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, in vitro drug release, and shape. Creams loaded with optimized ethosomal dispersion of piperine were formulated and evaluated for physicochemical parameters, ex vivo 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 in vivo 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

研究工作的目的是研究与传统乳膏相比，负载胡椒碱脂质纳米载体（ethosomes）的乳膏在治疗特应性皮炎（AD）方面的功效。胡椒碱的 Ethosomes 由不同浓度的磷脂酰胆碱和乙醇配制而成；并评估包封效率 (EE)、沉降行为、囊泡大小、zeta 电位、体外药物释放和形状。配制了装载有优化的胡椒碱的 ethosomal 分散体的乳膏，并评估了离体的物理化学参数皮肤层的渗透和药物滞留。类似地，配制和评估了相同浓度的常规胡椒碱乳膏。使用 HaCat 细胞系和体内评估优化的 ethosomal 常规乳膏的细胞毒性在 BALB/c 小鼠模型上。EE (%) 和囊泡大小分别为 74.30 ± 3.88% 和 318.1 nm，以优化 ethosomal 分散。zeta 电位为 -32.6 mV，囊泡呈球形。ethosomal 霜在表皮和真皮中显示出较高的沉积。乳膏对 HaCat 细胞系没有细胞毒性。与阴性对照相比，ethosomal (0.1%) 和常规 (0.125%) 乳膏均显着降低了耳朵和皮肤厚度、皮肤严重程度；和 BALB/c 小鼠模型中的 WBC、粒细胞和 IgE 抗体水平。与他克莫司 (0.1%) 相比，Ethosomal 乳膏的功效显着高于传统乳膏。与传统乳膏相比，胡椒碱的 Ethosomal 乳膏在 AD 管理方面显示出良好的潜力。