Enhancing 6-Shogaol Bioavailability via β-Cyclodextrin Inclusion Complex: Synthesis, Characterization, and Anticancer Efficacy in Breast Cancer
Abstract
6-Shogaol, a bioactive phytochemical derived from Zingiber officinale, demonstrates potent anticancer activity but is hindered by poor aqueous solubility, instability, pungent odor, and low bioavailability. This study aimed to enhance 6-Shogaol’s solubility and therapeutic efficacy through β-cyclodextrin (β-CD) inclusion complexation and evaluate its anticancer potential in breast cancer cells. Additionally, the study explores the co-formulation of 6-Shogaol with a β-CD inclusion complex of allicin to enhance cytotoxic potential. Inclusion complexes were prepared using physical mixture, kneading, solvent evaporation, and co-precipitation methods. The optimal complex (1:1 drug: β-CD ratio) was characterized by FTIR, XRD, SEM, and phase-solubility studies. Solubility, dissolution, and cytotoxicity were assessed in MCF-7 cells via MTT assay. The physical mixture method achieved the highest solubility enhancement (from 0.96 ± 0.02 to 3.14 ± 0.10 mg/mL), with drug loading (50.00% ± 0.075) and entrapment efficiency (76.05% ± 0.99). The stability constant (Kc = 2119.04 M⁻¹) confirmed robust complexation. In-vitro dissolution showed 95.26 ± 0.7% drug release within 2 hours. The β-CD complex exhibited improved cytotoxicity (IC₅₀ = 69.67 ± 2.3 µg/mL) versus the free drug (IC₅₀ = 95.66 ± 2.1 µg/mL), while the co-delivery of 6-Shogaol with allicin further enhanced cytotoxicity (IC₅₀ = 23.32 µg/mL). β-CD complexation significantly improved 6-Shogaol’s solubility, stability, and anticancer activity. The combination of 6-Shogaol and allicin β-CD complexes demonstrated enhanced cytotoxic potential, highlighting a promising phytopharmaceutical strategy for breast cancer therapy.
Keywords
References
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Details
Primary Language
English
Subjects
Pharmaceutical Delivery Technologies
Journal Section
Research Article
Authors
Shital Patil
This is me
India
Gandhali Koshti
This is me
India
Kiran Wadkar
This is me
0000-0002-4312-6223
India
Publication Date
March 15, 2026
Submission Date
April 30, 2025
Acceptance Date
July 3, 2025
Published in Issue
Year 2026 Volume: 30 Number: 2