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Formulation and evaluation of a topical liposomal gel containing a combination of zedoary turmeric oil and tretinoin for psoriasis activity
Journal of Liposome Research ( IF 4.4 ) Pub Date : 2020-04-17 , DOI: 10.1080/08982104.2020.1748646
Ji Chen 1, 2 , Yanqiao Ma 3 , Yueying Tao 2 , Xiaoqian Zhao 1 , Yongai Xiong 2 , Zehui Chen 1 , Yingbiao Tian 1, 2
Affiliation  

This study was to develop a combination of zedoary turmeric oil (ZTO) and tretinoin (TRE)-loaded liposomal gel as a topical drug delivery system. We used a combination of single factor experiment and orthogonal experiment to systematically optimize encapsulation process of the compound liposomes. The optimized liposome vesicles were incorporated into Carbopol gel matrix and studied by continuous in vitro (skin penetration and retention) and in vivo (anti-psoriatic activity using mouse vaginal model and mouse tail model) experiments. The optimized liposomes had an entrapment efficiency (EE) of ZTO was (64.63 ± 1.00)%, EE of TRE was (90.33 ± 0.72)%, drug loading (DL) of ZTO was (9.09 ± 0.14)%, DL of TRE was (1.43 ± 0.02)%, particle size of 257.41 ± 7.58 nm, polydispersity index (PDI) of 0.10 ± 0.04 and zeta potential of -38.77 ± 0.81 mV. Transmission electron microscopy showed liposomes had a regular spherical surface. After 1 month storage at (4 ± 2) °C, the optimized liposome preparations maintained its stability. In vitro study indicated that liposome formulations could significantly prolong the penetration of drugs into the hair follicles of mice and keep more drugs in the skin compared with conventional gel formulations. In vivo study showed that liposomal gel was more effective than conventional gel in treating psoriasis and had a significant dose-dependent effect on psoriasis. In summary, liposomal gel is expected to be an ideal carrier for topical drug delivery systems of ZTO and TRE.

中文翻译:

含有 zedoary 姜黄油和维甲酸的组合的局部脂质体凝胶的配制和评估用于银屑病活性

本研究旨在开发一种结合了莪术油 (ZTO) 和维甲酸 (TRE) 的脂质体凝胶作为局部给药系统。我们采用单因素实验和正交实验相结合的方法,系统地优化了复合脂质体的包封工艺。将优化的脂质体囊泡掺入 Carbopol 凝胶基质中,并通过连续的体外(皮肤渗透和保留)和体内(使用小鼠阴道模型和小鼠尾部模型的抗银屑病活性)实验进行研究。优化后的脂质体ZTO的包封率(EE)为(64.63±1.00)%,TRE的EE为(90.33±0.72)%,ZTO的载药量(DL)为(9.09±0.14)%,TRE的DL为(1.43 ± 0.02)%,粒径为 257.41 ± 7.58 nm,多分散指数 (PDI) 为 0.10 ± 0.04,zeta 电位为 -38.77 ± 0.81 mV。透射电子显微镜显示脂质体具有规则的球形表面。在 (4 ± 2) °C 下储存 1 个月后,优化的脂质体制剂保持其稳定性。体外研究表明,与常规凝胶制剂相比,脂质体制剂可显着延长药物对小鼠毛囊的渗透时间,并在皮肤中保留更多药物。体内研究表明,脂质体凝胶在治疗银屑病方面比常规凝胶更有效,并且对银屑病具有显着的剂量依赖性作用。总之,脂质体凝胶有望成为 ZTO 和 TRE 局部给药系统的理想载体。体外研究表明,与常规凝胶制剂相比,脂质体制剂可显着延长药物对小鼠毛囊的渗透时间,并在皮肤中保留更多药物。体内研究表明,脂质体凝胶在治疗银屑病方面比常规凝胶更有效,并且对银屑病具有显着的剂量依赖性作用。总之,脂质体凝胶有望成为 ZTO 和 TRE 局部给药系统的理想载体。体外研究表明,与常规凝胶制剂相比,脂质体制剂可显着延长药物对小鼠毛囊的渗透时间,并在皮肤中保留更多药物。体内研究表明,脂质体凝胶在治疗银屑病方面比常规凝胶更有效,并且对银屑病具有显着的剂量依赖性作用。总之,脂质体凝胶有望成为 ZTO 和 TRE 局部给药系统的理想载体。
更新日期:2020-04-17
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