A topical gel nanoformulation of amphotericin B (AmB) for the treatment of cutaneous leishmaniasis (CL)

This study aimed to improve the water solubility and cutaneous permeability of Amphotericin B (AmB) for the topical treatment of Leishmania major-induced cutaneous leishmaniasis (CL) using two topical liposome-and polyethylene glycol (PEG)ylated liposome-gel formulations. The topical gel formulations of AmB were developed by its encapsulation into liposome (Lip-AmB) and (PEG)ylated liposome (PEG-Lip-AmB) using the reverse-phase evaporation method. The nanoformulations were characterized using dynamic light scattering and spectrophotometry. Their biological effects were evaluated in vitro and in vivo using Wright-Giemsa staining, limiting dilution assay, and pathological studies. Lip-AmB and PEG-Lip-AmB with the size of 257 +/- 12.5 nm and 237 +/- 12 nm, respectively, were synthesized. PEG-Lip-AmB compared to Lip-AmB, was more potent to decrease the drug toxicity and increase the drug's therapeutic effects. The results of in vivo studies were in agreement with the results of in vitro studies, in which PEG-Lip-AmB-loaded gel (PEG-Lip-AmB-Gel), compared to Lip-AmB-loaded gel, could decrease the lesion size and parasite burden by 1.7-and 1.6-fold, respectively. These results suggest PEG-Lip-AmB-Gel can be used as a promising carrier to improve the properties of AmB for topical application against CL.

Automated summary

This study aimed to improve the solubility and permeability of Amphotericin B (AmB) for the topical treatment of cutaneous leishmaniasis (CL) caused by Leishmania major. Two formulations of AmB, Lip-AmB and PEG-Lip-AmB, were developed using liposomes and polyethylene glycol (PEG)ylated liposomes. The results showed that PEG-Lip-AmB was more effective in reducing drug toxicity and increasing therapeutic effects compared to Lip-AmB. In vivo studies also demonstrated that PEG-Lip-AmB-Gel could significantly reduce lesion size and parasite burden compared to Lip-AmB-Gel. These findings suggest that PEG-Lip-AmB-Gel is a promising carrier for improving the properties of AmB for topical treatment of CL.