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 µg/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 µg/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.
Highlights
Leishmaniasis is caused by protozoan parasites, including more than 20 Leishmania species, and is transmitted through the bites of infected female phlebotomine sandflies
It is a neglected tropical disease that is prevalent in low-income countries [1] and is endemic in 98 countries with tropical, temperate and mild temperate climates, with an estimated 12 million people infected by the disease
TwhitehdaekgirnaedticatcioonnstoafnMt kA= g0e.0l1wmaisn−c1o(mr2 p= leted in 1P5hmarminacae0un.9tdi9cs9f52o)0l1l(oF9i,wg1u1e,rdex a2FBOo)R,naePnEpdEhRthaReseEPVepIxEeprWcoennetangteiaolfmMoAdgeellwwiatsh~a89k.3in7 e±t0ic.1c5o%n. stant k = 0.01 min−1 (r2 = 0.799o9f51)6 (Figure 2B), and the P percentage of meglumine antimoniate (MA) gel was ~89.37 ± 0.15%
Summary
Leishmaniasis is caused by protozoan parasites, including more than 20 Leishmania species, and is transmitted through the bites of infected female phlebotomine sandflies. It is a neglected tropical disease that is prevalent in low-income countries [1] and is endemic in 98 countries with tropical, temperate and mild temperate climates, with an estimated 12 million people infected by the disease. In the Mediterranean area, Leishmania infantum is the main species responsible for CL and VL [3]. Depending on the Leishmania species involved, manifestations of CL range from self-resolving ulcerative lesions, which may take up to two years to heal, to painful open wounds that leave permanent scars or even disseminate and affect other areas of the body [4]
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