莫匹罗星温敏水凝胶的制备和性能研究

Study on Preparation and Properties of Thermo-sensitive Mupirocin Hydrogels

关键词:  莫匹罗星  水凝胶  温敏性  载药  药物控释  抗菌性

Key words:  mupirocin  hydrogels  thermo-sensitivity  drug loading  drug control release  antibacterial activity

摘要:

目的 制备具有温敏效应的莫匹罗星水凝胶，以达到控释作用。方法 将明胶用马来酸酐改性后得酰化明胶，与热敏材料N-异丙基丙烯酰胺在引发剂和促引发剂的作用下通过自由基聚合的方式制备5种不同配比的水凝胶，然后用干态浸泡法制备1，0.5 mg·mL^-1莫匹罗星溶液浸泡的莫匹罗星温敏水凝胶，并进行表面结构、温敏性、溶胀率、力学性能、载药率、控释率及抑菌性能的研究。结果 本研究制备的莫匹罗星水凝胶具有温敏性，其中酰化明胶与N-异丙基丙烯酰胺比例为1∶1时，表面孔洞结构最致密均匀，25℃时的溶胀率最高，制备的莫匹罗星温敏水凝胶的载药率和释放率以及抑菌率都最高，力学性能随酰化明胶增加而增强；1 mg·mL^-1莫匹罗星溶液制备的水凝胶的载药率和抑菌率高于0.5 mg·mL^-1溶液制备的，释药率则相反，而且水凝胶在2 h左右可达到释药平衡。结论 制备的莫匹罗星水凝胶可达到控释效果，对减少细菌耐药性具有长远的意义。当酰化明胶与N-异丙基丙烯酰胺比例为1∶1时，各个性能相对较好。

Abstract:

OBJECTIVE To prepare mupirocin hydrogels with thermo-sensitive for controlling drug release. METHODS Gelatin was modified by maleic anhydride to obtain acylated gelatin, and then five kinds of hydrogels were prepared via free radical polymerization of acylated gelatin and N-isopropyl acrylamide in the presence of the initiator and promoting initiator. Finally, mupirocin were loaded into as-prepared thermo-sensitive hydrogels by dry soaking methord with mupirocin solution of 1 mg·mL^-1 and 0.5 mg·mL^-1 to obtain hydrogels. The surface morphology, thermo-sensitivity, swelling rate, mechanical compression properties, drug-loading rate, controlled release rate and antibacterial performance of mupirocin hydrogels were investigated in detail. RESULTS The mupirocin hydrogels prepared in this study had obvious thermo-sensitivity. When the molar ratio of acylated gelatin to N-isopropyl acrylamide was 1:1, the prepared hydrogels had the most uniform and dense pore structure, exhibited the highest swelling rate at 25℃, and had the best drug-loading and drug-releasing rate as well as antibacterial properties. In addition, the compression property of mupirocin hydrogel was enhanced with the increase of acylated gelatin. The drug loading rate and antibacterial properties of hydrogels prepared with 1 mg·mL^-1 mupirocin solution were higher than those prepared with 0.5 mg·mL^-1 mupirocin solution, while the drug release rate was opposite. The overall drug-releasing of the mupirocin hydrogels can be equilibrium in 2 h. CONCLUSION The prepared mupirocin hydrogels can control the drug release which has a long-term significance for reducing drug resistance. When the ratio of acylated gelatin to N-isopropyl acrylamide is 1:1, the performance of mupirocin hydrogels is the relatively best.