Theranostics 2020; 10(10):4308-4322. doi:10.7150/thno.41322 This issue Cite

Research Paper

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

Shuangming Kang1*, Wenjuan Duan2*, Shangqian Zhang2, Dawei Chen1✉, Jianfang Feng3✉, Na Qi2✉

1. Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 110016, China
2. Department of Pharmacy, Guilin Medical University, Guilin, 541004, China
3. Department of Pharmacy ,Guangxi University of Chinese Medicine, Nanning, 530299, China
*These authors contributed equally to this work.

Citation:
Kang S, Duan W, Zhang S, Chen D, Feng J, Qi N. Muscone/RI7217 co-modified upward messenger DTX liposomes enhanced permeability of blood-brain barrier and targeting glioma. Theranostics 2020; 10(10):4308-4322. doi:10.7150/thno.41322. https://www.thno.org/v10p4308.htm
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Abstract

Graphic 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.

Keywords: glioma, blood-brain barrier, muscone, RI7217, liposome


Citation styles

APA
Kang, S., Duan, W., Zhang, S., Chen, D., Feng, J., Qi, N. (2020). Muscone/RI7217 co-modified upward messenger DTX liposomes enhanced permeability of blood-brain barrier and targeting glioma. Theranostics, 10(10), 4308-4322. https://doi.org/10.7150/thno.41322.

ACS
Kang, S.; Duan, W.; Zhang, S.; Chen, D.; Feng, J.; Qi, N. Muscone/RI7217 co-modified upward messenger DTX liposomes enhanced permeability of blood-brain barrier and targeting glioma. Theranostics 2020, 10 (10), 4308-4322. DOI: 10.7150/thno.41322.

NLM
Kang S, Duan W, Zhang S, Chen D, Feng J, Qi N. Muscone/RI7217 co-modified upward messenger DTX liposomes enhanced permeability of blood-brain barrier and targeting glioma. Theranostics 2020; 10(10):4308-4322. doi:10.7150/thno.41322. https://www.thno.org/v10p4308.htm

CSE
Kang S, Duan W, Zhang S, Chen D, Feng J, Qi N. 2020. Muscone/RI7217 co-modified upward messenger DTX liposomes enhanced permeability of blood-brain barrier and targeting glioma. Theranostics. 10(10):4308-4322.

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