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首页> 外文期刊>Drug Design, Development and Therapy >Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies
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Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies

机译：醋氯芬酸纳米晶体具有增强的体外和体内性能：配方优化，表征，镇痛和急性毒性研究

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摘要

This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation–ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01?nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvinylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0.12%, w/w). The characterization of AC was performed using zeta sizer, scanning electron microscopy, transmission electron microscopy, powder X-ray diffraction and differential scanning calorimetry. The saturation solubility of the AC nanocrystals was substantially increased 2.6- and 4.5-fold compared to its unprocessed active pharmaceutical ingredient in stabilizer solution and unprocessed drug. Similarly, the dissolution rate of the AC nanocrystals was substantially enhanced compared to its other counterpart. The results showed that >88% of AC nanocrystals were dissolved in first 10 min compared to unprocessed AC (8.38%), microsuspension (66.65%) and its marketed tablets (17.65%). The in vivo studies of the produced stabilized nanosuspension demonstrated that the Cmax were 4.98- and 2.80-fold while area under curve from time of administration to 24 h (AUC0→24?h) were found 3.88- and 2.10-fold greater when compared with unprocessed drug and its marketed formulation, respectively. The improved antinociceptive activity of AC nanocrystals was shown at much lower doses as compared to unprocessed drug, which is purely because of nanonization which may be attributed to improved solubility and dissolution rate of AC, ultimately resulting in its faster rate of absorption.
机译：这项研究的目的是使用经济有效的简单沉淀-超声方法，以纳米悬浮液的形式提高醋氯芬酸（AC）的溶出度，口服生物利用度和止痛潜力。使用研究AC的最佳条件生产纳米晶体。使用羟丙基甲基纤维素（1％，w / w），聚乙烯吡咯烷酮K30（1％，w / w）和十二烷基硫酸钠测得的最小粒径（PS）和多分散指数分别为112±2.01？nm和0.165。 （0.12％，w / w）。 AC的表征使用Zeta分级仪，扫描电子显微镜，透射电子显微镜，粉末X射线衍射和差示扫描量热法进行。与在稳定剂溶液和未加工的药物中未加工的活性药物成分相比，AC纳米晶体的饱和溶解度显着提高了2.6倍和4.5倍。同样，与其他纳米晶体相比，AC纳米晶体的溶解速度大大提高。结果表明，与未处理的AC（8.38％），微悬浮液（66.65％）和其市售片剂（17.65％）相比，在前10分钟内> 88％的AC纳米晶体溶解。体内制备的稳定的纳米悬浮液的体内研究表明，从给药时间到24 h（AUC 0→24？h <当与未加工的药物及其市售制剂相比时，发现分别高出3.88倍和2.10倍。与未加工的药物相比，AC纳米晶体具有更高的抗伤害感受活性，这是因为纳米化可能是由于改善了AC的溶解度和溶解速度，最终导致了其更快的吸收速率所致。

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