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载紫杉醇和索拉非尼白蛋白纳米粒系统的制备及其体内外评价。

Preparation of the albumin nanoparticle system loaded with both paclitaxel and sorafenib and its evaluation in vitro and in vivo.

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.

出版信息

J Microencapsul. 2011;28(6):528-36. doi: 10.3109/02652048.2011.590614. Epub 2011 Jun 27.

Abstract

Paclitaxel and sorafenib loaded albumin nanoparticles (PTX-SRF-BSA-NPs) were prepared and studied here to avoid the toxicities from the excipients in the Taxol® and explore the effect of such combination on the antitumour efficacy and toxicity. PTX-BSA-NPs and so on were used as controls. The particle size, zeta potential, encapsulation efficiency and morphology were evaluated. Less than 70% of each drug released within 24 h. PTX and SRF existed as molecular or amorphous form in the PTX-SRF-BSA-NPs. The particle size did not change much after 2-month storage in freeze-dried form or 24 h in suspension. The treatment with PTX-SRF-BSA-NPs (7.5 mg kg(-1) PTX + 7.5 mg kg(-1) SRF) exhibited lower myelosuppression than PTX-BSA-NPs (15 mg kg(-1) PTX) while it remained or increased the antitumour effect in mice tumour models. Compared with the solution containing the same level of PTX and SRF, PTX-SRF-BSA-NPs demonstrated significantly lower haemolysis and myelosuppression effect.

摘要

紫杉醇和索拉非尼载白蛋白纳米粒(PTX-SRF-BSA-NPs)被制备并进行了研究,以避免泰素®中的赋形剂的毒性,并探索这种联合用药对肿瘤疗效和毒性的影响。PTX-BSA-NPs 等被用作对照。对粒径、Zeta 电位、包封效率和形态进行了评价。在 24 小时内,每种药物的释放量不到 70%。PTX 和 SRF 在 PTX-SRF-BSA-NPs 中以分子或无定形形式存在。在冷冻干燥或悬浮 24 小时后,粒径变化不大。与 PTX-BSA-NPs(15mg/kg PTX)相比,PTX-SRF-BSA-NPs(7.5mg/kg PTX+7.5mg/kg SRF)治疗后骨髓抑制程度较低,而在小鼠肿瘤模型中仍保持或增加了抗肿瘤作用。与含有相同水平的 PTX 和 SRF 的溶液相比,PTX-SRF-BSA-NPs 表现出明显更低的溶血和骨髓抑制作用。

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