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Benzoxonium chloride is an anti-infective agent that is used as anti-septic drugs for disinfection of the mucus membrane, skin surface and anti-bacterial, and it is also found to be effective against cutaneous leishmaniasis. The present study aims to evaluate the leishmanicidal activity of benzoxonium chloride and niosomal forms against Leishmania tropica stages. Benzoxonium chloride niosomes were prepared by the thin film hydration method and evaluated for morphology, particle size and release study and encapsulation efficiency. This study measured the cytotoxicity, leishmanicidal activity against promastigote and intra macrophage amastigote, apoptosis, and mRNA transcripts by quantitative real time PCR (qPCR) of free solution and niosomal-encapsulated benzoxonium chloride. Span/Tween 60 niosomal formulation of benzoxonium chloride showed superior physical stability and high encapsulation efficiency (96%) than the other forms. Release from the formulations showed that the Span/Tween 60 containing drug had a milder gradient so that 10% of the drug was not released after 4 h. The benzoxonium chloride and niosomal forms inhibited the in vitro growth of promastigote and amastigote forms of L. tropica after 48 h of incubation and represented IC50 values of 90.7 ± 2.7 and 25.4 ± 0.6 μg/ mL, respectively. The rate of apoptosis in niosomal formulations was approximately equal to the positive control (meglumine antimoniate) at the same concentration. Also, an increase in the concentration of this drug reduced the expression of IL-10, but increased the expression of IL-12. The niosomal formulations provided improved anti-leishmanial activities of benzoxonium chloride and played an immunomodulatory role as the mode of action in the treatment of anthroponotic CL. [ABSTRACT FROM AUTHOR]

The strategy for improving the treatment of leishmaniasis by the World Health Organization, is the development of new drugs and combination therapy. The aim of this survey was to investigate the effect of amphotericin B (AmB) in combination with selenium, in a simple or niosomal form, on Leishmania tropica (L. tropica) by in vitro advanced assays. In this study, a niosomal formulation of AmB with selenium was prepared and characterized based on size and morphology. Using MTT assay, macrophage model, flow cytometry, and qPCR, the cytotoxicity and efficiency of the niosomal formulation and simple form of combination were evaluated. No toxicity was reported for both the niosomal and simple form of the combination. The niosomal formulation significantly showed higher inhibitory effect on the promastigote and amastigote forms of L. tropica than simple combination form. Interleukin (IL)-10 significantly decreased while the level of IL-12 and metacasoase as Th-1 activator significantly increased (P < 0.001). The findings of this study indicated that niosomes are the stable carriers for this combination, easy to produce and provide promising results as an effective formulation in the inhibition of extracellular and intracellular forms of L. tropica in compared with simple combination form. [ABSTRACT FROM AUTHOR]

Current treatment modalities in cutaneous leishmaniasis have low efficacy and high toxicity as well as high rate of resistance to treatment. In this study, for the first time we decided to evaluate efficacy of intralesional Glucantime plus niosomal zinc sulphate in comparison with intralesional Glucantime plus cryotherapy in the treatment of acute cutaneous leishmaniasis. This is a case-control study on 64 patients with cutaneous leishmaniasis in Kerman-Iran. Patients were categorized in 2 groups A and B whom were treated with weekly intralesional meglumine antimonite plus twice daily niosomal topical zinc sulphate versus weekly intralesional Glucantime plus every other week cryotherapy, respectively. We assessed the efficacy of treatment modalities (as partial and complete response) and their adverse effects by measuring size of the lesions every 2 weeks up to maximum of 12 weeks and 3 months after the end of the treatment. Partial response rate was 16.6% and 12.9% in group A and B, respectively (P = 0.784). Complete response rate was 73.3% and 80.6% in group A and B, respectively (P = 0.784). Complete response rate was achieved in 4.73 ± 0.29 weeks and 4.69 ± 0.28 weeks in group A and B, respectively (P = 0.925). Partial response rate was achieved in 2.92 ± 0.23 weeks and 2.65 ± 0.18 weeks, respectively (P = 0.365). Combination of niosomal zinc sulphate with intralesional Glucantime has equal efficacy versus combination of cryotherapy plus intralesional Glucantime in the treatment of acute cutaneous leishmaniasis. So, it can be used in cases that have resistance to first-line treatments. [ABSTRACT FROM AUTHOR]

Leishmaniasis is a spectrum of disease condition with considerable health impacts, caused by different species of Leishmania. This disease is currently endemic in 98 countries and territories in the world. There are many treatment modalities for cutaneous leishmaniasis. The use of topical terbinafine in the treatment of cutaneous leishmaniasis has recently been considered. Eighty-eight participants more than two years old with proven acute CL by a positive direct smear were randomly allocated to one of the two study arms: first group received meglumine antimoniate (Glucantime) 20 mg/kg/day intramuscular injection (IM) plus a placebo ointment (Mahan Vaseline) for 20 days. The second group received meglumine antimoniate (Glucantime) 20 mg/kg/day IM plus topical terbinafine, for 20 days and were monitored closely by dermatologist during the course of the study. Crude regression analysis showed that there was no significant difference between placebo and intervention group regarding partial or complete treatment (partial treatment: HR = 1.1, CI 95 % = 0.7-1.7; complete treatment: HR = 1.1, CI 95 % = 0.8-1.7). Although, there was no statistically significant different between the two treatment groups, but clinically it seems that the treatment rate in those who receive glucantime plus terbinafine was more effective than the other group. However this rate depended on the type of lesions. As data indicated ulcerated nodules, papules and plaque in experimental group have been completely improved two times faster than placebo group. Ulcerated nodules, nodules and plaque were partially improved faster in those used tebinafine than placebo ointment. [ABSTRACT FROM AUTHOR]

Zinc sulfate (ZS) has been used for the treatment of acute cutaneous leishmaniasis (CL) in both forms of in vivo and in vitro recently. The aim of the present study was to compare the efficacy of intralesional injection of ZS 2 % solution with intralesional glucantime in the treatment of acute CL. In this double-blind randomized clinical trial, 80 cases with acute old world dry type CL were enrolled in the study. The treatment protocol in the first group consisted of intralesional injection of ZS 2 % vials once a week for 10 weeks or sooner in case of complete resolution of the lesions. In the second group, intralesional glucantime once a week for 10 weeks or sooner in case of complete resolution of the lesions were used. In both groups cryotherapy was performed once every other week for 10 weeks. In ZS versus second group, partial and complete clinical response was observed with fewer injections although this difference was not statistically significant. In addition, we found that the trend of treatment in second group was faster but again it was not significant [partial treatment: hazard ratio (HR) 1.4, 95 % CI 0.7-2.9; complete treatment: HR 1.3, 95 % CI 0.6-2.8]. The results of this study showed that the intralesional injection of ZS 2 % solution was as effective as glucantime on the healing of the acute old world dry type CL. [ABSTRACT FROM AUTHOR]