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用于银屑病和痤疮的蒽林微乳凝胶靶向递送的优化

Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne.

作者信息

Sakarkar Samiksha, Jagdale Swati, Dargude Shrikant, Chabukswar Anuruddha, Urooj Shabana, Bilal Anusha, Mengash Hanan Abdullah

机构信息

Department of Pharmaceutical Sciences, School of Health Sciences and Technology, Dr. Vishwanath Karad MIT World Peace University, Kothrud, Pune 411038, India.

Department of Electrical Engineering, College of Engineering, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia.

出版信息

Molecules. 2025 Jun 17;30(12):2629. doi: 10.3390/molecules30122629.

Abstract

Anthralin is known for its efficacy in treating psoriasis and acne, possessing poor solubility. Addressing these limitations, the present study endeavors to develop a microemulgel formulation of anthralin aimed at enhancing solubility. The solubility study was performed in various solvents. An o/w (oil-in-water) emulsion was formed using the water titration method, which was optimized by statistical experimental design half-run CCD. The final optimized batch was evaluated for physicochemical and in vitro properties The final optimized batch showed a particle size (PS) of 417 nm, -25.2 mV zeta potential (ZP) and pH 5.8, which remained stable upon centrifugation, heating-cooling and freeze-thawing cycle. Furthermore, microemulsion with Carbopol 943 5% / was selected as the gel base for the formation of microemulgel characterized by PS, ZP, pH, and viscosity of 230 nm, -50.6 mV, 6.9 and 14,200 cps, respectively, that ensured it a high enough stability. In silico molecular docking between ligand and protein provides the binding energies validating the interaction. Hence, the in silico study was performed for psoriasis and proteins. An in vitro antibacterial activity study on Propionibacterium revealed a significant efficiency of the formulation and MTT assay using L929 cell line in the presence of the drug-loaded microemulgel indicated an inhibition of growth proving that formulation has anti-psoriatic activity. Combination therapy with Clindamycin might improve efficacy while reducing antibiotic resistance risks.

摘要

蒽林以其治疗银屑病和痤疮的功效而闻名,但溶解性较差。为了解决这些局限性,本研究致力于开发一种蒽林微乳凝胶制剂,以提高其溶解度。在各种溶剂中进行了溶解度研究。采用水滴定法形成了水包油(o/w)乳液,并通过统计实验设计半运行CCD进行了优化。对最终优化批次进行了理化性质和体外性质评估。最终优化批次的粒径(PS)为417nm,ζ电位(ZP)为-25.2mV,pH值为5.8,在离心、加热-冷却和冻融循环后保持稳定。此外,选择含有5%卡波姆943的微乳液作为凝胶基质来形成微乳凝胶,其PS、ZP、pH值和粘度分别为230nm、-50.6mV、6.9和14200cps,确保了其足够高的稳定性。配体与蛋白质之间的计算机模拟分子对接提供了验证相互作用的结合能。因此,对银屑病和相关蛋白质进行了计算机模拟研究。对痤疮丙酸杆菌的体外抗菌活性研究表明该制剂具有显著效果,并且在存在载药微乳凝胶的情况下使用L929细胞系进行的MTT试验表明其生长受到抑制,证明该制剂具有抗银屑病活性。与克林霉素联合治疗可能会提高疗效,同时降低抗生素耐药风险。

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