Development of bozepinib-loaded nanocapsules for nose-to-brain delivery: preclinical evaluation in glioblastoma-Reference-Cited by-同舟云学术

Development of bozepinib-loaded nanocapsules for nose-to-brain delivery: preclinical evaluation in glioblastoma

Published:2021-10 Issue:23 Volume:16 Page:2095-2115
ISSN:1743-5889
Container-title:Nanomedicine
language:en
Short-container-title:Nanomedicine

Author:

Fraga Dias Amanda de¹^ORCID,Dallemole Danieli Rosane²^ORCID,Bruinsmann Franciele Aline²^ORCID,Lopes Silva Luiz Fernando¹^ORCID,Cruz-López Olga³⁴^ORCID,Conejo-García Ana³⁴^ORCID,Oliveira Battastini Ana Maria¹^ORCID,Campos Joaquín María³⁴^ORCID,Guterres Silvia Stanisçuaski²^ORCID,Pohlmann Adriana Raffin²^ORCID,Figueiró Fabrício¹⁵^ORCID

Affiliation:

1. Programa de Pós-Graduação em Ciências Biológicas: Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil

2. Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil

3. Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, c/Campus de Cartuja s/n, Granada, Spain

4. Instituto de Investigación Biosanitaria de Granada (ibs.GRANADA), Granada, Spain

5. Departamento de Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil

Abstract

Aim: To develop and characterize bozepinib-loaded lipid-core nanocapsules (BZP-LNC+) as a potential treatment for glioblastoma (GBM). Methods: Characterization of nanocapsules was performed by diameter, polydispersity index, Zeta potential, pH and encapsulation efficiency. GBM cell viability, cell cycle and Annexin/PI were evaluated after BZP-LNC+ treatment. Synergism between BZP-LNC+ and temozolomide (TMZ) was performed by CompuSyn software and confirmed in vitro and in vivo. Results: BZP-LNC+ showed adequate particle sizes, positive Zeta potential, narrow size distribution and high encapsulation efficiency. BZP-LNC+ reduces GBM growth by inducing apoptosis. BZP-LNC+ and TMZ showed synergistic effect in vitro and reduced the in vivo glioma growth by approximately 81%. Conclusion: The present study provides proof-of-principle insights for the combination of these drugs for GBM treatment.

Funder

Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul

Conselho Nacional de Desenvolvimento Científico e Tecnológico

Publisher

Future Medicine Ltd

Subject

Development,General Materials Science,Biomedical Engineering,Medicine (miscellaneous),Bioengineering

Link

https://www.futuremedicine.com/doi/pdf/10.2217/nnm-2021-0164

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