Drug nanoparticles: formulating poorly water-soluble compounds.

Abstract:

:More than 40% of compounds identified through combinatorial screening programs are poorly soluble in water. These molecules are difficult to formulate using conventional approaches and are associated with innumerable formulation-related performance issues. Formulating these compounds as pure drug nanoparticles is one of the newer drug-delivery strategies applied to this class of molecules. Nanoparticle dispersions are stable and have a mean diameter of less than 1 micron. The formulations consist of water, drug, and one or more generally regarded as safe excipients. These liquid dispersions exhibit an acceptable shelf-life and can be postprocessed into various types of solid dosage forms. Drug nanoparticles have been shown to improve bioavailability and enhance drug exposure for oral and parenteral dosage forms. Suitable formulations for the most commonly used routes of administration can be identified with milligram quantities of drug substance, providing the discovery scientist with an alternate avenue for screening and identifying superior analogs. For the toxicologist, the approach provides a means for dose escalation using a formulation that is commercially viable. In the past few years, formulating poorly water-soluble compounds using a nanoparticulate approach has evolved from a conception to a realization whose versatility and applicability are just beginning to be realized.

journal_name

Toxicol Pathol

journal_title

Toxicologic pathology

authors

Merisko-Liversidge EM,Liversidge GG

doi

10.1177/0192623307310946

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

43-8

issue

1

eissn

0192-6233

issn

1533-1601

pii

36/1/43

journal_volume

36

pub_type

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