The efficacy of nimodipine drug delivery using mPEG-PLA micelles and mPEG-PLA/TPGS mixed micelles.

OBJECTIVE: In order to develop and compare mPEG-PLA micelles and mPEG-PLA/TPGS mixed micelles, with the intention to develop a highly efficient formulation for nimodipine (NIM), NIM-loaded micelles and mixed micelles were made and their pharmacokinetics were studied. METHODS: Single factor experiments and orthogonal experiments were designed to optimize the final preparation process, characterizations and drug release behaviors were studied. Pharmacokinetics of NIM micelles, NIM mixed micelles were researched and were compared to NIM solution. RESULTS: Micelles and mixed micelles were prepared by solvent evaporation method, with relatively high drug loading efficiency and within nano-particle size range. The CMC value of mPEG-PLA was lower than that of mPEG-PLA/TPGS. The results of FTIR and TEM confirmed the spherical core-shell structure of micelles as well as mixed micelles, and the encapsulation of NIM inside the cores. In vitro release showed that micelles and mixed micelles had sustained release effect in the forms of passive diffusion and dissolution process, respectively. Following intraperitoneal administration (5mg/kg), micelles and mixed micelles were absorbed faster than solution, and with larger MRT(0-t), smaller CLz and larger AUC(0-t) as compared to that of solution, which showed micelles and mixed micelles had higher retention, slower elimination and higher bioavailability. This experiment also showed that mixed micelles released NIM more stably than micelles. By evaluate the bioequivalence, NIM micelles and NIM mixed micelles were testified non-bioequivalent to NIM solution. CONCLUSION: Micelles and mixed micelles could sustain the NIM concentrations more efficiently in plasma as compared to solution. Mixed micelles were the best ones since they had high loading content and released more stably. Thus, apprehending micelles and mixed micelles were suited as poor aqueous solubility drug carriers, and mixed micelles were better due to their high loading content and more stable release.

[Experimental study of periosteal osteoblasts adhesion to artificial bone scaffolds based on rapid prototype].

OBJECTIVE: To study the biocompatibility of bone engineering scaffolds designed and fabricated by CAD and Rapid Prototyping techniques. METHODS: Infant rat calvarias osteoblasts were isolated and expanded in vitro and the cells (2nd passage) were seeded onto scaffolds with porosity 80%, 90%, 95% at a density of 2.06 x 10(9)/L. Cell adhesion number and morphology were measured with SEM after 4 days, 10 days co-culture. RESULTS: (1) The osteoblasts' adhesion amounts increased with culture time in three porosity group (P < 0.05), but the increase were different among three groups, 80% group was 0.35 x 10(5), 90% group was 2.84 x 10(5); (2) Through SEM observations, it showed that osteoblasts adhered to all scaffolds well. CONCLUSION: The scaffolds designed and fabricated by CAD and rapid prototyping own a good cellular biocompatibility. The results suggest the feasibility of using such scaffold fabricating method for bone tissue engineering research and clinical therapy.