State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
J Microencapsul. 2011;28(6):528-36. doi: 10.3109/02652048.2011.590614. Epub 2011 Jun 27.
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.
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。