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载棕榈酸抗坏血酸阿霉素聚乙二醇脂质体在荷瘤鼠体内的分布。

Biodistribution of ascorbyl palmitate loaded doxorubicin pegylated liposomes in solid tumor bearing mice.

机构信息

Nanotechnology and Drug Targeting Laboratory, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506 009, Andhra Pradesh, India.

出版信息

J Microencapsul. 2011;28(2):142-9. doi: 10.3109/02652048.2010.542496.

Abstract

The aim of this study is to develop ascorbyl palmitate (ASP) loaded doxorubicin (DOX) pegylated liposomes and to evaluate their targeting potential to tumor. We have prepared conventional (DL), pegylated DOX liposomes with (SDL) and without ascorbyl palmitate (SDL-A). The vesicle size in all the formulations was within the range 105-120 nm and in vitro release studies in serum confirmed the stability of the liposomes. Biodistribution studies carried out in Ehrlich ascites tumor bearing mice indicate higher area under the curve for SDL and SDL-A liposomes compared to DL and plain drug solution. Drug targeting index assessed from tumor-to-serum concentration ratio and therapeutic availability of DOX in tumor tissue was also significantly higher for pegylated liposomes. In conclusion, biodistribution study reveals that the presence of ascorbyl palmitate alters the distribution pattern of liposomes and paves way for better drug targeting.

摘要

本研究旨在开发抗坏血酸棕榈酸酯(ASP)负载阿霉素(DOX)的聚乙二醇化脂质体,并评估其对肿瘤的靶向潜力。我们已经制备了常规(DL)、聚乙二醇化 DOX 脂质体(SDL)和不含抗坏血酸棕榈酸酯(SDL-A)。所有制剂的囊泡大小均在 105-120nm 范围内,血清中的体外释放研究证实了脂质体的稳定性。在荷 Ehrlich 腹水瘤的小鼠中进行的生物分布研究表明,与 DL 和普通药物溶液相比,SDL 和 SDL-A 脂质体的曲线下面积更高。从肿瘤-血清浓度比评估的药物靶向指数和肿瘤组织中 DOX 的治疗效果也明显更高。总之,生物分布研究表明,抗坏血酸棕榈酸酯的存在改变了脂质体的分布模式,为更好的药物靶向铺平了道路。

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