Development and Pharmaceutical Evaluation of Azelaic Acid and Vitamin E Oil-Based Nanoemulgel of Tacrolimus for Topical Application in Plaque Psoriasis

Kumar, Vineet; Roy, Ankita; Sharma, Anita; Rath, Goutam; Kar, Biswakanth; Ghosh, Goutam; Pradhan, Deepak; Halder, Jitu

doi:10.1007/s12247-023-09740-7

Cited by 8 publications

(2 citation statements)

References 18 publications

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“…An ex vivo study was conducted on freshly excised skin from pig ears to assess the skin permeation. Despite the water-based nature of the gel, it demonstrated considerable efficacy in maintaining skin moisture levels and delivering the drug accurately [ 116 ].…”

Section: Current Nanotechnology-based Approaches For the Topical Trea...mentioning

confidence: 99%

Recent Approaches for the Topical Treatment of Psoriasis Using Nanoparticles

Bodnár,

Fehér,

Ujhelyi

et al. 2024

Pharmaceutics

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Psoriasis (PSO) is a chronic autoimmune skin condition characterized by the rapid and excessive growth of skin cells, which leads to the formation of thick, red, and scaly patches on the surface of the skin. These patches can be itchy and painful, and they may cause discomfort for patients affected by this condition. Therapies for psoriasis aim to alleviate symptoms, reduce inflammation, and slow down the excessive skin cell growth. Conventional topical treatment options are non-specific, have low efficacy and are associated with adverse effects, which is why researchers are investigating different delivery mechanisms. A novel approach to drug delivery using nanoparticles (NPs) shows promise in reducing toxicity and improving therapeutic efficacy. The unique properties of NPs, such as their small size and large surface area, make them attractive for targeted drug delivery, enhanced drug stability, and controlled release. In the context of PSO, NPs can be designed to deliver active ingredients with anti-inflammatory effect, immunosuppressants, or other therapeutic compounds directly to affected skin areas. These novel formulations offer improved access to the epidermis and facilitate better absorption, thus enhancing the therapeutic efficacy of conventional anti-psoriatic drugs. NPs increase the surface-to-volume ratio, resulting in enhanced penetration through the skin, including intracellular, intercellular, and trans-appendage routes. The present review aims to discuss the latest approaches for the topical therapy of PSO using NPs. It is intended to summarize the results of the in vitro and in vivo examinations carried out in the last few years regarding the effectiveness and safety of nanoparticles.

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Section: Current Nanotechnology-based Approaches For the Topical Trea...mentioning

confidence: 99%

Recent Approaches for the Topical Treatment of Psoriasis Using Nanoparticles

Bodnár,

Fehér,

Ujhelyi

et al. 2024

Pharmaceutics

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“…Phototherapy and systemic therapies are used to treat those with severe illness. Due to its intrinsic benefits, such as higher patient compliance, localized therapeutic activity, and little systemic toxicity, topical therapy is still currently the preferred method of treatment for the management of psoriasis [19]. However, a significant downside of topical therapies is insufficient medication penetration through the scaly psoriatic skin.…”

Section: Introductionmentioning

confidence: 99%

Microsponge-Based Gel Loaded with Immunosuppressant as a Simple and Valuable Strategy for Psoriasis Therapy: Determination of Pro-Inflammatory Response through Cytokine IL-2 mRNA Expression

Mehmood,

Shahid,

ul Huq

et al. 2023

Gels

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Tacrolimus (TL) is a topical calcineurin inhibitor immunosuppressive drug widely used to manage various skin disorders. Herein, we report a TL-loaded microsphere gel formulation with severe atopic dermatitis effects that are required to manage skin disorders. The current study adopted a modified emulsion solvent evaporation technique to synthesize TL-loaded microspheres, which were further converted into gels for skin use. Characterization of the synthesized formulation was performed by differential dynamic light scattering, scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, X-ray crystallography, Brunauer–Emmett–Teller (BET) analysis, differential scanning calorimetry, and drug release. A Franz diffusion cell was used to study the diffusion of TL for up to 8 h at pH 6.8 and 5.5. Evaluation of cell viability was determined by MTT assay and showed higher IC50 values compared to the plain drug. RNA extraction, real-time polymerase chain reaction (RT–PCR), and reverse transcription were also performed to determine the expression levels of the anti-inflammatory cytokine IL-2. Particle size determination was performed by a zeta sizer, and the TL microsphere size was 1745 ± 70 nm with a good polydispersity (0.337 ± 0.12). The drug entrapment efficiency was also very good at 60% ± 10, and the drug release was 93.9% ± 3.5 within 8 h. An in vitro diffusion study of the formulation also showed improved permeability at both pH values (4.5 and 5.5). The findings of the hemolytic tests demonstrated that TL-MG at concentrations of 50, 100, and 200 mg/mL did not produce any hemolysis. A dose-dependent pattern of cytotoxicity was found during the cell viability assay, with an IC50 value of 787.55 ± 12.78 µg/mL. There was a significant decrease in the IL-2 level in the TL-MG group compared to the other groups. TL-MG microspheres were nontoxic carriers for tacrolimus delivery, with greater loading capacity, a significant release profile, and enhanced cellular uptake with improved permeability.

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