Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, Seville, Spain.
Drug Dev Ind Pharm. 2010 Jun;36(6):666-75. doi: 10.3109/03639040903419640.
The influence of liposome composition, lamellarity, preparation method, and charge on the encapsulation efficiency, size, polydispersity, and surface charge of sumatriptan liposomes was studied. For this purpose, we studied multilamellar, unilamellar, and frozen and thawed liposomes. Positively or negatively charged liposomes were obtained using both phosphatidylcholine and cholesterol, in combination with stearylamine or dicetylphosphate. Liposomal formulations were characterized by confocal laser scanning microscopy and optical microscopy for vesicle formation, morphology, and lamellarity by dynamic laser light scattering for size distribution and polydispersity, and electrophoretic mobility for zeta potential determination. To obtain more information about the sumatriptan encapsulation, dynamic dialysis technique was employed. The sumatriptan amount was quantified by high-performance liquid chromatography.
Overall obtained results showed that liposomes may be interesting carriers for sumatriptan succinate. Statistical analysis evidenced that the preparation method does not affect the evaluated characterization parameters. However, the presence of charge inducer agents modified these characteristics. Highest loading efficiency of sumatriptan was exhibited for positively charged liposomes containing 6.58:10.34:3.73 mmolar ratio for phosphatidylcholine : cholesterol : stearylamine. The mean size was affected by the charge inducer, being smaller in positively charged liposomes. Logically, surface charge of liposomes varied as a function of the employed charged agent. Also, interesting results were obtained when vesicles were loaded with sumatriptan, showing a statistical significance between all pairs, comparing the formulations with and without drug.
Results obtained revealed that the presence of sumatriptan into the vesicles has a different behavior in negatively and positively charged liposomes.
研究了脂质体的组成、层状结构、制备方法和荷电性对舒马曲坦脂质体包封效率、粒径、多分散性和表面电荷的影响。为此，我们研究了多层、单层和冷冻-解冻脂质体。使用磷脂酰胆碱和胆固醇，并与硬脂胺或二乙酰基焦磷酸结合，获得带正电荷或负电荷的脂质体。通过共聚焦激光扫描显微镜和光学显微镜对囊泡形成、形态和层状结构进行表征，通过动态激光散射对粒径分布和多分散性进行表征，通过电泳迁移率对 zeta 电位进行测定。为了获得更多关于舒马曲坦包封的信息，采用了动态透析技术。通过高效液相色谱法定量舒马曲坦的量。
总体结果表明，脂质体可能是舒马曲坦琥珀酸盐的一种有前途的载体。统计分析表明，制备方法不会影响评价的特征参数。然而，荷电诱导剂的存在会改变这些特性。含有 6.58:10.34:3.73 毫摩尔比的磷脂酰胆碱：胆固醇：硬脂胺的带正电荷的脂质体表现出最高的舒马曲坦包封效率。平均粒径受荷电诱导剂的影响，带正电荷的脂质体较小。逻辑上，脂质体的表面电荷随所使用的带电试剂而变化。此外，当将舒马曲坦载入囊泡时，还获得了有趣的结果，显示出所有配对之间的统计学意义，比较了载药和未载药的制剂。
研究结果表明，舒马曲坦在带负电荷和带正电荷的脂质体中的存在具有不同的行为。
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