title: Preparation and evaluation of PEG-PCL nanoparticles for local tetradrine delivery.
abstract: To establish a satisfactory delivery system for local delivery of Tetradrine (Tet), four kinds of core-shell nanoparticles were prepared from di-block copolymer of methoxy poly(ethylene glycol)-polycaprolactone (MePEG-PCL) and tri-block copolymer of polycaprolactone-poly(ethylene glycol)-polycaprolactone (PCL-PEG-PCL). The physiochemical traits of the four kinds of nanoparticles including morphology, particle size, zeta-potential, drug-loading content, stability, and in vitro release profile were studied. We also evaluated the four kinds of nanoparticles by in vitro cellular uptake experiment, cytotoxicity assay against LoVo cells, and biocmpatibility study. Histoculture Drug Response Assay (HDRA), a more predictive method usually used to evaluate chemosensitivity was firstly applied in our study to evaluate the antitumor potency of polymeric nanoparticles. The current study showed that all the four kinds of copolymers exhibited remarkable in vitro antitumor effects, especially in HDRA assay. The configuration and composition of the copolymers were important for the properties and functions of the nanoparticles. Nanoparticles prepared from the di-block copolymer with a particle size around 300nm and the hydrophobic composition about 80% was determined as the most effective drug carrier for further studies.
authors.affiliation: The Comprehensive Cancer Center of Drum-Tower Hospital, Medical School of Nanjing University & Clinical Cancer Institute of Nanjing University, Nanjing 210008, PR China.
authors.forename: Rutian
authors.initials: R
authors.lastname: Li
authors.forename: Xiaolin
authors.initials: X
authors.lastname: Li
authors.forename: Li
authors.initials: L
authors.lastname: Xie
authors.forename: Dan
authors.initials: D
authors.lastname: Ding
authors.forename: Yong
authors.initials: Y
authors.lastname: Hu
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Qian
authors.forename: Lixia
authors.initials: L
authors.lastname: Yu
authors.forename: Yitao
authors.initials: Y
authors.lastname: Ding
authors.forename: Xiqun
authors.initials: X
authors.lastname: Jiang
authors.forename: Baorui
authors.initials: B
authors.lastname: Liu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage; D044182:Benzylisoquinolines / Q000008:administration & dosage*; D045744:Cell Line, Tumor; D015179:Colorectal Neoplasms / Q000188:drug therapy; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D053758:Nanoparticles; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D044182:Benzylisoquinolines; D004337:Drug Carriers; D011091:Polyesters; C439611:methoxy poly(ethylene glycol-co-epsilon-caprolactone); C492324:poly(epsilon-caprolactone)-poly(oxyethylene)-poly(epsilon-caprolactone); C009438:tetrandrine; D011092:Polyethylene Glycols