载有芹菜素的 HA 涂层 PLGA 纳米粒用于 CD44 高表达的结肠癌。

HA-Coated PLGA Nanoparticles Loaded with Apigenin for Colon Cancer with High Expression of CD44.

机构信息

School of Pharmacy, Harbin University of Commerce, Harbin 150076, China.

Department of Pharmacology, Medical College, University of Shaoxing, Shaoxing 312000, China.

出版信息

Molecules. 2023 Nov 13;28(22):7565. doi: 10.3390/molecules28227565.

Abstract

Apigenin (API) possesses excellent antitumor properties but its limited water solubility and low bioavailability restrict its therapeutic impact. Thus, a suitable delivery system is needed to overcome these limitations and improve the therapeutic efficiency. Poly (lactic-co-glycolic acid) (PLGA) is a copolymer extensively utilized in drug delivery. Hyaluronic acid (HA) is a major extracellular matrix component and can specifically bind to CD44 on colon cancer cells. Herein, we aimed to prepare receptor-selective HA-coated PLGA nanoparticles (HA-PLGA-API-NPs) for colon cancers with high expression of CD44; chitosan (CS) was introduced into the system as an intermediate, simultaneously binding HA and PLGA through electrostatic interaction to facilitate a tighter connection between them. API was encapsulated in PLGA to obtain PLGA-API-NPs, which were then sequentially coated with CS and HA to form HA-PLGA-API-NPs. HA-PLGA-API-NPs had a stronger sustained-release capability. The cellular uptake of HA-PLGA-API-NPs was enhanced in HT-29 cells with high expression of CD44. In vivo, HA-PLGA-API-NPs showed enhanced targeting specificity towards the HT-29 ectopic tumor model in nude mice in comparison with PLGA-API-NPs. Overall, HA-PLGA-API-NPs were an effective drug delivery platform for API in the treatment of colon cancers with high expression of CD44.

摘要

芹菜素(API)具有优异的抗肿瘤特性,但由于其有限的水溶性和低生物利用度,限制了其治疗效果。因此,需要一个合适的传递系统来克服这些限制,提高治疗效率。聚(乳酸-共-乙醇酸)(PLGA)是一种广泛用于药物传递的共聚物。透明质酸(HA)是细胞外基质的主要成分,能够特异性地与结肠癌细胞上的 CD44 结合。在此,我们旨在为高表达 CD44 的结肠癌制备受体选择性的透明质酸(HA)包覆的 PLGA 纳米粒(HA-PLGA-API-NPs);壳聚糖(CS)被引入该体系中,同时通过静电相互作用结合 HA 和 PLGA,以促进它们之间更紧密的连接。API 被包裹在 PLGA 中以获得 PLGA-API-NPs,然后依次用 CS 和 HA 进行包覆,形成 HA-PLGA-API-NPs。HA-PLGA-API-NPs 具有更强的持续释放能力。在高表达 CD44 的 HT-29 细胞中,HA-PLGA-API-NPs 的细胞摄取能力增强。在体内,与 PLGA-API-NPs 相比,HA-PLGA-API-NPs 对裸鼠 HT-29 异位肿瘤模型表现出增强的靶向特异性。总的来说,HA-PLGA-API-NPs 是一种有效的 API 药物传递平台,可用于治疗高表达 CD44 的结肠癌。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/694a/10673172/d16018215ec8/molecules-28-07565-g001.jpg

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