title: Influence of surface passivation of 2-Methoxyestradiol loaded PLGA nanoparticles on cellular interactions, pharmacokinetics and tumour accumulation.
abstract: 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.
authors.affiliation: Amrita Centre for Nanosciences and Molecular Medicine, Amrita Vishwa Vidyapeetham, Kochi - 682041, Kerala, India.
authors.forename: Gopikrishna J
authors.initials: GJ
authors.lastname: Pillai
authors.affiliation: Amrita Centre for Nanosciences and Molecular Medicine, Amrita Vishwa Vidyapeetham, Kochi - 682041, Kerala, India.
authors.forename: Bindhu
authors.initials: B
authors.lastname: Paul-Prasanth
authors.affiliation: Amrita Centre for Nanosciences and Molecular Medicine, Amrita Vishwa Vidyapeetham, Kochi - 682041, Kerala, India. Electronic address: shantinair@aims.amrita.edu.
authors.forename: Shantikumar V
authors.initials: SV
authors.lastname: Nair
authors.affiliation: Amrita Centre for Nanosciences and Molecular Medicine, Amrita Vishwa Vidyapeetham, Kochi - 682041, Kerala, India. Electronic address: deepthymenon@aims.amrita.edu.
authors.forename: Deepthy
authors.initials: D
authors.lastname: Menon
mesh_terms: D000077584:2-Methoxyestradiol; D020533:Angiogenesis Inhibitors / Q000737:chemistry; D000818:Animals; D002364:Caseins / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004958:Estradiol / Q000031:analogs & derivatives* / Q000737:chemistry; D005260:Female; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry; D009369:Neoplasms / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011485:Protein Binding; D051381:Rats; D017207:Rats, Sprague-Dawley; D013499:Surface Properties
chemical_list: D020533:Angiogenesis Inhibitors; D002364:Caseins; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D004958:Estradiol; D000077584:2-Methoxyestradiol
keywords: 2-Methoxyestradiol; Breast cancer; Drug delivery; PLGA nanoparticles; Pharmacokinetics; Protein binding; Tumour accumulation