Preparation, Characterization, and Evaluation of Mesoporous Silica Nanoparticles in Enhancing Oral Bioavailability of Poorly Water-Soluble Drugs.

Hong Zhang, Fanjiao Zuo, Boyao Wang, Xilong Qiu
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Abstract

Background: Breviscapine (BVP) is one of the extracts of several flavonoids of Erigeron breviscapus, which has been widely used in the treatment of cerebral infarction and its sequelae, cerebral thrombus, coronary heart disease, and angina pectoris. But BVP has poor solubility.

Objective: The objective of the study is to develop mesoporous silica nanoparticles (MSNs) that can be loaded with a drug with poor water solubility. The MSNs, which were designed for oral administration, enhanced both the dissolution rate and drug loading capacity.

Methods: The use of MSNs as an oral drug delivery system was investigated by SEM, TEM, BETBJH, XRD, FT-IR, and HPLC. Additionally, we examined the oral bioavailability of BVP loaded onto MSNs and examined the cellular cytotoxicity of MSNs.

Results: The results indicate that the oral bioavailability of BVP after loading onto MSNs was greater than that of a marketed product. Furthermore, we studied the mechanism by which MSNs enhance the oral absorption of BVP.

Conclusion: MSNs have the potential to enhance the oral bioavailability of poorly water-soluble drugs by accelerating the drug dissolution rate.

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介孔二氧化硅纳米颗粒的制备、表征和在提高水溶性差药物口服生物利用度方面的评估
背景:布维司卡平(BVP)是布维司卡平(Erigeron breviscapus)几种黄酮类化合物的提取物之一,已被广泛用于治疗脑梗塞及其后遗症、脑血栓、冠心病和心绞痛。但 BVP 的溶解性较差:本研究的目的是开发可装载水溶性差的药物的介孔二氧化硅纳米粒子(MSNs)。方法:将介孔二氧化硅纳米颗粒用作口服药物,可以提高药物的溶解速率和载药量:方法:通过扫描电镜、电子显微镜、BETBJH、XRD、傅立叶变换红外光谱和高效液相色谱法研究了 MSNs 作为口服给药系统的用途。此外,我们还考察了载入 MSNs 的 BVP 的口服生物利用度,并考察了 MSNs 的细胞毒性:结果表明,负载到 MSN 上的 BVP 的口服生物利用度高于市售产品。此外,我们还研究了 MSNs 促进 BVP 口服吸收的机制:结论:MSN 有可能通过加快药物溶解速度来提高水溶性差的药物的口服生物利用度。
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