溶解介质对黄芩苷脂质体主要特性的影响!

Effects of dissolved medium on baicalin liposome main characteristics

关键词:  黄芩苷  脂质体  包封率  渗漏率  溶解介质

Key words:  baicalin  liposome  encapsulation efficiency  leakage rate  dissolution medium

摘要:

[目的]考察溶解介质对黄芩苷脂质体主要特性的影响。[方法]测定黄芩苷在水相[水、磷酸盐缓冲液（PBS）]和有机相（95%乙醇、无水乙醇、甲醇中）中的溶解度；分别将黄芩苷全部溶解在水相、有机相及在两相中以一定比例存在，采用薄膜超声法制备黄芩苷脂质体，测定粒径、电位，并用高效液相色谱法测定包封率和渗漏率。[结果]黄芩苷在水、pH6.8 PBS溶液、95%乙醇、无水乙醇、甲醇中的溶解度分别为0.1、10.58、0.45、0.71、4.36 g/L。以pH6.8 PBS溶液、甲醇以及甲醇和pH6.8 PBS溶液为溶解介质制备的脂质体粒径分别为（179.4±15.10）、（145.31±7.35）、（133.84±4.67）nm；Zeta表面电位（-8.93±0.40）、（-8.69±1.08）、（-8.64±1.13）mV；包封率为（82.64±0.02）%、（48.87±0.01）%、（55.53±0.07）%；渗漏率为（9.30±0.02）%、（49.72±0.04）%、（55.41±0.01）%。[结论]以pH6.8 PBS溶液为溶解介质所得脂质体粒径均匀、包封率高、渗漏量少，稳定性好。

Abstract:

[Objective] To investgate the effects of dissolution medium on main characteristics of baicalin liposome.[Methods] Determination of baicalin solubility in methanol, PBS and the mixture of both. Baicalin liposome was prepared by thin-film dispersion method based on the measuring content of baicalin. The particle size, zeta potential and distribution of baicalin was measured with zeta potential and particle size analyzer, the leakage and encapsulation efficiency were examined by HPLC.[Results] The results showed that solubility of baicalin were 0.1, 10.58, 0.45, 0.71, 4.36 g/L in water, PBS, 95% ethanol, absolute ethanol and methanol. Particle size of liposomes prepared by PBS, methanol, methanol and PBS as the solvent medium were 179.4±15.10, 145.31±7.35, 133.84±4.67 nm; zeta potential were -(8.93±0.40), -(8.69±1.08), -(8.64±1.13) mV; encapsulation efficiency were (82.64±0.02)%, (48.87±0.01)%, (55.53±0.07)%; the leakage rate were 9.30%±0.02, 49.72%±0.04, 55.41%±0.01.[Conclusion] The size distribution of baicalin liposome prepared by PBS as solvent medium was symmetrical and high coated rate, good stability.