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Nose-to-brain delivery of temozolomide-loaded PLGA nanoparticles functionalized with anti-EPHA3 for glioblastoma targeting

delete2018-09-03
delete97
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OA
AI
L
Liuxiang Chu
王爱萍 (Aiping Wang)
倪玲 cover
倪玲 (Ling Ni)
X
Xiuju Yan
Y
Yina Song
M
Mingyu Zhao
K
Kaoxiang Sun *
H
Hongjie Mu
S
Sha Liu
Z
Zimei Wu
C
Chunyan Zhang
DOI:10.1080/10717544.2018.1494226delete
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Abstract

Abstract

En 中文
Glioblastoma is the most common malignant brain tumor. Efficient delivery of drugs targeting glioblastomas remains a challenge. Ephrin type-A receptor 3 (EPHA3) tyrosine kinase antibody-modified polylactide-co-glycolide (PLGA) nanoparticles (NPs) were developed to target glioblastoma via nose-to-brain delivery. Anti-EPHA3-modified, TBE-loaded NPs were prepared using an emulsion-solvent evaporation method, showed a sustained in vitro release profile up to 48 h and a mean particle size of 145.9 +/- 8.7 nm. The cellular uptake of anti-EPHA3-modified NPs by C6 cells was significantly enhanced compared to that of nontargeting NPs (p < .01). In vivo imaging and distribution studies on the glioma-bearing rats showed that anti-EPHA3-modified NPs exhibited high fluorescence intensity in the brain and effectively accumulated to glioma tissues, indicating the targeting effect of anti-EPHA3. Glioma-bearing rats treated with anti-EPHA3-modified NPs resulted in significantly higher tumor cell apoptosis (p < .01) than that observed with other formulations and prolonged the median survival time of glioma-bearing rats to 26 days, which was 1.37-fold longer than that of PLGA NPs. The above results indicated that anti-EPHA3-modified NPs may potentially serve as a nose-to-brain drug carrier for the treatment of glioblastoma.
Keywords:
Glioblastoma
EPHA3 antibody
temozolomide butyl ester
nose-to-brain delivery
nanoparticles
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Drug Delivery cover
Drug Delivery
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8.1
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Yantai University
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shandong university
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