文章摘要
胡莹莹,芮 雪,吴晶晶,杨 晔,尹登科.自供氧光敏载体系统的制备工艺优化及释氧性能研究[J].,2019,19(6):1049-1054
自供氧光敏载体系统的制备工艺优化及释氧性能研究
Optimization and in Vitro Oxygen Release Performance of the Oxygen Self-supplying Photosensitizer Carrier System
投稿时间:2018-12-06  修订日期:2018-12-26
DOI:10.13241/j.cnki.pmb.2019.06.010
中文关键词: 自供氧微球  单因素考察  单线态氧
英文关键词: Oxygen self-supplying particles  Single factor investigation  Singlet oxygen
基金项目:国家自然科学基金项目(81874348);安徽省教育厅高校自然科学研究重点项目(KJ2018A0282,KJ2017A290);安徽中医药大学校探索性基金项目(2016ts076)
作者单位E-mail
胡莹莹 安徽中医药大学药学院 安徽 合肥 230012 huyingying199204@163.com 
芮 雪 安徽中医药大学药学院 安徽 合肥 230012  
吴晶晶 安徽中医药大学药学院 安徽 合肥 230012  
杨 晔 1 安徽中医药大学药学院 安徽 合肥 2300122 安徽省中医药科学院药物制剂研究所 安徽 合肥 230012  
尹登科 1 安徽中医药大学药学院 安徽 合肥 2300122 安徽省中医药科学院药物制剂研究所 安徽 合肥 230012  
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中文摘要:
      摘要 目的:制备乙基纤维素(EC)载过氧化钙(CaO2)和光敏剂血卟啉单甲醚(HMME)的自供氧微球,对其制备工艺进行优化,并考察其体外自释氧行为。方法:采用液中干燥法制备自供氧微球,设计单因素考察实验,以粒径和CaO2/HMME包封率作为微球的质量评价指标,研究EC浓度、有机/水相体积比、水相温度、CaO2投料量对微球性能的影响,从而筛选最优工艺,采用动态透析法测定微球中氧气的释放行为,以单线态氧荧光探针(SOSG)评价其促单线态氧生成能力。结果:通过单因素考察实验获得自供氧微球的最佳制备处方为:EC浓度为1%、有机/水相体积比1:3、水相温度30 ℃、CaO2投料量40 mg;按照优化工艺制备的自供氧微球的粒径为(1198±147) nm、HMME包封率(91.83±3.48)%、CaO2包封率(89.14±1.67)%、3 h内氧气累计释放量(99.87±4.32) mM、单线态氧释放量显著高于无CaO2对照组。结论:优化的自供氧微球制备工艺合理可行,药物包封率高,且可增加单线态氧的生成。
英文摘要:
      ABSTRACT Objective: To prepare an oxygen self-supplying particles of ethyl cellulose(EC) for photosensitizer of hematoporphyrin monomethyl ether (HMME), optimize the preparation processes and evaluate the properties of in vitro oxygen release. Methods: The oxygen self-supplying particles were prepared by the in-liquid drying method. The prescription and processing of ethyl cellulose concentration, organic-water phase ratio, water phase temperature and calcium peroxide dosage were optimized through the single-factor experimental design, taking the particle size and drug encapsulation efficiency as the quality indices. The drug release of oxygen from microspheres was monitored by dynamic dialysis method and the singlet oxygen fluorescence probe (SOSG) was used to evaluate its ability to promote singlet oxygen production. Results: The optimal preparation processing for the oxygen self-supplying particles was 1% of ethyl cellulose concentration, 1:3 of organic phase to aqueous phase, 30 ℃ of water phase temperature and 40 mg of CaO2 dose. The obtained particles exhibited average diameter of (1198±147) nm, HMME encapsulation efficiency of (91.83±3.48)% and CaO2 encapsulation efficiency of (89.14±1.67)%. The oxygen self-supplying particles exhibited (99.87±4.32) mM of oxygen cumulative release in the initial 3 h and significantly higher oxygen supplying than that of control group. Conclusion: The optimized prescription and preparation process of the oxygen self-supplying particles is reasonable and feasible, and the drug encapsulation efficiency is high. Meanwhile, it can increase the generation of singlet oxygen.
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