, Mazyar
生物可降解的纳曲酮原位释药系统在药物依赖者的后处理中具有广阔的应用前景。本文研究了甘油和庚酸乙酯两种不同添加剂对聚乳酸-羟基乙酸酯（PLGA）注射种植体中盐酸纳曲酮释放和溶剂去除的影响。实验结果表明，这些添加剂的存在降低了药物的体外初始释放。然而，庚酸乙酯比甘油更有效，并且将PLGA溶液中的添加剂添加量增加到5% （w/w）可使纳曲酮的初始释放率降低高达50%。利用扫描电镜对植入物进行形态学评价表明，添加剂产生了较少的多孔结构，并产生了手指状到海绵状的转变。热重和形态分析可以很好地描述可注射植入物的溶剂去除特征，与药物释放特征吻合良好。版权所有(C) 2006 John Wiley & Sons, Ltd。
Biodegradable in situ forming drug delivery systems for naltrexone release are promising for post-treatment of drug addicts. The effect of two different additives, glycerol and ethyl heptanoate, on the naltrexone hydrochloride release and solvent removal from a poly(DL-lactide-co-glycolide) (PLGA) injectable implant is presented in this article. The experimental results showed that the in vitro initial release of the drug was decreased in the presence of these additives. Ethyl heptanoate was, however, more effective than glycerol and increasing the amount of additives in PLGA solution up to 5% (w/w) resulted in a decrease of initial naltrexone release rate up to 50%. The morphological evaluation of implants using scanning electron microscopy indicated that the additives generated a less porous structure together with a finger-like to sponge-like transition. The solvent removal profiles of injectable implants, which can be well described by thermogravimetric and morphological analysis, were in good agreement with drug release profiles. Copyright (C) 2006 John Wiley & Sons, Ltd.