Detail publikace

Apoferritin/Vandetanib Association Is Long-Term Stable But Does Not Improve Pharmacological Properties of Vandetanib

JÁKLOVÁ, K. FEGLAROVÁ, T. REX, S. HEGER, Z. ECKSCHLAGER, T. HRABĚTA, J. HODEK, P. KOLÁRIK, M. INDRA, R.

Originální název

Apoferritin/Vandetanib Association Is Long-Term Stable But Does Not Improve Pharmacological Properties of Vandetanib

Typ

článek v časopise ve Web of Science, Jimp

Jazyk

angličtina

Originální abstrakt

A tyrosine kinase inhibitor, vandetanib (Van), is an anticancer drug affecting the signaling of VEGFR, EGFR and RET protooncogenes. Van is primarily used for the treatment of advanced or metastatic medullary thyroid cancer; however, its usage is significantly limited by side effects, particularly cardiotoxicity. One approach to minimize them is the encapsulation or binding of Van in- or onto a suitable carrier, allowing targeted delivery to tumor tissue. Herein, we constructed a nanocarrier based on apoferritin associated with Van (ApoVan). Based on the characteristics obtained by analyzing the average size, the surface zeta-potential and the polydispersive index, ApoVan nanoparticles exhibit long-term stability and maintain their morphology. Experiments have shown that ApoVan complex is relatively stable during storage. It was found that Van is gradually released from its ApoVan form into the neutral environment (pH 7.4) as well as into the acidic environment (pH 6.5). The effect of free Van and ApoVan on neuroblastoma and medullary thyroid carcinoma cell lines revealed that both forms were toxic in both used cell lines, and minimal differences between ApoVan and Van were observed. Thus, we assume that Van might not be encapsulated into the cavity of apoferritin, but instead only binds to its surface.

Klíčová slova

vandetanib; apoferritin; neuroblastoma; medullary thyroid cancer; cancer targeting

Autoři

JÁKLOVÁ, K.; FEGLAROVÁ, T.; REX, S.; HEGER, Z.; ECKSCHLAGER, T.; HRABĚTA, J.; HODEK, P.; KOLÁRIK, M.; INDRA, R.

Vydáno

30. 4. 2021

Nakladatel

MDPI

ISSN

1422-0067

Periodikum

International Journal of Molecular Sciences

Ročník

22

Číslo

8

Stát

Švýcarská konfederace

Strany od

1

Strany do

12

Strany počet

12

URL

Plný text v Digitální knihovně

BibTex

@article{BUT171626,
  author="Kateřina {Jáklová} and Tereza {Feglarová} and Simona {Rex} and Zbyněk {Heger} and Tomáš {Eckschlager} and Jan {Hraběta} and Petr {Hodek} and Matúš {Kolárik} and Radek {Indra}",
  title="Apoferritin/Vandetanib Association Is Long-Term Stable But Does Not Improve Pharmacological Properties of Vandetanib",
  journal="International Journal of Molecular Sciences",
  year="2021",
  volume="22",
  number="8",
  pages="1--12",
  doi="10.3390/ijms22084250",
  issn="1422-0067",
  url="https://www.mdpi.com/1422-0067/22/8/4250"
}