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

被引：6
|
作者：
Dias, Amanda de Fraga [1 ]
Dallemole, Danieli Rosane [2 ]
Bruinsmann, Franciele Aline [2 ]
Lopes Silva, Luiz Fernando [1 ]
Cruz-Lopez, Olga [3 ,4 ]
Conejo-Garcia, Ana [3 ,4 ]
Oliveira Battastini, Ana Maria [1 ]
Maria Campos, Joaquin [3 ,4 ]
Guterres, Silvia Staniscuaski [2 ]
Pohlmann, Adriana Raffin [2 ]
Figueiro, Fabricio [1 ,5 ]
机构：
[1] Univ Fed Rio Grande do Sul, Inst Ciencias Basicas Saude, Programa Posgrad Ciencias Biol Bioquim, Porto Alegre, RS, Brazil
[2] Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, Porto Alegre, RS, Brazil
[3] Fac Farm, Dept Quim Farmaceut & Organ, C Campus Cartuja S-N, Granada, Spain
[4] Inst Invest Biosanitaria Granada Ibs GRANADA, Granada, Spain
[5] Univ Fed Rio Grande do Sul, Inst Ciencias Basicas Saude, Dept Bioquim, Porto Alegre, RS, Brazil
来源：
NANOMEDICINE | 2021年 / 16卷 / 23期
关键词：
bozepinib; drug delivery; glioblastoma; intranasal; lipid-core nanocapsules; temozolomide; LIPID-CORE NANOCAPSULES; DRUG-DELIVERY; POLYMERIC NANOPARTICLES; INTRANASAL DELIVERY; EXPERIMENTAL-DESIGN; GROWTH-INHIBITION; IN-VITRO; CHITOSAN; COMBINATION; GLIOMA;
D O I：
10.2217/nnm-2021-0164
中图分类号：
Q81 [生物工程学（生物技术）]; Q93 [微生物学];
学科分类号：
071005 ; 0836 ; 090102 ; 100705 ;
摘要：
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.
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页码：2095 / 2115
页数：21
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