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姜黄素/夫西地酸双疗法负载混合胶束纳米凝胶治疗寻常痤疮:体外和体内研究。

Curcumin/Fusidic Acid Bitherapy Loaded Mixed Micellar Nanogel for Acne Vulgaris Treatment: In Vitro and In Vivo Studies.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 11795, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Cairo, Egypt.

出版信息

AAPS PharmSciTech. 2023 Sep 11;24(7):182. doi: 10.1208/s12249-023-02641-5.

Abstract

The combination of herbal drugs with a topical antibacterial for managing a chronic disease like acne vulgaris has emerged lately to settle side effects and bacterial multidrug resistance. Mixed micelles (MMs) incorporated into nanogel were explored for hybrid delivery of curcumin (Cur) and fusidic acid (FA) combination presenting a multi-strategic treatment. Curcumin-fusidic acid-loaded mixed micelles (Cur-FA-MMs) were assessed for size, surface charge, compatibility, in vitro release, and encapsulation. The selected formula was further loaded into nanogel and investigated for viscosity, ex vivo permeation, and in vivo potential. Cur-FA-MMs exhibited uniform nanosized spherical morphology, and negative surface charge affording high encapsulation for both drugs with a biphasic in vitro release over a period of 48h and good colloidal stability. The attained Cur-FA-MM-loaded nanogel had optimum viscosity with remarkable permeation coefficient values nearly 2-fold that related to plain nanogel. The pharmacodynamic effect of Cur on FA was pronounced by the significant improvement of the skin's degree of inflammation, epidermal hypertrophy, and congestion in animals treated with Cur-FA-MM-loaded nanogel. In conclusion, micellar nanogel could enable the progressive effect of Cur (an antioxidant with reported antibiotic activity) on FA (antibiotic) and decrease the risk of emerging antibiotic resistance by enhancing the solubility and permeation of Cur.

摘要

草药药物与局部抗菌药物联合用于治疗痤疮等慢性疾病,以解决副作用和细菌多重耐药性问题。最近,人们探索将混合胶束(MMs)纳入纳米凝胶中,以实现姜黄素(Cur)和夫西地酸(FA)联合的混合递送,提供多策略治疗。评估了载有姜黄素-夫西地酸的混合胶束(Cur-FA-MMs)的粒径、表面电荷、相容性、体外释放和包封率。进一步将选定的配方载入纳米凝胶中,研究其黏度、体外渗透和体内潜力。Cur-FA-MMs 表现出均匀的纳米级球形形态,带负表面电荷,对两种药物都具有高包封率,具有双相体外释放特性,在 48 小时内释放两种药物,胶体稳定性良好。所得载有 Cur-FA-MM 的纳米凝胶具有最佳的黏度,其渗透系数值显著提高,接近普通纳米凝胶的 2 倍。载有 Cur-FA-MM 的纳米凝胶对 FA 的 Cur 药效作用明显,通过显著改善动物皮肤炎症程度、表皮肥大和充血程度来实现。总之,胶束纳米凝胶可以增强 Cur(一种具有报道的抗生素活性的抗氧化剂)对 FA(抗生素)的渐进作用,并通过提高 Cur 的溶解度和渗透性来降低抗生素耐药性的风险。

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