Gold(I) compounds have emerged as potential anticancer chemotherapeutics with Auranofin ([(2R,3R,4S,5R,6S)-3,4,5-tris(acetyloxy)-6-{[(triethyl-l5-phosphanylidene)aurio]sulfanyl} oxan-2-yl]methyl acetate, a compound containing the [AuPEt3]+ fragment) being evaluated in clinical trials. Despite the efficacy in patients or in pre-clinical models of these gold compounds and FDA approved platinum derivatives, there are some difficulties in most cases, related to pharmaceutical deficiencies such as poor water solubility, low bioavailability and short circulating time. Thus, there is a need to improve the delivery of these drugs so that they can be efficiently released at the specific tumor site without affecting healthy tissues. We will report on delivery vehicles for gold(I)-based cytotoxic agents (conatining phosphanes and N-Heterocyclic NHC-carbene ligands) consisting on: a) “smart” peptide nanocarriers, and b) antibodies such as trastuzumab. We will report on synthetic strategies to obtain antibody-drug conjugates and to encapsulate gold compounds in MMP-9 responsive peptide-based nanocarriers. We will describe preliminary results for cellular viability assays in human renal and breast cancer cell lines and non-cancerous cell lines to highlight the tumor targeting properties of these systems.

“Smart” biodegradable nanocarriers and antibodies as targeting delivery vehicles for gold-based metallodrugs

2019 Spring National Meeting

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