title: N-Succinyl-chitosan nanoparticles coupled with low-density lipoprotein for targeted osthole-loaded delivery to low-density lipoprotein receptor-rich tumors.
abstract: N-Succinyl-chitosan (NSC) was synthesized and NSC nanoparticles (NPs) with loaded osthole (Ost) (Ost/NSC-NPs) were prepared by emulsion solvent diffusion. Subsequently, low-density lipoprotein (LDL)-mediated NSC-NPs with loaded Ost (Ost/LDL-NSC-NPs) were obtained by coupling LDL with Ost/NSC-NPs through amide linkage. The average particle size of Ost/NSC-NPs was approximately 145 nm, the entrapment efficiency was 78.28%±2.06%, and the drug-loading amount was 18.09%±0.17%. The release of Ost from Ost/NSC-NPs in vitro showed a more evident sustained effect than the native material. The half maximal inhibitory concentration of Ost/LDL-NSC-NPs was only 16.23% that of the free Ost at 24 hours in HepG2 cells. Ost inhibited HepG2 cell proliferation by arresting cells in the synthesis phase of the cell cycle and by triggering apoptosis. Cellular uptake and subcellular localization in vitro and near-infrared fluorescence real-time imaging in vivo showed that Ost/LDL-NSC-NPs had high targeting efficacy. Therefore, LDL-NSC-NPs are a promising system for targeted Ost delivery to liver tumor.
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Chun-ge
authors: CG
authors: Zhang
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Qiao-ling
authors: QL
authors: Zhu
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China ; The Children's Hospital of Wuxi People's Hospital, Nanjing Medical University, Wuxi, People's Republic of China.
authors: Yi
authors: Y
authors: Zhou
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Yang
authors: Y
authors: Liu
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Wei-liang
authors: WL
authors: Chen
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Zhi-Qiang
authors: ZQ
authors: Yuan
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Shu-di
authors: SD
authors: Yang
authors: College of Radiological Medicine and Protection, Soochow University, Suzhou, People's Republic of China ; Changshu Hospital of Traditional Chinese Medicine, Changshu, People's Republic of China.
authors: Xiao-feng
authors: XF
authors: Zhou
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Ai-jun
authors: AJ
authors: Zhu
authors: Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China.
authors: Xue-nong
authors: XN
authors: Zhang
authors: Invasive Technology Department, The Second Affiliated Hospital of Soochow University, Suzhou, People's Republic of China.
authors: Yong
authors: Y
authors: Jin
mesh_terms: D000818:Animals; D048271:Chitosan / Q000737:chemistry*; D003374:Coumarins / Q000008:administration & dosage* / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D006801:Humans; D008074:Lipoproteins / Q000737:chemistry / Q000493:pharmacokinetics*; D051379:Mice; D008819:Mice, Nude; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry; D058726:Nanoconjugates / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D011973:Receptors, LDL / Q000378:metabolism*; D016896:Treatment Outcome
chemical_list: D003374:Coumarins; D008074:Lipoproteins; C118639:N-succinyl-chitosan; D053769:Nanocapsules; D058726:Nanoconjugates; D011973:Receptors, LDL; D048271:Chitosan; C046627:osthol
keywords: antitumor activity; liver cancer; targeting efficacy