Objective: To develop an oral sustained release formulation of mycophenolate mofetil (MMF) for once-daily dosing, using chitosan-coated polylactic acid (PLA) or poly(lactic-co-glycolic) acid (PLGA) nanoparticles. The role of polymer molecular weight (MW) and drug to polymer ratio in encapsulation efficiency (EE) and release from the nanoparticles was explored in vitro.
Methods: Nanoparticles were prepared by a single emulsion solvent evaporation method where MMF was encapsulated with PLGA or PLA at various polymer MW and drug: polymer ratios. Subsequently, chitosan was added to create coated cationic particles, also at several chitosan MW grades and drug: polymer ratios. All the formulations were evaluated for mean diameter and polydispersity, EE as well as in vitro drug release. Differential scanning calorimetry (DSC), surface morphology, and in vitro mucin binding of the nanoparticles were performed for further characterization.
Results: Two lead formulations comprise MMF: high MW, PLA: medium MW chitosan 1:7:7 (w/w/w), and MMF: high MW, PLGA: high MW chitosan 1:7:7 (w/w/w), which had high EE (94.34% and 75.44%, respectively) and sustained drug release over 12?h with a minimal burst phase. DSC experiments revealed an amorphous form of MMF in the nanoparticle formulations. The surface morphology of the MMF NP showed spherical nanoparticles with minimal visible porosity. The potential for mucoadhesiveness was assessed by changes in zeta potential after incubation of the nanoparticles in mucin.
Conclusion: Two chitosan-coated nanoparticles formulations of MMF had high EE and a desirable sustained drug release profile in the effort to design a once-daily dosage form for MMF. 相似文献
The present study was aimed to utilize low‐cost alumina (Al2O3) nanoparticles for improving the heat transfer behavior in an intercooler of two‐stage air compressor. Experimental investigation was carried out with three different volume concentrations of 0.5%, 0.75%, and 1.0% Al2O3/water nanofluids to assess the performance of the intercooler, that is, counterflow heat exchanger at different loads. Thermal properties such as thermal conductivity and overall heat transfer coefficient of nanofluid increased substantially with increasing concentration of Al2O3 nanoparticles. Specific heat capacity of nanofluids were lower than base water. The intercooler performance parameters such as effectiveness and efficiency improved appreciably with the employment of nanofluid. The efficiency increased by about 6.1% with maximum concentration of nanofluid, that is, 1% at 3‐bar compressor load. It is concluded from the study that high concentration of Al2O3 nanoparticles dispersion in water would offer better heat transfer performance of the intercooler. 相似文献
The very good extraction selectivity of Cu2+ from water was demonstrated with a new microchannel equipment, by employing di-(2-ethylhexyl)phosphoric acid (D2EHPA) as an extractant and kerosene as a solvent. The effects of different experimental parameters on the extraction efficiency E, the volumetric mass transfer coefficient KLa, and the entrainment were experimentally investigated. The results showed that the extraction efficiency increased with increasing temperature, extractant concentration, phase ratio (organic/aqueous), and pH. The total flow rate, phase ratio, and pH were found to have a great effect on the mass transfer, whereas the temperature and the extractant concentration showed little effect. 相似文献