Enhancement Antimicrobial Activity of Clarithromycin by Amine functionalized Mesoporous Silica Nanoparticles as Drug Delivery System

LETTERS IN DRUG DESIGN & DISCOVERY(2018)

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摘要
Background: Nano-drug delivery systems as mesoporous silica nanoparticles ( MSNs) with unique properties have the potential to improve drug efficacy. The purpose of the present study was to design of CLM loaded MSNs-NH2 to improve the physicochemical properties and antibacterial activity with enhancement delivery to infected tissues. Methods: A large pore amine functionalized MSN (MSNs-NH2) is described here to facilitate delivery of clarithromycin (CLM) as an antibacterial drug and enhance the efficacy against Gram positive and Gram negative bacterial samples. Prepared particles were characterized by Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), nitrogen adsorption/desorption isotherms, Fourier Transform Infrared (FT-IR) spectroscopy and X-ray Diffraction (XRD) spectroscopy. The antimicrobial activity was evaluated by agar well diffusion and broth dilution methods. Therefore, the biodistribution of FITC-MSNs was investigated by measure the NIR intensity fluorescent of fluorescent images from whole animal and dissected organs of NMRI mice. Results: The results showed that the CLM loaded MSNs-NH2 (CLM/MSNs-NH2) were successfully prepared having good payload and pH-sensitive drug release kinetics. The antimicrobial investigation against Staphylococcus aureus and Escherichia coli was showed better performance of antimicrobial activity of these nanoparticles. In vivo and ex vivo fluorescent imaging investigation on NMRI mice were shown that FITC-MSNs-NH2 accumulated in the liver and kidney and notably in lung tissue. Conclusion: The CLM/MSNs-NH2 exhibited higher antimicrobial activity and enhanced the possibility of microbial infection therapy especially at respiratory infections.
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关键词
Drug delivery,mesoporous silica nanoparticle,clarithromycin,antimicrobial activity,TEM,SEM
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