De Capua A, Palladino A, Chino M, Attanasio C, Lombardi A, Vecchione R, Netti P A
Center for Advanced Biomaterials for Health Care@CRIB, Istituto Italiano di Tecnologia Largo Barsanti e Matteucci 53 Napoli 80125 Italy
Department of Chemical, Materials & Industrial Production Engineering, University of Naples Federico II Naples 80125 Italy.
RSC Adv. 2021 Jul 13;11(40):24487-24499. doi: 10.1039/d1ra03322k.
Selectivity in tumor targeting is one of the major issues in cancer treatment. Therefore, surface functionalization of drug delivery systems with active moieties, able to selectively target tumors, has become a worldwide-recognized strategy. The CD44 receptor is largely used as a biomarker, being overexpressed in several tumors, and consequently as a target thanks to the identification of the CD44 binding peptide. Here we implemented the CD44 binding peptide logic onto an oil core-polymer multilayer shell, taking into account and optimizing all relevant features of drug delivery systems, such as small size (down to 100 nm), narrow size distribution, drug loading capability, antifouling and biodegradability. Besides promoting active targeting, the oil core-based system enables the delivery of natural and synthetic therapeutic compounds. Biological tests, using curcumin as a bioactive compound and fluorescent tag, demonstrated that CD44 binding peptide-functionalized nanocapsules selectively accumulate and internalize in cancer cells, compared to the control, thanks to ligand-receptor binding.
肿瘤靶向的选择性是癌症治疗中的主要问题之一。因此，用能够选择性靶向肿瘤的活性部分对药物递送系统进行表面功能化，已成为一种全球公认的策略。CD44受体在多种肿瘤中大量表达，因此被广泛用作生物标志物，并且由于鉴定出了CD44结合肽，它也成为了一个靶点。在此，我们将CD44结合肽逻辑应用于油核-聚合物多层壳上，同时考虑并优化了药物递送系统的所有相关特性，如小尺寸（低至100 nm）、窄尺寸分布、药物负载能力、抗污性和生物降解性。除了促进主动靶向外，基于油核的系统还能够递送天然和合成治疗化合物。使用姜黄素作为生物活性化合物和荧光标签进行的生物学测试表明，与对照相比，由于配体-受体结合，CD44结合肽功能化的纳米胶囊在癌细胞中选择性积累并内化。
