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. 2025 Apr 25;26(5):115.
doi: 10.1208/s12249-025-03103-w.

Integration of Synchronizing In Silico, In Vitro, and In Vivo Strategies for the Development of Antipsoriatic Apremilast-loaded Nanostructured Lipid Carrier Embedded in Hydrogel

Nikita Patel  1 , Aneri Desai  1 , Bhavin Vyas  1 , Pranav Shah  2 , Mangrulkar Shubhada  3 , Umekar Milind  3 , Kamla Pathak  4 , Mahavir Bhupal Chougule  5
Affiliations

Integration of Synchronizing In Silico, In Vitro, and In Vivo Strategies for the Development of Antipsoriatic Apremilast-loaded Nanostructured Lipid Carrier Embedded in Hydrogel

Nikita Patel et al. AAPS PharmSciTech. .

Abstract

One of the major challenges in the psoriasis therapies is the systemic side effects. This research investigation intended to design, formulate, and characterize topical Apremilast (APR) nanostructured lipid carriers (NLCs) embedded hydrogel. APR-loaded NLCs were prepared using the hot melt ultrasonication technique using glyceryl monostearate (GMS) and Capmul® MCM, followed by high-speed homogenization. The entrapment and size were 85.5 ± 2.1% and 242.5 ± 3.1 nm, respectively. Using molecular docking, the interactions between APR-GMS and APR-Capmul® MCM were investigated. 32 factorial designs were used to optimize APR-loaded NLCs, employing a quality-by-design approach. The spherical shape of the nanocarriers was depicted in the SEM images of NLCs dispersion. With a regression value of 0.9745, the in vitro drug release of APR-NLCs dispersion matched the Higuchi model and demonstrated extended-release up to 28 hrs (99.0 ± 1.7%). An in vitro cellular toxicity depicted that formulation excipients had minimal effect, as cell viability was still > 80% at concentrations of up to 30 µg/mL. APR-NLC hydrogel exhibited extended release up to 36 hrs (97.1 ± 0.8%), with diffusion as a release mechanism. Since there was no significant difference observed in viscosity (cp) or % CDR throughout 24 hrs at 5°, indicate APR-NLCs hydrogel was stable in a refrigerated condition. Compared to the positive control, APR liquid, and pure drug, APR-NLCs hydrogel showed a substantial decrease in PASI score. Topical APR-loaded NLCs embedded in Hydrogel enhanced efficacy in the imiquimod-induced psoriasis in the murine model found to be non-irritating with minimal systemic side effects. The findings imply that APR-loaded NLCs embedded in Hydrogel can be used topically to treat psoriasis by focusing on the skin's outer layers.

Keywords: Apremilast; Hydrogel; Molecular docking; Nanostructured lipid carriers; Psoriasis; Topical.

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Conflict of interest statement

Declarations. Ethics Approval and Consent to Participate: No humans were utilized in this research work. The caution and use of laboratory animals were conducted in according with all institution and national guidelines. The study protocol number was (MPC/IAEC/08/2022) and Protocol number (853/IAEC/2023 - 24/27). Competing Interest: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. Consent for Publication: The permission to publish has been granted by each author.

References

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