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Colloidal, in vitro and in vivo anti-leishmanial properties of transfersomes containing paromomycin sulfate in susceptible BALB/c mice.

Abstract：

:The aim of this study was to develop transfersomal formulation with respect to dermal delivery of paromomycin sulfate (PM) for possible topical therapy of cutaneous leishmaniasis (CL). PM transfersomal formulations (PMTFs) with different percent of soy phosphatidylcholine, sodium cholate (Na-Ch) and ethanol were prepared and characterized for the size, zeta potential and encapsulation efficiency. The results showed that the most stable formulations with suitable colloidal properties were obtained by 2% Na-Ch which had average size of around 200 nm. The in vitro permeation study using Franz diffusion cells fitted with mouse skin at 37°C for 24h showed that almost 23% of the PMTFs applied penetrated the mouse skin, and the amount retained in the skin was about 67% for both formulations; however, the percent of penetration and retention for PM conventional cream was 49 and 13, respectively. The 50% effective doses of PMTFs against Leishmania major promastigotes and amastigotes in culture were significantly less than cream and/or solution of PM. Selected PMTFs and empty transfersomes showed no cytotoxicity in J774 A.1 mouse macrophage cell line. Selected PMTFs was used topically twice a day for 4 weeks to treat L. major lesions on BALB/c mice, and the results showed a significantly (P<0.05) smaller lesion size in the mice in the treated groups than in the mice in the control groups, which received either empty transfersomes or phosphate-buffered saline (PBS) and also PM cream. The spleen parasite burden was significantly (P<0.01) lower in mice treated with selected PMTFs than in mice treated with PBS or control transfersomes, and PM cream. The results of this study showed that PMTFs prepared with 2% of Na-Ch with and without 5% ethanol might be useful as a candidate for the topical treatment of CL.

journal_name

Acta Trop

journal_title

Acta tropica

authors

Bavarsad N,Fazly Bazzaz BS,Khamesipour A,Jaafari MR

doi

10.1016/j.actatropica.2012.06.004

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

33-41

issue

eissn

0001-706X

issn

1873-6254

pii

S0001-706X(12)00230-6

journal_volume

124

pub_type

杂志文章

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Colloidal, in vitro and in vivo anti-leishmanial properties of transfersomes containing paromomycin sulfate in susceptible BALB/c mice.