title: Polymer based microspheres of aceclofenac as sustained release parenterals for prolonged anti-inflammatory effect.
abstract: Poly(lactic-co-glycolic acid) (PLGA) (75:25) and polycaprolactone (PCL) microspheres were fabricated for prolonged release of aceclofenac by parenteral administration. Microspheres encapsulating aceclofenac were designed to release the drug at controlled rate for around one month. Biodegradable microspheres were prepared by solvent emulsification evaporation method in different polymer:drug ratios (1:1, 2:1 and 3:1). After drug loading, PLGA and PCL microspheres showed a controlled size distribution with an average size of 11.75μm and 3.81μm respectively and entrapment efficiency in the range of 90±0.72% to 91.06±4.01% with PLGA and 83.01±2.13% to 90.4±2.11% with PCL. Scanning electron microscopy has confirmed good spherical structures of microspheres. The percent yield of biodegradable polymeric microspheres ranged between 30.95±10.14% to 92.84±3.15% and 47.33±4.72% to 80±3.60% for PLGA and PCL microspheres respectively. PLGA microspheres followed Higuchi release pattern while Korsmeyer-Peppas explained the release pattern of PCL microspheres. Stability studies of microspheres were also carried out by storing the preparations at 2-8°C for 30, 60 and 90days and evaluating them for entrapment efficiency, residual drug content and polymer drug compatability. In-vivo studies showed significant anti-inflammatory activity of microspheres upto 48hours using the carrageenan induced rat paw oedema model.
authors.affiliation: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
authors.forename: Manpreet
authors.initials: M
authors.lastname: Kaur
authors.affiliation: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
authors.forename: Sumit
authors.initials: S
authors.lastname: Sharma
authors.affiliation: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.. Electronic address: sinha_vr@rediffmail.com.
authors.forename: V R
authors.initials: VR
authors.lastname: Sinha
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D004008:Diclofenac / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D011091:Polyesters / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D011091:Polyesters; D004008:Diclofenac; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C016240:polycaprolactone; D011100:Polyglycolic Acid; D019344:Lactic Acid; C056498:aceclofenac
keywords: Aceclofenac; Anti-inflammatory; Microspheres; PCL; PLGA; Parenterals