College of Pharmacy, Jiangsu University, Zhenjiang, China.
Department of Biochemistry and Forensic Sciences, School of Chemical and Biochemical Sciences, C. K. Tedam University of Technology and Applied Sciences (CKT-UTAS), Navrongo, Ghana.
Pharm Dev Technol. 2022 Sep;27(7):829-841. doi: 10.1080/10837450.2022.2122506. Epub 2022 Sep 13.
Hyperoside (Hyp) self-assembled polymeric micelles (Hyp-PMs) were purposely developed to enhance aqueous solubility, availability and anti-oxidative effect of Hyp. In preparing Hyp-PMs, we employed the thin film dispersion method with the micelles consisting of TPGs and mPEG2000-PDLLA3000. The particle size, polydispersity index and zeta potential of Hyp-PMs were 67.42 ± 1.44 nm, 0.229 ± 0.015 and -18.67 ± 0.576 mV, respectively, coupled with high encapsulation efficiency （EE）of 90.63 ± 1.45% and drug loading (DL) of 6.97 ± 1.56%. Furthermore, the value of critical micelle concentration (CMC) was quite low, which indicated good stability and improved self-assembly ability of Hyp-PMs. Also, trend of Hyp release from Hyp-PMs demonstrated enhanced solubility of Hyp. Similarly, in comparison with free Hyp, oral bioavailability of Hyp-PMs was improved (about 8 folds) whilst half-life of Hyp-PMs was extended (about 3 folds). anti-oxidative effect showed obvious strong scavenging DPPH capability of Hyp-PMs, which may be attributed to its smaller size and better solubility. Altogether, Hyp-PMs may serve as a possible strategy to potentially enhance aqueous solubility, bioavailability and anti-oxidative effect of Hyp, which may play a key role in Hyp application in the pharmaceutical industries.
目的在于提高 Hyp 的水溶性、生物利用度和抗氧化效果，我们专门开发了 Hyp 自组装聚合物胶束（Hyp-PMs）。在制备 Hyp-PMs 时，我们采用薄膜分散法，胶束由 TPGs 和 mPEG2000-PDLLA3000 组成。Hyp-PMs 的粒径、多分散指数和 Zeta 电位分别为 67.42±1.44nm、0.229±0.015 和-18.67±0.576mV，包封效率（EE）高达 90.63±1.45%，载药量（DL）为 6.97±1.56%。此外，临界胶束浓度（CMC）值相当低，表明 Hyp-PMs 具有良好的稳定性和自组装能力。同样，Hyp 从 Hyp-PMs 中的释放趋势表明 Hyp 的溶解度提高。同样，与游离 Hyp 相比，Hyp-PMs 的口服生物利用度提高（约 8 倍），半衰期延长（约 3 倍）。Hyp-PMs 具有明显的强清除 DPPH 能力，这可能归因于其较小的尺寸和更好的溶解度。总的来说，Hyp-PMs 可能是一种提高 Hyp 水溶性、生物利用度和抗氧化效果的潜在策略，这可能在 Hyp 在制药行业的应用中发挥关键作用。
