pH-Sensitive Nanoaggregates for Site-Specific Drug-Delivery as Well as Cancer Cell Imaging

[Image: see text] Multifunctional polymeric nanoaggregates could enable targeted cancer therapy and imaging, which eventually facilitate monitoring of the therapeutic effect. A fluorescent nanoaggregate is constructed for theranostic application. Chlorambucil (Chl), a fluorescent inactive chemotherapeutic agent, is covalently attached to the nanoaggregate for therapeutic action. The pyrene (Py) motif is also covalently attached to the nanoaggregates, with the motivation of cancer cell imaging. This nanoaggregate is further functionalized with biotin (Btn) for receptor-mediated drug delivery. The efficiency of this system is evaluated by in vitro cell studies to prove its receptor-mediated internalization as well as theranostic capabilities. This newly designed nanocarrier, Nor–Chl–Py–Btn (Nor, norbornene), has the ability to combine both therapeutic and diagnostic capabilities into a single polymer that offers existing prospects for the development of nanomedicine.