title: The effect of hydrophilic chain length and iRGD on drug delivery from poly(ε-caprolactone)-poly(N-vinylpyrrolidone) nanoparticles.
abstract: Poly(ε-caprolactone)-b-Poly(N-vinylpyrrolidone) (PCL-b-PVP) copolymers with different PVP block length were synthesized by xanthate-mediated reverse addition fragment transfer polymerization (RAFT) and the xanthate chain transfer agent on chain end was readily translated to hydroxy or aldehyde for conjugating various functional moieties, such as fluorescent dye, biotin hydrazine and tumor homing peptide iRGD. Thus, PCL-PVP nanoparticles were prepared by these functionalized PCL-b-PVP copolymers. Furthermore, paclitaxel-loaded PCL-PVP nanoparticles with satisfactory drug loading content (15%) and encapsulation efficiency (>90%) were obtained and used in vitro and in vivo antitumor examination. It was demonstrated that the length of PVP block had a significant influence on cytotoxicity, anti-BSA adsorption, circulation time, stealth behavior, biodistribution and antitumor activity for the nanoparticles. iRGD on PCL-PVP nanoparticle surface facilitated the nanoparticles to accumulate in tumor site and enhanced their penetration in tumor tissues, both of which improved the efficacy of paclitaxel-loaded nanoparticles in impeding tumor growth and prolonging the life time of H22 tumor-bearing mice.
authors: Laboratory of Mesoscopic Chemistry and Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
authors: Zhenshu
authors: Z
authors: Zhu
authors: Chen
authors: C
authors: Xie
authors: Qin
authors: Q
authors: Liu
authors: Xu
authors: X
authors: Zhen
authors: Xianchuang
authors: X
authors: Zheng
authors: Wei
authors: W
authors: Wu
authors: Rutian
authors: R
authors: Li
authors: Yin
authors: Y
authors: Ding
authors: Xiqun
authors: X
authors: Jiang
authors: Baorui
authors: B
authors: Liu
mesh_terms: D000327:Adsorption; D000510:Alpha-Globulins / Q000378:metabolism; D000818:Animals; D016923:Cell Death; D002460:Cell Line; D016503:Drug Delivery Systems / Q000379:methods*; D005455:Fluorescent Antibody Technique; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D053758:Nanoparticles / Q000737:chemistry*; D009842:Oligopeptides / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry*; D011091:Polyesters / Q000138:chemical synthesis / Q000737:chemistry*; D011205:Povidone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D012710:Serum Albumin, Bovine / Q000378:metabolism; D013050:Spectrometry, Fluorescence; D014018:Tissue Distribution; D016896:Treatment Outcome
chemical_list: D000510:Alpha-Globulins; C569656:N-end cysteine peptide tumor-homing peptide; D009842:Oligopeptides; D010455:Peptides; D011091:Polyesters; C550000:poly(N-vinylpyrrolidone)-b-poly(epsilon-caprolactone); D012710:Serum Albumin, Bovine; D011205:Povidone