Soybean lecithin stabilizes disulfiram nanosuspensions with a high drug-loading content: remarkably improved antitumor efficacy
Open accessAbstract
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 IC 50 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.
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The drug-loading content of nanoformulation-based delivery systems is unsatisfactory (almost <20%), requiring substantial amounts of nanomaterials.
“The drug-loading content of nanoformulation-based delivery systems is unsatisfactory (almost < 20%), requiring substantial amounts of nanomaterials.”
From Off-label and repurposed use of disulfiram beyond alcohol dependence: A systematic review of clinical and preclinical evidence (2026) · cites this paper as [136]
The Background says that the disulfiram delivery systems discussed have unsatisfactory drug loading, “almost < 10%,” and consequently require a large amount of nanomaterials. The citing sentence broadens this to nanoformulation-based delivery systems generally and changes the reported threshold to “almost < 20%.” (LLM, conf=0.88)
Experimental — accuracy not yet measuredNanoformulations enhance drug stability, protect against rapid in vivo degradation, and promote greater tumor accumulation.
“Nanoformulations, predominantly developed for repurposing DIS in cancer treatment, but also in infectious and inflammatory diseases, enhance drug stability, protect against rapid in vivo degradation, and promote greater tumor accumulation136”
From Off-label and repurposed use of disulfiram beyond alcohol dependence: A systematic review of clinical and preclinical evidence (2026) · cites this paper as [136]
The Background (page unavailable) explicitly says that disulfiram nanoparticles improve stability, protect against rapid in vivo degradation, and increase tumor accumulation. The paper discusses their use in cancer treatment, but does not support the citing sentence’s additional reference to infectious and inflammatory diseases. (LLM, conf=0.85)
Experimental — accuracy not yet measuredExcessive use of such nanomaterials as pharmaceutical excipients contravenes regulatory bodies' safety guidelines and risks severe side effects.
“Excessive use of such nanomaterials, as pharmaceutical excipients, contravenes regulatory bodies' safety guidelines and risks severe side effects.136”
From Off-label and repurposed use of disulfiram beyond alcohol dependence: A systematic review of clinical and preclinical evidence (2026) · cites this paper as [136]
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- Authors
- Li, H., Liu, B., Ao, H., Fu, J., Wang, Y., Feng, Y., Guo, Y., & Wang, X.
- Affiliations
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- Harbin University of Commerce (CN)
- Corresponding author
- Guo, Yifei
- Wang, Xiangtao
- Venue
- Journal of Nanobiotechnology
- Published
- 2020-01-06
- Volume
- 18
- Issue
- 1
- Pages
- 4-4
- ISSN
- 1477-3155 (ISSN-L)
- PMC
- PMC6943900
- OpenAlex
- W3004447098
- Cited by
- 28
- References
- 52
- Citations by year
- 2026: 5 · 2025: 4 · 2024: 3 · 2023: 4 · 2022: 3 · 2021: 5 · 2020: 4
- FWCI
- 1.04
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Locations
- Journal of Nanobiotechnology (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- National Natural Science Foundation of China (U1401223)
- CAMS Innovation Fund for Medical Sciences (2016-I2M-1-012)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- disulfiram, soy lecithin, nanoparticle suspensions, drug repurposing, antitumor efficacy, breast cancer chemotherapy, drug loading, sustained drug release, cytotoxicity, tissue distribution, oral drug delivery, paclitaxel comparison, 4T1 cells
- MeSH terms
- Animals, Antineoplastic Agents, Calorimetry, Differential Scanning, Disulfiram, Drug Stability, Female, Mice, Inbred BALB C, Particle Size, Glycine max, Suspensions, Tissue Distribution, X-Ray Diffraction, Treatment Outcome, Cell Line, Tumor, Nanoparticles, Lecithins, Static Electricity, Drug Liberation
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