title: Formulation in vitro and in vivo evaluation of SRMS-based heterolipid-templated homolipid delivery system for diclofenac sodium.
abstract: The sole objective of this work was to design successful dosage oral forms of diclofenac sodium (DiNa)-loaded solid lipid microparticles (SLM) based on solidified reverse micellar solution (SRMS). Hot homogenization technique was employed to prepare DicNa SLM using a mixture goat fat and Phospholipon® 90 G as lipid matrix and Tween®-80 as mobile surfactant. Characterization based on percentage yield, morphology, particle size, zeta potential, percentage encapsulation, pH and stability of SLMs were investigated. Anti-inflammatory, gastrointestinal tract (GIT) sparing effect and pharmacokinetics were carried out in rat model after oral administration. Results showed that the SLMs were spherical and smooth. The optimized formulation (SLM-4) had particle size of 79.40 ± 0.31 µm, polydispersity index of 0.633 ± 0.190, zeta potential of -63.20 ± 0.12 mV and encapsulation efficiency of 91.2 ± 0.1% with good stability after 8 months of storage. The DicNa SLM had sustained release effect with good anti-inflammatory activity. Higher and prolonged plasma DicNa concentration was shown by the SLM-4 compared to pure drug and a conventional sample. These studies demonstrate that DicNa-loaded SLM based on SRMS could be a promising oral formulation for enhanced bioavailability, pharmacologic activity and gastrointestinal sparing effect of the NSAID, DicNa.
authors: a Department of Pharmaceutics , University of Nigeria , Nsukka , Nigeria and.
authors: Momoh
authors: M
authors: Mumuni
authors: a Department of Pharmaceutics , University of Nigeria , Nsukka , Nigeria and.
authors: A A
authors: AA
authors: Attama
authors: b Department of Pharmaceutical Technology and Raw Material Development , National Institute for Pharmaceutical Research and Development , Abuja , Nigeria.
authors: O O
authors: OO
authors: Kunle
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004008:Diclofenac / Q000008:administration & dosage* / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D004355:Drug Stability; D005260:Female; D008055:Lipids / Q000737:chemistry*; D008297:Male; D008823:Micelles; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012996:Solutions / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D008055:Lipids; D008823:Micelles; D012996:Solutions; D013501:Surface-Active Agents; D004008:Diclofenac
keywords: Anti-inflammatory; SLMs; bioavailability; diclofenac sodium; release study