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用于治疗特应性皮炎的胡椒碱负载脂质纳米载体外用乳膏:使用BALB/c小鼠模型进行的研发、表征及研究

Topical creams of piperine loaded lipid nanocarriers for management of atopic dermatitis: development, characterization, and investigation using BALB/c mice model.

作者信息

Kumar Pravin, Sharma Dinesh Kumar, Ashawat Mahendra Singh

机构信息

Department of Pharmaceutics, Laureate Institute of Pharmacy, Jwalamukhi, India.

Department of Pharmaceutics, Himalayan Institute of Pharmacy and Research, Dehradun, India.

出版信息

J Liposome Res. 2022 Mar;32(1):62-73. doi: 10.1080/08982104.2021.1880436. Epub 2021 May 4.

Abstract

The aim of the research work was to investigate the efficacy of cream loaded with lipid nanocarriers (ethosomes) of piperine for the management of atopic dermatitis (AD) in comparison to conventional cream. Ethosomes of piperine were formulated with varying concentration of phosphatidylcholine and ethanol; and evaluated for entrapment efficiency (EE), sedimentation behaviour, vesicle size, zeta potential, drug release, and shape. Creams loaded with optimized ethosomal dispersion of piperine were formulated and evaluated for physicochemical parameters, permeation and drug retention in skin layers. Similarly, conventional creams of piperine in the same concentrations were formulated and evaluated. The optimized ethosomal a conventional cream was evaluated for cytotoxicity using HaCat cell lines and on BALB/c mice model. The EE (%) and vesicle size was 74.30 ± 3.88% and 318.1 nm, respectively, for optimized ethosomal dispersion. The zeta potential was -32.6 mV and vesicles were spherical in shape. The ethosomal cream showed higher deposition in the epidermis and dermis. The creams were non-cytotoxic to HaCat cell lines. In comparison to the negative control, the ethosomal (0.1%) and conventional (0.125%) cream, both significantly decreased the ear and skin thickness, skin severity; and WBC, granulocytes, and IgE antibodies level in the BALB/c mice model. The efficacy of ethosomal cream was significantly higher than conventional cream as compared to tacrolimus (0.1%). Ethosomal cream of piperine showed good potential for the management of AD in comparison to conventional cream.

摘要

本研究工作的目的是比较含胡椒碱脂质纳米载体(醇质体)的乳膏与传统乳膏治疗特应性皮炎(AD)的疗效。用不同浓度的磷脂酰胆碱和乙醇制备胡椒碱醇质体;并对其包封率(EE)、沉降行为、囊泡大小、zeta电位、药物释放和形状进行评估。制备含优化胡椒碱醇质体分散体的乳膏,并对其理化参数、皮肤各层的渗透和药物滞留情况进行评估。同样,制备相同浓度的传统胡椒碱乳膏并进行评估。使用HaCat细胞系和BALB/c小鼠模型对优化的醇质体乳膏和传统乳膏进行细胞毒性评估。优化后的醇质体分散体的包封率(%)和囊泡大小分别为74.30±3.88%和318.1nm。zeta电位为-32.6mV,囊泡呈球形。醇质体乳膏在表皮和真皮中的沉积较高。这些乳膏对HaCat细胞系无细胞毒性。与阴性对照相比,醇质体(0.1%)乳膏和传统(0.125%)乳膏均显著降低了BALB/c小鼠模型的耳部和皮肤厚度、皮肤严重程度以及白细胞、粒细胞和IgE抗体水平。与他克莫司(0.1%)相比,醇质体乳膏的疗效显著高于传统乳膏。与传统乳膏相比,胡椒碱醇质体乳膏在治疗特应性皮炎方面显示出良好的潜力。

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