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首页> 外文期刊>Colloids and Surfaces, B. Biointerfaces >Novel scheme for rapid synthesis of hollow mesoporous silica nanoparticles (HMSNs) and their application as an efficient delivery carrier for oral bioavailability improvement of poorly water-soluble BCS type II drugs
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Novel scheme for rapid synthesis of hollow mesoporous silica nanoparticles (HMSNs) and their application as an efficient delivery carrier for oral bioavailability improvement of poorly water-soluble BCS type II drugs

机译：快速合成中空介孔二氧化硅纳米粒子（HMSNS）的新颖方案及其作为用于口服生物利用度的高效递送载体的应用，改善不良水溶性BCS II型药物

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Hollow mesoporous silica nanoparticles (HMSNs) are one of the most promising carriers for drug delivery. However, a facile method to synthesize HMSNs has hardly been reported so far. The primary objective of our current study was to develop HMSNs using a simple, quick, and inexpensive method and evaluate their ability to enhance solubility, dissolution rate, and bioavailability of poorly water-soluble model BSC type II drug Carvedilol. Traditional mesoporous silica nanoparticles (MSNs) are synthesized using classical Stober method and HMSNs with an entire hollow core was induced by immersing cetyltrimethylammonium bromide (CTAB) in hot water. Initial MSNs were added in boiling distilled water to synthesize hollow structure, to enhance pore size, and also to remove CTAB template. HMSNs prepared in our current study has exhibited high surface area (886.84 m(2)/g), pore volume (0.79 cm(3)/g), and uniform pore size (3.18 nm), which also enabled the greater encapsulation of the model BSC II drug Carvedilol (CAR) inside the HMSNs. This technique also helped in achieving a high drug loading of (40.22 +/- 0.73)%. Add to all this, in vitro studies conducted in the present work showed that compared with pure CAR and CAR loaded MSNs (CAR-MSNs) synthesized by Stober method, the drug-loaded HMSNs (CAR-HMSNs) exhibit sustained drug release performance. The high drug loading and sustained release can be attributed to the hollow porous structure of the HMSNs. Finally, a pharmacokinetic analysis in rats indicated a significant increase in bioavailability of carvedilol HMSNs in vivo compared to the pure carvedilol and carvedilol loaded MSNs. This study, therefore, offered a new, simple, and quick method to develop HMSNs with the ability to support higher loading and controlled release behavior in vitro and enhanced absorption of poorly-aqueous soluble drugs in-vivo.
机译：中空介孔二氧化硅纳米粒子（HMSNS）是最有前途的药物递送载体之一。然而，到目前为止，几乎没有报告了合成HMSNS的容易方法。我们目前的研究的主要目标是使用简单，快速，廉价的方法开发HMSNS，并评估其增强溶解度，溶出速率和水溶性较差模型BSC型药物卡维源性的溶解度，溶出速率和生物利用度的能力。使用经典的阶级甲型二氧化硅纳米颗粒（MSN）合成使用经典的斯普尔方法合成，并通过将甲基三甲基溴化铵（CTAB）浸入热水中诱导具有整个中空芯的HMSN。在沸腾的蒸馏水中加入初始MSN以合成中空结构，以增强孔径，也可以去除CTAB模板。在我们目前的研究中制备的HMSNS表现出高表面积（886.84米（2）/ g），孔体积（0.79厘米（3）/ g）和均匀的孔径（3.18nm），这也使得能够更大的封装模型BSC II药物Carvedilol（CAR）在HMSNS内。该技术还有助于实现（40.22 +/- 0.73）％的高药物载量。添加至所有这些，在本作中进行的体外研究表明，与通过STOPER方法合成的纯汽车和载荷的MSNS（CAR-MSNS）相比，药物负载的HMSN（CAR-HMSNS）表现出持续的药物释放性能。高药物载荷和持续释放可归因于HMSN的中空多孔结构。最后，与纯Carvedilol和Carvedilol负载的MSNS相比，大鼠的药代动力学分析表明Carvedilol HMSNs在体内的生物利用度显着增加。因此，本研究提供了一种新的，简单，快速的方法来开发HMSNS，其能够在体外支持更高的载荷和控制释放行为和增强的体内贫瘠水溶性药物的吸收。

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