DSPC based polymeric micelles loaded with Amphotericin B: synthesis, characterization, and in vitro study

Amphotericin B (AmB) is one of the toxic drugs that with appropriate micelles structure for encapsulation can be effectively used in fungal infections and leishmaniasis treatments. The present work focuses on the design and development of micelles containing amphotericin B to decrease toxicity and improve antifungal activity. To this end, AmB was encapsulated in 1, 2-distearoyl-S-glycero-3-phosphorylcholine (DSPC) based micelles in the sensitive range of structural change with different ratios of DSPC and DSPE-PEG2000 (10:1, 9:2, 8:3; w/w ) using the solvent evaporation method in methanol/chloroform medium. The effect of solvent composition and the combination of different ratios on the morphological and structural characteristics of unloaded and drug-loaded micelles were investigated by TEM and FESEM analyses. With a ratio of 9:2 w/w, spherical shape, and more uniform were successfully synthesized and considered as an optimal preferable microstructure for drug loading. Moreover, due to the slow release of the micelles system, the maximum drug release within 72 hours in the buffer environment is 86.2 %. The DLS analysis reported the mean particle size of drug-loaded Micelles as 55.1 nm and unloaded micelles as 51.6 nm. TEM-based particle size determination of the AmB-loaded sample revealed that the mean diameter of the micelles with optimum formulation was 27 ± 0.7 nm and for unloaded micelles 24 ± 0.6 nm. Furthermore, the Cytotoxicity of the AmB’s micelles was tested using the MTT assay. In addition, S. aureus,  E. coli, and C. Albicans strains were employed during the antimicrobial and antifungal tests.