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Sodium Alginate Nanogels Encapsulating Cholecalciferol (Vitamin D3): A Topical Therapeutic Approach Targeting LOX
Hadil Faris Alotaibi1, Mustafa A Al-Qadhi2
1Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint Abdulrahman University, Riyadh 11671, Saudi Arabia.
Abstract:
The study explores sodium alginate nanogels encapsulating cholecalciferol (vitamin D3) as a novel topical therapeutic for skin cancer, targeting LOX IMVI (melanoma) and A431 (epidermoid carcinoma) cell lines. Nanogels were prepared using magnetic stirring and sonication, resulting in a uniform dispersion and enhanced stability. Physicochemical characterization revealed a particle size of 67.6 ± 13.43 nm, a polydispersity index (PDI) of 0.30 ± 0.02, and a ζ-potential of -25.00 ± 2.00 mV, confirming good colloidal stability and suitability for topical application. In vitro drug release studies demonstrated a sustained-release profile, with 89.73 ± 2.1% cholecalciferol released over 34 h, as predicted by a first-order kinetic model (R 2 = 0.9871). Cytotoxicity assays showed significant anticancer activity, with IC50 values of 29.51 ± 1.56 and 24.95 ± 1.32 μM for LOX IMVI and A431 cell lines, respectively, while exhibiting reduced cytotoxicity against normal HSF cells (IC50 = 83.88 ± 4.43 μM). Cell-cycle analysis indicated G1/S phase arrest, and Annexin V-FITC/PI staining confirmed apoptosis induction with minimal necrosis. Molecular docking studies validated the mechanism of action, revealing strong binding of cholecalciferol to the vitamin D receptor (VDR) through hydrogen bonding with SER278 and SER275, π-cation interaction with TRP286, and hydrophobic interactions, with a docking score of -11.7 kcal/mol. These findings suggest sodium alginate nanogels encapsulating cholecalciferol as a promising, biocompatible therapeutic for the topical treatment of skin cancer, paving the way for future clinical investigations.
Insights
Sodium alginate nanogels loaded with vitamin D3 show potent topical anticancer activity against melanoma and epidermoid carcinoma cell lines. This novel formulation demonstrates sustained release and induces apoptosis, offering a promising skin cancer therapy.
Area of Science:
- Nanotechnology
- Dermatology
- Oncology
Background:
- Skin cancer presents a significant global health challenge.
- Novel therapeutic strategies are needed for effective topical treatment.
- Vitamin D3 (cholecalciferol) has shown potential anticancer properties.
Purpose of the Study:
- To develop and evaluate sodium alginate nanogels encapsulating cholecalciferol for topical skin cancer therapy.
- To assess the physicochemical properties, drug release kinetics, and in vitro anticancer efficacy of the nanogels.
- To elucidate the mechanism of action of cholecalciferol-loaded nanogels.
Main Methods:
- Sodium alginate nanogels encapsulating cholecalciferol were prepared using magnetic stirring and sonication.
- Nanogel characterization included particle size, polydispersity index (PDI), and ζ-potential measurements.
- In vitro drug release, cytotoxicity assays (IC50), cell-cycle analysis, apoptosis assays, and molecular docking studies were performed.
Main Results:
- Nanogels exhibited optimal physicochemical properties (67.6 nm size, 0.30 PDI, -25 mV ζ-potential) for topical application.
- Sustained release of cholecalciferol (89.73% over 34 h) followed first-order kinetics (R²=0.9871).
- Significant cytotoxicity against LOX IMVI and A431 cells (IC50: 29.51 and 24.95 μM) with reduced toxicity to normal cells (IC50: 83.88 μM).
- G1/S phase arrest and apoptosis induction were confirmed, with minimal necrosis.
- Molecular docking revealed strong cholecalciferol binding to the vitamin D receptor (VDR) (-11.7 kcal/mol).
Conclusions:
- Sodium alginate nanogels provide a stable and effective delivery system for topical cholecalciferol.
- The nanogels demonstrate significant, selective anticancer activity against skin cancer cell lines.
- Cholecalciferol's VDR binding is a key mechanism in its observed anticancer effects.
- This formulation represents a promising biocompatible therapeutic for topical skin cancer treatment.
