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新型复合脂肪酸囊泡-泊洛沙姆-卵磷脂有机凝胶用于增强在皮肤癌治疗中厚朴酚的递送。

Novel composite fatty acid vesicles-in-Pluronic lecithin organogels for enhanced magnolol delivery in skin cancer treatment.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Abbassia, P.O. Box 11566, Cairo, Egypt; Department of Pharmaceutical Technology, Faculty of Pharmacy, Misr International University, Cairo, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Abbassia, P.O. Box 11566, Cairo, Egypt.

出版信息

Eur J Pharm Biopharm. 2024 Aug;201:114379. doi: 10.1016/j.ejpb.2024.114379. Epub 2024 Jun 21.

Abstract

A novel composite carrier composed of Pluronic lecithin organogels and fatty acid vesicles was used to enhance the stability and facilitate the topical delivery of a natural bioactive drug, magnolol (Mag), for treatment of skin cancer. Jojoba oil was incorporated in the organogel (OG) base to provide a synergistic effect in treatment of skin cancer. The organoleptic properties, rheological behavior, morphology, and drug content of the OG formulations were investigated with emphasis on the impact of vesicle loading on the OG characteristics. The effect of OG on Mag release and ex-vivo permeation studies were evaluated and compared to free Mag in OG. The biological anti-tumor activity of the OG formulae was assessed using a skin cancer model in mice. All OG formulations exhibited uniform drug distribution with drug content ranging from 92.22 ± 0.91 to 100.45 ± 0.77 %. Rheological studies confirmed the OG shear-thinning flow behavior. Ex-vivo permeation studies demonstrated that the permeation of Mag from all OG formulations surpassed that obtained with free Mag in the OG. The anti-tumor activity studies revealed the superior efficacy of 10-hydroxy-decanoic acid (HDA)-based vesicles incorporated in OG formulations in mitigating 7,12- dimethylbenz(a)anthracene (DMBA)-induced skin cancer, thereby offering a promising platform for the local delivery of Mag.

摘要

一种新型的复合载体由泊洛沙姆卵磷脂有机凝胶和脂肪酸囊泡组成,用于增强天然生物活性药物厚朴酚(Mag)的稳定性并促进其局部递送,以治疗皮肤癌。将霍霍巴油纳入有机凝胶(OG)基质中,以在治疗皮肤癌方面发挥协同作用。研究了 OG 制剂的感官特性、流变行为、形态和药物含量,重点研究了囊泡负载对 OG 特性的影响。评估了 OG 对 Mag 释放和离体渗透研究的影响,并与 OG 中的游离 Mag 进行了比较。使用小鼠皮肤癌模型评估了 OG 配方的生物抗肿瘤活性。所有 OG 制剂均表现出均匀的药物分布,药物含量范围为 92.22±0.91%至 100.45±0.77%。流变学研究证实了 OG 的剪切稀流动行为。离体渗透研究表明,所有 OG 制剂中 Mag 的渗透都超过了 OG 中游离 Mag 的渗透。抗肿瘤活性研究表明,10-羟基癸酸(HDA)基囊泡在 OG 制剂中的加入能更好地减轻 7,12-二甲基苯并蒽(DMBA)诱导的皮肤癌,从而为 Mag 的局部递送提供了一个有前途的平台。

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