关键词: 介孔生物活性玻璃, 米诺环素, 载药系统, 装载, 释放

Abstract: Objective： To construct mesoporous nano-bioactive glass (MNBG) microspheres load-release minocycline as an antibacterial drug delivery system. Methods: Sol-gel method was used to synthesze MNBG microspheres as drug carrier. The MNBG consisted of SiO2, CaO, and P2O5. According to the content of silicon, MNBG microspheres were divided into four groups (60S, 70S, 80S and 90S). Scanning electron microscopy (SEM) was used to observe the surface characteristic and particle size of MNBG; Nitrogen adsorption-desorption experiment was performed to calculate the MNBG’s specific surface area and the pore sizes; The Fourier transform infrared spectrum (FT-IR) and the thermogravimetric analysis were conducted to calculate the loading efficiencies of minocycline hydrochloride; UV spectrophotometric was used to determine the cumulative release of minocycline from drug-loaded particles in PBS solution within 21 d. Agar diffusion test (ADT) was performed to evaluate the antibacterial properties on Enterococcus faecalis. The inhibition zone was observed and the diameter was measured. Results: The MNBG microspheres had good dispersion, large surface area, and even particle size. The pore sizes ranged from 4.77 nm to 7.33 nm. The loading experiment results showed that the minocycline hydrochloride loading efficiency of MNBG was related to the pore size of the microspheres. Among 60S, 70S, 80S and 90S, 60S MNBG had the highest loading efficiency of 16.33% due to its high calcium content and large pore sizes. A slow minocycline release rate from MNBG particles in PBS solution until d 21 was observed. It was showed that a burst release of 28% of the total drug for the first 24 h. A cumulative release of 35% was found, and the final concentration of minocycline maintained at about 47 mg/L. ADT showed that mino-MNBG had inhibitory effect on the growth of Enterococcus faecalis. 1 g/L minocycline, 1 g/L mino-MNBG, and 0.1 g/L minocycline presented inhibition zone, however, PBS and 1 g/L MNBG didn’t. The diameter of the inhibition zone of minocycline groups was significant larger than that of mino-MNBG group (P<0.05), which was also significant larger than those of PBS and MNBG groups (P<0.05). It showed that mino-MNBG drug delivery system had antibacterial properties on Enterococcus faecalis.  Conclusion: The 60S MNBG that can effectively load and release minocycline may be an ideal drug carrier.

Key words: Mesoporous bioactive glass, Minocycline, Drug delivery system, Load, Release