An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy
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...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2022-12-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2022.2147601 |
| _version_ | 1828178057363456000 |
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| author | Huating Zeng Xiaoqi Li Yuping Liu Xia Li Ding Qu Yan Chen |
| author_facet | Huating Zeng Xiaoqi Li Yuping Liu Xia Li Ding Qu Yan Chen |
| author_sort | Huating Zeng |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-12T05:08:38Z |
| format | Article |
| id | doaj.art-bf991adb1f6942bfa1f4dc59d21529de |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-12T05:08:38Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-bf991adb1f6942bfa1f4dc59d21529de2022-12-22T03:46:49ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642022-12-012913454346610.1080/10717544.2022.2147601An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacyHuating Zeng0Xiaoqi Li1Yuping Liu2Xia Li3Ding Qu4Yan Chen5Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, ChinaAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, ChinaAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, ChinaAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, ChinaAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, ChinaAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, ChinaCombinational 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.https://www.tandfonline.com/doi/10.1080/10717544.2022.2147601Icaritincoix seed oil-based microemulsionhepatocellular carcinomasynergistic effectautophagy |
| spellingShingle | Huating Zeng Xiaoqi Li Yuping Liu Xia Li Ding Qu Yan Chen An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy Drug Delivery Icaritin coix seed oil-based microemulsion hepatocellular carcinoma synergistic effect autophagy |
| title | An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy |
| title_full | An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy |
| title_fullStr | An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy |
| title_full_unstemmed | An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy |
| title_short | An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy |
| title_sort | icaritin loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy |
| topic | Icaritin coix seed oil-based microemulsion hepatocellular carcinoma synergistic effect autophagy |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2022.2147601 |
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