Na, Jin Hee Lee, Seung-Young Lee, Sangmin Koo, Heebeom Min, Kyung Hyun Jeong, Seo Young Yuk, Soon Hong Kim, Kwangmeyung Kwon, Ick Chan 2024-01-20T13:35:05Z 2024-01-20T13:35:05Z 2021-09-04 2012-10-10 0168-3659 https://pubs.kist.re.kr/handle/201004/128768 To evaluate the tumor targeting efficiency of self-assembled polymeric nanoparticles, four glycol chitosan nanoparticles (CNPs) with different degrees of hydrophobic substitution were prepared by coupling 7.5, 12, 23, and 35 wt.% of 5 beta-cholanic acid to hydrophilic glycol chitosan polymer (GC). The sizes and zeta-potentials of different CNPs in aqueous condition were not significantly different, but their stability and deformability were greatly dependent upon the degree of substitution (DS) of 5 beta-cholanic acid. With an increase in hydrophobicity, CNPs became more stable and rigid, as characterized by SDS-PAGE and filtration tests. To compare with CNPs, linear GC and polystyrene nanoparticles (PSNPs) were employed as controls. In vivo tumor accumulation of Cy5.5-labeled linear GC, polystyrene nanoparticles (PSNPs) and CNPs were monitored in flank tumors and liver tumor-bearing mice models using near-infrared fluorescence (NIRF) imaging systems. CNPs displayed higher tumor accumulation than GC and PSNPs via the enhanced permeability and retention (EPR) effect. Interestingly, CNPs containing 23 wt.% of 5 beta-cholanic acid (CNP-23%) showed the highest tumor-targeting efficiency compared to other CNPs. As exemplified in this study, the stability of CNP-23% is better than CNP-7.5% and CNP-12% containing 7.5 wt.% and 12 wt.% of 5 beta-cholanic acid, respectively, and the deformability of CNP-23% is better than that of CNP-35% containing 35 wt.% of 5 beta-cholanic acid. We proposed that the superior tumor-targeting efficiency of CNP-23% is mainly due to their balanced stability and deformability in vivo. This study demonstrates that the degree of hydrophobic substitution of self-assembled nanoparticles could determine their stability and deformability. Importantly, they were founded to be the key factors which affect their tumor-targeting efficiency in vivo, and so that these factors should be highly considered during developing nanoparticles for tumor-targeted imaging or drug delivery. (C) 2012 Elsevier B. V. All rights reserved. English ELSEVIER SCIENCE BV POLYMERIC MICELLES THERAPY DELIVERY DIAGNOSIS SYSTEMS SIZE Effect of the stability and deformability of self-assembled glycol chitosan nanoparticles on tumor-targeting efficiency Article 10.1016/j.jconrel.2012.07.028 1 JOURNAL OF CONTROLLED RELEASE, v.163, no.1, pp.2 - 9 JOURNAL OF CONTROLLED RELEASE 163 1 2 9 scie scopus 000310507600002 2-s2.0-84866735034 Chemistry, Multidisciplinary Pharmacology & Pharmacy Chemistry Pharmacology & Pharmacy Article; Proceedings Paper POLYMERIC MICELLES THERAPY DELIVERY DIAGNOSIS SYSTEMS SIZE Glycol chitosan nanoparticles Degree of substitution Stability Deformability Tumor targeting In vivo imaging