title: Pharmacodynamics of diclofenac from novel Eudragit entrapped microspheres.
abstract: Effective clinical utilization of non-steroidal anti-inflammatory drugs such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration, thus necessitating the need for a better carrier to minimize these obvious limitations. The objective of this study was to evaluate Eudragit® RS100/RL100 microspheres formulated by the solvent-evaporation technique for improved delivery of diclofenac. Three batches of (DF1, DF2 and DF3) microspheres were prepared using different ratios of Eudragit RS-100 and RL-100 polymers based on the solvent-evaporation method. The microspheres were characterized based on morphological properties, particle size analysis and encapsulation efficiency (EE%). In vitro release of DS was investigated in both 0.1 N HCl (pH 1.2) and phosphate-buffered saline (pH 7.4), while anti-inflammatory studies were evaluated in the rat model. Maximum EE% of 86.61 ± 0.11, 88.14 ± 0.16 and 85.50 ± 0.21 was obtained for DF1, DF2 and DF3, respectively. Discrete, smooth and brownish microspheres of size range 437 ± 0.01-479 ± 0.21 µm were obtained. Release of DS from the formulation depends on the polymer ratio. All the batches exhibited good anti-inflammatory activities. Microsphere formulations based on Eudragit® polymers would likely offer a reliable and alternative means of delivering DS orally.
authors.affiliation: Drug Delivery Research Unit, Department of Pharmaceutics, University of Nigeria , Nsukka , Nigeria .
authors.forename: M A
authors.initials: MA
authors.lastname: Momoh
authors.forename: F C
authors.initials: FC
authors.lastname: Kenechukwu
authors.forename: M O
authors.initials: MO
authors.lastname: Adedokun
authors.forename: C E
authors.initials: CE
authors.lastname: Odo
authors.forename: A A
authors.initials: AA
authors.lastname: Attama
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry*; D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan; D002626:Chemistry, Pharmaceutical; D004008:Diclofenac / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D004337:Drug Carriers; D005260:Female; D006863:Hydrogen-Ion Concentration; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control*; D008297:Male; D008863:Microspheres; D010316:Particle Size; D017208:Rats, Wistar; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D004008:Diclofenac; C050528:Eudragit RS; D002351:Carrageenan