Application of Nanoparticles in Oral Delivery of Immediate Release Formulations

An increasing percentage of drug development candidates suffer from poor aqueous solubility which in turn often times leads to poor oral absorption. This poses significant challenges in formulation development to ensure bioavailability following oral administration. Traditional approaches to increase dissolution of immediate release formulations include incorporation of surfactants, reduction of particle size and liquid vehicle formulations. More recently, size reduction of either the active pharmaceutical ingredient (API) particle or the drug delivery system down to the sub-micron range appears as a new promising approach to further increase dissolution rates of hydrophobic molecules. Nanonization of either the API, in the form of nanosuspensions typically stabilized with surfactants, or of the formulation vehicle such as with the use of self-nanoemulsified drug delivery systems and solid lipid nanoparticles has been successfully utilized to increase in vivo dissolution. Such nanotechnology has demonstrated significant impact on enhancing the bioavailability of drug candidates and addressing issues such as inadequate exposure or food effect. The goal of this review is to summarize recent advances in the utilization of nanosuspensions, solid lipid nanoparticles or nanoemulsions in drug delivery of immediate release dosage forms.