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含有吴茱萸碱-磷脂纳米复合物的纳米乳剂的吸收及体内动力学特征得到改善。

Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine-phospholipid nanocomplex.

作者信息

Hu Jiangbo, Chen Dilong, Jiang Rong, Tan Qunyou, Zhu Biyue, Zhang Jingqing

机构信息

Medicine Engineering Research Center, Chongqing Medical University, Chongqing, People's Republic of China.

Department of Histology and Embryology, Laboratory of Stem Cell and Tissue Engineering, Chongqing Medical University, Chongqing, People's Republic of China.

出版信息

Int J Nanomedicine. 2014 Sep 17;9:4411-20. doi: 10.2147/IJN.S59812. eCollection 2014.

DOI:10.2147/IJN.S59812
PMID:25258531
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4172252/
Abstract

PURPOSE: The purpose of this study was to assess the improved absorption and in vivo kinetic characteristics of a novel water-in-oil nanoemulsion containing evodiamine-phospholipid nanocomplex (NEEPN) when administered orally. METHODS: NEEPN was fabricated by loading an evodiamine-phospholipid nanocomplex into a water-in-oil nanoemulsive system. The gastrointestinal absorption of NEEPN was investigated using an in situ perfusion method. The modified in vivo kinetic characteristics of evodiamine (EDA) in NEEPN were also evaluated. RESULTS: Compared with EDA or conventional nanoemulsions containing EDA instead of evodiamine-phospholipid complex, NEEPN with its favorable in vivo kinetic characteristics clearly enhanced the gastrointestinal absorption and oral bioavailability of EDA; for example, the relative bioavailability of NEEPN to free EDA was calculated to be 630.35%, and the effective permeability of NEEPN in the colon was 8.64-fold that of EDA. CONCLUSION: NEEPN markedly improved the oral bioavailability of EDA, which was probably due to its increased gastrointestinal absorption. NEEPN also increased efficacy and reduced adverse effects for oral delivery of EDA. Such finding demonstrates great clinical significance as an ideal drug delivery system demands high efficacy and no adverse effects.

摘要

目的：本研究旨在评估口服一种含有吴茱萸碱 - 磷脂纳米复合物（NEEPN）的新型油包水纳米乳剂时其改善的吸收情况及体内动力学特征。 方法：通过将吴茱萸碱 - 磷脂纳米复合物载入油包水纳米乳剂系统来制备NEEPN。采用原位灌注法研究NEEPN的胃肠道吸收情况。还评估了NEEPN中吴茱萸碱（EDA）的体内动力学特征变化。 结果：与EDA或含有EDA而非吴茱萸碱 - 磷脂复合物的传统纳米乳剂相比，具有良好体内动力学特征的NEEPN显著增强了EDA的胃肠道吸收及口服生物利用度；例如，NEEPN相对于游离EDA的相对生物利用度经计算为630.35%，且NEEPN在结肠的有效渗透率是EDA的8.64倍。 结论：NEEPN显著提高了EDA的口服生物利用度，这可能归因于其胃肠道吸收增加。NEEPN还提高了EDA口服给药的疗效并减少了不良反应。这一发现作为理想的药物递送系统要求高效且无不良反应，具有重大的临床意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/44aaf6e0c04b/ijn-9-4411Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/cf668e83cfce/ijn-9-4411Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/f4d639202c04/ijn-9-4411Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/cbf2bfa2cc3f/ijn-9-4411Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/0d1707b5137a/ijn-9-4411Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/4e73f1eaadb3/ijn-9-4411Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/44aaf6e0c04b/ijn-9-4411Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/cf668e83cfce/ijn-9-4411Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/f4d639202c04/ijn-9-4411Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/cbf2bfa2cc3f/ijn-9-4411Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/0d1707b5137a/ijn-9-4411Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/4e73f1eaadb3/ijn-9-4411Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3b3/4172252/44aaf6e0c04b/ijn-9-4411Fig6.jpg

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Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine-phospholipid nanocomplex.

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引用本文的文献

[1]
Evodiamine: A Extremely Potential Drug Development Candidate of Alkaloids from .

Int J Nanomedicine. 2024

[2]
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Pharmaceutics. 2023-1-3

[3]
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[4]
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[5]
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[6]
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Molecules. 2016-10-19

本文引用的文献

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Ex vivo and in situ approaches used to study intestinal absorption.

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[2]
A superparamagnetic Fe3O4-loaded polymeric nanocarrier for targeted delivery of evodiamine with enhanced antitumor efficacy.

Colloids Surf B Biointerfaces. 2013-5-16

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Development of water-in-oil microemulsions with the potential of prolonged release for oral delivery of L-glutathione.

Pharm Dev Technol. 2013-6-6

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Topoisomerase I inhibitor evodiamine acts as an antibacterial agent against drug-resistant Klebsiella pneumoniae.

Planta Med. 2012-11-16

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Effect of novel synthetic evodiamine analogue on sexual behavior in male rats.

J Chem Biol. 2012-1

[10]
Influence of the nanocomposite MgAl-HTlc on gastric absorption of drugs: in vitro and ex vivo studies.

Pharm Res. 2012-8-23

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