title: Preparation, characterization and anticoagulation of curcumin-eluting controlled biodegradable coating stents.
abstract: Curcumin is pharmaceutically active in many ways, having properties including anticoagulation, anti-proliferation, anti-inflammatory, and may be used to fabricate drug-eluting stents to treat in-stent restenosis after stent implantation. Here we describe our investigations of curcumin-eluting PLGA coatings formed using the biodegradable polymer PLGA (polylactic acid-co-glycolic acid) as drug carrier and uniformly fabricated on the surface of 316L stainless steel stents by an ultrasonic spray method. Three doses were explored--low dose ( approximately 140 microg per stent or 115 microg/cm(2)), moderate dose ( approximately 280 microg per stent or 230 microg/cm(2)), and high dose ( approximately 490 microg per stent or 408 microg/cm(2)). Pre- and post-expansion morphologies of the stent coating were examined by optical microscopy (OM) and scanning electron microscopy (SEM), indicating that the coating not only was very smooth and uniform but also had the ability to withstand the compressive and tensile strains imparted without cracking from the stent during the expansion process. Atomic force microscopy (AFM) images indicated the topography of the PLGA-only and moderate dose curcumin-eluting stent that showed an average roughness below 1 nm; no drug particles could be seen on the stent surface, indicating that curcumin can be mixed with PLGA at the molecular level using an ultrasonic atomization spray method. The structure of the coating films was characterized by Fourier Transform Infrared (FTIR) spectroscopy and X-ray electron spectroscopy (XPS), with results suggesting that there was no chemical reaction between curcumin and the drug. The results of in vitro measurements of drug release from curcumin-eluting stents showed that all the curcumin-eluting stents studied exhibited a nearly linear sustained-release profile with no significant burst releases within the measurement period. The in vitro anticoagulation behavior of curcumin-eluting stents was investigated by static platelet adhesion and APTT (activated partial thromboplastin time) tests, revealing that the anticoagulation properties of curcumin-eluting stents are superior to those for stainless steel stents and PLGA-only-coated stents. The anticoagulation behavior of curcumin stents improved significantly as the drug dose was increased.
authors.affiliation: Key Laboratory for Advanced Technologies of Materials, The Ministry of Education, Southwest Jiaotong University, Chengdu 610031, China.
authors.forename: Ch J
authors.initials: ChJ
authors.lastname: Pan
authors.forename: J J
authors.initials: JJ
authors.lastname: Tang
authors.forename: Y J
authors.initials: YJ
authors.lastname: Weng
authors.forename: J
authors.initials: J
authors.lastname: Wang
authors.forename: N
authors.initials: N
authors.lastname: Huang
mesh_terms: D000925:Anticoagulants / Q000008:administration & dosage*; D001711:Biotransformation; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D003474:Curcumin / Q000008:administration & dosage*; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D016193:G1 Phase / Q000187:drug effects; D019344:Lactic Acid; D018625:Microscopy, Atomic Force; D008855:Microscopy, Electron, Scanning; D010314:Partial Thromboplastin Time; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D016192:Resting Phase, Cell Cycle / Q000187:drug effects; D016196:S Phase / Q000187:drug effects; D017550:Spectroscopy, Fourier Transform Infrared; D015607:Stents
chemical_list: D000925:Anticoagulants; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D003474:Curcumin