盐酸莫西沙星眼用壳聚糖纳米粒温度敏感原位凝胶的制备与评价

摘要

目的：考察离子交联法制备盐酸莫西沙星眼用壳聚糖纳米粒温度敏感原位凝胶的效果。方法以泊洛沙姆407和188为温敏基质，采用离子交联法制备盐酸莫西沙星眼用壳聚糖纳米粒，检测该纳米粒形态，测定其粒径、zeta电位和包封率，利用Poloxamer 407 and Poloxamer 188将该纳米粒制成温敏原位凝胶。结果扫描电镜图显示纳米粒球形度良好，平均粒径（207.2±6.9）nm（PDI＝0.157±0.030），zeta电位（32.1±1.5）mV，包封率（41.6±1.7）％。结论离子交联法制备盐酸莫西沙星眼用壳聚糖纳米粒温敏原位凝胶具有良好的凝胶特性及缓释效果，药物释放机制符合Korsmeyer-Peppas方程。%Objective To prepare thermosensitive in situ gel containing moxifloxacin hydrochloride chitosan nanoparticle for ophthalmic use.Methods The moxifloxacin hydrochloride chitosan nanoparticles were prepared by using the ionotropic gelation meth-od.The morphology of the nanoparticles was observed.The diameter,zeta potential and entrapment efficiency of the nanoparticles were measured.The in situ gel loaded with moxifloxacin hydrochloride chitosan nanoparticle for ophthalmic use was prepared with Poloxamer 407 and Poloxamer 188 as temperature sensitive matrices.The formulation of gel was optimized.The in vitro release characteristics of the gel were investigated.Results The scanning electron microscope image demonstrated that the nanoparticles were well dispersed as individual particles with a regular spherical shape.The mean diameter was (207.2 ±6.9) nm (PDI =0.157 ±0.030) and the zeta potential was (32.1 ±1.5) mV.The entrapment efficiency was (41.6 ±1.7)%.Conclusion The gel possesses a good gelling and sustained release effect.The release mechanism of moxifloxacin hydrochloride from the gel was in accordance with the Korsmeyer-Pep-pas model.