Department of Pharmacy, Jiangxi Provincial People's Hospital, Nanchang, China.
Department of Pharmacy, The First Affiliated Hospital of Nanchang Medical College, Nanchang, China.
Drug Dev Ind Pharm. 2021 Dec;47(12):1975-1985. doi: 10.1080/03639045.2022.2077957. Epub 2022 May 25.
The purpose of this study was to develop pluronic F127/d-a-tocopheryl polyethylene glycol 1000 succinate mixed micelles-based hydrogel (MMs-gel) for topical delivery of glycyrrhizic acid (GL) to improve its skin permeability and atopic dermatitis (AD) treatment.
GL loaded MMs-gel (GL-MMs-gel) could be potentially used as a promising nanocarrier for the treatment of AD.
GL-MMs were prepared by thin film hydration method and then loaded into carbopol gel. The formulation of GL-MMs-gel was optimized by full factorial design and systematically characterized for drug content, pH, spreadability, drug release and percutaneous permeation, etc. The therapeutic effect of GL-MMs-gel was also investigated in AD-like skin lesion model in BALB/c mice and compared with GL solution-based gel (GL-sol-gel).
Spherical GL-MMs with particle size of ∼30 nm were successfully incorporated into carbopol gel to form GL-MMs-gel with drug content of (98.80 ± 1.30) %, pH of 6.0 ± 0.08, and spreadability of (7.1 ± 0.2) cm. drug release profile of GL-MMs-gel exhibited a sustained-release behavior. The permeation flux for GL-MMs-gel (5.15 ± 0.33 µg/cm/h) was significantly higher than that of GL-sol-gel (3.08 ± 0.34 µg/cm/h) and GL-MMs-gel increased the accumulative amounts of GL in rats' skin 8.41 times than GL-sol-gel. The GL-MMs-gel was more effective than GL-sol-gel in suppressions of various AD symptoms including skin lesions, edema, high IgE levels, epidermal hyperplasia, and mast cell infiltration.
All results revealed that MMs-gel could be a promising carrier for topical delivery of GL for the treatment of AD.
本研究旨在开发泊洛沙姆 F127/d-a-生育酚聚乙二醇 1000 琥珀酸混合胶束水凝胶（MMs-凝胶），用于甘草酸（GL）的局部递送，以提高其皮肤渗透性和治疗特应性皮炎（AD）。
GL 负载的 MMs-凝胶（GL-MMs-凝胶）可能有望成为治疗 AD 的有前途的纳米载体。
GL-MMs 通过薄膜水化法制备，然后载入卡波姆凝胶中。通过全因子设计优化 GL-MMs-凝胶的配方，并对其药物含量、pH 值、铺展性、药物释放和经皮渗透等进行系统表征。还在 BALB/c 小鼠的 AD 样皮肤损伤模型中研究了 GL-MMs-凝胶的治疗效果，并与 GL 溶液基凝胶（GL-sol-凝胶）进行了比较。
成功地将粒径约为 30nm 的球形 GL-MMs 掺入卡波姆凝胶中，形成药物含量为（98.80±1.30）%、pH 值为 6.0±0.08、铺展性为（7.1±0.2）cm 的 GL-MMs-凝胶。GL-MMs-凝胶的药物释放曲线呈缓释行为。GL-MMs-凝胶的渗透通量（5.15±0.33µg/cm/h）明显高于 GL-sol-凝胶（3.08±0.34µg/cm/h），GL-MMs-凝胶使 GL 在大鼠皮肤中的累积量增加了 8.41 倍，高于 GL-sol-凝胶。GL-MMs-凝胶在抑制各种 AD 症状方面比 GL-sol-凝胶更有效，包括皮肤损伤、水肿、高 IgE 水平、表皮增生和肥大细胞浸润。
所有结果表明，MMs-凝胶有望成为 GL 局部递药治疗 AD 的理想载体。
