1. Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
- Author
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Roser Fisa, Carme Guillén, Diana Berenguer, Ana C. Calpena-Campmany, Magdalena Alcover, Lyda Halbaut, Lilian Sosa, Marcella Sessa, Cristina Riera, and Universitat de Barcelona
- Subjects
Meglumine antimoniate ,leishmania infantum ,030231 tropical medicine ,Pharmaceutical Science ,lcsh:RS1-441 ,Human skin ,02 engineering and technology ,sepigel 305® ,Dosage form ,Article ,lcsh:Pharmacy and materia medica ,03 medical and health sciences ,Sepigel 305® ,cutaneous leishmaniasis ,0302 clinical medicine ,Cutaneous leishmaniasis ,Leishmaniosi ,medicine ,Leishmania infantum ,Cytotoxicity ,Leishmaniasis ,Chromatography ,biology ,Chemistry ,Permeation ,021001 nanoscience & nanotechnology ,medicine.disease ,biology.organism_classification ,Skin diseases ,topical treatment ,Malalties de la pell ,meglumine antimoniate ,0210 nano-technology ,Ex vivo ,medicine.drug - Abstract
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 (SbV) 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 µ, g/g/cm2 of SbV, respectively). The formulation did not have a toxic effect on the cell lines, and presented lower SbV IC50 values against amastigotes (15.76 ±, 4.81 µ, g/mL) in comparison with the MA solution. The high amount of drug retained in the skin and the SbV IC50 values obtained suggest that this semi-solid dosage form has potential as an alternative treatment of CL.
- Published
- 2019