Abstract
The aim of our work was the synthesis and physicochemical characterization of a unique conjugate consisting of gold nanoparticles (AuNPs) and a pharmacologically active anticancer substance abiraterone (AB). The direct coupling of AB with gold constitutes an essential feature of the unique AuNPs–AB conjugate that creates a promising platform for applications in nanomedicine. In this work, we present a multidisciplinary, basic study of the obtained AuNPs–AB conjugate. Theoretical modeling based on the density functional theory (DFT) predicted that the Aun clusters would interact with abiraterone preferably at the N-side. A sharp, intense band at 1028 cm−1 was observed in the Raman spectra of the nanoparticles. The shift of this band in comparison to AB itself agrees well with the theoretical model. AB in the nanoparticles was identified by means of electrochemistry and NMR spectroscopy. The sizes of the Au crystallites measured by XRPD were about 9 and 17 nm for the nanoparticles obtained in pH 7.4 and 3.6, respectively. The size of the particles as measured by TEM was 24 and 30 nm for the nanoparticles obtained in pH 7.4 and pH 3.6, respectively. The DLS measurements revealed stable, negatively charged nanoparticles.
Highlights
Abiraterone (AB) is administered as an acetate ester prodrug which is rapidly converted in vivo to abiraterone [1]
Challenges related to modern drug form technology consist, among other things, in using techniques and technologies that allow us to deliver the drug directly to the drug target, extend the time of the API’s (Active Pharmaceutical Ingredient) activity in the drug target, and influence the API’s distribution
Deuterated solvents for Nuclear Magnetic Resonance (NMR) spectroscopy were purchased from ARMAR AG (Döttingen, Switzerland)
Summary
Abiraterone (AB) is administered as an acetate ester prodrug which is rapidly converted in vivo to abiraterone [1]. In the light of the above, nanotechnology gains primary importance [2,3,4,5]. Inorganic nanoparticles and their combinations with organic substances in the hybrid form are characterized by unique physical, chemical, and biological properties. A shift into the nano-scale causes a significant increase in the specific grain boundary area per unit volume. This in turn results in a remarkable increase of the reactivity of the material, adsorption, anti-microbiological, and anticancer activity [6,7,8,9,10]
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