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载丝裂霉素 C 的阳离子纳米粒用于膀胱癌腔内化疗的体内保留时间和评价。

Prolonged retention and in vivo evaluation of cationic nanoparticles loaded with Mitomycin C designed for intravesical chemotherapy of bladder tumours.

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Technology, Hacettepe University, 06100 Sıhhiye-Ankara, Turkey.

出版信息

J Microencapsul. 2012;29(6):576-82. doi: 10.3109/02652048.2012.668957. Epub 2012 Apr 3.

Abstract

To overcome the recurrence problem in bladder tumours; nanoparticles with positive surface charge may improve interaction with biological membranes for intravesical administration. The aim of this study was to design, develop and evaluate (in vitro-in vivo) cationic nanoparticles based on chitosan, poly-L-lysine or polycaprolactone for the effective intravesical delivery of chemotherapeutic agent MMC in a rat model. Poly-L-lysine-coated polycaprolactone nanoparticles and chitosan-coated polycaprolactone nanoparticles were prepared by the double emulsion technique. Chitosan nanoparticles were prepared by ionic gelation. It was found that nanoparticle formulations of 160-320 nm in size can be produced in 14-35% encapsulation efficiency. Variability in the particle size of nanoparticles depended on the preparation method. Encapsulation was increased by two-fold for CS-PCL as a result of the double emulsion technique. Commercial MMC product in solution form and cationic nanoparticle formulations were compared for in vivo bladder retention properties and effect of formulations on urine volume.

摘要

为了克服膀胱肿瘤的复发问题;带正表面电荷的纳米粒子可能会改善与生物膜的相互作用,从而实现膀胱内给药。本研究旨在设计、开发和评估(体内外)基于壳聚糖、聚-L-赖氨酸或聚己内酯的阳离子纳米粒子,以在大鼠模型中有效实现化疗药物丝裂霉素 C 的膀胱内递药。聚-L-赖氨酸包覆的聚己内酯纳米粒子和壳聚糖包覆的聚己内酯纳米粒子通过复乳技术制备。壳聚糖纳米粒子通过离子凝胶化制备。结果发现,可以制备出粒径为 160-320nm、包封效率为 14-35%的纳米粒子制剂。纳米粒子的粒径变化取决于制备方法。由于采用了复乳技术,CS-PCL 的包封率增加了一倍。对溶液形式的商业丝裂霉素 C 产品和阳离子纳米粒子制剂进行了体内膀胱保留特性以及制剂对尿量影响的比较。

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