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开发一种口服生物利用度的甘草素自微乳给药系统，有效治疗卵清蛋白诱导的哮喘。

Development of an Orally Bioavailable Isoliquiritigenin Self-Nanoemulsifying Drug Delivery System to Effectively Treat Ovalbumin-Induced Asthma.

机构信息

Academy of Chinese Medical Sciences, Henan University of Chinese Medicine, Zhengzhou 450058, People's Republic of China.

College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450058, People's Republic of China.

出版信息

Int J Nanomedicine. 2020 Nov 13;15:8945-8961. doi: 10.2147/IJN.S269982. eCollection 2020.

DOI:10.2147/IJN.S269982
PMID:33223829
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7671486/
Abstract

PURPOSE

Isoliquiritigenin (ILQ), an important component of Anti-Asthma Herbal Medicine Intervention (ASHMI), had shown potent anti-asthma effect in vitro in our previous study. However, poor solubility and low bioavailability hindered in vivo application to treat asthma. This study was to develop a novel ILQ loaded self-nanoemulsifying drug delivery system (ILQ-SMEDDS) with enhanced bioavailability.

METHODS

The optimized SMEDDS formulation was composed of ethyl oleate (oil phase), Tween 80 (surfactant) and PEG400 (co-surfactant) at a mass ratio of 3:6:1. The physiochemical properties of ILQ-SMEDDS, including drug content, globule size, zeta potential, scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, were characterized. And the in vitro release profile, in situ intestinal absorption, in vivo pharmacokinetic parameters and the anti-asthma effect of ILQ suspension and ILQ-SMEDDS were evaluated.

RESULTS

The ILQ-SMEDDS had an average globule size of 20.63 ± 1.95 nm with a polydispersity index (PDI) of 0.11 ± 0.03, and its zeta potential was -12.64 ± 2.12 mV. The cumulative release rate of ILQ from ILQ-SMEDDS to the simulated gastrointestinal tract was significantly higher than that of free ILQ suspension. And area under curve with ILQ-SMEDDS was found to be 3.95 times higher than that of ILQ suspension indicating improved bioavailability by SMEDDS. Although ILQ-SMEDDS showed a slight less effective inhibitory effect on eotaxin-1 in human lung fibroblast (HFL-1) cells than free ILQ, in an ovalbumin-induced asthma model, ILQ-SMEDDS exhibited more efficacy than ILQ suspension in improving asthma-associated inflammation, including eosinophil production, ovalbumin-specific immunoglobulin E (OVA-sIgE), interleukin 4 (IL 4), interleukin 5 (IL 5) and interferon-γ (IFN-γ). Even the low dose of ILQ-SMEDDS group (10 mg/kg) showed better anti-asthma effect than that of the ILQ suspension group (20 mg/kg).

CONCLUSION

Compared with ILQ suspension, ILQ-SMEDDS showed significantly improved bioavailability and anti-asthma effect, revealing its potential as a favorable pharmaceutical agent for treating asthma.

摘要

目的

异甘草素（ILQ）是一种重要的抗哮喘中药干预（ASHMI）的成分，在我们之前的研究中已显示出体外抗哮喘的强大作用。然而，较差的溶解度和低生物利用度阻碍了其用于治疗哮喘的体内应用。本研究旨在开发一种新的载有异甘草素的自微乳给药系统（ILQ-SMEDDS），以提高生物利用度。

方法

优化的 SMEDDS 配方由油酸乙酯（油相）、吐温 80（表面活性剂）和聚乙二醇 400（助表面活性剂）以质量比 3:6:1 组成。对 ILQ-SMEDDS 的理化性质，包括药物含量、粒径、Zeta 电位、扫描电子显微镜（SEM）、傅里叶变换红外（FTIR）光谱进行了表征。并评价了 ILQ 混悬液和 ILQ-SMEDDS 的体外释放曲线、原位肠吸收、体内药代动力学参数和抗哮喘作用。

结果

ILQ-SMEDDS 的平均粒径为 20.63 ± 1.95nm，多分散指数（PDI）为 0.11 ± 0.03，Zeta 电位为-12.64 ± 2.12mV。ILQ-SMEDDS 从模拟胃肠道向 ILQ 的累积释放率明显高于游离 ILQ 混悬液。ILQ-SMEDDS 的曲线下面积（AUC）是 ILQ 混悬液的 3.95 倍，表明 SMEDDS 提高了生物利用度。尽管 ILQ-SMEDDS 对人肺成纤维细胞（HFL-1）细胞中的嗜酸性粒细胞趋化因子-1的抑制作用略低于游离 ILQ，但在卵清蛋白诱导的哮喘模型中，ILQ-SMEDDS 改善哮喘相关炎症的效果优于 ILQ 混悬液，包括嗜酸性粒细胞产生、卵清蛋白特异性免疫球蛋白 E（OVA-sIgE）、白细胞介素 4（IL-4）、白细胞介素 5（IL-5）和干扰素-γ（IFN-γ）。即使 ILQ-SMEDDS 的低剂量（10mg/kg）组也比 ILQ 混悬液（20mg/kg）组表现出更好的抗哮喘作用。

结论

与 ILQ 混悬液相比，ILQ-SMEDDS 显示出明显改善的生物利用度和抗哮喘作用，显示出其作为治疗哮喘的有利药物制剂的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/1e472eeb16eb/IJN-15-8945-g0009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/83c6496d37b9/IJN-15-8945-g0001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/e2df0a42eabe/IJN-15-8945-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/815f02a2bffe/IJN-15-8945-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/53b9142b0851/IJN-15-8945-g0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/1e472eeb16eb/IJN-15-8945-g0009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/83c6496d37b9/IJN-15-8945-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/52cf9cba6aca/IJN-15-8945-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/4683efe8bb1b/IJN-15-8945-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/e0ed5d39c5eb/IJN-15-8945-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/6b34985336de/IJN-15-8945-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/e2df0a42eabe/IJN-15-8945-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/815f02a2bffe/IJN-15-8945-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/53b9142b0851/IJN-15-8945-g0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15c1/7671486/1e472eeb16eb/IJN-15-8945-g0009.jpg

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