Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy
Abstract Disulfiram (DSF) has been considered as “Repurposing drug” in cancer therapy in recent years based on its good antitumor efficacy. DSF is traditionally used as an oral drug in the treatment of alcoholism. To overcome its rapid degradation and instability, DSF nanosuspensions (DSF/SPC-NSps)...
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doaj-0ace7f3a1cae443d8058601af4c33fe82021-01-10T12:10:42ZengBMCJournal of Nanobiotechnology1477-31552020-01-0118111110.1186/s12951-019-0565-0Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacyHaowen Li0Biao Liu1Hui Ao2Jingxin Fu3Yian Wang4Yue Feng5Yifei Guo6Xiangtao Wang7Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical CollegeHarbin University of Commerce China, Research Center ON Life Sciences and Environmental SciencesInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical CollegeInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical CollegeInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical CollegeGuangdong Jiabo Pharmaceutical CO., LTDInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical CollegeInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical CollegeAbstract Disulfiram (DSF) has been considered as “Repurposing drug” in cancer therapy in recent years based on its good antitumor efficacy. DSF is traditionally used as an oral drug in the treatment of alcoholism. To overcome its rapid degradation and instability, DSF nanosuspensions (DSF/SPC-NSps) were prepared using soybean lecithin (SPC) as a stabilizer of high drug-loaded content (44.36 ± 1.09%). Comprehensive characterization of the nanosuspensions was performed, and cell cytotoxicity, in vivo antitumor efficacy and biodistribution were studied. DSF/SPC-NSps, having a spherical appearance with particle size of 155 nm, could remain very stable in different physiological media, and sustained release. The in vitro MTT assay indicated that the cytotoxicity of DSF/SPC-NSps was enhanced remarkably compared to free DSF against the 4T1 cell line. The IC50 value decreased by 11-fold (1.23 vs. 13.93 μg/mL, p < 0.01). DSF/SPC-NSps groups administered via intravenous injections exhibited better antitumor efficacy compared to the commercial paclitaxel injection (PTX injection) and had a dose-dependent effect in vivo. Notably, DSF/SPC-NSps exhibited similar antitumor activity following oral administration as PTX administration via injection into a vein. These results suggest that the prepared nanosuspensions can be used as a stable delivery vehicle for disulfiram, which has potential application in breast cancer chemotherapy.https://doi.org/10.1186/s12951-019-0565-0DisulfiramSoybean lecithin (SPC)Nanosuspensions4T1 cellsBreast cancer |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Haowen Li Biao Liu Hui Ao Jingxin Fu Yian Wang Yue Feng Yifei Guo Xiangtao Wang |
spellingShingle |
Haowen Li Biao Liu Hui Ao Jingxin Fu Yian Wang Yue Feng Yifei Guo Xiangtao Wang Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy Journal of Nanobiotechnology Disulfiram Soybean lecithin (SPC) Nanosuspensions 4T1 cells Breast cancer |
author_facet |
Haowen Li Biao Liu Hui Ao Jingxin Fu Yian Wang Yue Feng Yifei Guo Xiangtao Wang |
author_sort |
Haowen Li |
title |
Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy |
title_short |
Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy |
title_full |
Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy |
title_fullStr |
Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy |
title_full_unstemmed |
Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy |
title_sort |
soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy |
publisher |
BMC |
series |
Journal of Nanobiotechnology |
issn |
1477-3155 |
publishDate |
2020-01-01 |
description |
Abstract Disulfiram (DSF) has been considered as “Repurposing drug” in cancer therapy in recent years based on its good antitumor efficacy. DSF is traditionally used as an oral drug in the treatment of alcoholism. To overcome its rapid degradation and instability, DSF nanosuspensions (DSF/SPC-NSps) were prepared using soybean lecithin (SPC) as a stabilizer of high drug-loaded content (44.36 ± 1.09%). Comprehensive characterization of the nanosuspensions was performed, and cell cytotoxicity, in vivo antitumor efficacy and biodistribution were studied. DSF/SPC-NSps, having a spherical appearance with particle size of 155 nm, could remain very stable in different physiological media, and sustained release. The in vitro MTT assay indicated that the cytotoxicity of DSF/SPC-NSps was enhanced remarkably compared to free DSF against the 4T1 cell line. The IC50 value decreased by 11-fold (1.23 vs. 13.93 μg/mL, p < 0.01). DSF/SPC-NSps groups administered via intravenous injections exhibited better antitumor efficacy compared to the commercial paclitaxel injection (PTX injection) and had a dose-dependent effect in vivo. Notably, DSF/SPC-NSps exhibited similar antitumor activity following oral administration as PTX administration via injection into a vein. These results suggest that the prepared nanosuspensions can be used as a stable delivery vehicle for disulfiram, which has potential application in breast cancer chemotherapy. |
topic |
Disulfiram Soybean lecithin (SPC) Nanosuspensions 4T1 cells Breast cancer |
url |
https://doi.org/10.1186/s12951-019-0565-0 |
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