Biophysics and Nanotechnology Research Laboratory, CBSH, G.B. Pant University of Agriculture and Technology, Pantnagar, Uttarakhand, India.
Int J Nanomedicine. 2010 Mar 9;5:101-8. doi: 10.2147/ijn.s8030.
The purpose of the present study was to formulate effective and controlled release albendazole liposomal formulations. Albendazole, a hydrophobic drug used for the treatment of hydatid cysts, was encapsulated in nanosize liposomes. Rapid evaporation method was used for the preparation of albendazole-encapsulated conventional and PEGylated liposomes consisting of egg phosphatidylcholine (PC) and cholesterol (CH) in the molar ratios of (6:4) and PC:CH: polyethylene glycol (PEG) (5:4:1), respectively. In this study, PEGylated and conventional liposomes containing albendazole were prepared and their characteristics, such as particle size, encapsulation efficiency, and in vitro drug release were investigated. The drug encapsulation efficiency of PEGylated and conventional liposomes was 81% and 72%, respectively. The biophysical characterization of both conventional and PEG-coated liposomes were done by transmission electron microscopy and UV-vis spectrophotometry. Efforts were made to study in vitro release of albendazole. The drug release rate showed decrease in albendazole release in descending order: free albendazole, albendazole-loaded conventional liposomes, and least with albendazole-loaded PEG-liposomes. Biologically relevant vesicles were prepared and in vitro release of liposome-entrapped albendazole was determined.
本研究旨在制备有效的阿苯达唑脂质体控释制剂。阿苯达唑是一种用于治疗包虫囊肿的疏水性药物，被包裹在纳米脂质体中。采用快速蒸发法制备了由蛋黄卵磷脂（PC）和胆固醇（CH）以摩尔比（6:4）组成的载阿苯达唑的常规和聚乙二醇化脂质体，以及由 PC:CH:聚乙二醇（PEG）（5:4:1）组成的载阿苯达唑的聚乙二醇化脂质体。在本研究中，制备了载阿苯达唑的聚乙二醇化和常规脂质体，并对其特性，如粒径、包封效率和体外药物释放进行了研究。聚乙二醇化和常规脂质体的药物包封效率分别为 81%和 72%。通过透射电子显微镜和紫外可见分光光度法对常规和聚乙二醇化脂质体的生物物理特性进行了研究。对阿苯达唑的体外释放进行了研究。药物释放率表明，阿苯达唑的释放率依次降低：游离阿苯达唑、载阿苯达唑的常规脂质体、载阿苯达唑的聚乙二醇化脂质体。制备了具有生物学相关性的囊泡，并测定了脂质体包封的阿苯达唑的体外释放。
