期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 150, 期 -, 页码 242-249出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2016.11.040
关键词
2-Methoxyestradiol; PLGA nanoparticles; Drug delivery; Breast cancer; Pharmacokinetics; Tumour accumulation; Protein binding
资金
- Nanomission initiative and the Nanotheragnostics Grant from Department of Science and Technology, India [SR/NM/NS-99/2009]
- Indian Council of Medical Research
In the present work, 2-Methoxyestradiol [2ME2] loaded PLGA nanoparticles [NPs] were stabilized with Casein or poly(ethylene glycol) [PEG] and evaluated for its cellular interactions, pharmacokinetics and tumour accumulation. Surface stabilized PLGA nanoparticles prepared through a modified emulsion route possessed similar size, surface charge, drug loading and release characteristics. Particle-cell interactions as well as the anti-angiogenesis activity were similar for both nanoformulations in vitro. However, in vivo pharmacokinetics and tumour accumulation of the drug were substantially improved for the PEGylated nanoformulation. Reduced protein binding was observed for PEG stabilized PLGA NPs. Thus, it was demonstrated that nanoencapsulation of 2-ME2 within PEGylated PLGA nanocarrier could improve its half-life and plasma concentration and thereby increase the tumour accumulation. (C) 2016 Elsevier B.V. All rights reserved.
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