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载白藜芦醇壳聚糖微球的制备、体外特性、药代动力学和药效学评价及其在荷 B16F1 黑素瘤小鼠中的应用。

Preparation, in vitro characterization, pharmacokinetic, and pharmacodynamic evaluation of chitosan-based plumbagin microspheres in mice bearing B16F1 melanoma.

机构信息

Division of Radiobiology and Toxicology, Manipal Life Sciences Centre, Manipal, Karnataka, India.

出版信息

Drug Deliv. 2010 Apr;17(3):103-13. doi: 10.3109/10717540903548447.

DOI:10.3109/10717540903548447
PMID:20100068
Abstract

The present study was aimed to evaluate the anti-tumor efficacy and systemic toxicity of chitosan-based plumbagin microspheres in comparison to free plumbagin. The optimized formulation had a mean particle size of 106.35 mum with an encapsulation efficiency of 80.12%. Pharmacokinetic studies showed a 22.2-fold increase in elimination half-life (t(1/2)) of plumbagin from chitosan microspheres as compared to free plumbagin. Administration of plumbagin microspheres resulted in a significant tumor growth inhibition and reduced systemic toxicity. These results suggest that chitosan-based microspheres could be a promising strategy for the systemic delivery of anti-cancer agents like plumbagin.

摘要

本研究旨在评估壳聚糖载白藜芦醇微球与游离白藜芦醇相比的抗肿瘤疗效和全身毒性。优化后的配方平均粒径为 106.35 微米,包封率为 80.12%。药代动力学研究表明,与游离白藜芦醇相比,壳聚糖微球中白藜芦醇的消除半衰期(t(1/2))延长了 22.2 倍。白藜芦醇微球的给药导致肿瘤生长抑制显著,全身毒性降低。这些结果表明,壳聚糖基微球可能是一种有前途的策略,用于系统递送达泊苷等抗癌药物。

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