RESUMO
Solid lipid nanoparticles (SLNs) loaded with ibuprofen (IBU) were prepared by solvent-free high-pressure homogenization (HPH). The produced SLNs consisted of stearic acid, triluarin or tripalmitin as lipid matrixes and various stabilizers. The produced empty and IBU-loaded SLNs were characterized for particle size stability over 8 months. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were implemented to characterize the IBU state of freeze-dried SLNs. IBU was found to be in both amorphous and crystalline form within the lipid matrix. The lyophilized powders showed increased dissolution rates for IBU depending on the lipid nature. SLNs were incubated in Caco-2 cells for 24 h showing negligible cell cytotoxicity up to 15 mg/mL.
Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Ibuprofeno/administração & dosagem , Lipídeos/química , Nanopartículas/química , Células CACO-2 , Varredura Diferencial de Calorimetria , Sobrevivência Celular , Liofilização , Humanos , Nanopartículas/efeitos adversos , Nanopartículas/ultraestrutura , Tamanho da Partícula , Solubilidade , Ácidos Esteáricos/química , Triglicerídeos/química , Difração de Raios XRESUMO
Cyclosporine (CyA) solid lipid nanoparticles were prepared by using a solvent free high pressure homogenization process. CyA was incorporated into SLNs that consisted of stearic acid, trilaurin or tripalmitin lipid solid cores in order to enhance drug solubility. The process was conducted by varying lipid compositions, drug initial loading and applied homogenization pressure. The processing temperatures were above the lipid melting points for all formulations. The empty and CyA loaded SLN particles made were characterized for particle size stability over six months. Atomic force microscopy (AFM) and photon correlation spectroscopy (PCS) showed particle sizes ranging from 112-177 nm for empty and 181-215 nm for loaded SLNs each with narrow particle size distributions. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) techniques were used to characterize the CyA state, which was found to be amorphous, within the lipid cores of freeze-dried SLNs. The CyA metastable form showed a profound effect on the drug dissolution rates. SLNs were incubated in Caco-2 cells for 24 hr showing negligible cell cytotoxicity up to 15 mg/ml.
