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

IF 6.5 2区医学 Q1 PHARMACOLOGY & PHARMACY Drug Delivery Pub Date : 2022-12-01 DOI:10.1080/10717544.2022.2147601

Huating Zeng, Xiaoqi Li, Yuping Liu, Xia Li, Ding Qu, Yan Chen

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引用次数: 3

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.

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一种以薏苡仁油为基础的含有淫羊藿素的微乳，用于改善药代动力学和增强抗肿瘤疗效。

淫羊藿素(IC)和薏苡仁油(CSO)联合治疗肝细胞癌具有广阔的应用前景。然而，传统的鸡尾酒疗法由于药代动力学的不同步，难以优化其协同抗肿瘤效果。因此，我们开发了薏苡仁油(IC-MEs)微乳，以改善药代动力学和增强抗肿瘤效果。采用Box-Behnken设计优化了IC-MEs的制备工艺，并对其药物性能进行了详细表征。与单药治疗相比，IC-MEs对HepG2细胞具有协同抗增殖作用。其机制与通过增强caspase -3活性诱导更强的细胞凋亡有关。由于薏苡仁油微乳的包封性，IC- mes显著提高了IC的生物利用度，并获得了理想的肝脏蓄积和消除。更重要的是，IC-MEs在HepG2异种移植小鼠的所有治疗中表现出压倒性的抗肿瘤能力。本研究验证了薏苡仁油基微乳提高水不溶性成分抗肿瘤效果的可行性。

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来源期刊

Drug Delivery 医学-药学

CiteScore

11.80

自引率

5.00%

发文量

250

审稿时长

3.3 months

期刊介绍： Drug Delivery is an open access journal serving the academic and industrial communities with peer reviewed coverage of basic research, development, and application principles of drug delivery and targeting at molecular, cellular, and higher levels. Topics covered include all delivery systems including oral, pulmonary, nasal, parenteral and transdermal, and modes of entry such as controlled release systems; microcapsules, liposomes, vesicles, and macromolecular conjugates; antibody targeting; protein/peptide delivery; DNA, oligonucleotide and siRNA delivery. Papers on drug dosage forms and their optimization will not be considered unless they directly relate to the original drug delivery issues. Published articles present original research and critical reviews.

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