Preparation, characterization and application of pyrene-loaded methoxy poly(ethylene glycol)–poly(lactic acid) copolymer nanoparticles |
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Authors: | Yan Zhang Qizhi Zhang Liusheng Zha Wuli Yang Changchun Wang Xinguo Jiang Shoukuan Fu |
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Institution: | (1) Department of Macromolecular Science of Fudan University and the Key Laboratory of Molecular Engineering of Polymers, Ministry of Education, 200433 Shanghai, China;(2) School of Pharmacy, Fudan University, 200032 Shanghai, China;(3) College of Material Science and Technology, Donghua University, 200051 Shanghai, China |
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Abstract: | 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. |
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Keywords: | Biodegradable polymer Pyrene-loaded nanoparticle Methoxy poly(ethylene glycol)– poly(lactic acid) Fluorescent marker Tissue distribution |
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