BODIPYs are photosensitizers activatable by light to generate highly reactive singlet oxygen (O) from molecular oxygen, leading to tissue damage in the photoirradiated region. Despite their extraordinary photophysical characteristics, they are not featured in clinical photodynamic therapy. This review discusses the recent advances in the design and/or modifications of BODIPYs since 2013, to improve their potential in photodynamic cancer therapy and related areas.
For the purpose of this review, active targeting in cancer research encompasses strategies wherein a ligand for a cell surface receptor expressed on tumor cells is used to deliver a cytotoxic or imaging cargo. This area of research is more than two decades old, but in those 20 and more years, how many receptors have been studied extensively? What kinds of the ligands are used for active targeting? Are they mostly naturally occurring molecules such as folic acid, or synthetic substances developed in campaigns for medicinal chemistry efforts? This review outlines the most important receptor or ligand combinations that have been used in active targeting to answer these questions, and therefore to address the most important one of all: is research in active targeting affording diminishing returns, or is this an area for which the potential far exceeds progress made so far?
The chick embryo chorioallantoic membrane (CAM) is a preclinical model widely used for
vascular and anti-vascular effects of therapeutic agents in vivo. In this
study, we examine the suitability of CAM as a predictive model for acute toxicology
studies of drugs by comparing it to conventional mouse and rat models for 10 FDA-approved
anticancer drugs (paclitaxel, carmustine, camptothecin, cyclophosphamide, vincristine,
cisplatin, aloin, mitomycin C, actinomycin-D, melphalan). Suitable formulations for
intravenous administration were determined before the average of median lethal dose
(LD50) and median survival dose (SD50) in the CAM were measured
and calculated for these drugs. The resultant ideal LD50 values were correlated
to those reported in the literature using Pearson’s correlation test for both intravenous
and intraperitoneal routes of injection in rodents. Our results showed moderate
correlations (r2=0.42 − 0.68, P<0.005–0.05) between the
ideal LD50 values obtained using the CAM model with LD50 values from
mice and rats models for both intravenous and intraperitoneal administrations, suggesting
that the chick embryo may be a suitable alternative model for acute drug toxicity
screening before embarking on full toxicological investigations in rodents in development
of anticancer drugs.
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