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Article

The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation

by
Yingzheng Wang
†,
Xunhua Huang
†,
Hanzhi Chen
,
Qianyuan Wu
,
Qianqian Zhao
,
Dezhuang Fu
,
Qinghua Liu
* and
Yinghao Wang
*
College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2023, 28(18), 6532; https://doi.org/10.3390/molecules28186532
Submission received: 17 August 2023 / Revised: 2 September 2023 / Accepted: 7 September 2023 / Published: 9 September 2023
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Abstract

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.
Keywords: iRGD peptide-modified liposome; curcumin; piperine; synergistic antitumour activity; lung cancer background iRGD peptide-modified liposome; curcumin; piperine; synergistic antitumour activity; lung cancer background
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MDPI and ACS Style

Wang, Y.; Huang, X.; Chen, H.; Wu, Q.; Zhao, Q.; Fu, D.; Liu, Q.; Wang, Y. The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation. Molecules 2023, 28, 6532. https://doi.org/10.3390/molecules28186532

AMA Style

Wang Y, Huang X, Chen H, Wu Q, Zhao Q, Fu D, Liu Q, Wang Y. The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation. Molecules. 2023; 28(18):6532. https://doi.org/10.3390/molecules28186532

Chicago/Turabian Style

Wang, Yingzheng, Xunhua Huang, Hanzhi Chen, Qianyuan Wu, Qianqian Zhao, Dezhuang Fu, Qinghua Liu, and Yinghao Wang. 2023. "The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation" Molecules 28, no. 18: 6532. https://doi.org/10.3390/molecules28186532

APA Style

Wang, Y., Huang, X., Chen, H., Wu, Q., Zhao, Q., Fu, D., Liu, Q., & Wang, Y. (2023). The Antitumour Activity of a Curcumin and Piperine Loaded iRGD-Modified Liposome: In Vitro and In Vivo Evaluation. Molecules, 28(18), 6532. https://doi.org/10.3390/molecules28186532

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