Abstract
A surprisingly large proportion of new chemical entities (NCE) is emerging from the drug discovery pipeline, and many active components extracted from herbal medicines are water insoluble, which represents a great challenge for their development. Nanosuspensions, which are submicron colloidal dispersions of pure drug particles that are stabilised by a small percentage of the excipients, could dramatically enhance the saturated solubility, dissolution rate and adhesion of drug particles to cell membranes. Nanosuspensions are the most suitable for drugs that require high dosing or have limited administrative volume. After 20 years of development, several oral products and one injectable product are commercially available. The aim of this review is to fill the gap between rational formulation designs and the in vivo performance of poorly water-soluble drug nanosuspensions. Specifically, this review will correlate characteristics of nanosuspension formulations, including drug property, particle size, crystallinity, stabiliser and surface property, with their transport, pharmacokinetics, bioactivity and toxicity after delivery by different administration routes. The elucidation of the mechanisms of targeted drug delivery, cellular transport and internalisation of nanosuspensions are also reviewed to interpret the in vivo performance of these nanosuspensions. Moreover, the recent application of nanosuspensions for poorly water-soluble herbal medicines is highlighted.
Keywords: Nanosuspensions, absorption, pharmacokinetics, drug targeting, transport, efficacy, toxicity.
Current Pharmaceutical Design
Title:Effects of Nanosuspension Formulations on Transport, Pharmacokinetics, In Vivo Targeting and Efficacy for Poorly Water-soluble Drugs
Volume: 20 Issue: 3
Author(s): Yancai Wang, Xiaoqing Miao, Lin Sun, Ju Song, Chao Bi, Xiao Yang and Ying Zheng
Affiliation:
Keywords: Nanosuspensions, absorption, pharmacokinetics, drug targeting, transport, efficacy, toxicity.
Abstract: A surprisingly large proportion of new chemical entities (NCE) is emerging from the drug discovery pipeline, and many active components extracted from herbal medicines are water insoluble, which represents a great challenge for their development. Nanosuspensions, which are submicron colloidal dispersions of pure drug particles that are stabilised by a small percentage of the excipients, could dramatically enhance the saturated solubility, dissolution rate and adhesion of drug particles to cell membranes. Nanosuspensions are the most suitable for drugs that require high dosing or have limited administrative volume. After 20 years of development, several oral products and one injectable product are commercially available. The aim of this review is to fill the gap between rational formulation designs and the in vivo performance of poorly water-soluble drug nanosuspensions. Specifically, this review will correlate characteristics of nanosuspension formulations, including drug property, particle size, crystallinity, stabiliser and surface property, with their transport, pharmacokinetics, bioactivity and toxicity after delivery by different administration routes. The elucidation of the mechanisms of targeted drug delivery, cellular transport and internalisation of nanosuspensions are also reviewed to interpret the in vivo performance of these nanosuspensions. Moreover, the recent application of nanosuspensions for poorly water-soluble herbal medicines is highlighted.
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Cite this article as:
Wang Yancai, Miao Xiaoqing, Sun Lin, Song Ju, Bi Chao, Yang Xiao and Zheng Ying, Effects of Nanosuspension Formulations on Transport, Pharmacokinetics, In Vivo Targeting and Efficacy for Poorly Water-soluble Drugs, Current Pharmaceutical Design 2014; 20 (3) . https://dx.doi.org/10.2174/13816128113199990403
DOI https://dx.doi.org/10.2174/13816128113199990403 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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