title: PCL films incorporated with paclitaxel/5-fluorouracil: Effects of formulation and spacial architecture on drug release.
abstract: The bi/tri-layered poly(ɛ-caprolactone) (PCL)-based films co-loaded with 5-fluorouracil (5-FU) and paclitaxel (PTX) are presented for biodegradable film-based stent application. A gradient elution HPLC analytical method was used for simultaneous quantification of 5-FU and PTX. Scanning electron microscopy (SEM) was performed to observe the microscopic architecture and morphologies, and X-ray diffraction (XRD) was employed for analyzing the physical state of the components in the single layer film. Horizontal cells diffusion test results indicated that the multi-layered structure endowed the film with drug release in unidirectional pattern. The in vitro release results showed that drug release was dependent on the drug loading, the ratio of 5-FU/PTX, the composition of surface layer, as well as the addition of hydrophilic PEG. The cytotoxicity results indicated that the PCL-based films co-loaded with 5-FU and PTX could effectively inhibit the proliferation of Eca-109 cells. The in vivo drug release results showed that the in vivo drug release was highly correlative with the in vitro drug releases. This study provided PCL-based films co-loaded with 5-FU and PTX with great potential for anti-tumor stent application, due to their unidirectional and rate-tunable drug release characteristics and dual drug loading capacity.
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.
authors.forename: Hao-Jun
authors.initials: HJ
authors.lastname: Rong
authors.forename: Wei-Luan
authors.initials: WL
authors.lastname: Chen
authors.forename: Sheng-Rong
authors.initials: SR
authors.lastname: Guo
authors.forename: Lei
authors.initials: L
authors.lastname: Lei
authors.forename: Yuan-Yuan
authors.initials: YY
authors.lastname: Shen
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004396:Coloring Agents; D003692:Delayed-Action Preparations; D004058:Diffusion; D054855:Drug-Eluting Stents; D005260:Female; D005472:Fluorouracil / Q000008:administration & dosage* / Q000494:pharmacology; D051379:Mice; D008855:Microscopy, Electron, Scanning; D017239:Paclitaxel / Q000008:administration & dosage* / Q000494:pharmacology; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013499:Surface Properties; D013778:Tetrazolium Salts; D013844:Thiazoles; D014961:X-Ray Diffraction
chemical_list: D000964:Antimetabolites, Antineoplastic; D000972:Antineoplastic Agents, Phytogenic; D004396:Coloring Agents; D003692:Delayed-Action Preparations; D011091:Polyesters; D013778:Tetrazolium Salts; D013844:Thiazoles; C016240:polycaprolactone; D011092:Polyethylene Glycols; C022616:thiazolyl blue; D017239:Paclitaxel; D005472:Fluorouracil