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The Thai Journal of Pharmaceutical Sciences

Abstract

Background: Psoriasis is a dynamic and chronic disease characterized by inflammatory changes and an increased rate of keratinocyte proliferation leading to the formation of erythematous scleroderma plaques with a silvery sheen. The existing therapies come with shortcomings in terms of effectiveness and leave behind a trail of side effects. Hence, there is a need of alternative therapeutic measures. Objectives: This study aimed to assess the therapeutic potential of Apremilast Niosomal Gel (APR Nio Gel) in treating psoriasis, comparing its effectiveness with conventional gel (APR Gel) and oral suspension (APR Oral) formulations. Materials and Methods: Apremilast niosomes were prepared by thin film hydration technique with change in Cholesterol and Poloxamer 188 concentrations. The niosomes were evaluated for particle size by dynamic light scattering technique, and entrapment efficiency by centrifugation method. In addition, zeta potential and surface characterization by transmission electron microscopy (TEM) were performed on selected AP2 niosomes. AP2 niosomes were formulated into topical carbomer-based gel and further evaluated for pH, viscosity by rheometer, drug content/ drug loading by high-performance liquid chromatography (HPLC), in vitro drug release, and skin deposition studies in pig skin. The formulation was further evaluated for stability studies and in vivo study in Imiquimod induced psoriasis Swiss albino mice for morphological assessments by psoriasis area scoring index (PASI), Moisture content in skin by MoistureMeterSC, trans-epidermal water loss (TEWL) by vapometer, spleen index and histology of psoriatic skin by hematoxylin and eosin staining. Results: The selected AP2 niosomal formulations showed a particle size of 147.3 ± 26.5 nm, entrapment efficiency of 65.27 ± 5.7%, and further analyzed for zeta potential (−54.9 ± 9.6 mV) and TEM image showed a spherical shape of the niosomes. The AP2 niosomes were loaded into Carbomer gel to get APR Nio Gel. The pH was observed to be 6.83 ± 0.14, viscosity to be 1564.1 ± 86.1 Pa.s, and drug content of 98.1 ± 0.3%. Similarly, APR Gel was prepared. The morphology and PASI scoring showed the improvement of psoriasis condition in APR Nio Gel group (total PASI score: 1.4 ± 1.2) compared to APR Gel group (total PASI score: 9.9 ± 1.3) and APR Oral (total PASI score: 4.8 ± 1.1) at the end of the study. Similarly, APR Nio Gel showed moisture content (40.1 ± 11.5), TEWL (18.2 ± 4.2 g/m2.h), spleen index (7.5 ± 1.8) and histology of skin showed significant improvement in psoriasis condition (P < 0.05) when compared with APR Gel and APR Oral. Conclusion: APR Nio Gel might offer a better solution due to its improved skin permeation and deposition. These findings indicate that niosomal formulations may provide a more efficient and focused method for the treatment of psoriasis and reduce the systemic exposure of the drugs.

DOI

10.56808/3027-7922.2978

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