Formulation in vitro and in vivo evaluation of SRMS-based heterolipid-templated homolipid delivery system for diclofenac sodium

Drug Delivery

O. O. Kunle¹  A. A. Attama²  Momoh Mumuni² 

[1] Department of Pharmaceutical Technology and Raw Material Development, National Institute for Pharmaceutical Research and Development, Abuja, Nigeri;Department of Pharmaceutics, University of Nigeria, Nsukka, Nigeria an;

关键词: Anti-inflammatory;    bioavailability;    diclofenac sodium;    release study;    SLMs;   

DOI  :  10.3109/10717544.2014.923062

来源: publisher

【 摘 要 】

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.

【 授权许可】

Unknown