基于槲皮素纳米海绵的槲皮素口腔片剂的设计和体内评估

P. Gujjula, A. Parameswari
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摘要

研究的目的是利用基于环糊精的纳米海绵制成控释配方,从而提高槲皮素的生物利用率。在早期测试的基础上,采用冷冻干燥工艺将槲皮素装入纳米海绵,并进行了 3 因子、3 层盒-贝肯设计。制备的纳米海绵经描述和制成片剂后进行了检验。槲皮素纳米海绵的粒径为 36.45 至 135.27 nm,包封效率为 42.37 至 88.44%,6 小时药物释放率为 53.04 至 82.64%。傅立叶变换红外光谱(FTIR)、电致发光扫描(DSC)和X射线衍射(XRD)研究验证了槲皮素与纳米海绵的相互作用。纳米海绵咀嚼片的体外药物释放率为 99.75%,稳定性测试表明,纳米海绵转化为咀嚼片后的 6 个月内无明显变化。在大鼠体内进行的研究表明,槲皮素优化纳米海绵片剂的 Cmax 为 6.27 ± 0.06 ng/mL,明显高于其他纳米海绵片剂的 Cmax(p<0.05)。
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Design and In-vivo Evaluation of Quercetin Nanosponges-based Buccal Tablets of Quercetin
The objective was to increase the bioavailability of quercetin by creating a controlled release formulation using nanosponges based on cyclodextrin. Based on the early testing, a 3-factor, 3-level Box-Behnken design with quercetin was loaded into nanosponges using the freeze-drying process. The prepared nanosponges were examined after being described and made into tablets. The quercetin-loaded nanosponges have particle sizes ranging from 36.45 to 135.27 nm, encapsulation efficiencies ranging from 42.37 to 88.44%, and drug release percentages at 6 hours ranging from 53.04 to 82.64%. The FTIR, DSC, and XRD investigations validated the Quercetin interaction with nanosponges. The medicine released from the nanosponges buccal tablets in-vitro at a rate of 99.75%, and stability testing showed no significant changes within six months after the nanosponges were transformed into tablets. In-vivo studies in rats showed that quercetin optimised nanosponges tablets Cmax of 6.27 ± 0.06 ng/mL was significantly higher (p
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