Abstract
While 2-amino-4-(4-chlorophenyl)thiazole (AT) drug and thiazole derivatives have several biological applications, these compounds present some drawbacks, such as low aqueous solubility and instability. A new complex of βCD-AT has been synthesized to increase AT solubility and has been used as a substrate for the deposit of solid-state AuNPs via magnetron sputtering, thus forming the βCD-AT-AuNPs ternary system, which is stable in solution. Complex formation has been confirmed through powder X-ray diffraction and 1D and 2D nuclear magnetic resonance. Importantly, the amine and sulfide groups of AT remained exposed and can interact with the surfaces of the AuNPs. The complex association constant (970 M-1) has been determined using phase solubility analysis. AuNPs formation (32 nm average diameter) has been studied by UV-Visible spectroscopy, transmission/scanning electron microscopy and energy-dispersive X-ray analysis. The in vitro permeability assays show that effective permeability of AT increased using βCD. In contrast, the ternary system did not have the capacity to diffuse through the membrane. Nevertheless, the antibacterial assays have demonstrated that AT is transferred from βCD-AT-AuNPs, being available to exert its antibacterial activity. In conclusion, this novel βCD-AT-AuNPs ternary system is a promising alternative to improve the delivery of AT drugs in therapy.
Highlights
The concept of drug delivery is linked to the investigation of entry and release processes, and to the creation of increasingly complex and efficient mechanisms that support the entire drug-administration cycle—from the generation of a pharmaceutical productto elimination from the organism
The trace obtained for the physical mixture (Fig 3D) superimposed this intense peak against the diffraction pattern of βCD and it is clearly different from the trace of the formed complex (Fig 3C).The crystallographic pattern of the βCD-AT complex (Fig 3C) has been indexed for a monoclinic type P21 system [57], the network parameters of which are specified in the S1 Appendix
The results show that AT only exhibited activity on E. faecalis (MIC = 64 μg/ml)
Summary
The concept of drug delivery is linked to the investigation of entry and release processes, and to the creation of increasingly complex and efficient mechanisms that support the entire drug-administration cycle—from the generation of a pharmaceutical productto elimination from the organism. Optimizing drug administration requires, for example, that. Investigacion en Areas Prioritarias (FONDAP), number 15130011; http://www.conicyt.cl/fondap/
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