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负载胸腺肽的脱氧胆酸钠/磷脂混合纳米胶束可改善药物吸收。

Mixed nanomicelles loaded with thymopeptides-sodium deoxycholate/phospholipid improve drug absorption.

作者信息

Shi-Xiao Jin, Shi-Ying Jin, Lv Qing-Yuan, Shan-Shan Fu, Jin Han, Yuan Hai-Long

机构信息

Department of Pharmacy, 302 Military Hospital, Beijing 100039, China; School of pharmaceutics, Chengdu University of TCM, Chengdu 611730, China.

Department of Pharmacy, 302 Military Hospital, Beijing 100039, China.

出版信息

Chin J Nat Med. 2014 Jan;12(1):65-70. doi: 10.1016/S1875-5364(14)60011-X.

Abstract

AIM

To improve the absorption of thymopeptides (TH) by preparing sodium deoxycholate/phospholipid-mixed nanomicelles (SDC/PL-MMs).

METHODS

TH-SDC/PL-MMs were prepared by a film dispersion method, and then evaluated using photon correlation spectroscopy (PCS), zeta potential measurement, as well as their physical stability after storage for several days. Furthermore, in situ intestinal single-pass perfusion experiments and pharmacodynamics in immunodeficient mice were performed to make a comparison with TH powders and the control drug in absorption properties.

RESULTS

A narrow size distribution of nanomicelles, with a mean particle size of (149 ± 8.32) nm and a zeta potential of (-31.05 ± 2.52) mV, was obtained. The in situ intestine perfusion experiments demonstrated a significant advantage in absorption characteristics for TH compared to the other formulations, and oral administration of TH-SDC/PL-MMs potentiated an equivalent effect with i.h. TH in pharmacodynamic studies in immunodeficient mice.

CONCLUSIONS

TH-SDC/PL-MMs prepared by a film dispersion method are able to improve the absorption of TH. SDC/PL-MMs might be a good approach for the more effective delivery of drugs like TH.

摘要

目的

通过制备脱氧胆酸钠/磷脂混合纳米胶束(SDC/PL-MMs)来提高胸腺肽(TH)的吸收。

方法

采用薄膜分散法制备TH-SDC/PL-MMs,然后用光子相关光谱法(PCS)、ζ电位测量法对其进行评估,并观察其储存数天后的物理稳定性。此外,进行了原位肠道单通道灌注实验和免疫缺陷小鼠的药效学实验,以比较TH粉末和对照药物的吸收特性。

结果

获得了纳米胶束窄尺寸分布,平均粒径为(149±8.32)nm,ζ电位为(-31.05±2.52)mV。原位肠道灌注实验表明,与其他制剂相比,TH在吸收特性方面具有显著优势,并且在免疫缺陷小鼠的药效学研究中,口服TH-SDC/PL-MMs与皮下注射TH具有等效效果。

结论

通过薄膜分散法制备的TH-SDC/PL-MMs能够提高TH的吸收。SDC/PL-MMs可能是更有效地递送如TH这类药物的良好方法。

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