Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability
Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of &ldqu...
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doaj-art-d995200578a046a08f50dfbafd65d3ea2018-08-22T08:24:16ZengMDPI AGPharmaceutics1999-49232018-08-0110313410.3390/pharmaceutics10030134pharmaceutics10030134Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical StabilityMaria Rosa Gigliobianco0Cristina Casadidio1Roberta Censi2Piera Di Martino3School of Pharmacy, University of Camerino, via S. Agostino, 1, 62032 Camerino, ItalySchool of Pharmacy, University of Camerino, via S. Agostino, 1, 62032 Camerino, ItalySchool of Pharmacy, University of Camerino, via S. Agostino, 1, 62032 Camerino, ItalySchool of Pharmacy, University of Camerino, via S. Agostino, 1, 62032 Camerino, ItalyMany approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of “pure drugs and a minimum of surface active agents required for stabilization”. They are defined as “carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10–800 nm”. The primary importance of these nanoparticles was the reduction of particle size to nanoscale dimensions, with an increase in the particle surface area in contact with the dissolution medium, and thus in bioavailability. This approach has been proven successful, as demonstrated by the number of such drug products on the market. Nonetheless, despite the definition that indicates nanocrystals as a “carrier-free” system, surface active agents are necessary to prevent colloidal particles aggregation and thus improve stability. In addition, in more recent years, nanocrystal properties and technologies have attracted the interest of researchers as a means to obtain colloidal particles with modified biological properties, and thus their interest is now also addressed to modify the drug delivery and targeting. The present work provides an overview of the achievements in improving the bioavailability of poorly soluble drugs according to their administration route, describes the methods developed to overcome physicochemical and stability-related problems, and in particular reviews different stabilizers and surface agents that are able to modify the drug delivery and targeting.http://www.mdpi.com/1999-4923/10/3/134nanocrystalspoorly soluble drugnanotechnologystabilitydrug deliverydrug targeting |
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Article |
author |
Maria Rosa Gigliobianco Cristina Casadidio Roberta Censi Piera Di Martino |
spellingShingle |
Maria Rosa Gigliobianco Cristina Casadidio Roberta Censi Piera Di Martino Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability Pharmaceutics nanocrystals poorly soluble drug nanotechnology stability drug delivery drug targeting |
author_facet |
Maria Rosa Gigliobianco Cristina Casadidio Roberta Censi Piera Di Martino |
author_sort |
Maria Rosa Gigliobianco |
title |
Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability |
title_short |
Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability |
title_full |
Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability |
title_fullStr |
Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability |
title_full_unstemmed |
Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability |
title_sort |
nanocrystals of poorly soluble drugs: drug bioavailability and physicochemical stability |
publisher |
MDPI AG |
series |
Pharmaceutics |
issn |
1999-4923 |
publishDate |
2018-08-01 |
description |
Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of “pure drugs and a minimum of surface active agents required for stabilization”. They are defined as “carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10–800 nm”. The primary importance of these nanoparticles was the reduction of particle size to nanoscale dimensions, with an increase in the particle surface area in contact with the dissolution medium, and thus in bioavailability. This approach has been proven successful, as demonstrated by the number of such drug products on the market. Nonetheless, despite the definition that indicates nanocrystals as a “carrier-free” system, surface active agents are necessary to prevent colloidal particles aggregation and thus improve stability. In addition, in more recent years, nanocrystal properties and technologies have attracted the interest of researchers as a means to obtain colloidal particles with modified biological properties, and thus their interest is now also addressed to modify the drug delivery and targeting. The present work provides an overview of the achievements in improving the bioavailability of poorly soluble drugs according to their administration route, describes the methods developed to overcome physicochemical and stability-related problems, and in particular reviews different stabilizers and surface agents that are able to modify the drug delivery and targeting. |
topic |
nanocrystals poorly soluble drug nanotechnology stability drug delivery drug targeting |
url |
http://www.mdpi.com/1999-4923/10/3/134 |
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