Actively targeted polymersomes for tumor imaging and therapy

Nanomedicine, the application of nanotechnology for medical purpose, has attracted a great deal of attention over the past decades, particularly in the field of cancer therapy where more effective and safer diagnosis and treatment modalities are highly needed. Nanomedicines promise and have shown to offer significant advantages over traditional therapeutic and diagnostic approaches in cancer therapy including enhanced efficacy and/or mitigated toxicity benefits owing to ameliorated pharmacokinetics and favorably altered tissue distribution profile (including the distribution to pathological areas) of the associated drug molecules. Particulate nanomedicines have received a great deal of interest as nanomaterials for achieving above mentioned advantages.
Polymersomes (Ps) are structures self-assembled from various amphiphilic block copolymers and exhibit a nano-vesicular architecture that enables encapsulation of hydrophilic or hydrophobic molecules in the internal aqueous compartment or the surrounding polymeric bilayer, respectively. In comparison to the safety concerns of inorganic nanoparticulates for clinical translation, the biocompatibility and/or biodegradability of Ps promise to result in lower or no toxicity in vivo. Actively targeted reduction-responsive Ps were developed exhibiting the following features: high stability in the blood circulation, significant tumor accumulation, enhanced tumor cell uptake and fast intracellular drug release. Besides, Ps also enable the possibility of image-guided drug delivery for optimized and personalized treatment (theranostics). In this thesis, we designed and evaluated Ps systems based on either PEG-disulfide polycarbonate and/or PEG-iodinated polycarbonate for targeted tumor imaging and therapy.