Novel C60 Fullerenol-Gentamicin Conjugate–Physicochemical Characterization and Evaluation of Antibacterial and Cytotoxic Properties

Abstract

This study aimed to develop, characterize, and evaluate antibacterial and cytotoxic properties of novel fullerene derivative composed of C60 fullerenol and standard aminoglycoside antibiotic–gentamicin (C60 fullerenol-gentamicin conjugate). The successful introduction of gentamicin to fullerenol was confirmed by X-ray photoelectron spectroscopy which together with thermogravimetric and spectroscopic analysis revealing the formula of the composition as C60(OH)12(GLYMO)11(Gentamicin)0.8. The dynamic light scattering (DLS) revealed that conjugate possessed ability to form agglomerates in water (size around 115 nm), while Zeta potential measurements demonstrated that such agglomerates possessed neutral character. In vitro biological assays indicated that obtained C60 fullerenol-gentamicin conjugate possessed the same antibacterial activity as standard gentamicin against Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, and Escherichia coli, which proves that combination of fullerenol with gentamicin does not cause the loss of antibacterial activity of antibiotic. Moreover, cytotoxicity assessment demonstrated that obtained fullerenol-gentamicin derivative did not decrease viability of normal human fibroblasts (model eukaryotic cells) compared to control fibroblasts. Thus, taking into account all of the results, it can be stated that this research presents effective method to fabricate C60 fullerenol-gentamicin conjugate and proves that such derivative possesses desired antibacterial properties without unfavorable cytotoxic effects towards eukaryotic cells in vitro. These promising preliminary results indicate that obtained C60 fullerenol-gentamicin conjugate could have biomedical potential. It may be presumed that obtained fullerenol may be used as an effective carrier for antibiotic, and developed fullerenol-gentamicin conjugate may be apply locally (i.e., at the wound site). Moreover, in future we will evaluate possibility of its applications in inter alia tissue engineering, namely as a component of wound dressings and implantable biomaterials.

Incorporating the Antioxidant Fullerenol into Calcium Phosphate Bone Cements Increases Cellular Osteogenesis without Compromising Physical Cement Characteristics

“…[ 37,38,77–81 ] When the concentration of Ful reached 0.25 mg mL −1 , it was discovered that it increased the viability of MC3T3‐E1 cells over 24 h, as shown in Figure 7A. Literature also emphasizes that Ful is a highly biocompatible material, [ 37,38,77–81 ] and previous assessments with Ful concentrations up to 10 mg mL −1 were shown to be noncytotoxic using human skin fibroblasts, [ 77,78 ] murine macrophage cells, [ 80 ] and human epidermal keratinocytes. [ 79 ]…”

Potential Medical Use of Fullerenols After Two Decades of Oncology Research

“…The efficacy of well know antibiotic gentamicin was improved by FRL as a carrier for local administration at the wound site Nurzynksa et al 74 Overall impression of the presented works provided a clear conclusion that most of the positive outcomes (organprotection) were related to the antioxidative properties of FRLs. However, in dose-dependent studies with FRL, its cytostatic effect may be much stronger than its antioxidative ability.…”

“…Therefore, future investigations should focus on diseases in which oxidative stress might be one of the key causes or consequences. The past 2 decades have confirmed the potential use of FRL in some CNS diseases, 54,55,68,72 infections, 57,65,73,74 ophthalmology, 63 dermatology, 66,69 respiratory, 58 gynecology, 59 osteoporosis, 60,71 alcoholism, 62 thrombosis, 64 and diabetes. 67 Several studies have focused on the central nervous system (CNS), where the antioxidative properties of FRL may have a positive influence on patients with depression, 54 Alzheimer's disease, 55,72 and brain stroke.…”

“…57,65,73,74 Only one publication covered the antibacterial effect of FRL itself, 57 whereas 2 focused on conjugates with better efficacy and fewer side effects. 73,74 In one study, FRL was used as an adjuvant in the development of vaccines for HIV prevention. 65 Aoshima et al 57 44 exhibited a strong and wide-ranging antimicrobial activity, comparable to that of catechin.…”

Editorial: Nanomedicine-Based Drug Delivery Systems: Recent Developments and Future Prospects

“…In another article, the antibacterial and cytotoxic properties of a novel fullerene derivative composed of C 60 fullerenol and standard aminoglycoside antibiotic–gentamicin (C 60 fullerenol–gentamicin conjugate) were evaluated [ 8 ]. In vitro assays suggested that the developed C 60 fullerenol–gentamicin conjugate possessed the same antibacterial activity as standard gentamicin against various bacterial strains.…”