Preparation, characterization, and in vitro evaluation of bleomycin‐containing nanoliposomes. (10th November 2016)

• Record Type: Journal Article
• Authors: Chiani, Mohsen; Shokrgozar, Mohammad Ali; Azadmanesh, Kayhan; Norouzian, Dariush; Mehrabi, Mohammad Reza; Najmafshar, Aazam; Akbarzadeh, Azim
• Is Part Of: Chemical biology & drug design. Volume 89:Number 4(2017)
• Page Start: 492
• Page End: 497
• Publication Date: 2016-11-10
• Subjects: bleomycin -- cytotoxicity -- drug delivery -- nanoliposomes; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12869
• Languages: English
• ISSNs: 1747-0277

Abstract

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 and −34.83 ± 4.7 mV; and 112.2 ± 7.2 nm and −27.5 ± 3.2 mV, respectively, which were stable for at least 2 months. Encapsulation and loading efficiency of BLM for PEG‐nLip‐BLM and nLip‐BLM were obtained about 83.1 ± 4.2% and 14.3 ± 2.5%; and 78.3 ± 8.6% and 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 was significantly higher than free drug. The results of this study indicated that PEG‐nLip‐BLM can be a suitable candidate for drug delivery to solid tumors. Abstract : 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.