Piroxicam-Loaded Self-Emulsifying Drug Delivery System
Keywords:
sesame seeds, piroxicam, self-emulsifying, anti-inflammatoryAbstract
Background: A self-emulsifying drug delivery systems (SEDDS) is an oral lipid dosage form for improving the biopharmaceutical performance of hydrophobic drugs. SEDDS are able to self-emulsify rapidly in the gastrointestinal fluids under the influence of gentle agitation provided by peristaltic and other movements of the gastro intestinal tract to produce ultrafine oil-in-water emulsion, thereby providing a large interfacial area for enhancement in both the rate and the extent of drug absorption. Objective: This work aimed to formulate piroxicam, a poorly water-soluble drug into a self-emulsifying drug delivery system using a natural lipophile (N-L) (crude oil) from pressed sesame seeds and to compare it with using labrafac CC as the oil phase.
Methodology: Using a natural lipophile (N-L) and labrafac CC as the oil phase, Coliphor HS-15 or Cremophor EL as the surfactant and polyethylene glycol-400 as the co-surfactant, pseudo-ternary phase diagrams were generated following phase titration studies. The proportion of oil, surfactant and co-surfactant that can result in stable, maximum self-emulsification was selected, loaded with piroxicam and characterized with respect to percentage drug loading efficiency (%DLE), emulsification ti me, stability, infinite aqueous diluti on, post-diluti on drug precipitation, globule size and polydispersity index (PDI). The in vitro drug release rate of the optimal formulation was investigated using a polycarbonate dialysis membrane and it's in vivo anti-inflammatory activity was evaluated using carrageenan-induced paw edema in adult wistar rats.
Results: The optimized formulation consisted of 30 % oil, 56 % surfactant and 14 % co-surfactant, it gave an emulsification time of 6.0 s, had a % DLE of 91.1, a mean globule size of 32.0 nm, PDI of 0.175, released > 95.0 % of the drug within 20 min while the pure drug showed only 13.8 % drug release over a period of 1 h and demonstrated significantly (P < 0.05) higher anti-inflammatory activity than the unformulated drug.
Conclusion: The developed SEDDS highlight the potential applications of the indigenous natural lipophile in the development of colloidal drug carriers for biopharmaceutical performance enhancement of piroxicam.
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