期刊
INTERNATIONAL JOURNAL OF NANOMEDICINE
卷 14, 期 -, 页码 7447-7460出版社
DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S208267
关键词
RADA16-I; hydrophobic drug; delivery system; antitumor
资金
- National Natural Science Foundation of China [31460246]
- 2011 Collaborative Innovation Center of Guizhou Traditional Chinese Medicine and Ethnic Medicine [Qianjiaokeyanfa (2012) 311]
- Education Department of Guizhou Province of China [GNYL (2017) 006, YLXKJS-YS-05]
- Guizhou Provincial and Municipal Science and Technology Cooperation Special Fund Project [Shengshikehe (2015) 53]
Objective: This study aimed to investigate the interaction between the ion-complementary self-assembling peptide RADA16-I and the hydrophobic drug mangiferin (MA), and the potential of the self-assembling peptide to be exploited as a drug carrier of MA. Methods: The RADA16-I-MA suspension was prepared by magnetic stirring, followed by fluorescence spectrophotometry, particle size determination, rheological properties analysis, and in vitro release assay to characterize the interaction between RADA16-I and MA. Then, the effects of in situ MA-loaded hydrogel on the proliferation of KYSE 30 and DLD-1 tumor cells and the toxic effect of the hydrogel on 293T renal epithelial cells were studied by the Cell Counting Kit 8 method. Results: The RADA16-I-MA suspension was formed in water under magnetic stifling; the in situ hydrogel was formed when the suspension was added to PBS. The particle size in the RADA16-I-MA suspension was around 300-600 nm with an average size of 492 nm. Within 24 h, the cumulative release of MA from the RADA16-I-MA hydrogel was about 80%. The release rate of MA from the hydrogel was dependent on the concentration of RADA16-I and the release can be fitted with a first-order kinetic equation. The results suggested that the self-assembling peptide can stabilize MA in water to form a relatively stable suspension; the results also indicated that controlled release of MA from the RADA16-I-MA in situ hydrogel formed from the RADA16-I-MA suspension can be achieved by adjusting the concentration of the peptide in suspension. The cell viability studies showed that the RADA16-I-MA in situ hydrogel not only can maintain or enhance the intrinsic proliferation inhibition effects of MA on tumor cells, but also can reduce the toxicity of MA to normal cells. Conclusion: The self-assembling peptide RADA16-I can be a potential candidate for constructing a delivery system of the hydrophobic drug MA.
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