Background: Micellization provides numerous merits for the delivery of water insoluble anti-cancer
therapeutic agents including a nanosized ‘core–shell' drug delivery system. Recently, hydrophobically-modified
polysaccharides and proteins are attracting much attention as micelle forming polymers to entrap poorly soluble
Method: By virtue of their small size, the self-assembled micelles can passively target tumor tissues via enhanced
permeation and retention effect (EPR). Moreover, the amphiphilic micelles can be exploited for active-targeted
drug delivery by attaching specific targeting ligands to the outer micellar hydrophilic surface.
Results: Here, we review the conjugation techniques, drug loading methods, physicochemical characteristics of
the most important amphiphilic polysaccharides and proteins used as anti-cancer drug delivery systems. Attention
focuses on the mechanisms of tumor-targeting and enhanced anti-tumor efficacy of the encapsulated drugs. This
review will highlight the remarkable advances of hydrophobized polysaccharide and protein micelles and their
potential applications as anti-cancer drug delivery nanosystems.
Conclusion: Micellar nanocarriers fabricated from amphiphilic natural polymers hold great promise as vehicles
for anti-cancer drugs.