Abstract
Oral delivery remains the preferred route for chronic drug administration thanks to its patient convenience and compliance. However, many drug candidates are unsuitable for conventional oral formulations due to low solubility, poor membrane permeability, or extensive pre-systemic metabolism. This review describes a promising strategy that incorporates or encapsulates the molecules with biodegradable and biocompatible nanoparticulate carriers. The entrapped drug substances can be protected against degradation by gastrointestinal fluids, while drug absorption through the gastrointestinal epithelium or lymphatic transport can be enhanced. Possible mechanisms for transport of these nanocarriers across gastrointestinal mucosa are introduced that focus on effects of size and surface properties of the nanocarriers on the non-specific or targeted uptake by enterocytes and/or M cells. Applications of various oral nanocarrier formulations, such as lipid nanoparticles, nanoemulsions and chitosan nanoparticles, are reviewed. Nanoparticulate drug carriers show great potential for improving the bioavailability of orally administered drugs.
Keywords: Bioavailability, drug carrier, gastrointestinal absorption, nanoparticle, oral delivery, pharmacokinetics, pre-systemic metabolism
Current Drug Metabolism
Title: Nanocarriers: A General Strategy for Enhancement of Oral Bioavailability of Poorly Absorbed or Pre-Systemically Metabolized Drugs
Volume: 11 Issue: 2
Author(s): Zheng Cai, Yan Wang, Li-Jun Zhu and Zhong-Qiu Liu
Affiliation:
Keywords: Bioavailability, drug carrier, gastrointestinal absorption, nanoparticle, oral delivery, pharmacokinetics, pre-systemic metabolism
Abstract: Oral delivery remains the preferred route for chronic drug administration thanks to its patient convenience and compliance. However, many drug candidates are unsuitable for conventional oral formulations due to low solubility, poor membrane permeability, or extensive pre-systemic metabolism. This review describes a promising strategy that incorporates or encapsulates the molecules with biodegradable and biocompatible nanoparticulate carriers. The entrapped drug substances can be protected against degradation by gastrointestinal fluids, while drug absorption through the gastrointestinal epithelium or lymphatic transport can be enhanced. Possible mechanisms for transport of these nanocarriers across gastrointestinal mucosa are introduced that focus on effects of size and surface properties of the nanocarriers on the non-specific or targeted uptake by enterocytes and/or M cells. Applications of various oral nanocarrier formulations, such as lipid nanoparticles, nanoemulsions and chitosan nanoparticles, are reviewed. Nanoparticulate drug carriers show great potential for improving the bioavailability of orally administered drugs.
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Cite this article as:
Cai Zheng, Wang Yan, Zhu Li-Jun and Liu Zhong-Qiu, Nanocarriers: A General Strategy for Enhancement of Oral Bioavailability of Poorly Absorbed or Pre-Systemically Metabolized Drugs, Current Drug Metabolism 2010; 11 (2) . https://dx.doi.org/10.2174/138920010791110836
DOI https://dx.doi.org/10.2174/138920010791110836 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
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