Chime S.A., Attama A.A., Builders P.F., Onunkwo G.C.
Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Nigeria; Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria; Department of Pharmaceutical Technology and Raw Materials Developme
Chime, S.A., Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Nigeria; Attama, A.A., Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria; Builders, P.F., Department of Pharmaceutical Technology and Raw Materials Development, National Institute for Pharmaceutical Research and Development, Abuja, Nigeria; Onunkwo, G.C., Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Nigeria
Objective: To formulate sustained-release diclofenac potassium-loaded solid lipid microparticles (SLMs) based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties. Methods: SRMS consisting of mixtures of Phospholipon® 90H and Softisan® 154 were used to formulate diclofenac potassium-loaded SLMs. Characterization based on the particle size and morphology, stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release was carried out in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties were studied using rats. Results: Maximum EE% of 95%, 94% and 93% were obtained for SLMs formulated with SRMS 1:1, 2:1 and 1:2, respectively. In vitro release showed about 85-90% drug release at 13h. Diclofenac potassium-loaded SLMs showed good anti-inflammatory and gastro-protective properties. Conclusion: Diclofenac potassium-loaded SLMs based on SRMS could be used orally or parenterally under controlled conditions, for once daily administration. © 2013 Informa UK Ltd.
diclofenac potassium; phosphatidylcholine; polysorbate 80; sorbitol; animal experiment; animal model; antiinflammatory activity; article; controlled study; drug formulation; drug screening; encapsulation; freeze drying; in vitro study; in vivo study; intestine fluid; micelle; nonhuman; particle size; paw edema; rat; sustained drug release; ulcerogenesis; Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac; Drug Carriers; Drug Evaluation, Preclinical; Female; Lipids; Male; Micelles; Rats; Rats, Wistar
