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首页> 外文期刊>Journal of biomedical materials research. Part B, Applied biomaterials. >Evaluation of in vitro release and in vivo efficacy of mPEG-PLA-haloperidol conjugate micelle-like structures.
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Evaluation of in vitro release and in vivo efficacy of mPEG-PLA-haloperidol conjugate micelle-like structures.

机译：mPEG-PLA-氟哌啶醇缀合物胶束样结构的体外释放和体内功效评估。

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摘要

Polymeric prodrugs of mPEG-PLA-haloperidol (methoxy poly(ethylene glycol)-b-poly (lactic acid)), self-assemble into nanoscale micelle-like structures in aqueous solutions. The micelles range in size from 28 to 52 nm in diameter and have been shown to be spherical in shape using cryogenic transmission electron microscopy. In this current work there is evidence shown that suggests these micelle-like structures do not dissociate below their critical micelle concentration (CMC) when the PEG weight percent is at least 68, releasing physically entrapped drug from intact micelles over a 3-day period. However, 55 wt % PEG micelles dissociate below their CMC, and release their physically entrapped drug within 8 h. Conjugate polymer micelles most closely approach a linear release profile over a 5-day period. Conjugate micelles with free drug incorporated, known as combination micelle-like structures, release drug over 4 days. However, these combination micelles have the fastest burst release indicating that freedrug was potentially dominating the first 8 h of release, after which hydrolysis of covalently linked drug took over. In vivo behavioral studies can assess haloperidol bioactivity from drug loaded micelle-like structures on ketamine induced hyperlocomotion. Results are consistent with in vitro release data, showing that conjugate and combination micelles continue to release haloperidol 4 days post injection, attenuating the effects of the ketamine induced hyperlocomotion. Furthermore, results indicate that the sedative side effects of haloperidol were reduced with the micelle delivery systems as compared to the acute haloperidol injection.
机译：mPEG-PLA-氟哌啶醇（甲氧基聚（乙二醇）-b-聚（乳酸））的聚合前药在水溶液中自组装成纳米级胶束状结构。胶束的直径范围为直径28至52nm，并且使用低温透射电子显微镜已显示为球形。在目前的工作中，有证据表明，当PEG重量百分比至少为68时，这些胶束状结构不会在其临界胶束浓度（CMC）以下解离，在3天的时间内从完整的胶束中释放出包裹在体内的药物。但是，有55 wt％的PEG胶束在CMC以下解离，并在8小时内释放了其物理包埋的药物。共轭聚合物胶束在5天的时间内最接近线性释放曲线。与掺入的游离药物（称为组合胶束样结构）结合的胶束在4天内释放出药物。然而，这些组合的胶束具有最快的爆发释放，表明游离药物可能在释放的前8小时内占据主导地位，此后，共价连接的药物的水解就接管了。体内行为研究可以从氯胺酮引起的超运动上载药的胶束样结构评估氟哌啶醇的生物活性。结果与体外释放数据一致，表明缀合物和组合胶束在注射后4天继续释放氟哌啶醇，从而减弱了氯胺酮诱导的运动过度的影响。此外，结果表明，与急性氟哌啶醇注射液相比，采用微团递送系统降低了氟哌啶醇的镇静副作用。

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