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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Niosomes encapsulating paclitaxel for oral bioavailability enhancement: preparation, characterization, pharmacokinetics and biodistribution
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Niosomes encapsulating paclitaxel for oral bioavailability enhancement: preparation, characterization, pharmacokinetics and biodistribution

机译:含紫杉醇的脂质体可增强口服生物利用度:制备,表征,药代动力学和生物分布

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摘要

In this study, niosome formulations were prepared and evaluated for their effects on improving the oral bioavailability of paclitaxel (PCT). Niosomes were prepared from Span 40 and coated with bioadhesive carbopol polymers. The niosomes encapsulated 98.7% ± 0.8 of the initially added PCT and their size ranged from 133 ± 6 nm to 320 ± 6 nm. The stability of Carbopol 974P coated niosomes in bile salts was better than uncoated niosomes. Extended release of PCT was observed. After oral administration of formulations to Wistar rats, higher drug plasma concentrations were observed for niosomes comparing to PCT suspension. The high PCT accumulation in intestine and liver obtained after Carbopol 974P coated niosomes administration indicated their potential regarding effective treatment of localized carcinomas in intestine and liver. The relative bioavailability of PCT was increased 3.8-and 1.4-fold by uncoated and Carbopol 974P coated niosomes emphasizing the ability of niosomes on improving the oral bioavailability of PCT.
机译:在这项研究中,制备了脂质体制剂,并评估了它们对改善紫杉醇(PCT)口服生物利用度的作用。由Span 40制备脂质体,并用生物粘附性卡波姆聚合物包被。脂质体封装了最初添加的PCT的98.7%±0.8,其大小范围为133±6 nm至320±6 nm。 Carbopol 974P包覆的脂质体在胆汁盐中的稳定性优于未包覆的脂质体。观察到PCT的延长释放。向Wistar大鼠口服给药后,与PCT悬浮液相比,对于脂质体观察到更高的药物血浆浓度。施用Carbopol 974P包覆的脂质体后,在肠和肝中的PCT积累量很高,表明它们在有效治疗肠和肝中局部癌方面具有潜力。未包被的和Carbopol 974P包被的脂质体将PCT的相对生物利用度提高了3.8倍和1.4倍,强调了脂质体改善PCT的口服生物利用度的能力。

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