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A repurposing Dapagliflozin via polymeric nanogels for colorectal cancer therapy
Samaa Abdullah1,2, Samar Thiab3, Abeer A Altamimi4
1Faculty of Pharmacy, Applied Science Private University, Amman, 11937, Jordan. abdullahtsamaa@gmail.com.
Abstract:
Dapagliflozin (DAPA), a selective SGLT2 inhibitor approved for type 2 diabetes, shows emerging potential for repurposing in oncology due to its anti-inflammatory and antiproliferative properties. However, its poor solubility and rapid systemic clearance limit its therapeutic utility in cancer treatment. Here, we report the development of an oral novel gravity-induced nano hydrogel mass system encapsulating DAPA using sodium alginate (SA) and polyvinyl alcohol (PVA) nanoparticles (DAPA-PVA-SA-NPs). The formulation exhibited enhanced solubility (1.8-fold increase), high encapsulation efficiency (88.37%), and sustained release in simulated gastrointestinal conditions. In vitro studies demonstrated improved cytotoxicity against HCT-116 colorectal cancer cells and significant downregulation of oncogenic and inflammatory markers (KRAS, IL-6, TGF-β, TNF-α). In vivo pharmacokinetic evaluation in rats showed delayed Tmax, extended half-life, and a 7% increase in AUC, indicating prolonged systemic exposure with modest AUC improvement. This delivery platform improves oral exposure in rats, shows in vitro activity in HCT-116 cells and supporting further exploratory evaluation for repurposing DAPA in colorectal cancer, pending confirmation in additional models.
Insights
A novel nano hydrogel system enhances dapagliflozin (DAPA) solubility and delivery for potential colorectal cancer treatment. This formulation shows improved cancer cell killing and reduced inflammatory markers in vitro.
Area of Science:
- Pharmaceutical Sciences
- Oncology
- Biomaterials
Background:
- Dapagliflozin (DAPA), an SGLT2 inhibitor for type 2 diabetes, has potential anticancer properties.
- Poor solubility and rapid clearance limit DAPA's efficacy in cancer therapy.
Purpose of the Study:
- To develop a novel nano hydrogel system for improved oral delivery of DAPA.
- To evaluate the anti-cancer efficacy and pharmacokinetic profile of the DAPA-loaded nano hydrogel.
Main Methods:
- Encapsulation of DAPA into sodium alginate and polyvinyl alcohol nanoparticles (DAPA-PVA-SA-NPs).
- In vitro assessment of solubility, encapsulation efficiency, drug release, and cytotoxicity against HCT-116 cells.
- In vivo pharmacokinetic studies in rats.
Main Results:
- The DAPA-PVA-SA-NPs formulation showed a 1.8-fold increase in solubility and 88.37% encapsulation efficiency.
- Sustained drug release was observed in simulated gastrointestinal conditions.
- In vitro studies demonstrated enhanced cytotoxicity against colorectal cancer cells and downregulation of oncogenic/inflammatory markers (KRAS, IL-6, TGF-β, TNF-α).
- In vivo studies indicated delayed Tmax, extended half-life, and a modest increase in AUC, suggesting prolonged systemic exposure.
Conclusions:
- The developed nano hydrogel system effectively improves DAPA's solubility and oral bioavailability.
- The formulation exhibits promising in vitro anti-cancer activity, supporting further investigation for colorectal cancer treatment.
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