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Table 1 A comparison of various nanoparticle systems: all of these systems are in preclinical stages for targeted delivery of anti-retroviral and/or anti-addiction drugs to the drug-impenetrable physiological barrier and more rigorous research-homework (particularly in vivo) has to be elucidated to sort out various associated shortcomings

From: Magnetic nanotherapeutics for dysregulated synaptic plasticity during neuroAIDS and drug abuse


Current research standings

Technical limitations and potential improvements


Preclinical: in vitro BBB model shows increased transmigration of therapeutics; however, yet to be supported by in vivo transendothelial migration assay.

Synthesis process is complex and drug release is inconsistent or premature as well.

Polycationic moieties of dendrimers induce cytotoxicity and as such, its toxicity on various brain cells must be well defined.


Preclinical: In vitro and mouse model studies shows increased transendothelial migration of therapeutics.

Induces transient inflammation and found less ideal for delivery of polar/ionic compounds. As such occurrences of adverse effect, if any, on neuronal cells must be defined and potential of natural polymers should also be explored.


Preclinical: In vitro and rat model studies shows increased migration of therapeutics across BBB.

Drug entrapment ability, in general, is low and it worsens for the water-soluble drugs. Further, drug leaching and carrier instability during storage is also a concern.

Surface modifications such as PEGylation improves the inherent poor stability of conventional liposomes and can also reduce their uptake by reticuloendothelial system resulting in improved bioavailability. Further, it can be developed as “Trojan nanocarrier” residing in the monocytes/macrophages which naturally transmigrate across BBB.


Preclinical: in vitro BBB model shows increased trans-endothelia migration of therapeutics.

Although natural ability of lipophilic material (building block of Solid-lipid nanoparticles (SLN)) to cross the BBB makes SLN a favorable carrier for brain drug delivery, in vivo trans-endothelial migration studies are required to authenticate its applicability.


Preclinical: In vitro and mouse model studies shows increased migration of therapeutics across BBB.

Intrinsic nature of particles instability cause premature drug release. In this regard, neuronal cells specific ligand tethering on surface of nanocarrier may improve the active brain targeting.


Preclinical: in vitro BBB model shows increased trans-endothelial migration of therapeutics and several in vivo study show successful brain delivery of MNPs.

Limited in vivo study showing site-specific targeting and lab-to-land transfer ability for anti-retroviral and anti-addiction drugs.

Advantages over other nanoparticles: Movement and speed of nanocarrier can be controlled by external magnetic force which helps in escape of nanocarriers’ uptake from reticuloendothelial system and subsequently accelerated active targeting and increased bioavailability is achieved.

Also, MNPs can be hybridized with liposomes as “Magneto-liposomes” for development of magnetized “Trojan nanocarrier” residing in the monocytes/macrophages. While monocytes/macrophages can naturally transmigrate across BBB, presence of “magneto-liposomes” in its cytoplasmic space can add to its movement influenced by external magnetic force.