核iferine 脂质体的制备、药物动力学及对狗的抗肥胖作用。

IF 1.8 3区 农林科学 Q2 VETERINARY SCIENCES Veterinary Medicine and Science Pub Date : 2024-09-01 DOI:10.1002/vms3.70017
Jiang Lu, Yi-Tian Xu, Xiao-Liang Qian, Dao-Xian Zhu, Jin-Ye Lu, Hui Ma, Jing Liu
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引用次数: 0

摘要

背景:从荷叶中提取的天然化合物 Nuciferine(NUC)已被证实具有抗肥胖作用。然而,由于 NUC 的水溶性差、生物利用度低等原因,其作为犬用抗肥胖药物的开发和应用受到了阻碍:为了促进狗用 NUC 相关抗肥胖产品的开发,本研究将 NUC 制备成脂质体制剂,并评估了其特性、在狗体内的药代动力学以及对高脂饮食狗的抗肥胖效果:方法:以NUC、鸡蛋卵磷脂和β-谷甾醇为原料,采用乙醇注射法制备NUC脂质体。分别用粒度分析仪和透析法评价了脂质体的特性和体外释放率。采用高效液相色谱法(HPLC)对狗口服 NUC 脂质体后的药代动力学进行了研究。此外,我们还研究了 NUC 脂质体对以高脂饮食喂养的肥胖犬的抗肥胖作用:结果:成功制备了 NUC 脂质体,其 EE 为 (79.31 ± 1.06)%,粒径为 (81.25 ± 3.14) nm,zeta 电位为 (-18.75 ± 0.23) mV,PDI 为 0.175 ± 0.031。NUC 脂质体中 NUC 的体外累积释放速率比 NUC 慢。与 NUC 相比,NUC 脂质体在狗体内的 T1/2 和相对生物利用度增加,CL 降低。此外,与 NUC 相比,NUC 脂质体对高脂饮食犬肥胖症的预防作用更强:结论:NUC脂质体制剂有利于提高其在狗体内的相对生物利用度和抗肥胖效果。
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Preparation, pharmacokinetics and anti-obesity effects on dogs of nuciferine liposomes.

Background: Nuciferine (NUC), a natural compound extracted from lotus leaves, has been proven to have anti-obesity effects. However, the development and application of NUC as an anti-obesity drug in dogs are hindered due to its poor water solubility and low bioavailability.

Objective: To promote the development of NUC-related products for anti-obesity in dogs, this study prepared NUC into a liposome formulation and evaluated its characteristics, pharmacokinetics in dogs, and anti-obesity effects on high-fat diet dogs.

Methods: NUC liposomes were prepared by the ethanol injection method, using NUC, egg lecithin, and β-sitosterol as raw materials. The characteristics and release rate in vitro of liposomes were evaluated by particle size analyser and dialysis method, respectively. The pharmacokinetics in dogs after oral administration of NUC-liposomes was carried out by the high-performance liquid chromatography (HPLC) method. Moreover, we investigated the anti-obesity effect of NUC-liposomes on obese dogs fed with a high-fat diet.

Results: NUC-liposome was successfully prepared, with an EE of (79.31 ± 1.06)%, a particle size of (81.25 ± 3.14) nm, a zeta potential of (-18.75 ± 0.23) mV, and a PDI of 0.175 ± 0.031. The cumulative release rate in vitro of NUC from NUC-liposomes was slower than that of NUC. The T1/2 and relative bioavailability of NUC-liposomes in dogs increased, and CL reduced compared with NUC. In addition, the preventive effect of NUC-liposomes on obesity in high-fat diet dogs is stronger than that of NUC.

Conclusions: The liposome formulation of NUC was conducive to improve its relative bioavailability and anti-obesity effect in dogs.

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来源期刊
Veterinary Medicine and Science
Veterinary Medicine and Science Veterinary-General Veterinary
CiteScore
3.00
自引率
0.00%
发文量
296
期刊介绍: Veterinary Medicine and Science is the peer-reviewed journal for rapid dissemination of research in all areas of veterinary medicine and science. The journal aims to serve the research community by providing a vehicle for authors wishing to publish interesting and high quality work in both fundamental and clinical veterinary medicine and science. Veterinary Medicine and Science publishes original research articles, systematic reviews, meta-analyses, and research methods papers, along with invited editorials and commentaries. Original research papers must report well-conducted research with conclusions supported by the data presented in the paper. We aim to be a truly global forum for high-quality research in veterinary medicine and science, and believe that the best research should be published and made widely accessible as quickly as possible. Veterinary Medicine and Science publishes papers submitted directly to the journal and those referred from a select group of prestigious journals published by Wiley-Blackwell. Veterinary Medicine and Science is a Wiley Open Access journal, one of a new series of peer-reviewed titles publishing quality research with speed and efficiency. For further information visit the Wiley Open Access website.
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