银杏双黄酮TPGS/Soluplus混合纳米胶束的体内药动学研究

doi:10.5246/jcps.2026.04.023

中国药学(英文版) ›› 2026, Vol. 35 ›› Issue (4): 340-347.DOI: 10.5246/jcps.2026.04.023

• 【研究论文】 • 上一篇

银杏双黄酮TPGS/Soluplus混合纳米胶束的体内药动学研究

张玉倩¹, 牛海英², 张晓炜¹, 解伟伟¹, 靳怡然¹^,^*()

^1. 河北医科大学第二医院, 河北石家庄 050000
^2. 河北医科大学第一医院, 河北石家庄 050000

收稿日期:2025-12-26 修回日期:2026-01-28 接受日期:2026-02-15 出版日期:2026-05-05 发布日期:2026-05-07
通讯作者: 靳怡然

Preparation, characterization, and pharmacokinetics study of ginkgetin TPGS/Soluplus mixed nanomicelles

Yuqian Zhang¹, Haiying Niu², Xiaowei Zhang¹, Weiwei Xie¹, Yiran Jin¹^,^*()

^1. The Second Hospital of Hebei Medical University, Shijiazhuang 050000, Hebei, China
^2. The First Hospital of Hebei Medical University, Shijiazhuang 050000, Hebei, China

Received:2025-12-26 Revised:2026-01-28 Accepted:2026-02-15 Online:2026-05-05 Published:2026-05-07
Contact: Yiran Jin
Supported by:
Hebei Administration of Traditional Chinese Medicine (Grant No. 2024040).

摘要/Abstract

摘要：

本研究目的是考察银杏双黄酮TPGS/Soluplus混合纳米胶束在大鼠体内的药代动力学特征。采用薄膜水化法制备银杏双黄酮混合纳米胶束, 从纳米胶束粒径、Zeta电势、载药量、包封率及临界胶束浓度对其性能进行表征; 以银杏双黄酮原料药为参考, 比较其纳米胶束的口服药动学行为, 将SD大鼠分为银杏双黄酮组和银杏双黄酮纳米胶束组, 每组6只, 分别灌胃100 mg/kg 银杏双黄酮组和银杏双黄酮纳米胶束组(以负载的银杏双黄酮计); 于给药后进行眼内眦采血, 计算药动学参数。本研究所制银杏双黄酮纳米胶束的平均粒径为66.33 ± 2.11 nm, 多分散性指数为0.061 ± 0.013, Zeta电位为–25.67 ± 0.21 mV, 包封率为97.92% ± 0.66%, 载药量为2.47% ± 0.02%。药动学结果显示, 与银杏双黄酮组比较, 银杏双黄酮纳米胶束组大鼠的t_max、t_1/2、C_max、AUC_0–t和AUC_0–∞均显著增加/延长(P < 0.05)。本研究建立的方法可用于测定银杏双黄酮的浓度, 大鼠口服银杏双黄酮纳米胶束后, 可显著增加银杏双黄酮口服吸收生物利用度。

关键词: 银杏双黄酮, TPGS/Soluplus, 纳米胶束, 药代动力学, 生物利用度

Abstract:

This study aimed to investigate the pharmacokinetic properties of ginkgetin TPGS/Soluplus mixed nano-micelles (ginkgetin nanomicelles) in rats. The nanomicelles were prepared using the film hydration method and subsequently characterized in terms of particle size, zeta potential, drug loading, entrapment efficiency, and critical micelle concentration. The oral pharmacokinetic profile of the nanomicelles was compared with that of free ginkgetin. Sprague-Dawley rats were randomly assigned to either the ginkgetin group or the ginkgetin nanomicelles group, with six rats per group. Each group received an intragastric dose of 100 mg/kg (calculated based on the ginkgetin content). Blood samples were collected from the inner canthus at designated time points, and pharmacokinetic parameters were calculated. The prepared ginkgetin nanomicelles exhibited an average particle size of 66.33 ± 2.11 nm, a polydispersity index of 0.061 ± 0.013, and a zeta potential of –25.67 ± 0.21 mV. The entrapment efficiency and drug loading were 97.92% ± 0.66% and 2.47% ± 0.02%, respectively. Pharmacokinetic analysis revealed that, compared with free ginkgetin, the nanomicelles significantly prolonged t_max and t_1/2, and increased C_max, AUC_0–t, and AUC_0–∞ (P < 0.05). The analytical method established in this study proved effective for determining ginkgetin concentrations. Oral administration of ginkgetin nanomicelles markedly enhanced the bioavailability of ginkgetin.

Key words: Ginkgetin, TPGS/Soluplus, Nano-micelles, Pharmacokinetics, Bioavailability

Supporting:

张玉倩, 牛海英, 张晓炜, 解伟伟, 靳怡然. 银杏双黄酮TPGS/Soluplus混合纳米胶束的体内药动学研究[J]. 中国药学(英文版), 2026, 35(4): 340-347.

Yuqian Zhang, Haiying Niu, Xiaowei Zhang, Weiwei Xie, Yiran Jin. Preparation, characterization, and pharmacokinetics study of ginkgetin TPGS/Soluplus mixed nanomicelles[J]. Journal of Chinese Pharmaceutical Sciences, 2026, 35(4): 340-347.

图/表 5

Figure 1. The size distribution spectrum of ginkgetin nanomicelles (A) and the zeta potential spectrum (B).

Figure 2. Measurement of the CMC of ginkgetin nanomicelles.

Figure 3. LC-MS/MS chromatograms. (A) Blank plasma; (B) Blank plasma containing 1 ng/mL of ginkgetin (lower limit of quantification); (C) Peak of ginkgetin in rat plasma sample; (D) Peak of IS in rat plasma sample.

Figure 4. Pharmacokinetic curve (x ± s, n ＝ 6).

Table 1. Main pharmacokinetic parameters (x ± s, n ＝ 6).

参考文献 12

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银杏双黄酮TPGS/Soluplus混合纳米胶束的体内药动学研究

Preparation, characterization, and pharmacokinetics study of ginkgetin TPGS/Soluplus mixed nanomicelles

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