Nanocarrier fabrication and macromolecule drug delivery

What is it about?

Macromolecules (proteins/peptides) have the potential for the development of new therapeutics. Due to their specific mechanism of action, macromolecules can be administered at relatively low doses compared with small-molecule drugs. Unfortunately, the therapeutic potential and clinical application of macromolecules is hampered by various obstacles including their large size, short in vivo half-life, phagocytic clearance, poor membrane permeability and structural instability. These challenges have encouraged researchers to develop novel strategies for effective delivery of macromolecules. In this review, various routes of macromolecule administration (invasive/noninvasive) are discussed. The advantages/limitations of novel delivery systems and the potential role of nanotechnology for the delivery of macromolecules are elaborated. In addition, fabrication approaches to make nanoformulations in different shapes and sizes are also summarized.

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Why is it important?

Macromolecule (protein/peptide) drug delivery • The therapeutic potential and clinical application of macromolecules is hampered by various obstacles including their large size, short in vivo half-life, phagocytic clearance, poor membrane permeability and structural instability. • Several challenges of delivering macromolecule drugs. Future prospects of nanotechnology-based system of macromolecule (protein/peptide) therapeutics • Efforts should be concentrated on noninvasive and intracellular delivery to overcome the problems associated with invasive routes of macromolecule delivery. • A long drug circulation time of NCs is highly desired to enhance the therapeutic efficacy of active molecules. Recently, CD47 ‘marker of self’ recognition system has been explored as a key factor toward the long RBC circulation time. Thus, the incorporation of such a ‘marker of self’ peptide into NCs may improve immune compatibility in vivo. • The formulation development of active molecules through design of experiment approaches may provide a potential way for the efficient delivery of macromolecule drugs. • The advantages of nanotechnology approaches in macromolecule formulation development may provide solutions to several problems encountered in their delivery. However, there are several challenges those need to be resolved in their clinical applications.