Discovery of novel pharmacological effects of berberine hydrochloride (BH) has made its clinical application valuable. However, further development and applications of BH are hampered by its short half-life and the side effects associated with its intravenous (iv) injection. To improve the hypolipidemia efficacy and reduce side effects, we encapsulated BH into biocompatible red blood cells (RBCs) to explore its sustained-release effect by hypotonic pre-swelling method. From in vitro evaluation, BH loaded RBCs (BH-RBCs) presented similar morphology and osmotic fragility to native RBCs (NRBCs). After the loading process, the BH-RBCs maintained around 69% of Na+/K+-ATPase activity of NRBCs and phosphatidylserine externalization value of BH-RBCs was about 26.1 ± 2.9%. The survival test showed that the loaded cells could circulate in plasma for over 9 d. For in vivo evaluation, a series of tests including pharmacokinetics study and hypolipidemic effect were carried out to examine the long-acting effect of BH-RBCs. The results showed that the release of BH in the loaded cells could last for about 5 d and the hypolipidemic effect can still be observed on 5 d after injection. BH-loaded autologous erythrocytes seem to be a promising sustained releasing delivery system with long hypolipidemic effect.

中文翻译：

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自体红细胞递入盐酸小ber碱具有长效作用，可用于低脂血症的治疗。

盐酸小ber碱（BH）的新药理作用的发现使其临床应用有价值。但是，BH的半衰期短以及与其静脉内（iv）注射相关的副作用阻碍了BH的进一步开发和应用。为了提高降血脂功效并减少副作用，我们将BH封装在生物相容性红细胞（RBC）中，以通过低渗预溶胀法探索其持续释放作用。通过体外评估，负载BH的RBC（BH-RBC）具有与天然RBC（NRBC）相似的形态和渗透脆性。加载过程后，BH-RBCs维持NRBCs的Na + / K + -ATPase活性约69％，BH-RBCs的磷脂酰丝氨酸外化值约为26.1±2.9％。存活测试表明，加载的细胞可以在血浆中循环9天以上。为了进行体内评估，进行了一系列试验，包括药代动力学研究和降血脂作用，以检查BH-RBC的长效作用。结果表明，BH在上样细胞中的释放可持续约5 d，注射后5 d仍可观察到降血脂作用。加载BH的自体红细胞似乎是一种有前途的降血脂作用的持续释放传递系统。结果表明，BH在上样细胞中的释放可持续约5 d，注射后5 d仍可观察到降血脂作用。加载BH的自体红细胞似乎是一种有前途的降血脂作用的持续释放传递系统。结果表明，BH在上样细胞中的释放可持续约5 d，注射后5 d仍可观察到降血脂作用。加载BH的自体红细胞似乎是一种有前途的降血脂作用的持续释放传递系统。