Costas Kiparissides and Olga Kammona

Department of Chemical Engineering, Aristotle University of Thessaloniki, PO Box 472, 54124, Thessaloniki, Greece

Abstract:

Macromolecular drugs (e.g., peptides, proteins, etc.) have the unique ability to tackle challenging diseases but their structure, physicochemical properties, stability, pharmacodynamics, and pharmacokinetics place stringent demands on the way they are delivered to a specific site/tissue in the body. However, they are susceptible to loss of their native structure and conformation, are prone to rapid clearance in the liver and other no-specific tissues and require precise dosing. At present, protein drugs and antigens are usually administered parenterally, but this route is less desirable. It also poses problems of oscillating blood drug concentrations. Moreover, their short biological half-lives necessitate in some cases multiple injections per week causing considerable discomfort to the patients. Carrier-based drug delivery systems can diminish the toxicity of biomolecules, improve their bioavailability and make possible their administration via less-invasive routes. Thus, the development of functionalized nanocarriers for the delivery of macromolecular drugs is considered an important scientific challenge and at the same time a business breakthrough for the biopharmaceutical industry. In order to be translated to the clinical application, a nanocarrier-based DDS needs to be biocompatible, biodegradable, non toxic and non immunogenic, to cross the designated mucosal barrier, to protect their sensitive payload and deliver it to the specific target site in a controlled manner, thus increasing significantly its bioavailability and efficacy. In this paper, a review of present state-of-the-art nanocarrier-based systems for controlled delivery of biopharmaceutics via the various mucosal barriers will be presented and critically assessed.