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Therefore, vectors have demanding property requirements, such as stability under various pH and, more importantly, efficient uptake in different intestinal segments. In this study, a functional polymer, cholesterol\u2010grafted poly(\u03b2\u2010amino ester) (poly[hexamethylene diacrylate\u2010\u03b2\u2010(5\u2010amino\u20101\u2010pentanol)] (CH\u2010PHP)), is synthesized and electrostatically interacted with plasmid DNA to form a CH\u2010PHP\/DNA complex (CPNC). This complex is designed to target the Niemann\u2013Pick C1\u2010like receptor, a cholesterol receptor, to improve oral gene delivery efficacy. With the presence of cholesterol, CH\u2010PHP shows mitigated cytotoxicity, enhanced enzyme resistance, and improved gene condensing ability. CPNC further contributes to \u224843.1\u2010 and 2.3\u2010fold increases in luciferase expression in Caco\u20102 cells compared with PNC and Lipo 2000\/DNA complexes, respectively. In addition, the in vivo transfection efficacy of CPNC is \u22484.1\u2010, 2.1\u2010, and 1.6\u2010fold higher than that of Lipo 2000\/DNA complexes in rat duodenum, jejunum, and ileum, respectively. Therefore, CPNC may be a promising delivery vector for gene delivery, and using a cholesterol\u2010specific endocytic pathway can be a novel approach to achieve efficient oral gene transfection.<\/jats:p>","DOI":"10.1002\/adhm.201800934","type":"journal-article","created":{"date-parts":[[2019,2,18]],"date-time":"2019-02-18T04:07:22Z","timestamp":1550462842000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["NPC1L1\u2010Targeted Cholesterol\u2010Grafted Poly(\u03b2\u2010Amino Ester)\/pDNA Complexes for Oral Gene Delivery"],"prefix":"10.1002","volume":"8","author":[{"given":"Yuan","family":"Liu","sequence":"first","affiliation":[{"name":"Department of Chemistry Shanghai University  Shanghai 200444 P. R. 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