Formulation of bendamustine hydrochloride in long circulating DPPC:CHOL liposomes, surface modified with a PEO-based co-polymer bearing four lipid mimetic units

Authors: D. Momekova, G. Momekov, I. Pencheva, N. Lambov, S. Rangelov,


This study was aimed at determining the feasibility of DPPC:CHOL liposomes, sterically stabilized with a PEO-based polymer (DDGG)4(EO)114, previously validated as serum stable and long circulating formulation, to serve as a drug delivery platform for bendamustine hydrochloride. The drug loaded DPPC:CHOL:(DDGG)4(EO)114 LUVs were prepared by the lipid film hydration method, with successive freeze-thaw and extrusion cycles using an acidic solution of the drug in HBS (pH=2) as the dispersion medium. The liposomal formulation was characterized with average size of 153 nm, monomodal size distribution, and sustained release kinetics. The cytotoxicity evaluation has shown that liposomal bendamustine retains the biological activity of free drug and moreover after 4 day treatment is equieffective to it. These findings give us reason to consider DPPC:CHOL:(DDGG)4(EO)114 LUVs as a versatile drug delivery system for bendamustine hydrochloride.

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