摘要
药物活性成分负载于空心多孔纳米载体材料上时,既可分布在载体的孔道和空腔内部,即内部载药(DI,DrugInside),也可存在于载体的外部表面区域,即外部载药(DO,DrugOutside)。了解DI与DO的分布情况,对于进一步改善载药技术,研究和控制药物剂型的缓释性能,提高药物的利用率等都具有很重要的意义。今提出采用热重分析和溶出实验相结合的方法,先由热重分析测出载体的整体载药量,再根据内部载药(DI)和外部载药(DO)不同的溶出特性,即外部载药可全部快速释放而内部载药是在外部载药溶解后才缓慢溶出,来确定外部载药(DO)量,并最终确定DI/DO值。此外还探讨了载药分子和载药方式对DI/DO的影响,结果表明:小分子药物能更快进入纳米空心载体的内腔,具有更高的DI/DO值,因此根据载体选择药物或根据药物设计载体是制备药物控释剂的一个要素;与直接浸渍工艺相比,超临界包埋法可得到较大的整体载药量,且DI/DO值更大,缓释性能好,但操作成本也比较大,因此权衡性能指标和经济因素来选择载药方法也是制备控释剂所需要考虑的因素之一。
For porous hollow silica nanoparticles （PHSN）, drug can be loaded not only in its inner cavity and in the pores formed in its shell （drug inside, DI）, but also on its external surface （drug outside, DO）. Determination of DI/DO value of the drug loaded PHSN is of great importance for the study of the drug loading technology and the sustained release behaviors of the prepared formulation. This study proposed a method combining the thermal gravity （TG） analysis with the dissolution test method to evaluate the DI/DO value, in which the TG analysis could measure the total amount of loaded drug, while the DO could be obtained from the dissolution test due to the rapid release property of DO. The effects of molecular size of the loaded drug and different loading methods on DI/DO value were investigated, and it was found that the drug with smaller molecular size could be encapsulated much easier into the inner part of the nano-carrier and higher DI/DO value would be obtained. As compared with the impregnating drug loading （IDL） method, the supercritical fluids drug loading （SFDL） method can achieve the drug loaded PHSN with higher DI/DO value and better sustained release behavior. However, the operating cost of SFDL method is much higher than that of IDL method.
出处
《高校化学工程学报》
EI
CAS
CSCD
北大核心
2007年第5期832-837,共6页
Journal of Chemical Engineering of Chinese Universities
基金
教育部新世纪优秀人才支持计划(NCET-04-0123)
国家自然科学基金(20325621
20506001)
北京市教委资助项目(JD100100403)资助课题
关键词
纳米空心SiO2颗粒
药物缓释
内外药量
超临界包埋法
浸渍包埋法
hollow silica nanoparticles （PHSN）
sustained drug release
drug inside and drug outside
supercritical fluids drug loading
impregnating drug loading
作者简介
刘安琪（1981-）,女,广西柳州人，北京化工大学硕士生。
通讯联系人：文利雄，E-mail：wenlx@mail.buct．edu.cn
