Preparation of silica nanoparticles loaded with nootropics and their in vivo permeation through blood-brain barrier.

Josef Jampilek,Ingrid Brezaniova,Martin Kunes,Pavel Ulbrich,Michal Oravec,Pavel Suchy,Radka Opatrilova,Jan Triska,Kamil Zaruba,Petr Babula

doi:10.1155/2015/812673

Abstract

The blood-brain barrier prevents the passage of many drugs that target the central nervous system. This paper presents the preparation and characterization of silica-based nanocarriers loaded with piracetam, pentoxifylline, and pyridoxine (drugs from the class of nootropics), which are designed to enhance the permeation of the drugs from the circulatory system through the blood-brain barrier. Their permeation was compared with non-nanoparticle drug substances (bulk materials) by means of an in vivo model of rat brain perfusion. The size and morphology of the nanoparticles were characterized by transmission electron microscopy. The content of the drug substances in silica-based nanocarriers was analysed by elemental analysis and UV spectrometry. Microscopic analysis of visualized silica nanocarriers in the perfused brain tissue was performed. The concentration of the drug substances in the tissue was determined by means of UHPLC-DAD/HRMS LTQ Orbitrap XL. It was found that the drug substances in silica-based nanocarriers permeated through the blood brain barrier to the brain tissue, whereas bulk materials were not detected in the brain.

Highlights

Nootropics are a wide and structurally heterogeneous class of drugs that improve one or more aspects of mental function, such as working memory, motivation, and attention
The content of drug substances in silica-based nanocarriers was analysed by elemental analysis and confirmed by UV absorption analysis of supernatants
It was found that the average particle size of all prepared nanoparticles was approximately 120 nm (TEM microphotographs of pure silica nanoparticles and nanocarriers with loaded drugs in Figure 2 are shown with 105x magnification)

Summary

Introduction

Nootropics are a wide and structurally heterogeneous class of drugs ( supplements, nutraceuticals, and functional foods) that improve one or more aspects of mental function, such as working memory, motivation, and attention. They can be referred to as smart drugs, memory enhancers, neuroenhancers, cognitive enhancers, and intelligence enhancers. Their therapeutic effect is based on positive affection of metabolic pathways in brain tissue (improved utilization of nutrients and mediators) and their impact manifests after some time of administration.

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