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. 2023 Nov 13;28(22):7565.
doi: 10.3390/molecules28227565.

HA-Coated PLGA Nanoparticles Loaded with Apigenin for Colon Cancer with High Expression of CD44

Bo Yang  1 , Yongqing Mao  2 , Yanjun Zhang  1 , Yue Hao  2   3 , Meitong Guo  1   2 , Bian Li  1   2 , Haisheng Peng  2
Affiliations

HA-Coated PLGA Nanoparticles Loaded with Apigenin for Colon Cancer with High Expression of CD44

Bo Yang et al. Molecules. .

Abstract

Apigenin (API) possesses excellent antitumor properties but its limited water solubility and low bioavailability restrict its therapeutic impact. Thus, a suitable delivery system is needed to overcome these limitations and improve the therapeutic efficiency. Poly (lactic-co-glycolic acid) (PLGA) is a copolymer extensively utilized in drug delivery. Hyaluronic acid (HA) is a major extracellular matrix component and can specifically bind to CD44 on colon cancer cells. Herein, we aimed to prepare receptor-selective HA-coated PLGA nanoparticles (HA-PLGA-API-NPs) for colon cancers with high expression of CD44; chitosan (CS) was introduced into the system as an intermediate, simultaneously binding HA and PLGA through electrostatic interaction to facilitate a tighter connection between them. API was encapsulated in PLGA to obtain PLGA-API-NPs, which were then sequentially coated with CS and HA to form HA-PLGA-API-NPs. HA-PLGA-API-NPs had a stronger sustained-release capability. The cellular uptake of HA-PLGA-API-NPs was enhanced in HT-29 cells with high expression of CD44. In vivo, HA-PLGA-API-NPs showed enhanced targeting specificity towards the HT-29 ectopic tumor model in nude mice in comparison with PLGA-API-NPs. Overall, HA-PLGA-API-NPs were an effective drug delivery platform for API in the treatment of colon cancers with high expression of CD44.

Keywords: API; CD44; HA; PLGA nanoparticles; colon cancer; targeted delivery.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The size distributions (A,B) and zeta potentials (C) of PLGA-API-NPs, CS-PLGA-API-NPs, and HA-PLGA-API-NPs. The data are presented as means ± SD, n = 3.
Figure 2
Figure 2
The release of API from API, PLGA-API-NPs, and HA-PLGA-API-NPs in release media (pH 7.4 phosphate buffer containing 20% ethanol). The data are presented as means ± SD (n = 3).
Figure 3
Figure 3
Cell uptake. (A) Uptake of PLGA-DiO-NPs and HA-PLGA-DiO-NPs by HT-29 and HRT-18 cells. (B) Fluorescence pictures of HA-PLGA-DiO-NP uptake by HT-29 and HRT-18 cells. (C) Uptake of HA-PLGA-DiO-NPs by HT-29 and HRT-18 cells with and without HA treatment. All data are presented as means ± SD (n = 3), ** p < 0.01.
Figure 4
Figure 4
Cells and cytotoxicity (n = 6). (A) Cytotoxicity assay using HT-29 and HRT-18 cells treated with blank nanoparticles. (B) Cytotoxicity assay using HT-29 and HRT-18 cells treated with HA-PLGA-API-NPs. (C) Cytotoxicity of free API and different modified nanoparticles towards HT-29 cells. The data are presented as means ± SD, n = 3, * p < 0.05, ** p < 0.01.
Figure 5
Figure 5
CD44-mediated tumor targeting delivery of HA-PLGA-DiR-NPs. (A) In vivo fluorescent small animal imaging of two model rats injected with PLGA-DiR-NPs or HA-PLGA-DiR-NPs. (B) Visceral fluorescence images of two model rats after injection of PLGA-DiR-NPs or HA-PLGA-DiR-NPs. The data are presented as means ± SD (n = 3).
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References

    1. Salehi B., Venditti A., Sharifi-Rad M., Kręgiel D., Sharifi-Rad J., Durazzo A., Lucarini M., Santini A., Souto E.B., Novellino E., et al. The Therapeutic Potential of Apigenin. Int. J. Mol. Sci. 2019;20:1305. doi: 10.3390/ijms20061305. - DOI - PMC - PubMed
    1. Majma Sanaye P., Mojaveri M.R., Ahmadian R., Sabet Jahromi M., Bahramsoltani R. Apigenin and its dermatological applications: A comprehensive review. Phytochemistry. 2022;203:113390. doi: 10.1016/j.phytochem.2022.113390. - DOI - PubMed
    1. Imran M., Aslam Gondal T., Atif M., Shahbaz M., Batool Qaisarani T., Hanif Mughal M., Salehi B., Martorell M., Sharifi-Rad J. Apigenin as an anticancer agent. Phytother. Res. 2020;34:1812–1828. doi: 10.1002/ptr.6647. - DOI - PubMed
    1. Singh D., Gupta M., Sarwat M., Siddique H.R. Apigenin in cancer prevention and therapy: A systematic review and meta-analysis of animal models. Crit. Rev. Oncol. Hematol. 2022;176:103751. doi: 10.1016/j.critrevonc.2022.103751. - DOI - PubMed
    1. Yoon J.H., Kim M.Y., Cho J.Y. Apigenin: A Therapeutic Agent for Treatment of Skin Inflammatory Diseases and Cancer. Int. J. Mol. Sci. 2023;24:1498. doi: 10.3390/ijms24021498. - DOI - PMC - PubMed

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