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Progress and perspectives on targeting nanoparticles for brain drug delivery

Acta Pharmaceutica Sinica B 2016年第4期6卷 268-286页

作者： Huile Gao Key Laboratory of Drug Targeting and Drug Delivery Systems West China School of Pharmacy Sichuan University

Due to the ability of the blood–brain barrier(BBB) to prevent the entry of drugs into the brain, it is a challenge to treat central nervous system disorders pharmacologically. The development of nanotechnology provides potential to overcome this problem. In this review, the barriers to brain-targeted drug delivery are reviewed, including the BBB, blood–brain tumor barrier(BBTB), and nose-to-brain barrier. Delivery strategies are focused on overcoming the BBB, directly targeting diseased cells in the brain, and dual-targeted delivery. The major concerns and perspectives on constructing brain-targeted delivery systems are discussed.

关键词： brain targeting Nanoparticles Dual targeting Intranasal delivery blood–brain barrier

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Menthol-modified casein nanoparticles loading 10-hydroxycamptothecin for glioma targeting therapy

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Acta Pharmaceutica Sinica B 2019年第4期9卷 843-857页

作者： Caifang Gao Jianming Liang Ying Zhu Chengli Ling Zhekang Cheng Ruixiang Li Jing Qin Weigen Lu Jianxin Wang Department of Pharmaceutics School of PharmacyFudan University&Key Laboratory of Smart Drug DeliveryMinistry of EducationShanghai 201203China Shanghai Institute of Pharmaceutical Industry China State Institute of Pharmaceutical IndustryShanghai 201203China Guangzhou University of Chinese Medicine Guangzhou 510006China School of Pharmacy Chengdu University of Traditional Chinese MedicineChengdu 611137China School of Pharmacy Minzu University of ChinaBeijing 100081China

Chemotherapy outcomes for the treatment of glioma remains unsatisfactory due to the inefficient drug transport across the blood–brain barrier(BBB) and insufficient drug accumulation in the tumor region. Although many approaches, including various nanosystems, have been developed to promote the distribution of chemotherapeutics in the brain tumor, the delivery efficiency and the possible damage to the normal brain function still greatly restrict the clinical application of the ***, it is urgent and necessary to discover more safe and effective BBB penetration and gliomatargeting strategies. In the present study, menthol, one of the strongest BBB penetration enhancers screened from traditional Chinese medicine, was conjugated to casein, a natural food protein with brain targeting capability. Then the conjugate self-assembled into the nanoparticles to load anti-cancer *** nanoparticles were characterized to have appropriate size, spheroid shape and high loading drug capacity. Tumor spheroid penetration experiments demonstrated that penetration ability of mentholmodified casein nanoparticles(M-CA-NP) into the tumor were much deeper than that of unmodified nanoparticles. In vivo imaging further verified that M-CA-NPs exhibited higher brain tumor distribution than unmodified nanoparticles. The median survival time of glioma-bearing mice treated with HCPT-MCA-NPs was significantly prolonged than those treated with free HCPT or HCPT-CA-NPs. HE staining ofthe organs indicated the safety of the nanoparticles. Therefore, the study combined the advantages of traditional Chinese medicine strategy with modern delivery technology for brain targeting, and provide a safe and effective approach for glioma therapy.

关键词： Glioma Casein Menthol Nanoparticles brain targeting blood–brain barrier 10-Hydroxycamptothecin

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维普期刊数据库

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