Influenza A virus (IAV), which causes one of the most contagious diseases is a global health concern, and is responsible for seasonal epidemics and pandemics. Despite great efforts towards contriving antiviral agents and drugs, a vast majority of these, especially intracellular drugs, have shown limited efficacy due to non-specificity and low viability under physiological or endosomal conditions. Polymersomes consist of phenylboronic acid (PBA) pendant group polymers (PBASomes) and can act as drug carriers; they have sialic acid-targeting property and can gain more efficient access to the intracellular space for transport of antivirals within the host cell. Amphiphilic copolymers comprising methoxy-poly(ethylene glycol)-block-poly (phenylalanine) (mPEG-b-pPhe) formed polymersomes, which encapsulated mir-323a in the core and favipiravir in the exterior layer as hydrophilic and hydrophobic antivirals, respectively. For maximizing the cellular uptake of PBASomes via receptor-mediated endocytosis, the surface density of PBA was optimized with PBA-functionalized copolymers (PBA-PEG-pPhe). Combination therapy by employing polymersomes with PBA functional groups induced a synergistic effect against H1N1 virus infection in vitro. We believe that antiviral co-delivery using this polymersome would provide better opportunities to improve transfection of therapeutic substances for IAV treatment.

Efficient antiviral co-delivery polymersomes by optimization of surface density of cell-targeting phenylboronic acid functional groups for virus treatment

256th National Meeting (2018)

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