The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation
Lung cancer is one of the most common cancers around the world, with a high mortality rate. Despite substantial advancements in diagnoses and therapies, the outlook and survival of patients with lung cancer remains dismal due to drug tolerance and malignant reactions. New interventional treatments u...
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MDPI AG
2023-09-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/18/6532 |
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| author | Yingzheng Wang Xunhua Huang Hanzhi Chen Qianyuan Wu Qianqian Zhao Dezhuang Fu Qinghua Liu Yinghao Wang |
| author_facet | Yingzheng Wang Xunhua Huang Hanzhi Chen Qianyuan Wu Qianqian Zhao Dezhuang Fu Qinghua Liu Yinghao Wang |
| author_sort | Yingzheng Wang |
| collection | DOAJ |
| description | Lung cancer is one of the most common cancers around the world, with a high mortality rate. Despite substantial advancements in diagnoses and therapies, the outlook and survival of patients with lung cancer remains dismal due to drug tolerance and malignant reactions. New interventional treatments urgently need to be explored if natural compounds are to be used to reduce toxicity and adverse effects to meet the needs of lung cancer clinical treatment. An internalizing arginine-glycine-aspartic acid (iRGD) modified by a tumour-piercing peptide liposome (iRGD-LP-CUR-PIP) was developed via co-delivery of curcumin (CUR) and piperine (PIP). Its antitumour efficacy was evaluated and validated via in vivo and in vitro experiments. iRGD-LP-CUR-PIP enhanced tumour targeting and cellular internalisation effectively. In vitro, iRGD-LP-CUR-PIP exhibited enhanced cellular uptake, suppression of tumour cell multiplication and invasion and energy-independent cellular uptake. In vivo, iRGD-LP-CUR-PIP showed high antitumour efficacy, mainly in terms of significant tumour volume reduction and increased weight and spleen index. Data showed that iRGD peptide has active tumour targeting and it significantly improves the penetration and cellular internalisation of tumours in the liposomal system. The use of CUR in combination with PIP can exert synergistic antitumour activity. This study provides a targeted therapeutic system based on natural components to improve antitumour efficacy in lung cancer. |
| first_indexed | 2024-03-10T22:25:24Z |
| format | Article |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T22:25:24Z |
| publishDate | 2023-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-b4fae78ece2848188534859a6858f6032023-11-19T12:08:44ZengMDPI AGMolecules1420-30492023-09-012818653210.3390/molecules28186532The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo EvaluationYingzheng Wang0Xunhua Huang1Hanzhi Chen2Qianyuan Wu3Qianqian Zhao4Dezhuang Fu5Qinghua Liu6Yinghao Wang7College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaCollege of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, ChinaLung cancer is one of the most common cancers around the world, with a high mortality rate. Despite substantial advancements in diagnoses and therapies, the outlook and survival of patients with lung cancer remains dismal due to drug tolerance and malignant reactions. New interventional treatments urgently need to be explored if natural compounds are to be used to reduce toxicity and adverse effects to meet the needs of lung cancer clinical treatment. An internalizing arginine-glycine-aspartic acid (iRGD) modified by a tumour-piercing peptide liposome (iRGD-LP-CUR-PIP) was developed via co-delivery of curcumin (CUR) and piperine (PIP). Its antitumour efficacy was evaluated and validated via in vivo and in vitro experiments. iRGD-LP-CUR-PIP enhanced tumour targeting and cellular internalisation effectively. In vitro, iRGD-LP-CUR-PIP exhibited enhanced cellular uptake, suppression of tumour cell multiplication and invasion and energy-independent cellular uptake. In vivo, iRGD-LP-CUR-PIP showed high antitumour efficacy, mainly in terms of significant tumour volume reduction and increased weight and spleen index. Data showed that iRGD peptide has active tumour targeting and it significantly improves the penetration and cellular internalisation of tumours in the liposomal system. The use of CUR in combination with PIP can exert synergistic antitumour activity. This study provides a targeted therapeutic system based on natural components to improve antitumour efficacy in lung cancer.https://www.mdpi.com/1420-3049/28/18/6532iRGD peptide-modified liposomecurcuminpiperinesynergistic antitumour activitylung cancer background |
| spellingShingle | Yingzheng Wang Xunhua Huang Hanzhi Chen Qianyuan Wu Qianqian Zhao Dezhuang Fu Qinghua Liu Yinghao Wang The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation Molecules iRGD peptide-modified liposome curcumin piperine synergistic antitumour activity lung cancer background |
| title | The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation |
| title_full | The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation |
| title_fullStr | The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation |
| title_full_unstemmed | The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation |
| title_short | The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation |
| title_sort | antitumour activity of a curcumin and piperine loaded irgd modified liposome in vitro and in vivo evaluation |
| topic | iRGD peptide-modified liposome curcumin piperine synergistic antitumour activity lung cancer background |
| url | https://www.mdpi.com/1420-3049/28/18/6532 |
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