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用于局部递送载有依巴斯汀的固体脂质纳米粒以缓解过敏性接触性皮炎的壳聚糖水凝胶。

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

作者信息

Kazim Tasbiha, Tariq Abeer, Usman Muhammad, Ayoob Muhammad Faisal, Khan Ahmad

机构信息

Department of Pharmacy, Quaid-i-Azam University Islamabad Pakistan

National Veterinary Laboratory Islamabad Pakistan.

出版信息

RSC Adv. 2021 Nov 22;11(59):37413-37425. doi: 10.1039/d1ra06283b. eCollection 2021 Nov 17.

Abstract

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 th eentrapment 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. 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. 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.

摘要

依巴斯汀是一种抗组胺药物,口服后对人体具有治疗过敏性接触性皮炎(ACD)的作用,但它也有一些全身性副作用,如胃部不适、头痛、嗜睡和鼻出血。此外,局部用皮质类固醇用于治疗ACD,这会导致人体皮肤失去厚度和弹性。因此,制备了载依巴斯汀固体脂质纳米粒(E-SLNs),并测定了它们对过敏性接触性皮炎的局部疗效。采用Compritol 888 ATO和吐温80通过热微乳液的冷稀释法制备E-SLNs。使用Design-Expert® 11.0版本的中心复合设计对E-SLNs进行统计学优化。优化后的E-SLNs呈现球形表面形态,zeta电位为-15.6±2.4 mV,多分散指数(PDI)为0.256±0.03,粒径为155.2±1.5 nm,依巴斯汀的包封率超过78%。使用傅里叶变换红外光谱(FT-IR)、X射线衍射(XRD)和透射电子显微镜(TEM)对纳米粒进行表征。以壳聚糖为胶凝剂、戊二醛为交联剂制备了载E-SLNs水凝胶。对E-SLNs分散体和载E-SLNs水凝胶进行了24小时的药物释放研究,结果显示最大持续释放率分别为82.9%和73.7%。在BALB/c小鼠上进行研究,以评估载E-SLNs水凝胶对过敏性接触性皮炎的局部疗效。使用苦味酸溶液在小鼠耳部诱导ACD。诱导后,每天用载E-SLNs水凝胶治疗耳部15天。耳部的肿胀行为、肥大细胞计数和组织病理学研究证实,该水凝胶减轻了过敏性接触性皮炎的症状。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a4f/9043795/fb2772ce4400/d1ra06283b-f1.jpg

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