In vitro and in vivo antitumor effect of gefitinib nanoparticles on human lung cancer

Autor: Xiao Ling Ni, Long Xia Chen, Heng Zhang, Bo Yang, Shan Xu, Min Wu, Jing Liu, Ling Lin Yang, Yue Chen, Shao Zhi Fu, Jing Bo Wu
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Drug Delivery, Vol 24, Iss 1, Pp 1501-1512 (2017)
Druh dokumentu: article
ISSN: 1071-7544
1521-0464
10717544
DOI: 10.1080/10717544.2017.1384862
Popis: Gefitinib (GEF) is the first epidermal growth factor receptor (EGFR)-targeting agent launched as an anticancer drug. It is an accepted opinion that modifying GEF strong hydrophobicity and poor bioavailability would not only enhance its antitumor effects, but also reduce its side effects. In this study, GEF-loadedpoly(ε-caprolactone)-poly(ethyleneglycol)-poly(ε-caprolactone) (PCEC) -bearing nanoparticles (GEF-NPs) were prepared by a solid dispersion method and characterized. The particle sizes increased with the increase in GEF/PCEC mass ratio in feed. GEF-NPs (10%) were mono-dispersed, smaller than 24 nm, zeta potential was approximately −18 mV, percentage encapsulation and loading, were more than 9% and 92%, respectively, and drug was slowly released but without a biphasic pattern. Microscopy studies of the optimized formulation confirmed that the prepared nanoparticles are spherical in nature. Cytotoxicity results indicated that cell growth inhibition induced by free GEF and GEF-NPs were dose and time dependent. Compared with free GEF, GEF-NPs enhanced antitumor effects, reduced side effects and significantly prolonged survival time in vivo. CD31, ki-67 and EGFR expression were significantly lower in the GEF-NPs group compared with other groups (p
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