Huh, Myung Sook Lee, Seung-Young Park, Sangjin Lee, Seulki Chung, Hyunjin Lee, Sojin Choi, Yongseok Oh, Yu-Kyoung Park, Jae Hyung Jeong, Seo Young Choi, Kuiwon Kim, Kwangmeyung Kwon, Ick Chan 2024-01-20T19:03:07Z 2024-01-20T19:03:07Z 2021-09-02 2010-06-01 0168-3659 https://pubs.kist.re.kr/handle/201004/131341 Here, we designed a new nano-sized siRNA carrier system composed of biocompatible/biodegradable glycol chitosan polymer (GC) and strongly positively charged polyethylenimine (PEI) polymers. In order to make a stable and tumor-homing nano-sized carrier, each polymer was modified with hydrophobic 5 beta-cholanic acid, and they were simply mixed to form self-assembled GC-PEI nanoparticles (GC-PEI NPs), due to the strong hydrophobic interactions of 5 beta-cholanic acids in the polymers. The freshly prepared GC-PEI NPs showed a stable nanoparticle structure (350 nm) and they presented a strongly positive-charged surface (zeta potential = 23.8) that is enough to complex tightly with negatively charged RFP-siRNAs, designed for inhibiting red fluorescent protein (RFP) expression. The siRNA encapsulated nanoparticles (siRNA-GC-PEI NPs) formed more compact and stable nanoparticle structures (250 nm) at 1: 5 weight ratio of siRNA to GC-PEI nanoparticles. In vitro RFP expressing B16F10 tumor cell (RFP/B16F10) culture system, the siRNA-GC-PEI NPs presented a rapid time-dependent cellular uptake profile within 1 h. Moreover, the internalized siRNA-GC-PEI NPs lead to specific mRNA breaks down. Furthermore, our new formulation of siRNA-GC-PEI NPs presented a significant inhibition of RFP gene expression of RFP/B16F10-bearing mice, due to their higher tumor-targeting ability. These results revealed the promising potential of GC-PEI NPs as a stable and effective nano-sized siRNA delivery system for cancer treatment. (C) 2010 Elsevier B.V. All rights reserved. English ELSEVIER SMALL INTERFERING RNAS IN-VIVO DELIVERY CHITOSAN NANOPARTICLES CELLULAR UPTAKE CARRIERS GROWTH INFECTION RELEASE COMPLEX ACID Tumor-homing glycol chitosan/polyethylenimine nanoparticles for the systemic delivery of siRNA in tumor-bearing mice Article 10.1016/j.jconrel.2010.02.023 1 JOURNAL OF CONTROLLED RELEASE, v.144, no.2, pp.134 - 143 JOURNAL OF CONTROLLED RELEASE 144 2 134 143 scie scopus 000278652800004 2-s2.0-77952668878 Chemistry, Multidisciplinary Pharmacology & Pharmacy Chemistry Pharmacology & Pharmacy Article SMALL INTERFERING RNAS IN-VIVO DELIVERY CHITOSAN NANOPARTICLES CELLULAR UPTAKE CARRIERS GROWTH INFECTION RELEASE COMPLEX ACID Glycol chitosan Polyethylenimine siRNA Nanoparticle delivery system Tumor-targeting delivery Cancer treatment