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Open AccessArticle

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

1
Laboratory of Nanostructures, Institute of High Pressure Physics, Polish Academy of Sciences, Sokolowska 29/37, 01-142 Warsaw, Poland
2
Medicinal and Aromatic Plants Research Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), P.C. 12622 Dokki, Giza, Egypt
3
Biomedical Engineering Laboratory, Faculty of Chemical and Process Engineering, Warsaw University of Technology, 00-645 Warsaw, Poland
4
Department of Pharmaceutical Technology, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), P.C. 12622 Dokki Giza, Egypt
5
Faculty of Materials Engineering, Warsaw University of Technology, Wołoska 41, 02-507 Warsaw, Poland
6
Biochemistry Department, Faculty of Agriculture, Cairo University, P.C. 12613 Giza, Egypt
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(1), 70; https://doi.org/10.3390/pharmaceutics12010070
Received: 30 November 2019 / Revised: 31 December 2019 / Accepted: 8 January 2020 / Published: 16 January 2020
(This article belongs to the Special Issue Emergent Strategies for Natural Products Delivery)
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. View Full-Text
Keywords: 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 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
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AbouAitah, K.; Stefanek, A.; Higazy, I.M.; Janczewska, M.; Swiderska-Sroda, A.; Chodara, A.; Wojnarowicz, J.; Szałaj, U.; Shahein, S.A.; Aboul-Enein, A.M.; Abou-Elella, F.; Gierlotka, S.; Ciach, T.; Lojkowski, W. Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles. Pharmaceutics 2020, 12, 70.

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