Journal
DRUG DELIVERY
Volume 23, Issue 3, Pages 917-925Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/10717544.2014.923062
Keywords
Anti-inflammatory; bioavailability; diclofenac sodium; release study; SLMs
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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 (R) 90G as lipid matrix and Tween (R)-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 mu m, polydispersity index of 0.633 +/- 0.190, zeta potential of -63.20 +/- 0.12mV and encapsulation efficiency of 91.2 +/- 0.1% with good stability after 8months 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.
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