Background:
There is an unmet need for optimized drug delivery system of
psoriasis therapy because of various issues like adverse reaction, permeation problem associated
with convention treatment (oral and topical) available for psoriasis.
Objective:
The goal was to develop an ethosomal gel of methotrexate (MTX)-incorporated
ethosomes and salicylic acid (SA) and to evaluate and study its ethosomal gel potential in
Imiquimod-induced psoriasis animal model to treat symptoms of psoriasis.
Methods:
MTX-SA ethosomal gel was prepared by the cold method given by Touitou et
al. and optimized by comparing it with MTX ethosomal gel and drug solution. Particle
size, zeta potential, entrapment efficiency, and ex-vivo study were selected as the critical
quality checking attributes. Psoriatic Area and Severity Index (PASI) score & histopathological
examination were done for checking Antipsoriatic potential of MTX-SA ethosomal
gel by using the imiquimod-induced psoriasis model.
Results:
Optimized MTX-SA exhibited a particle size of 376.04 ± 3.47nm, EE(Entrapment
efficiency) of 91.77 ± 0.02%. At the end of 24h, MTX-SA ethosomal gel exhibited a slow
and prolonged release of MTX (26.13 ± 1.61% versus 6.97 ± 0.06%) compared to MTX
drug solution. It also attributes of 43% retention study as compared to drug solution (13%).
Besides, it essentially decreased the PASI score with the recuperation of normalcy of the
mice's skin, while the MTX-SA gel displayed indications of gentle hyper and parakeratosis
toward the completion of investigation when contrasted with the blank gel.
Conclusion:
The developed MTX-SA ethosomal gel formulation can be a promising alternative
to existing MTX formulation in topically treating psoriasis.
Background:Artabotrys hexapetalus [(L.F) Bhandari] a medicinal plant is commonly known as ‘Hari Champa’ and its roots and fruits are used for treating malaria and scrofula, respectively.Objective:The aim of this work was to develop a sensitive, fast and reproducible high-performance thin-layer chromatographic (HPTLC) method for simultaneous analysis of quercetin and apigenin in various extracts of Artabotrys hexapetalus (L. f.) Bhandari (Family Annonaceae) and further to assess antileishmanic effects of different extracts of A. hexapetalus against Leishmania donovani.Materials and Methods:Metabolic fingerprinting was developed using HPTLC with quantification of markers (quercetin and apigenin). The method was validated for linearity, specificity, precision, accuracy and robustness. Among the different combinations of mobile phases used, best separation was achieved in toluene:ethyl acetate:formic acid (6.5:3:0.5, v/v/v). Densitometric scanning of the plates directly at 254 nm was used for analysis of quercetin as well as apigenin. The concentration-response curve was plotted and IC50 values were determined using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assay.Results:Compact bands for quercetin and apigenin were obtained at Rf 0.52 ± 0.001 and 0.73 ± 0.002, linearity were found satisfactory for quercetin and apigenin. Linearity range for quercetin and apigenin were 100–1000 ng/spot and 100–2000 ng/spot, respectively, with r2 = 0.996 ± 0.002 and 0.993 ± 0.003, limit of detection (15.56 and 13.78 ng/spot), limit of quantification (51.8 and 45.94 ng/spot), recovery (98.7%–99.7% and 96.8%–98.8%) and precision with %RSD <2%. Various dried extracts were found to contain quercetin in the range of 0.35%–4.26% (w/w) and apigenin in the range of 0.64%–8.46% (w/w). Cytotoxicity assay of extracts over promastigotes showed that petroleum ether extract was found to be most cytotoxic (IC50 30.28 ± 1.06 μg/mL) after 96 h in comparison to other extracts. The finding of this study indicates that this plant is effective against L. donovani in vitro.Conclusion:The present HPTLC method is being reported for the first time and can be used for routine quality control. The petroleum ether extract of A. hexapetalus displayed potent antileishmanial activity and can be further explored for the development of antileishmanial treatment regimen.
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