Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis

• Main Authors: Diana Berenguer (Author), Lilian Sosa (Author), Magdalena Alcover (Author), Marcella Sessa (Author), Lyda Halbaut (Author), Carme Guillén (Author), Roser Fisa (Author), Ana Cristina Calpena-Campmany (Author), Cristina Riera (Author)
• Format: Book
• Published: MDPI AG, 2019-11-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

Cutaneous leishmaniasis (CL) is treated with painful intralesional injections of meglumine antimoniate (MA). With the aim of developing an alternative topical treatment for CL, a gel-based formulation with 30% MA was prepared and its physicochemical properties, stability and rheological behavior were studied. The following were assessed: drug release on propylene hydrophilic membranes ex vivo human skin permeation, tolerance in healthy volunteers, cytotoxicity in three cell lines and anti-leishmanial activity against <i>Leishmania infantum</i> promastigotes and amastigotes. The MA gel formulation was found to have suitable pH, and good spreadability and stability. Low quantities of pentavalent antimony (Sb^V) were observed in release and permeation tests, whereas retention was high in both non-damaged and damaged skin (71,043.69 ± 10,641.57 and 10,728 ± 2254.61 µg/g/cm² of Sb^V, respectively). The formulation did not have a toxic effect on the cell lines, and presented lower Sb^V IC₅₀ values against amastigotes (15.76 ± 4.81 µg/mL) in comparison with the MA solution. The high amount of drug retained in the skin and the Sb^V IC₅₀ values obtained suggest that this semi-solid dosage form has potential as an alternative treatment of CL.

Item Description

1999-4923
10.3390/pharmaceutics11110613