Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion

The purpose of this study was to improve the dissolution rate and anti-inflammatory effect of ibuprofen by a solid dispersion(SD)method.Initial screening was developed based on drug solubility in carriers in the liquid state to select a suitable water-soluble carrier system for the preparation of SDs.The dissolution of ibuprofen in urea was higher than in PEG4000 or mannitol.Thus,urea was selected as the carrier for the preparation of SDs.SDs were characterized in terms of dissolution,differential scanning calorimetry(DSC),X-ray diffraction(XRD),scanning electron microscopy(SEM),and Fourier transform infrared(FTIR)spectroscopy.Solid dispersionbased(SDBT)and conventional(CT)tablets were prepared by the wet granulation method.The antiinflammatory effect of SDBT was evaluated using the mouse ear edema test with xylene.In vitro release results indicated that the ibuprofen dissolution rate was improved by the SD.SD characterization results suggested that ibuprofen partly precipitates in crystalline and amorphous forms after SD preparation and that ibuprofen and urea do not interact.SDBT displayed more significant anti-inflammatory effects than CT.The dissolution rate and anti-inflammatory effect of ibuprofen were significantly enhanced by the ibuprofen-urea SD.

Preparation,characterization,and antibacterial activity of oleic acid-grafted chitosan oligosaccharide nanoparticles

An oleic acid-grafted chitosan oligosaccharide(CSO-OA)with different degrees of amino substitution(DSs)was synthesized by the 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide(EDC)-mediated coupling reaction.Fourier transform infrared spectroscopy(FT-IR)suggested the formation of an amide linkage between amino groups of chitosan oligosaccharide and carboxyl groups of oleic acid.The critical aggregation concentrations(CACs)of CSO-OA with 6%,11%,and 21%DSs were 0.056,0.042,and 0.028 mg·mL^(-1),respectively.Nanoparticles prepared with the sonication method were characterized by means of transmission electron microscopy(TEM)and Zetasizer,and the antibacterial activity against Escherichia coli and Staphylococcus aureus was investigated.The results showed that the CSO-OA nanoparticles were in the range of 60-200 nm with satisfactory structural integrity.The particle size slightly decreased with the increase of DS of CSO-OA.The antibacterial trial showed that the nanoparticles had good antibacterial activity against E.coli and S.aureus.