Investigation of radiolabelled chitosan nanoparticles bearing Cefpodoxime Proxetil, and in vitro antibacterial effect on
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Investigation of radiolabelled chitosan nanoparticles bearing Cefpodoxime Proxetil, and in vitro antibacterial effect on Gram‑positive Staphylococcus aureus and Gram‑negative Escherichia coli Derya Özel1 · Fatma Yurt1 Received: 20 April 2020 / Accepted: 26 September 2020 © Akadémiai Kiadó, Budapest, Hungary 2020
Abstract This study aims to investigate radiolabeled Cefpodoxime Proxetil loaded chitosan (CP–CS) nanoparticles as nuclear imaging infection agent to Gram-positive Staphylococcus aureus (S. aureus) and Gram-negative Escherichia coli (E. coli). The encapsulation efficiency of Cefpodoxime Proxetil was found 82 ± 2%. CP and CP–CS nanoparticles were radiolabeled with Tc-99 m. The radiochemical purity of 99mTc–CP and 99mTc–CP–CS nanoparticles were determined by RTLC as 89 ± 3% and 94 ± 2% respectively. In vitro bindings of 99mTc–CP–CS nanoparticles to S. aureus and E. coli were found higher than 99m Tc–CP bindings. Keywords Cefpodoxime proxetil · Chitosan nanoparticles · 99mTc · In vitro · Uptake efficiency
Introduction With the increased in antibiotics use, the rapid resistance of bacteria to antibiotics has emerged. For this reason, the development of new “talented agents” is needed to improve antibiotics effectiveness. Nanoparticles (NPs) are used as delivery agents for antibacterial, antiviral, antifungal and antiparasitic drugs. Since nanoparticles are 1–1000 nm in size, they can overcome many biological barriers in the body. These properties allow controlled release of the drug taken on target area of the body [1, 2]. Nanoparticles which cause low developing of microbial resistance could be used as new antimicrobial agents [3]. Also, the effects of antimicrobials can be improved by loading drugs on NP-based carriers, in contrast to its free drug counterparts. The use of NPs to increase the delivery of antimicrobial drug significantly in the serum solubility, prolong the lifetime of systemic circulation of the drug, sustained drug release in target tissues, and benefit in delivering multiple drugs to target tissue [4].
* Fatma Yurt [email protected]; [email protected] 1
Department of Nuclear Applications, Institute of Nuclear Science, Ege University, 35100, Bornova, Izmir, Turkey
Cefpodoxime Proxetil (CP) is a third-generation cephalosporin group antibiotic. CP is an effective pro-drug for oral administration which is characterized by its broad-spectrum activity against Gram-positive and Gram-negative microorganisms [5, 6]. According to the Biopharmaceutical Classification System (BCS), CP is a BCS class IV drug, which is characterized by low permeability and solubility, resulting in limited bioavailability [7]. The bioavailability of Cefpodoxime Proxetil is only 50% when it is administered in the conventional dosage form [8]. However, the application of CP is greatly limited by its disadvantageous properties, such as poor water solubility and poor bioavailability. Various types of drug delivery systems have been developed to improve the solubility, stability and bioavailability of C
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