Chen Hongli, Yang Wenzhi, Chen Han, Liu Lingrong, Gao Fuping, Yang Xindu, Jiang Qian, Zhang Qiqing, Wang Yinsong
Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, The Key Laboratory of Biomedical Material of Tianjin, Tianjin 300192, PR China.
Colloids Surf B Biointerfaces. 2009 Oct 15;73(2):212-8. doi: 10.1016/j.colsurfb.2009.05.020. Epub 2009 May 29.
The purpose of this research was to develop polylactic-co-glycolic acid (PLGA) nanospheres surface modified with chitosan (CS). Mitoxantrone- (MTO-) loaded PLGA nanospheres were prepared by a solvent evaporation technique. The PLGA nanospheres surface was modified with CS by two strategies (adsorption and covalent binding). PLGA nanospheres of 248.4+/-21.0 nm in diameter characterized by the laser light scattering technique, scanning electron microscopy (SEM) are spherical and its drug encapsulation efficiency is 84.1+/-3.4%. Zeta potential of unmodified nanospheres was measured to be negative -21.21+/-2.13 mV. The positive zeta potential of modified nanospheres reveals the presence of CS on the surface of the modified nanospheres. Modified nanospheres were characterized for surface chemistry by X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared (FT-IR). FT-IR spectra exhibited peaks at 3420 cm(-1) and 1570 cm(-1), XPS spectra shows the N 1s (atomic orbital 1s of nitrogen) region of the surface of the nanospheres, corresponding to the primary amide of CS. In vitro drug release demonstrated that CS-modified nanospheres have many advantages such as prolonged drug release property and decreased the burst release over the unmodified nanospheres, and the modified nanospheres by covalent binding method could achieve the release kinetics of a relatively constant release. These data demonstrate high potential of CS-modified PLGA nanospheres for the anticancer drug carrier.
本研究的目的是开发用壳聚糖（CS）表面改性的聚乳酸-乙醇酸共聚物（PLGA）纳米球。采用溶剂蒸发技术制备了载有米托蒽醌（MTO）的PLGA纳米球。通过两种策略（吸附和共价结合）用CS对PLGA纳米球表面进行改性。通过激光散射技术、扫描电子显微镜（SEM）表征的直径为248.4±21.0nm的PLGA纳米球呈球形，其药物包封率为84.1±3.4%。未改性纳米球的zeta电位测得为-21.21±2.13mV。改性纳米球的正zeta电位表明改性纳米球表面存在CS。通过X射线光电子能谱（XPS）和傅里叶变换红外光谱（FT-IR）对改性纳米球的表面化学进行了表征。FT-IR光谱在3420cm-1和1570cm-1处出现峰，XPS光谱显示纳米球表面的N 1s（氮的原子轨道1s）区域，对应于CS的伯酰胺。体外药物释放表明，CS改性纳米球具有许多优点，如延长药物释放性能并减少未改性纳米球的突释，通过共价结合法改性的纳米球可实现相对恒定释放的释放动力学。这些数据证明了CS改性PLGA纳米球作为抗癌药物载体的巨大潜力。
