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

Pharmaceutics

卷:11

Carme Guillén¹  Magdalena Alcover¹  Roser Fisa¹  Cristina Riera¹  Diana Berenguer¹  Marcella Sessa²  Lilian Sosa²  AnaCristina Calpena-Campmany²  Lyda Halbaut² 

[1] Department of Biology, Health and Environment, Laboratory of Parasitology, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain;

[2] Department of Pharmaceutical Technology and Physicochemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain;

关键词: leishmania infantum;    cutaneous leishmaniasis;    meglumine antimoniate;    sepigel 305^®;    topical treatment;   

DOI  :  10.3390/pharmaceutics11110613

来源: DOAJ

【 摘 要 】

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 Leishmania infantum 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.

【 授权许可】

Unknown