Brain targeting of Atorvastatin loaded amphiphilic PLGA-b-PEG nanoparticles

• Published in: Journal of microencapsulation Vol. 30; no. 1; pp. 10 - 20
• Main Authors: im ek, Soner, Ero lu, Hakan, Kurum, Bar, Ulubayram, Kezban
• Format: Journal Article
• Language: English
• Published: Colchester Informa UK, Ltd 01.01.2013; Taylor & Francis; Informa
• Subjects: Atorvastatin; Atorvastatin Calcium; Biological and medical sciences; Brain - metabolism; brain targeting; Fluorescent Dyes; General pharmacology; Heptanoic Acids - administration & dosage; Heptanoic Acids - pharmacokinetics; Hydroxymethylglutaryl-CoA Reductase Inhibitors - administration & dosage; Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics; Medical sciences; Nanoparticles; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; PLGA-b-PEG; Polyethylene Glycols - chemistry; Polyglactin 910 - chemistry; polysorbate 80; Pyrroles - administration & dosage; Pyrroles - pharmacokinetics; Spectroscopy, Fourier Transform Infrared; Targeting; Nanoparticle; Glycolic acid polymer; Hypocholesterolemic agent; Encephalon; Target; nanoparticles; Cyclic ether copolymer; HMG-CoA reductase inhibitor; Aliphatic polymer; Microparticle; Copolymer; brain targeting; PLGA-b-PEG; Pharmaceutical technology; Enzyme; Enzyme inhibitor; Statin derivative; Ethylene oxide copolymer; Polysorbate 80; Amphiphilic compound; Lactic acid polymer; Atorvastatin; Hydroxymethylglutaryl-CoA reductase; Oxidoreductases; Antilipemic agent
• ISSN: 0265-2048; 1464-5246
• DOI: 10.3109/02652048.2012.692400

The objective of this study was to develop polysorbate 80 coated and Atorvastatin loaded poly(lactic-co-glycolic acid)-block-poly(ethylene glycol) (PLGA-b-PEG) nanoparticles and to investigate advantages of coating on nanoparticles for brain delivery of Atorvastatin. The nanoparticles were prepared by nanoprecipitation method. The effects of polymer concentration, PEG content and polysorbate 80 coating on the particle size, drug loading efficiency and release behaviour of nanoparticles were investigated. Additionally, cellular uptake and brain targeting of formulated nanoparticles were studied. Particle sizes were in the range of 30-172 nm depending on formulation parameters. Increasing the polymer concentration significantly increased the nanoparticle size. Decreasing the PEG content from 15% to 5% (w/w) in polymer composition increased the nanoparticle size from 69 to 172 nm. Both coated and uncoated polysorbate 80 nanoparticles were effectively internalised within the endothelial cells. Moreover, both types of nanoparticles were able to penetrate the blood brain barrier and reach the maximum in brain 1 h post injection. It was concluded that these nanoparticles are promising nanosystems for treatment of neurological disorders.