2种方法制备银杏内酯长循环固体脂质纳米粒的比较

Ultrasonication Versus High Pressure Homogenization in the Preparation of Ginkgolides A and B Long-circulating Solid Lipid Nanoparticles

目的:研究银杏内酯AB长循环固体脂质纳米粒(GAB-LSLN)的制备方法,并探讨GAB-LSLN的主要理化性质。方法:分别采用超声法和高压乳匀法制备GAB-LSLN。在电镜下观察其形态,测定其粒径、Zeta电位和包封率,并在室温下放置4周,观察GAB-LSLN的稳定性。结果:超声法制备的GAB-LSLN在透射电镜下呈片状存在,形态不规则;高压乳匀法制备的GAB-LSLN呈球状,形态规则。超声法和高压乳匀法制备的GAB-LSLN粒径分别为(219.6±14.3)nm和(173.9±10.4)nm(P<0.001);Zeta电位分别为(—21.12±1.03)mv和(—27.43±2.14)mV(P<0.001),包封率分别为(85.05±0.67)%和(92.49±0.88)%(P<0.001)。高压乳匀法制备的GAB-LSLN室温放置4周后,粒径无显著增加(P>0.05)。结论:高压乳匀法制备GAB-LSLN具有粒径小、稳定性和包封率高的特点,优于超声法。

OBJECTIVE： To study the preparative methods of the long-circulating solid lipid nanoparticles （LSLN） carrying ginkgolides A and B （GAB） and to study the physicochemical characteristics of the GAB-LSLN. METHODS： GAB-LSLN was prepared by ultrasonication or high pressure homogenization. Transmission electron microscopy was employed to study its shape. Particle size, zeta potential, and entrapment efficiency of GAB-LSLN were determined, and its stability after storage under room temperature for 4 weeks was determined as well. RESULTS： The GAB-LSLN prepared by uhrasonication was platelet-shaped and irregular, and that prepared by high pressure homogenization was spherical and regular in shape. The particle diameters of GAB - L SLN prepared by uhrasonication and high pressure homogenization were （219.6±14.3） nm and （173.9± 10.4） nm respectively （P〈0.001） ; the Zeta potentials were （-21.12±1.03） mv and（-27.43± 2.14） mv respectively（P〈0.001） ; the entrapment efficiencies were（85.05±0.67） % and（92.49 ±0.88） % （P〈0.001） respectively. GAB-LSLN prepared by high pressure homogenization showed no obvious increase in particle size after storage at room temperature for 4 weeks （P 〉 0.05） .CONCLUSION： High pressure homogenization is superior to uhrasonication in that the pre- pared GAB-LSLN has small particle size, high stability and high entrapment efficiency.