CONTROLLED RELEASE IBUPROFEN NANOPARTICLES: PHYSICO-CHEMICAL CHARACTERIZATION AND DRUG RELEASE
Keywords:
Ibuprofen, Lipid matrix, Solid state, Kinetic release model, Lipid-surfactant nanoparticles, Controlled releaseAbstract
Objectives: The effect of lipid phase composition, concentration of lipid and surfactant on the entrapment, morphology, particle size and release profiles of ibuprofen-loaded lipid particles was evaluated.
Methods: Formulations containing only a solid lipid (Compritol® 888 ATO) and formulations containing mixture of solid and liquid lipids (Compritol® 888 ATO: Labrafil® M 1944 CS) were prepared at various lipid level (5%, 10% and 15% w/v) and surfactant (1.35% and 3%w/v) concentrations using the hot homogenization method.
Results: The particle size distribution was found to be polydisperse with a high concentration of microparticles. The particles were spherical in shape. The preparation method was effective in producing particles with high drug entrapment efficiencies (65% – 100%). Drug release studies showed a controlled release profile that follow diffusion kinetic model for all formulations. High lipid concentrations (10% and 15%) increased drug entrapment capacity and showed low initial burst of the drug during early time of testing dissolution. X-Ray diffraction and NMR studies showed coexistence of both amorphous and crystalline forms of the ibuprofen within the lipid matrix. Addition of Labrafil® led to a more amorphous internal structure by modifying the crystallinity of both ibuprofen and the lipid Compritol®.
Conclusions: This investigation solved problems associated with nanoparticles
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