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Title: | Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis. |
Author: | Berenguer, Diana Sosa Díaz, Lilian Elisa Alcover Amengual, Maria Magdalena Sessa, Marcella Halbaut, Lyda Guillen, Carmen Fisa Saladrigas, Roser Calpena Campmany, Ana Cristina Riera Lizandra, Ma. Cristina |
Keywords: | Leishmaniosi Leishmania infantum Malalties de la pell Leishmaniasis Leishmania infantum Skin diseases |
Issue Date: | 15-Nov-2019 |
Publisher: | MDPI |
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 microg/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 +/- 4.81microg/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. |
Note: | Reproducció del document publicat a: https://doi.org/10.3390/pharmaceutics11110613 |
It is part of: | Pharmaceutics, 2019 |
URI: | http://hdl.handle.net/2445/146042 |
Related resource: | https://doi.org/10.3390/pharmaceutics11110613 |
ISSN: | 1999-4923 |
Appears in Collections: | Articles publicats en revistes (Biologia, Sanitat i Medi Ambient) |
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