Li Songting, Long Meng, Li Jiaqi, Zhang Yongtai, Feng Nianping, Zhang Zhicheng
The People's Hospital of Yuhuan, 18 Changle Road, Yucheng Street, Yuhuan City, Zhejiang Province 317600, China.
Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New Area, Shanghai 201203, China.
Int J Pharm X. 2024 Dec 3;8:100310. doi: 10.1016/j.ijpx.2024.100310. eCollection 2024 Dec.
Curcumin (CUR) is highly promising for topical therapeutic applications, but water-insolubility is one of the major challenges plaguing its drugability, while conventional lipid nanocarriers are limited by low drug-carrying capacity, many additives, and complex processes. In the current work, we constructed a composite carrier integrated with cyclodextrin metal-organic framework (γ-CD-MOF) and cyclodextrin nanosponge (β-CDNS), in which the γ-CD-MOF had 13.9 % drug loading and 267.1-fold increase in solubility in water for CUR, and the β-CDNS showed bioadhesion and further increasing drug solubility. The composite carrier (γ-CD-MOF@β-CDNS) significantly improved the in vitro release and transdermal permeation of CUR, and its limited water absorption properties and excellent bioadhesion create an advantage in the local administration of the drug for treating diseases with high exudate, which prevents the affected area from deteriorating the condition by counter-absorption of water from the formulation. Thus, this composite carrier contributes a new option to address the local delivery of insoluble drugs and offers a promising strategy for the clinical application of CUR.
姜黄素(CUR)在局部治疗应用方面极具前景,但水不溶性是困扰其成药的主要挑战之一,而传统脂质纳米载体存在载药量低、添加剂多及工艺复杂等局限性。在当前工作中,我们构建了一种与环糊精金属有机框架(γ-CD-MOF)和环糊精纳米海绵(β-CDNS)整合的复合载体,其中γ-CD-MOF对CUR的载药量为13.9%,在水中的溶解度提高了267.1倍,β-CDNS表现出生物黏附性并进一步提高了药物溶解度。复合载体(γ-CD-MOF@β-CDNS)显著改善了CUR的体外释放和透皮渗透,其有限的吸水性和优异的生物黏附性为高渗出性疾病的局部给药创造了优势,可防止患病部位因从制剂中反吸收水分而使病情恶化。因此,这种复合载体为解决不溶性药物的局部递送提供了新选择,并为CUR的临床应用提供了有前景的策略。