Nanoscale Self-Assembly for Delivery of Therapeutics and Imaging Agents

Abstract

Self-assemblies are complex structures spontaneously organized from simpler subcomponents, primarily through noncovalent interactions. These structures are being exploited as delivery vehicles of therapeutic and imaging agents. They have two unique advantages in comparison to other vehicles: 1) they are able to assume complex structures that are difficult to attain by chemical synthesis, and 2) the dissociation of self-assembled structures can be triggered by external stimuli, which can serve as a mechanism of payload release. In this review, we discuss two naturally occurring (proteins and viral capsids) and five engineered self-assemblies (vesicles, micelles, proteins, hydrogels, and inclusion complexes) that are under development for delivery of drugs and imaging agents. For each class of self-assembled supramolecular structures, we examine its structural and physicochemical properties, and potential applications within the context of assembly, loading, and payload release.

iTEP Nanoparticle-Delivered Salinomycin Displays an Enhanced Toxicity to Cancer Stem Cells in Orthotopic Breast Tumors

“…27,36 Since Sali is hydrophobic with a LogD value of 3.24 at pH 7.4, we paired it with a hydrophilic iTEP that we recently invented (Chen, personnel communication). We expected that attaching Sali to one terminus of the iTEP would introduce sufficient, segmented amphiphilicity and the amphiphilicity can drive the conjugates to form NPs.…”

“…To design a nanocarrier to deliver Sali to solid tumors through the enhanced permeability and retention (EPR) effect, , we took advantage of a self-assembling principle of amphiphiles that amphiphlies with strong, spatially separated amphiphilicity are able to assemble into micelle-like NPs. , Since Sali is hydrophobic with a LogD value of 3.24 at pH 7.4, we paired it with a hydrophilic iTEP that we recently invented (Chen, personnel communication). We expected that attaching Sali to one terminus of the iTEP would introduce sufficient, segmented amphiphilicity and the amphiphilicity can drive the conjugates to form NPs.…”

Mn(II)-Based Lipidic Nanovesicles as High-Efficiency MRI Probes

“…The size of the self-assembled soft phospholipid-based nanoparticles is determined by several factors, among which are molecular shape and the hydrophobic/hydrophilic ratio of the amphiphilic components. These considerations are relevant because they define the curvature of the bilayer (in the case of vesicular systems) or the tendency of micellar aggregates to assume different shapes (spherical, disks, and rods). − Generally, cylindrical molecules, such as C 16 –C 18 phospholipids, prefer to self-assemble into bilayers, thus forming vesicles, whereas conical molecules, such as phospholipids with short chains, with a predominance of the hydrophilic portion, prefer to self-aggregate in micelles . It is likely that the results reported herein can be rationalized in terms of the shape and hydrophobic/hydrophilic ratio of complexes bearing C 12 and C 16 lipophilic tails.…”