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载莪术油和维 A 酸的局部脂质体凝胶的配方与评价及其对银屑病的疗效。

Formulation and evaluation of a topical liposomal gel containing a combination of zedoary turmeric oil and tretinoin for psoriasis activity.

机构信息

The Affiliated Hospital of Zunyi Medical University, Zunyi, China.

School of Pharmacy, Zunyi Medical University, Zunyi, China.

出版信息

J Liposome Res. 2021 Jun;31(2):130-144. doi: 10.1080/08982104.2020.1748646. Epub 2020 Apr 17.

DOI:10.1080/08982104.2020.1748646
PMID:32223352
Abstract

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 (skin penetration and retention) and (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. 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. 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.

摘要

本研究旨在开发一种莪术油(ZTO)和维 A 酸(TRE)负载脂质体凝胶的组合,作为一种局部药物传递系统。我们采用单因素实验和正交实验相结合的方法,系统地优化了复方脂质体的包封工艺。优化后的脂质体囊泡被掺入卡波姆凝胶基质中,并通过连续(皮肤渗透和保留)和(使用小鼠阴道模型和小鼠尾模型的抗银屑病活性)实验进行研究。优化后的脂质体的莪术油包封效率(EE)为(64.63±1.00)%,维 A 酸 EE 为(90.33±0.72)%,莪术油载药量(DL)为(9.09±0.14)%,维 A 酸 DL 为(1.43±0.02)%,粒径为 257.41±7.58nm,多分散指数(PDI)为 0.10±0.04,zeta 电位为-38.77±0.81mV。透射电子显微镜显示脂质体具有规则的球形表面。在(4±2)℃下储存 1 个月后,优化的脂质体制剂保持稳定。研究表明,与常规凝胶制剂相比,脂质体制剂能够显著延长药物渗透到小鼠毛囊的时间,并使更多的药物保留在皮肤中。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,且对银屑病具有显著的剂量依赖性作用。综上所述,脂质体凝胶有望成为莪术油和维 A 酸局部药物传递系统的理想载体。

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