Preparation, characterization and application of pyrene-loaded methoxy poly(ethylene glycol)–poly(lactic acid) copolymer nanoparticles
Preparation, characterization and application of pyrene-loaded methoxy poly(ethylene glycol)–poly(lactic acid) copolymer nanoparticles
复制标题
DOI：
10.1007/s00396-004-1068-5
复制
发表时间：
2004-02
影响因子：
2.4
通讯作者：
Yan Zhang;Qizhi Zhang;L. Zha;Wuli Yang;Changchun Wang;Xin-guo Jiang;S. Fu
中科院分区：
文献类型：
--
作者：
Yan Zhang;Qizhi Zhang;L. Zha;Wuli Yang;Changchun Wang;Xin-guo Jiang;S. Fu
通过将芘掺入由两亲性二嵌段共聚物甲氧基聚乙二醇-聚乳酸（MePEG-PLA）配制的聚合物纳米颗粒中，制备了负载芘的可生物降解聚合物纳米颗粒。通过核磁共振（NMR）、动态光散射、荧光光谱、透射电子显微镜和zeta电位测量对其形态结构和物理性质进行了表征。此外，将含有芘作为荧光标记的MePEG-PLA纳米颗粒鼻内给予大鼠，通过荧光显微镜观察纳米颗粒在鼻粘膜和嗅球中的分布。 NMR结果证实MePEG-PLA共聚物可以在水中形成纳米颗粒，并且亲水性PEG链位于纳米颗粒的表面。 MePEG-PLA 纳米粒子的粒径、zeta 电位和芘负载效率取决于共聚物中 PLA 嵌段的含量。鼻腔给药后，纳米粒子在上皮细胞上的吸收很快，5分钟后在嗅球中观察到荧光，并且嗅粘膜中持续存在的荧光水平高于呼吸道粘膜中的荧光水平。这些结果表明，芘可以作为一种有用的荧光探针，掺入聚合物纳米颗粒中以研究组织分布，而 MePEG-PLA 纳米颗粒作为疏水性药物的载体可能具有巨大的潜力。
Pyrene-loaded biodegradable polymer nanoparticles were prepared by incorporating pyrene into the polymer nanoparticles formulated from amphiphilic diblock copolymer, methoxy poly(ethylene glycol)–poly(lactic acid) (MePEG–PLA). Their morphological structure and physical properties were characterized by nuclear magnetic resonance (NMR), dynamic light scattering, fluorescence spectroscopy, transmission electronic microscopy and zeta potential measurements. Further, MePEG–PLA nanoparticles containing pyrene as fluorescent marker were administered intranasally to rats, and the distribution of nanoparticles in the nasal mucosa and the olfactory bulb were visualized by fluorescence microscopy. NMR results confirmed that MePEG–PLA copolymer can form nanoparticles in water, and hydrophilic PEG chains were located on the surface of the nanoparticles. The particle size, zeta potential and pyrene loading efficiency of MePEG–PLA nanoparticles were dependent on the PLA block content in the copolymer. Following nasal administration, the absorption of nanoparticles across the epithelium was rapid, with fluorescence observed in the olfactory bulb at 5 min, and a higher level of fluorescence persisted in the olfactory mucosa than that in the respiratory mucosa. These results show that pyrene could serve as a useful fluorescence probe for incorporation into polymer nanoparticles to study tissue distribution and MePEG–PLA nanoparticles might have a great potential as carriers of hydrophobic drugs.