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首页> 外文期刊>RSC Advances >Improved oral bioavailability of novel antithrombotic S002-333 via chitosan coated liposomes: a pharmacokinetic assessment
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Improved oral bioavailability of novel antithrombotic S002-333 via chitosan coated liposomes: a pharmacokinetic assessment

机译：通过壳聚糖包衣脂质体改善新型抗血栓形成剂S002-333的口服生物利用度：药代动力学评估

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S002-333, a novel anti-thrombotic agent, exhibits excellent platelet mediated antithrombotic action and subsequently has no effect on the coagulation cascade. However, its oral bioavailability is hampered due to inherent low aqueous solubility. In order to circumvent this issue, chitosan coated liposomes were prepared by an ethanol injection method. S002-333 loaded liposomes (CH-LIP-F9) were reproduced with homogeneous particle sizes. The liposomal formulation was characterized with respect to size and surface morphology by transmission electron microscopy (TEM). The optimized formulation exhibited spherical shapes with a nano-metric size (249.64 +/- 10.36 nm). The percentage entrapment efficiency (% EE) offered by the various developed formulations was found to be in the range between 72.36 +/- 1.76 and 76.87 +/- 2.32%. An in vitro release experiment demonstrated prolonged release of S002-333 from the optimized liposomal formulation. A cytotoxicity study represented that both blank liposomes (BLK-LIP) as well as the drug bearing liposomal formulation displayed negligible toxicity towards Caco-2 cells. The results of a pharmacokinetic study indicated that liposomal formulation significantly enhanced oral absorption of S002-333 in rats (AUC(0-t); 7016.02 +/- 128.96 h ng mL(-1)) compared to its aqueous suspension (AUC(0-t); 2382.02 +/- 77.17 h ng mL(-1)). These results together elicited that the developed liposomal formulation would improve preclinical and clinical application of S002-333.
机译：S002-333，一种新型的抗血栓形成剂，表现出优异的血小板介导的抗血栓形成作用，因此对凝血级联反应没有影响。然而，由于其固有的低水溶性，阻碍了其口服生物利用度。为了避免该问题，通过乙醇注射法制备了脱乙酰壳多糖包被的脂质体。载有S002-333的脂质体（CH-LIP-F9）具有均一的粒径。通过透射电子显微镜（TEM）表征脂质体制剂的大小和表面形态。优化的配方显示出具有纳米尺寸（249.64 +/- 10.36 nm）的球形。发现各种开发的制剂提供的包封率（EE％）在72.36 +/- 1.76和76.87 +/- 2.32％之间。体外释放实验表明，S002-333从优化的脂质体制剂中延长释放。细胞毒性研究表明空白脂质体（BLK-LIP）以及载有脂质体的药物对Caco-2细胞的毒性均可以忽略不计。药代动力学研究的结果表明，脂质体制剂与其水悬浮液（AUC（0）（0，-t; 7016.02 +/- 128.96 h ng mL（-1））相比，可显着提高大鼠中S002-333的口服吸收。 -t）; 2382.02 +/- 77.17 h ng mL（-1））。这些结果共同引发了开发的脂质体制剂将改善S002-333的临床前和临床应用。

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