Seite - (000365) - in Biomedical Chemistry: Current Trends and Developments

and tested, which increased the cell toxicity potential, and thus, enabled at least a 4–6-fold dose reduction of doxorubicin, independently of the cell line tested. Hence, this approach might be valid to overcome drug resistance and, at the same time, decrease the deleterious effects of doxorubicin (Fonseca, 2014). 3.5.3 Cancer Targeting Recent developments in nanotechnology are expected to revolutionize the current scenario of cancer therapy and diagnosis. This horizon has become closer with a considerable number of nano-formulations being recently approved for commercialization or reaching preclinical and clinical stages. The unique features of engineered nanotherapeutics can be translated into potential and attractive advantages over the conventionally practiced chemotherapeutic modalities, including: the reversion of unfavorable physicochemical properties of cytostatic drug molecules, resulting in improved pharmacokinetic and pharmacodynamics profiles (Alexis, 2008; Bertrand, 2012; Bertrand, 2014; Kipp, 2004); improvement of drug stability by confining the therapeutic agents inside the nanocarriers, preventing their degradation (Whitehead, 2009); delivery of the bioactive payload to the tumor site through passive and/or active targeting strategies, consequently improving its therapeutic efficacy and reducing adverse side effects by hindering the drug release during systemic circulation; and designing multifunctional nanoplatforms for combined therapy and/or theranostic applications, encompassing both therapeutic and diagnostic functions (Fernandez-Fernandez, 2011; Janib, 2010; Sanna, 2014). Since the concept of the “magic bullet” was introduced, nearly one hundred years ago (Strebhardt, 2008), significant efforts have been focused on a deeper understanding of the tumor biology and microenvironment, as well as on the screening of receptors overexpressed by the cancer cells, with the ultimate goal of defining strategies for specifically targeting the tumor tissues. In this context, remarkable advances in nanotechnology led to the emergence of targeting nanodelivery systems as innovative as complex, which exploit