Effective targeting of colon cancer cells with piperine natural anticancer prodrug using functionalized clusters of hydroxyapatite nanoparticles
Authors:
- Khaled AbouAitah,
- Agata Stefanek,
- Iman M. Higazy,
- Magdalena Janczewska,
- Anna Świderska-Środa,
- Agnieszka Chodara,
- Jacek Wojnarowicz,
- Urszula Szałaj,
- Samar A. Shahein,
- Ahmed M. Aboul-Enein,
- Faten Abou-Elella,
- Stanisław Gierlotka,
- Tomasz Ciach,
- Witold Łojkowski
Abstract
Targeted drug delivery offers great opportunities for treating cancer. Here, we developed a novel anticancer targeted delivery system for piperine (Pip), an alkaloid prodrug derived from black pepper that exhibits anticancer effects. The tailored delivery system comprises aggregated hydroxyapatite nanoparticles (HAPs) functionalized with phosphonate groups (HAP-Ps). Pip was loaded into HAPs and HAP-Ps at pH 7.2 and 9.3 to obtain nanoformulations. The nanoformulations were characterized using several techniques and the release kinetics and anticancer effects investigated in vitro. The Pip loading capacity was >20%. Prolonged release was observed with kinetics dependent on pH, surface modification, and coating. The nanoformulations fully inhibited monolayer HCT116 colon cancer cells compared to Caco2 colon cancer and MCF7 breast cancer cells after 72 h, whereas free Pip had a weaker effect. The nanoformulations inhibited ~60% in HCT116 spheroids compared to free Pip. The Pip-loaded nanoparticles were also coated with gum Arabic and functionalized with folic acid as a targeting ligand. These functionalized nanoformulations had the lowest cytotoxicity towards normal WI-38 fibroblast cells. These preliminary findings suggest that the targeted delivery system comprising HAP aggregates loaded with Pip, coated with gum Arabic, and functionalized with folic acid are a potentially efficient agent against colon cancer.
- Record ID
- WUT68cc279dc2c04fcbb22d1baf3d1623a3
- Author
- Journal series
- Pharmaceutics, ISSN 1999-4923
- Issue year
- 2020
- Vol
- 12
- No
- 1
- Pages
- 1-28
- Article number
- 70
- Keywords in English
- hydroxyapatite nanocarrier, piperine alkaloid prodrug, natural products, delivery system for cancer targeting, nanoformulations, colon cancer cells and spheroids, in vitro release kinetics, pH-sustained release effect, folic acid
- ASJC Classification
- DOI
- DOI:10.3390/pharmaceutics12010070 Opening in a new tab
- URL
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7022489/ Opening in a new tab
- Language
- (en) English
- License
- File
-
- File: 1
- Effective targeting of colon cancer cells with piperine natural anticancer prodrug using functionalized clusters of hydroxyapatite nanoparticles, File AbouAitah, K. (i in.) - Effective targeting of...pdf / 9 MB
- AbouAitah, K. (i in.) - Effective targeting of...pdf
- publication date: 11-03-2020
- Effective targeting of colon cancer cells with piperine natural anticancer prodrug using functionalized clusters of hydroxyapatite nanoparticles, File AbouAitah, K. (i in.) - Effective targeting of...pdf / 9 MB
-
- Score (nominal)
- 100
- Score source
- journalList
- Score
- = 100.0, 11-05-2022, ArticleFromJournal
- Publication indicators
- = 10; = 13; = 4; : 2016 = 1.097; : 2018 (2 years) = 4.773
- Citation count
- 18
- Additional fields
- Funding: We would like to thank the National Research Centre (NRC, Egypt) for supporting this work. We also wish to thank the National Center for Research and Development, Poland (STRATEGMED3/306888/3/ NCBR/2017, project iTE, Poland). This research was carried out using equipment funded by the CePT project (reference no. POIG.02.02.00-14-024/08), financed by the European Regional Development Fund within the Operational Programme “Innovative Economy” for 2007–2013.
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- Uniform Resource Identifier
- https://repo.pw.edu.pl/info/article/WUT68cc279dc2c04fcbb22d1baf3d1623a3/
- URN
urn:pw-repo:WUT68cc279dc2c04fcbb22d1baf3d1623a3
* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or PerishOpening in a new tab system.