Novel insight into Potential Leishmanicidal Activities of Transdermal Patches of Nigella Sativa: Formulation Development, Physical Characterizations and In vitro In vivo Assays

Abstract

Cutaneous Leishmaniasis (CL) is the most common type of Leishmaniasis which annually affects 1.5 million people worldwide. About 90% of cases are reported from countries such as Iran, Afghanistan, Pakistan, Iraq, and Saudi Arabia. The purpose of the present study was to fabricate transdermal patches of Nigella sativa (NS), characterize and to check its in vitro in vivo anti-Lieshmanial activity. Hydroalcohlic extract was analyzed for preliminary phytochemicals. Five formulations of transdermal patches (NS1, NS2, NS3, NS4 and NS5) were prepared by solvent evaporation method. The optimized formulation NS5 was characterized for FTIR, smoothness, brittleness, clarity, thickness, folding endurance, uniformity of weight, percent moisture content, in-vitro drug release, release kinetics, ex vivo drug permeation and in-vitro anti-Lieshmanial activity. In vivo anti-Lieshmanial activity was assessed in 30 patients (n = 30) suffering from CL. The FTIR studies showed no incompatibility among the active extract and polymers. In vitro anti-Lieshmanial assay was 194.6 ± 1.88 % as compared to standard drug (p > 0.05) and in vivo anti-Lieshmanial activity was 75 %. The drug release after 24 hours was 87.0 ± 0.94% in NS5 which showed non-Fickian diffusion mechanism while drug permeation across rabbit skin after 24 hours was up to 80.0 ± 0.91%. The results concluded that problems related to the medications parenterally used for Lieshmanial treatment can be managed by applying extract of Nigella sativa seeds in the form of transdermal patch.

Development of Chitosan-Based Nanoemulsion Gel Containing Microbial Secondary Metabolite with Effective Antifungal Activity: In vitro and in vivo Characterizations

“…The therapeutic efficacy of any drug depends upon the drug release from pharmaceutical dosage forms. 11 , 15 , 22 The drug release from topical formulation is dependent upon several factors including gelling polymeric agents, emulsifying agents, spreadability, and viscosity. 20 , 40 The drug release from F2 (Pure 2 compound-loaded NE) and F3 (Pure 2 compound-loaded NEG) formulations are presented in Figure 5 .…”

“…Skin permeation is an important feature for efficient transdermal drug delivery. 11 The ex vivo drug permeation studies were conducted for both F2 (Pure 2 compound-loaded NE) and F3 (Pure 2 compound-loaded NEG) using rabbit skin. The % drug permeation is given in Figure 6 .…”

“…The in vitro drug release study was performed according to the previous study conducted by Khan et al 11 Franz diffusion cell (IPS Technologies, India) was used for this purpose and consists of receptor and donor compartments having capacity of 6 mL and 3 mL, respectively. Prior to loading NE and NEG samples, the temperature was maintained at 37°C±1°C under stirring (300 rpm).…”

“…Topically applied transdermal formulations have numerous advantages including site targeting, 11 minimizing side effects associated with oral preparations, 12 high patient acceptance, enhanced patient compliance, and improved therapeutic efficacy. 13 The topical formulations show their efficacy if the drug from these formulations releases and penetrates the layers of skin, which will create an effective drug depot.…”