期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 512, 期 1, 页码 292-300出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2016.08.049
关键词
Doxorubicin; alpha-Tocopherol succinate (TS); alpha-Tocopherol polyethylene glycol-1000 succinate (TPGS); Solid lipid nanoparticles (SLN); Spheroids; Cancer
资金
- Minas Gerais State Agency for Research and Development (FAPEMIG, Brazil)
- CAPES
- CNPq
This work aimed to develop solid lipid nanoparticles (SLN) co-loaded with doxorubicin and a-tocopherol succinate (TS) and to evaluate its potential to overcome drug resistance and to increase antitumoral effect in MCF-7/Adr and NCI/Adr cancer cell lines. The SLN were prepared by a hot homogenization method and characterized for size, zeta potential, entrapment efficiency (EE), and drug loading (DL). The cytotoxicity of SLN or penetration was evaluated in MCF-7/Adr and NCI/adr as a monolayer or spheroid cancer cell model. The SLN showed a size in the range of 74-80 nm, negative zeta potential, EE of 99%, and DL of 67 mg/g. The SLN co-loaded with Dox and TS showed a stronger cytotoxicity against MCF-7/Adr and NCI/Adr cells. In the monolayer model, the doxorubicin co-localization as a free and encapsulated form was higher for the encapsulated drug in MCF-7/Adr and NCI/adr, suggesting a bypassing of P-glycoprotein bomb efflux. For cancer cell spheroids, the SLN co-loaded with doxorubicin and TS showed a prominent cytotoxicity and a greater penetration of doxorubicin. (C) 2016 Elsevier B.V. All rights reserved.
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