Published Paper


Development and Chbaracterization of Liposomal Formulation of Carfilzomib with Hydrogenated Palm Oil

*Raghuveera Hathibelagal Goruva1, Anjaneyulu Vinukonda2, Neelesh Chaubey3, Harish Pandey4

Page: 533-539
Published on: 2018 August

Abstract

Carfilzomib is a peptide epoxy ketone derivative, chemically; it is a tetra peptide epoxy ketone and an analog of epoxomicin. Carfilzomib is commercially available Carfilzomib for Injection, which is a lyophilized formulation available as 30 mg / vial and 60 mg / vial a sterile, white to off - white lyophilized powder and is available as a single - use vial. The current investigation was designed to alternative stable liposomal formulations.The inventors of the present invention have surprisingly found that it is possible to prepare a stable lipid Nano composition of Carfilzomib. Liposomal formulations are less toxic than drugs alone and have better pharmacological parameters. Although they seem to be the first choice for drug delivery systems for various diseases.The usage of natural products in pharmaceuticals has steadily seen improvements over the last decade, and this study focuses on the utilization of palm oil in formulating liposomal Carfilzomib. The liposomal form of Carfilzomib generally minimizes toxicity and enhances target delivery actions. Taking into account the antiproliferative and antioxidant properties of palm oil, the aim of this study is to design and characterize a new liposomal Carfilzomib by replacing phosphatidylcholine with 5% and 10% palm oil content. Liposomes were formed using the freeze thaw method, and Carfilzomib was loaded through pH gradient technique and characterized through in vitro and ex vivo terms. Based on TEM images, large lamellar vesicles (LUV) were formed, with sizes of 438 and 453 nm, having polydispersity index of 0.21 ± 0.8 and 0.22 ± 1.3 and zeta potentials of about −31 and −32 mV, respectively. In both formulations, the entrapment efficiency was about 99%, and whole Carfilzomib was released through 96 hours in PBS (pH = 7.4) at 37°C. Comparing cytotoxicity and cellular uptake of LUV with on MCF7 and MDA-MBA 231 breast cancer cell lines indicated suitable uptake and lower IC50 of the prepared liposomes4.

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