A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects.
A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects.
复制标题
一种新型白蛋白包裹的美洛昔康纳米混悬剂，可改善炎症靶向作用
DOI：
10.2147/ijn.s160714
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发表时间：
2018
影响因子：
8
通讯作者：
Pan W
中科院分区：
文献类型：
--
作者：
Li Q;Chen F;Liu Y;Yu S;Gai X;Ye M;Yang X;Pan W
本研究的目的是开发一种生物利用度更高、安全性更高的美洛昔康（MX）纳米混悬液，以显著改善炎症靶向性。方法与结果采用酸碱中和法制备了载mx的牛血清白蛋白（BSA）纳米悬浮液，并对所制备的纳米悬浮液进行了表征。结果表明，制备的纳米混悬液粒径分布较窄，平均粒径为78.67±0.22 nm，多分散性指数为0.133±0.01，zeta电位为- 11.87±0.91 mV。通过透射电镜观察，制备的MX纳米混悬液被牛血清白蛋白包裹成球形，表面光滑。稳定性研究表明，纳米混悬液在4°C时物理稳定，保质期至少为6个月。体外溶出试验表明，载mx -BSA纳米混悬液（MX-BSA-NS）具有缓释特性。此外，大鼠静脉注射后的体内药代动力学研究表明，MX- bsa - ns的半衰期（t1/2）、平均停留时间（MRT）和浓度-时间曲线下面积（AUC0 -∞）分别比MX常规溶液（MX溶液）增加169.83%、150.13%和148.80%。此外，炎症靶向研究结果显示，注射MX- bsa - ns后，与MX溶液组相比，炎症组织中MX浓度显著升高，正常组织中MX浓度降低。结论制备的MX- bsa - ns明显提高了MX的炎症靶向性和生物利用度，提示其在未来的临床应用中有潜力成为MX靶向给药的一种有前景的配方。
Background The objective of this study was to develop a more bio-available and safe nanosuspension of meloxicam (MX), which could dramatically improve inflammation targeting. Methods and results MX-loaded bovine serum albumin (BSA) nanosuspensions were prepared using acid–base neutralization in aqueous solution and the prepared nanosuspensions were characterized. The results obtained showed that the prepared nanosuspensions had a narrow size distribution with a mean particle size of 78.67±0.22 nm, a polydispersity index of 0.133±0.01, and a zeta potential of −11.87±0.91 mV. The prepared MX nanosuspensions were spherically wrapped by BSA with a smooth surface as shown by transmission electron microscopy. Stability studies showed that the nanosuspensions were physically stable at 4°C with a shelf life of at least 6 months. In the in vitro dissolution test, the MX-loaded BSA nanosuspension (MX-BSA-NS) exhibited sustained release. In addition, an in vivo pharmacokinetic study in rats following intravenous injection showed that the half-life (t1/2), mean residence time (MRT), and area under the concentration–time curve (AUC0–∞) of MX-BSA-NS was increased by 169.83%, 150.13%, and 148.80%, respectively, in comparison with MX conventional solution (MX solution). Furthermore, results from inflammation targeting studies showed that the concentration of MX increased significantly in inflamed tissues but was reduced in normal tissues compared with the MX solution group after injection of MX-BSA-NS. Conclusion The prepared MX-BSA-NS significantly increased the inflammation-targeting properties and bioavailability of MX, suggesting its potential as a promising formulation for the targeted drug delivery of MX in future clinical applications.