长循环脂质体两性霉素B的制剂与评价：一项在BALB/C小鼠中使用锝的闪烁动力学研究

Formulation and Evaluation of Long Circulating Liposomal Amphotericin B: A Scinti-kinetic Study using Tc in BALB/C Mice.

作者信息

Jadhav M P, Nagarsenker Mangal S, Gaikwad R V, Samad A, Kshirsagar Nilima A

机构信息

Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz, Mumbai - 400 098, India.

出版信息

Indian J Pharm Sci. 2011 Jan;73(1):57-64. doi: 10.4103/0250-474X.89757.

DOI:10.4103/0250-474X.89757

PMID:22131622

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3224410/

Abstract

In the present study, we formulated long circulating liposomes for amphotericin B and characterized them. The formulation was optimized using 2(3) factorial designs. Pegylated liposomal formulation showed favorable results with reference to particle size (247.33±9.60 nm), percent entrapment efficiency (94.55±3.34%). TEM studies revealed that the liposomes were essentially spherical, hollow, and appeared like powder puff structures. From DSC study it was concluded that the pegylated formulation containing Amp B showed better stability and membrane integrity of the formulation. During the stability studies the formulation was found to be stable. When subjected to gamma scintigraphy kinetic tracer studies the formulation showed longer residence time in the blood in BALB/C mice.

摘要

在本研究中，我们制备了两性霉素B的长循环脂质体并对其进行了表征。使用2（3）析因设计对制剂进行了优化。聚乙二醇化脂质体制剂在粒径（247.33±9.60 nm）、包封率（94.55±3.34%）方面显示出良好的结果。透射电镜研究表明，脂质体基本呈球形、中空，外观类似粉扑结构。差示扫描量热法研究得出结论，含两性霉素B的聚乙二醇化制剂显示出更好的稳定性和制剂膜完整性。在稳定性研究中，发现该制剂是稳定的。当进行γ闪烁显像动力学示踪研究时，该制剂在BALB/C小鼠血液中的停留时间更长。