Preparation, Characterization and In Vitro Evaluation of Bleomycin-Containing Nanoliposomes

Abstract

Bleomycin is an anticancer drug used against various types of cancers. The aim of this study was to prepare a new PEGylated and non-PEGylated nanoliposomal formulation of bleomycin (PEG-nLip-BLM and nLip-BLM) and evaluate their anticancer activity in different tumor cell lines. The liposomes were prepared by thin film-hydration method and then bleomycin (BLM) was loaded to the prepared vesicles. The size, zeta potential, entrapment efficiency, loading rate, release profile and cytotoxicity of liposomal formulations in TC-1, LLC1 and HFLF-PI5 cell lines were investigated. Mean particle size and zeta potential of the PEG-nLip-BLM and nLip-BLM were found to be 99.4±4.6 nm, -34.83±4.7 mV; and 112.2±7.2 nm and -27.5±3.2 mV, respectively which were stable for at least two months. Encapsulation and loading efficiency of BLM for PEG-nLip-BLM and nLip-BLM were obtained about 83.1±4.2 %, 14.3±2.5 %; and 78.3±8.6 %, 11.1±3.3 %, respectively. Drug release study showed a slow release pattern without considerable burst effect. The liposomal formulations indicated lower toxicity compared to free drug in case of TC-1 and HFLF-PI5 cells; but their cytotoxicity against LLC1 cells were significantly higher than free drug. The results of current study indicated that PEG-nLip-BLM can be a suitable candidate for drug delivery to solid tumors.

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Bleomycin-containing nanoliposomes were successfully prepared and characterized. PEG-nLip-BLM showed excellent stability, high loading efficacy and improved cytotoxicity against LLC1 cells and good retention capability compare to nLip-BLM and free drug. These findings will facilitate the production of a new formulation of BLM with long-acting action and more efficient anticancer activity for testing on human subjects

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