复合透明质酸微针制剂的制备及优化

目的:考察透明质酸复合微针的制备方法,并选择形态粘度适宜的高分子溶液制备透明质酸微针。方法:测定不同浓度透明质酸溶液的粘度,确定适宜制备微针的溶液浓度。利用聚乙烯醇反复冷冻-解冻的物理交联方法制备透明质酸复合微针,并加入其他辅料考察微针针形的优劣。利用高效液相色谱法考察优化后透明质酸微针的体外释放行为。结果:10%透明质酸溶液适宜用抽真空法制备微针,聚乙烯醇优化后的透明质酸微针柔韧性更佳,刚性减小,易于揭膜。微针针形良好,不易断裂。体外释放实验中显示有缓释效果,8小时内可释放40%的理论载药量。结论:通过加入聚乙烯醇等生物相容性良好的辅料制备透明质酸微针,既具有良好的物理性能,又有较好的释放行为,优于目前文献报道的纯透明质酸微针的性能,可继续优化处方,具有更进一步研究的价值。

The Fabrication and Optimization of Complex Hyaluronic Acid Microneedles

Objective:Investigate the preparation of complex hyaluronic acid microneedles, and select the appropriate viscosity of polymer solution to prepare microneedles.Methods:The viscosity of hyaluronic acid of different concentrations is measured to determine the suitable concentration of the solution to prepare the microneedles. The physical crosslinking preparation method of PVA is applied to prepare microneedles, and other ingredients are added to improve its performance. The in vitro release study is conducted to investigate the release behavior of the optimized hyaluronic acid microneedles.Results:10%hyaluronic acid solution is suitable for preparation with vacuum pumping. Hyaluronic acid microneedles optimized with PVA has better flexibility and shape. In addition, it has less rigidity but not easy to be fractured. The results of in vitro release study shows complex HA microneedles has sustained-release effect and can release 40 % of the theoretical drug loading within 8 hours.Conclusion:Hyaluronic acid microneedles prepared by adding biocompatible materials, such as polyvinyl alcohol not only has better physical properties, but also has improved release behavior, which has better performance than the pure hyaluronic acid microneedles reported in current literature. And the following work can be focused on optimizing the formulation, which has great value of further research.