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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Main Authors: Maria Rosa Gigliobianco, Cristina Casadidio, Roberta Censi, Piera Di Martino
Format: Article
Language:English
Published: MDPI AG 2018-08-01
Series:Pharmaceutics
Subjects:
Online Access:http://www.mdpi.com/1999-4923/10/3/134
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spelling 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
institution Open Data Bank
collection Open Access Journals
building Directory of Open Access Journals
language English
format 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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