The majority of new chemical entities discovered through modern drug development pipelines have poor water solubility, which leads to limited and irregular oral bioavailability, reduced drug exposure and increased risk of adverse reactions associated with excessive dosages. A key method of improving drug solubility is through the development of nanoparticulate drug delivery systems (NDDS) which will increase the effective solubility of the drug, provide a greater surface area available for dissolution, extend the residence time of the drug at the site of absorption and allow for targeted or controlled drug delivery. This article reviews methods of developing and evaluating nanoparticulate drug delivery systems to improve the bioavailability of poorly soluble drugs. Common classes of drug delivery vehicles including polymeric nanoparticles, lipid-based nanoparticles, nanosuspensions and inorganic/hybrid nanoparticles are reviewed along with key characteristics of each class and the physical and biological attributes which impact their ability to improve the bioavailability of poorly soluble drugs. Key aspects of characterizing the physical and biological properties of drug delivery vehicles including size distribution, zeta potential, morphology, crystallinity, drug loading and stability will be reviewed, as well as in vitro testing (e.g., dissolution and release studies) and in vivo testing (e.g., pharmacokinetics). Regulatory issues and scalability issues associated with transitioning NDDS to human clinical trials will be reviewed and how a Quality-by-Design (QbD) approach to the development of NDDS can be used to ensure consistent improvement in bioavailability and therapeutic effect of poorly soluble drugs.
Keywords: Nanoparticles, poorly soluble drugs, bioavailability, lipid nanoparticles, polymeric nanoparticles, nanosuspension, nanotechnology, QbD
How to cite this article: Venkatesan C., Nanoparticulate systems for poorly soluble drugs..Int J Drug Deliv Technol. 2026;16(1s): 188-191; DOI: 10.25258/ijddt.16. 188-191