Abstract

The phenomenal advances in pharmaceutical sciences over the last few decades have led to the development of new therapeutics like peptides, proteins, RNAs, DNAs and highly potent small molecules. Fruitful applications of these therapeutics have been challenged by several anatomical and physiological barriers that limit adequate drug disposition at the site-of-action and by off-target drug distribution to undesired tissues, which together result in the reduced effectiveness and increased side effects of therapeutic agents. As such, the development of drug delivery and targeting systems has been recognised as a cornerstone for future drug development. Research in pharmaceutical sciences is now devoted to tackling delivery challenges through engineering delivery systems that move beyond conventional dosage forms and regimens into state-of-the-art targeted drug delivery tailored toward specific therapeutic needs. Modern drug delivery systems comprise passive and active targeting approaches. While passive targeting relies on the natural course of distribution of drugs or drug carriers in the body, as governed by their physicochemical properties, active targeting often exploits targeting moieties that home preferentially into target tissues. Here, we provide an overview of theories of and approaches to passive and active drug delivery. As the design of drug delivery is dependent on the unique structure of target tissues and organs, we present our discussion in an organ-specific manner with the aim to inspire the development of new strategies for curing disease with high accuracy and efficiency.

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