Amphotericin B-loaded polymersomes (PAMBO): Formulation Development and Stability

摘要

Amphotericin B (AmB)-loaded polymersomes (PAMBO) were prepared from branched (mPEG)_3-PLA amphiphilic polymer with 0.1 PEG fraction by solvent injection method. PAMBO having size, PDI and loading of 266.45±34.47 nm, 0.258±0.180 and 16.26±2.50%, respectively were obtained. AmB was found to be intercalated in the wall of polymersomes. Release of AmB from PAMBO was faster up to 48 h and slows down thereafter. Lyophilization of PAMBO was also optimized. Free drug was not found in the formulation and different molecular forms of the drug (AmB) were observed by UV-Vis spectroscopy and circular dichroism. PAMBO caused negligible hemolysis. Stability of the lyophilized PAMBO was studied for 3 months in three different conditions viz. cold (2-8°C), ambient and accelerated conditions (40°C, 75% relative humidity-RH). Moisture and high temperature lead to dissolution of inulin during storage and aggregation of PAMBO. Lyophilized PAMBO formulation was stable on shelf at ambient conditions for 3 months. Reconstituted PAMBO showed stability in terms of size and PDI over a period of 10 days.