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首页> 外文期刊>Polymers for advanced technologies >The effect of additives on naltrexone hydrochloride release and solvent removal rate from an injectable in situ forming PLGA implant
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The effect of additives on naltrexone hydrochloride release and solvent removal rate from an injectable in situ forming PLGA implant

机译:添加剂对可注射原位形成PLGA植入物的盐酸纳曲酮释放和溶剂去除率的影响

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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.
机译:用于纳曲酮释放的可生物降解的原位形成药物递送系统有望用于吸毒者的后期治疗。本文介绍了两种不同的添加剂甘油和庚酸乙酯对纳曲酮盐酸盐释放和从聚(DL-丙交酯-共-乙交酯)(PLGA)可注射植入物中去除溶剂的影响。实验结果表明,在这些添加剂的存在下,药物的体外初始释放降低了。然而,庚酸乙酯比甘油更有效,将PLGA溶液中的添加剂量增加到5%(w / w),会导致纳曲酮的初始释放率降低多达50%。使用扫描电子显微镜对植入物进行形态学评估表明,这些添加剂产生的多孔性较低,并且具有手指状到海绵状的过渡。可通过热重分析和形态分析很好地描述了可注射植入物的溶剂去除曲线,与药物释放曲线非常吻合。

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