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Nanocrystal-loaded liposome for targeted delivery of poorly water-soluble antitumor drugs with high drug loading and stability towards efficient cancer therapy

文献类型：期刊论文

作者Liang, Huamin1,2; Zou, Fengming1,2; Liu, Qingwang1,2; Wang, Beilei1,2; Fu, Liyi1,2; Liang, Xiaofei1,2; Liu, Jing1,2,3; Liu, Qingsong1,2,3,4,5
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
出版日期2021-04-15
卷号599
ISSN号0378-5173
关键词Liposome Drug nanocrystal Core-shell Drug delivery Tumor therapy BCR-ABL
DOI10.1016/j.ijpharm.2021.120418
通讯作者Liu, Jing(jingliu@hmfl.ac.cn) ; Liu, Qingsong(qsliu97@hmfl.ac.cn)
英文摘要Nanocrystals (NCs) enable the delivery of poorly water-soluble drugs with improved dissolution and bioavailability. However, their uncontrolled release and instability make targeted delivery challenging. Herein, a nanoin-nano delivery system composed of a drug nanocrystal core and liposome shell (NC@Lipo) is presented, which merges the advantages of drug nanocrystals (high drug loading) and liposomes (easy surface functionalization and high stability) for targeted delivery of hydrophobic drugs to tumors. CHMFL-ABL-053 (053), a hydrophobic drug candidate discovered by our group, was employed as a model drug to demonstrate the performance of NC@Lipo delivery system. Surface PEGylated (053-NC@PEG-Lipo) and folic acid-functionalized (053-NC@FA-Lipo) formulations were fabricated by wet ball milling combined with probe sonication. 053-NC@Lipo enabled high drug loading (up to 19.51%), considerably better colloidal stability, and longer circulation in vivo than 053-NC. Compared with free 053, 053-NC@PEG-Lipo and 053-NC@FA-Lipo exhibited higher tumor accumulation and considerably better in vivo antitumor efficacy in K562 xenograft mice with tumor growth inhibition rate (TGI) of up to 98%. Additionally, more effective tumor cell targeting in vitro and higher TGI in vivo were achieved with 053-NC@FA-Lipo. The NC@Lipo strategy may contribute to the targeted delivery of poorly water-soluble drugs with high drug loading, high stability, and tailorable surface, and has potential for the development of more efficient nanocrystal- and liposome-based formulations for commercial and clinical applications. It may also provide new opportunities for potential clinical application of candidate 053.
资助项目National Natural Science Foundation of China[81872745] ; National Natural Science Foundation of China[81402797] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA09030301] ; Natural Science Foundation of Anhui Province[1808085MH268] ; Natural Science Foundation of Anhui Province[1808085QH260] ; National Major Science & Technology Project Key New Drug Creation and Manufacturing Program of China[2018ZX09711002] ; Frontier Science Key Research Program of CAS[QYZDB-SSW-SLH037] ; Collaborative Innovation Program of Hefei Science Center, CAS[2020HSC-CIP009] ; CASHIPS Director's Fund[BJPY2019A03] ; Leading Talent Program of Hefei[2018-1-006] ; Youth Innovation Promotion Association of CAS[2016385] ; High Magnetic Field Laboratory of Anhui Province
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者ELSEVIER
WOS记录号WOS:000637276400021
资助机构National Natural Science Foundation of China ; Strategic Priority Research Program of the Chinese Academy of Sciences ; Natural Science Foundation of Anhui Province ; National Major Science & Technology Project Key New Drug Creation and Manufacturing Program of China ; Frontier Science Key Research Program of CAS ; Collaborative Innovation Program of Hefei Science Center, CAS ; CASHIPS Director's Fund ; Leading Talent Program of Hefei ; Youth Innovation Promotion Association of CAS ; High Magnetic Field Laboratory of Anhui Province
源URL[http://ir.hfcas.ac.cn:8080/handle/334002/121747]  
专题中国科学院合肥物质科学研究院
通讯作者Liu, Jing; Liu, Qingsong
作者单位1.Chinese Acad Sci, Anhui Prov Key Lab Med Phys & Technol, Inst Hlth & Med Technol, Hefei Inst Phys Sci, Hefei 230031, Peoples R China
2.Chinese Acad Sci, Hefei Canc Hosp, Hefei 230031, Peoples R China
3.Precis Med Res Lab Anhui Prov, Hefei 230088, Peoples R China
4.Anhui Univ, Inst Phys Sci, Hefei 230601, Peoples R China
5.Anhui Univ, Inst Informat Technol, Hefei 230601, Peoples R China
推荐引用方式
GB/T 7714		 Liang, Huamin,Zou, Fengming,Liu, Qingwang,et al. Nanocrystal-loaded liposome for targeted delivery of poorly water-soluble antitumor drugs with high drug loading and stability towards efficient cancer therapy[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2021,599.
APA Liang, Huamin.,Zou, Fengming.,Liu, Qingwang.,Wang, Beilei.,Fu, Liyi.,...&Liu, Qingsong.(2021).Nanocrystal-loaded liposome for targeted delivery of poorly water-soluble antitumor drugs with high drug loading and stability towards efficient cancer therapy.INTERNATIONAL JOURNAL OF PHARMACEUTICS,599.
MLA Liang, Huamin,et al."Nanocrystal-loaded liposome for targeted delivery of poorly water-soluble antitumor drugs with high drug loading and stability towards efficient cancer therapy".INTERNATIONAL JOURNAL OF PHARMACEUTICS 599(2021).

入库方式： OAI收割

来源：合肥物质科学研究院

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