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Cited by 91Nanoparticle-Based Drug DeliveryBarrier Structure and Function StudiesDrug Transport and Resistance Mechanisms

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Muscone/RI7217 co-modified upward messenger DTX liposomes enhanced permeability of blood-brain barrier and targeting glioma

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Kang, Shuangming, Duan, Wenjuan, Zhang, Shangqian, Chen, Dawei, Feng, Jianfang, Qi, Na·2020·Theranostics
DOI 10.7150/thno.41322PMC PMC7150489
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Abstract

Rationale: The dual-targeted drug delivery system was designed for enhancing permeation of the blood-brain barrier (BBB) and providing an anti-glioma effect.As transferrin receptor (TfR) is over-expressed by the brain capillary endothelial (hCMEC/D3) and glioma cells, a mouse monoclonal antibody, RI7217, with high affinity and selectivity for TfR, was used to study the brain targeted drug delivery system.Muscone, an ingredient of traditional Chinese medicine (TCM) musk, was used as the "guide" drug to probe the permeability of the BBB for drug delivery into the cerebrospinal fluid.This study investigated the combined effects of TCM aromatic resuscitation and modern receptor-targeted technology by the use of muscone/RI7217 co-modified docetaxel (DTX) liposomes for enhanced drug delivery to the brain for anti-glioma effect.Methods: Cellular drug uptake from the formulations was determined using fluorescence microscopy and flow cytometry.The drug penetrating ability into tumor spheroids were visualized using confocal laser scanning microscopy (CLSM).In vivo glioma-targeting ability of formulations was evaluated using whole-body fluorescent imaging system.The survival curve study was performed to evaluate the anti-glioma effect of the formulations. Results:The results showed that muscone and RI7217 co-modified DTX liposomes enhanced uptake into both hCMEC/D3 and U87-MG cells, increased penetration to the deep region of U87-MG tumor spheroids, improved brain targeting in vivo and prolonged survival time of nude mice bearing tumor.Conclusion: Muscone and RI7217 co-modified DTX liposomes were found to show improved brain targeting and enhanced the efficacy of anti-glioma drug treatment in vivo.

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Metadata

Authors
Kang, S., Duan, W., Zhang, S., Chen, D., Feng, J., & Qi, N.
Affiliations
  • Shenyang Pharmaceutical University (CN)
  • Guilin Medical University (CN)
  • Guangxi University of Chinese Medicine (CN)
Corresponding author
  • Kang, Shuangming
  • Duan, Wenjuan
ORCID
Venue
Theranostics
Publisher
Ivyspring International Publisher
Published
2020
Volume
10
Issue
10
Pages
4308-4322
ISSN
1838-7640 (ISSN-L)
DOI
10.7150/thno.41322
PMC
PMC7150489
OpenAlex
W3012571258
Cited by
91
References
3
Citations by year
2026: 10 · 2025: 22 · 2024: 17 · 2023: 14 · 2022: 16 · 2021: 9 · 2020: 3
FWCI
2.73
Type
journal article
Language
en
Open access
Licence
cc-by
Locations
  • Theranostics (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
Funders
  • National Natural Science Foundation of China (81860707, 81560655)
  • Natural Science Foundation of Guangxi Province (2017GXNSFAA198061)
  • Guilin Medical University
Topics
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
  • Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Keywords
muscone, transferrin receptor, blood-brain barrier permeability, brain drug delivery, hCMEC/D3 endothelial cells, tumor spheroids, traditional Chinese medicine
MeSH terms
Docetaxel, Animals, Blood-Brain Barrier, Brain Neoplasms, Cell Survival, Cycloparaffins, Drug Therapy, Combination, Glioma, Liposomes, Medicine, Chinese Traditional, Mice, Nude, Permeability, Receptors, Transferrin, Antigens, CD, Case-Control Studies, Drug Delivery Systems, Cell Line, Tumor, Tubulin Modulators, Mice

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