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药物/表面活性剂混合囊泡的形成及其在药物缓释中的应用。

Formation of drug/surfactant catanionic vesicles and their application in sustained drug release.

机构信息

School of Pharmaceutical Science and Center for Pharmaceutical Research and Drug Delivery Systems, Shandong University, 44 West Wenhua Road, Jinan 250012, Shandong Province, PR China.

出版信息

Int J Pharm. 2012 Oct 15;436(1-2):806-14. doi: 10.1016/j.ijpharm.2012.07.053. Epub 2012 Jul 31.

Abstract

The aggregation behavior of the cationic drug/anionic surfactant vesicles formed by tetracaine hydrochloride (TH) and double-chain surfactant, sodium bis(2-ethylhexyl)sulfosuccinate (AOT), was investigated. By controlling the molar ratio of TH to AOT, a transition from catanionic vesicles to micelles was observed. The catanionic aggregates exhibited different charge properties, structures, interaction enthalpies and drug release behaviors depending on the composition. To characterize the cationic drug/anionic surfactant system, transmission electron microscopy (TEM), dynamic light scattering (DLS), isothermal titration calorimetry (ITC), conductivity, turbidity and zeta potential (ζ) measurements were performed. The drug release results indicate that the present drug-containing catanionic vesicles have promising applications in drug delivery systems. Furthermore, the percentage of drug distributed in the catanionic vesicles or micelles can be obtained by comparing the cumulative release of the corresponding aggregates with the pure drug solution.

摘要

研究了盐酸四卡因(TH)与双长链表面活性剂,双(2-乙基己基)磺基琥珀酸钠(AOT)形成的阳离子药物/阴离子表面活性剂囊泡的聚集行为。通过控制 TH 与 AOT 的摩尔比,观察到从反离子囊泡到胶束的转变。反离子聚集体的电荷性质、结构、相互作用焓和药物释放行为因组成而异。为了表征阳离子药物/阴离子表面活性剂体系,进行了透射电子显微镜(TEM)、动态光散射(DLS)、等温滴定量热法(ITC)、电导率、浊度和zeta 电位(ζ)测量。药物释放结果表明,本含药反离子囊泡在药物传递系统中具有广阔的应用前景。此外,通过比较相应聚集体的累积释放与纯药物溶液,可获得药物在反离子囊泡或胶束中的分布百分比。

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