NEW TOPICAL BIOADHESIVE ANFOTERICIN-B FORMULATIONS WITH POTENTIAL APPLICATION ON CUOTANEOUS LEISHMANIASIS TREATMENT. STABILITY AND PRELIMINAR IN-VIVO PERFORMANCE EVALUATION.

AMBROSIONI, FRANCO E.; JIMÉNEZ KAIRUZ, ÁLVARO F.; FERNANDA GARCIA BUSTOS

Encuentro; 6TA REUNIÓN INTERNACIONAL DE CIENCIAS FARMACÉUTICAS (RICIFA 2020+1; 2021

Cutaneous Leishmania (CL) is an endemic parasitic-disease in Latinoamérica. Currently, high cost, toxicity and adverse events incidence of available systemic treatments contribute to high morbi-mortality. Amphotericin-B (AmB) is recommended, as second line drug, in resistant infections, but poor solubility and stability are conditioning factors for its formulation. This work is focused on formulation of new topical dosage form containig AmB, based on ternary interpolyelectrolyte complexes (IPEC) with hyaluronic acid (HyA) and chitosan (Chi). From IPEC, three formulations were prepared containing 0,1% of AmB, one hydrogel and two spray forms, using arginine or lecithin as absorption enhancer or humectant. The quality attributes of formulation were assayed by dynamic/oscilatory reometry, texturometry and extensibility/sprayability determinations. HPLC and UV assays were used to AmB quantification. All formulations presented appropriate physico-mecanical and adhesive behaviours for facilitate the application, coverage and permanence on the skin. Complexes and formulations showed increased stability compared to AmB solution and their microbial activities, against S. cerevisiae, were not modified for complexing nor by the passage of time. Evaluations of topical lesions on murine model showed similar efficacy of formulation respect to systemic reference. Lecithin contain’ formulation showed loss of effectiveness.Bioadhesive topical modified release formulations of AmB are an interesting, efficient and safe alternative for optimize LC treatment.