Chitosan hydrogel for topical delivery of ebastine loaded solid lipid nanoparticles for alleviation of allergic contact dermatitis

Ebastine, is an antihistamine drug that exerts its effect upon oral administration in humans for the treatment of allergic contact dermatitis (ACD), it also has some systemic side effects like gastric distress, headache, drowsiness, and epistaxis. Moreover, topical corticosteroids are used for treatment of ACD, which causes the human skin to lose its thickness and elasticity. Hence, ebastine-loaded solid lipid nanoparticles (E-SLNs) were prepared and their topical efficacy against allergic contact dermatitis was determined. Compritol 888 ATO and tween 80 were used to prepare E-SLNs by cold dilution of the hot micro-emulsion.

E-SLNs were optimized statistically by employing a central composite design using Design-Expert® version 11.0. Optimized E-SLNs showed spherical surface morphology, zeta potential of −15.6 ± 2.4 mV, PDI of 0.256 ± 0.03, and particle sizes of 155.2 ± 1.5 nm and the entrapment efficiency of ebastine was more than 78%. Nanoparticles were characterized using FT-IR, XRD, and TEM. An E-SLNs loaded hydrogel was prepared using chitosan as a gelling agent and glutaraldehyde as a crosslinker. In vitro drug release studies performed for 24 hours on the E-SLNs dispersion and E-SLNs loaded hydrogel showed a sustained release of maximum 82.9% and 73.7% respectively.

In vivo studies were conducted on BALB/c mice to evaluate the topical efficacy of the E-SLNs loaded hydrogel for allergic contact dermatitis. ACD was induced on the ear using picryl chloride solution. After induction, ears were treated daily with the E-SLNs loaded hydrogel for 15 days. Swelling behavior, mast cell count, and histopathological studies of the ear confirmed that the hydrogel alleviated the symptoms of allergic contact dermatitis.

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Materials: Ebastine was obtained from the Global pharmaceuticals. Compritol 888 ATO (Glyceryl Behenate) was received as a gift from Morgan Chemicals (Gattefosse, Germany), glutaraldehyde 70% (Sigma-Aldrich Chemie). Chitosan was purchased from Sigma Aldrich, M.W. = 310–375 kDa (CAS-9012-76-4). Picryl Chloride was obtained from Sigma Aldrich. Tween-80 was gifted by Horizon Pharmaceuticals. Olive oil (pharmaceutical grade) was obtained from Scotmann pharmaceuticals.

Article information: Tasbiha Kazim, Abeer Tariq, Muhammad Usman, Muhammad Faisal Ayoob and Ahmad Khan. DOI: 10.1039/D1RA06283B (Paper) RSC Adv., 2021, 11, 37413-37425.