Abstract
The use of polymeric structures coupled with intelligent targeting properties is an integral part of the current chemotherapeutic strategies. In the current report, a polyplex polymersome decorated with histatin 5 (Hst5) is proposed as a smart doxorubicin (DOX) nanocarrier for targeted treatment and imaging of cancer cells. The approach consists of the synthesis of a methoxy (polyethylene glycol)-b-(polycaprolactone)-based polymersome (mPEG-b-PCL). The formulations are characterized by dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H NMR), and scanning electron microscopy (SEM). They are tested for their pH-dependent drug release and effect on cancer cells and imaging through fluorescence. The data demonstrate a pH-induced drug release in the presence of Hst5. This was further shown through cell culture data where Hst5 increased its effect by 26–41%. The advantages of polymeric encapsulation and Hst5 functionalization are further appreciated at high DOX doses where Hst5 could overcome drug tolerance. The dual features of DOX allow the imaging and tracking of the treatment due to its inherent fluorescence. The combination of natural peptides possessing special functions such as pH-responsiveness and cell penetration with novel polymeric-based nanocarriers offers an important tool for chemotherapy and biomedicine applications.
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