丁香苦苷mPEG-PLGA纳米载药系统的制备及性质表征

Preparation and Characteristics of m PEG-PLGA Carrier of Lilacgentiopicroside for Nano-medicinal Delivery System

目的:制备丁香苦苷聚乙二醇修饰的聚乳酸-聚羟基乙酸共聚物纳米载药系统(SYR-m PEGPLGA-NPs),考察制备的影响因素进行处方工艺优化,并对其性质进行表征。方法:采用乳化法制备SYR-m PEG-PLGA-NPs,以包封率、载药量和粒径等为指标参数,考察内水相与乳化剂(W1:O)比例、乳化剂种类与浓度、初乳与外水相体积比(W1/O:W2)等因素的影响,根据正交试验结果优化处方。结果:SYR-m PEG-PLGA-NPs的平均粒径为(87.69±0.39)nm、PDI值为0.1039、Zeta电位(-22.64±1.46)m V、包封率为(49.6±1.52)%、载药量为(11.01±0.39)%,其外观大多呈规则的圆形,部分呈椭圆形。在20天内包封率、粒径等无明显变化。结论:采用复乳乳化溶剂挥发法制备的SYR-m PEGPLGA-NPs具有良好的理化稳定性。

Objective ： To prepare the nano - medicinal delivery system （ SYR - mPEG - PLGA - NPs） of Poly- lactic of polyglycolic acid copolymer combined with clove gentiopicroside polyethylene glycol, to find the fac- tors of influencing the preparation process in order to improve the technique and characterize its properties. Methods： Prepare SYR- mPEG -PLGA -NPs by emulsification, according to the encapsulation efficiency, drug loading and particle size. Find the influencing factors such as ratio of inner water to emulsifier （ W1 ： O）, type and density of the emulsifier, the volumetric ratio between colostrums and external water （W1/O： W2 ） etc, in order to improve the technology according to the test result. Results ： Average diameter of SYR - mPEG - PLGA - NPs particles （ 87.69 ± 0.39 ）nm, PDI value ： 0. 1039, Zeta potential （ - 22.64 ± 1.46） mV, encapsulation efficiency （49.6 ± 1.52） %, drug loading （ 11.01 ±0.39） %. The majority appeared as reg- ular circles, with small proportion of ellipse shapes. There was no distinct change of the encapsulation effi- ciency and particle size within twenty days. Conclusion ： The SYR - mPEG - PLGA - NPs produced by double emulsion solvent evaporation method obtains good physical and chemical stability.