Design of docetaxel-loaded polymeric nanoparticles: characterization, radiolabeling with 99m Tc and in vitro evaluation

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Design of docetaxel‑loaded polymeric nanoparticles: characterization, radiolabeling with 99mTc and in vitro evaluation Oğuz Çetin1 · Çiğdem İçhedef2 · Burcu Aydın2 · Serap Teksöz1 Received: 16 June 2020 / Accepted: 7 October 2020 © Akadémiai Kiadó, Budapest, Hungary 2020

Abstract This research aims to develop a polymeric drug delivery system for docetaxel (DTX) and to investigate its radiotracer potential by in vitro. DTX loaded Poly(lactic acid)/Poly(ethylene glycol) diblock copolymer (PLA–PEG) was synthesized and radiolabeled with technetium-99m tricarbonyl core. PLA–PEG–DTX nanoparticles had a particle size and zeta potential 120 ± 7.3 nm and − 24.66 ± 1.5 mV respectively, which was further supported by SEM image. The radiolabeling efficiency of 99mTc(CO)3-PLA–PEG–DTX was found to be 90 ± 3.51%,. In vitro study was carried out on cancer cell lines (MCF7, MDA-MB-231) to examine the biological behavior of docetaxel loaded PLA–PEG nanoparticles. Graphic abstract

Keywords  Docetaxel · polymeric nanoparticles · Technetium tricarbonyl core · Drug delivery system · Cell culture

Introduction * Oğuz Çetin [email protected] 1



Department of Material Science and Engineering, Graduate Faculty of Natural and Applied Science, Ege University, Bornova 35100, İzmir, Turkey



Department of Nuclear Applications, Institute of Nuclear Sciences Ege University, Bornova 35100, İzmir, Turkey

2

Cytotoxic drugs which constitute an important part of the chemotherapy, are substances that kill or stop rapidly growing and dividing cells by showing toxic effects. However, despite the long history of the use of cytotoxic drugs and many newly developed drugs and diets, negative results are

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encountered in the treatment. Cytotoxic anticancer drugs compared to other types of drugs; It is accompanied by problems such as low specificity, high toxicity, and sensitivity to drug resistance. Therefore, different solutions are needed in order for the cytotoxic drug given for therapeutic purposes to be specific to the tumor and not cause undesirable side effects. It is promising to improve the therapeutic efficacy and safety of targeted drug delivery systems prepared with nanoparticles, which are seen as one of these solutions [1]. Docetaxel is a natural product with antitumor activity, which exerts its cytotoxic effects on microtubules obtained via a semi-synthetic process from Taxus baccata. Docetaxel is one of the active molecules that can be used alone in metastatic breast cancer. Pradhan et al. emphasized that docetaxel can be widely used in the treatment of breast cancer, small and non-small cell lung cancer and prostate cancer [2–4]. Since it is a water-insoluble drug combination of ethanol and tween 80 (polysorbate 80) was used in the commercial docetaxel formulation (taxotere) to increase its solubility [5]. On the other hand, in this century nanotechnology is an engineering and material science of substances in which examined at atomic and molecular scale. There is no doubt that nanotechnology has been a pr