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基于薏苡仁油的虎杖苷载药微乳，改善药代动力学和增强抗肿瘤疗效。

An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy.

机构信息

Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, China.

Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China.

出版信息

Drug Deliv. 2022 Dec;29(1):3454-3466. doi: 10.1080/10717544.2022.2147601.

DOI:10.1080/10717544.2022.2147601
PMID:36447364
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9848417/
Abstract

Combinational icaritin (IC) and coix seed oil (CSO) holds promising potential in the treatment of hepatocellular carcinoma. However, traditional cocktail therapy is facing difficulties to optimize the synergistic antitumor efficacy due to the asynchronous pharmacokinetics. Therefore, we developed an icaritin-loaded microemulsion based on coix seed oil (IC-MEs) for improved pharmacokinetics and enhanced antitumor efficacy. The preparation technology of IC-MEs was optimized by the Box-Behnken design and the pharmaceutical properties were characterized in detail. IC-MEs show synergistic antiproliferation against HepG2 cells compared with monotherapy. The mechanism is associated with stronger apoptosis induction via enhancing caspases-3 activity. IC-MEs significantly improve the bioavailability of IC due to the encapsulation of coix oil-based microemulsion and also obtain the desired liver accumulation and elimination. More importantly, IC-MEs exhibit the overwhelming antitumor ability among all of the treatments on the HepG2 xenograft-bearing mice. This study verifies the feasibility of using coix oil-based microemulsion to improve the antitumor effect of water-insoluble components.

摘要

联合使用淫羊藿苷（IC）和薏苡仁油（CSO）在治疗肝细胞癌方面具有很大的潜力。然而，由于药代动力学不同步，传统鸡尾酒疗法在优化协同抗肿瘤疗效方面面临困难。因此，我们开发了一种基于薏苡仁油的淫羊藿苷载药微乳（IC-MEs），以提高药代动力学和增强抗肿瘤疗效。采用 Box-Behnken 设计优化了 IC-MEs 的制备工艺，并对其药物特性进行了详细表征。与单药治疗相比，IC-MEs 对 HepG2 细胞具有协同的增殖抑制作用。其机制与通过增强半胱天冬酶-3 活性诱导更强的细胞凋亡有关。IC-MEs 通过包封薏苡仁油基微乳显著提高了 IC 的生物利用度，同时也获得了所需的肝脏积累和消除。更重要的是，IC-MEs 在 HepG2 荷瘤小鼠的所有治疗中表现出压倒性的抗肿瘤能力。本研究验证了使用薏苡仁油基微乳来提高水不溶性成分抗肿瘤效果的可行性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/7a668eadaf7b/IDRD_A_2147601_F0011_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/d481c7ee807e/IDRD_A_2147601_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/4ca6218663b7/IDRD_A_2147601_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/c3e472a70098/IDRD_A_2147601_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/19ebfa00c6db/IDRD_A_2147601_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/9e39d0ad6567/IDRD_A_2147601_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/84178c087b49/IDRD_A_2147601_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/837e749546c0/IDRD_A_2147601_F0008_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/4c9a54e21a51/IDRD_A_2147601_F0009_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/44efac9cd2c9/IDRD_A_2147601_F0010_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/7a668eadaf7b/IDRD_A_2147601_F0011_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/d481c7ee807e/IDRD_A_2147601_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/4ca6218663b7/IDRD_A_2147601_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/c3e472a70098/IDRD_A_2147601_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/19ebfa00c6db/IDRD_A_2147601_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/9e39d0ad6567/IDRD_A_2147601_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/84178c087b49/IDRD_A_2147601_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/837e749546c0/IDRD_A_2147601_F0008_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/4c9a54e21a51/IDRD_A_2147601_F0009_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/44efac9cd2c9/IDRD_A_2147601_F0010_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e1b/9848417/7a668eadaf7b/IDRD_A_2147601_F0011_C.jpg

相似文献

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[2]
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引用本文的文献

[1]
Natural anti-cancer products: insights from herbal medicine.

Chin Med. 2025-6-9

[2]
Nano- and Microemulsions in Biomedicine: From Theory to Practice.

Pharmaceutics. 2023-7-20

本文引用的文献

[1]
Efficacy of Applying Kanglaite Injection under Incentive Nursing Intervention in Treating Patients with Advanced Penile Carcinoma and Its Effect on Treatment Compliance.

Evid Based Complement Alternat Med. 2021-10-25

[2]
HM-3-HSA exhibits potent anti-angiogenesis and antitumor activity in hepatocellular carcinoma.

Eur J Pharm Sci. 2021-12-1

[3]
[Development of preparation process of icaritin-coix seed oil microemulsion based on quality by design concept].

Zhongguo Zhong Yao Za Zhi. 2020-8

[4]
Fabrication of Fine Puerarin Nanocrystals by Box-Behnken Design to Enhance Intestinal Absorption.

AAPS PharmSciTech. 2020-2-13

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Phytomedicine. 2019-12-19

[6]
The clinical efficacy and safety of kanglaite adjuvant therapy in the treatment of advanced hepatocellular carcinoma: A PRISMA-compliant meta-analysis.

Biosci Rep. 2019-11-29

[7]
Transferrin-Functionalized Microemulsions Coloaded with Coix Seed Oil and Tripterine Deeply Penetrate To Improve Cervical Cancer Therapy.

Mol Pharm. 2019-10-30

[8]
First-in-class immune-modulating small molecule Icaritin in advanced hepatocellular carcinoma: preliminary results of safety, durable survival and immune biomarkers.

BMC Cancer. 2019-3-28

[9]
Box-Behnken design to optimize the synthesis of new crosslinked chitosan-glyoxal/TiO nanocomposite: Methyl orange adsorption and mechanism studies.

Int J Biol Macromol. 2019-2-5

[10]
A Tf-modified tripterine-loaded coix seed oil microemulsion enhances anti-cervical cancer treatment.

Int J Nanomedicine. 2018-11-8

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