Objectives

In this study, a polymer micelle containing berberine (Ber) was prepared. The micelle was composed of Pluronic F127 and Ber. The hypoglycemic effect was verified by animal experiments.

Methods

The Ber-loaded micelles were prepared with a thin-film hydration method. Encapsulation efficiency, surface morphology, particle size, zeta potential, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were determined. The drug release profile of Ber was studied with the dialysis method. In addition, the streptozocin (STZ)-induced type 2 diabetic model in mice was used to examine the hypoglycemic effect.

Key Findings

The average size of the prepared micelles was 91.1 nm with a polydispersity of 0.285. Compared with the Ber ethanol solution, the in vitro release of Ber from micelles presented the sustained-release property. The animal experiments verified the micelles increased body weight and decreased food and water intake of type 2 diabetic mice. Also, the level of blood glycosylated hemoglobin (GHb), total cholesterol (TC), total triglyceride (TG), and non-esterified fatty (NEFA) was lowered, from which we inferred that the Ber-F127 micelles had the expected hypoglycemic effect.

Conclusions

Our results suggested that F127 micelles might serve as a promising nanocarrier to improve the solubility and bioavailability of Ber.

中文翻译：

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负载小檗碱的 Pluronic F127 聚合物胶束的物理化学表征和降血糖作用的体内评价

目标

在这项研究中，制备了一种含有小檗碱（Ber）的聚合物胶束。胶束由 Pluronic F127 和 Ber 组成。通过动物实验验证了降血糖作用。

方法

负载 Ber 的胶束采用薄膜水合法制备。测定了包封效率、表面形态、粒径、zeta 电位、差示扫描量热法 (DSC) 和 X 射线衍射 (XRD)。采用透析法研究了 Ber 的药物释放曲线。此外，链脲佐菌素（STZ）诱导的小鼠2型糖尿病模型用于检查降血糖作用。

主要发现

制备的胶束的平均尺寸为 91.1 nm，多分散性为 0.285。与Ber乙醇溶液相比，Ber从胶束中的体外释放呈现缓释特性。动物实验证实胶束增加了 2 型糖尿病小鼠的体重并减少了食物和水的摄入。此外，血液中的糖基化血红蛋白（GHb）、总胆固醇（TC）、总甘油三酯（TG）和非酯化脂肪（NEFA）水平降低，由此推断Ber-F127胶束具有预期的降血糖作用.

结论

我们的研究结果表明，F127 胶束可能作为一种有前途的纳米载体来提高 Ber 的溶解度和生物利用度。