Improving the Cytotoxic Activity of Hinokitiol from Drug-Loaded Phytosomal Formulation Against Breast Cancer Cell Lines - Original Research

Sep 21, 2026

This original research evaluates how formulation parameters affect hinokitiol-loaded phytosomes and whether the resulting nanoparticles can inhibit breast cancer cells. Phytosomal nanoparticles were prepared and characterized for size, zeta potential, entrapment efficiency, morphology, and pH-dependent hinokitiol solubility. In vitro release and cytotoxicity were measured, while apoptosis was assessed via Annexin V/propidium iodide staining and cell-cycle effects were analyzed. Optimized phytosomes showed sustained release and markedly improved cytotoxicity with lower IC50 values, inducing apoptosis and arrest at G2/M and S phases.

LanguageEnglish

CategoryHealthcare

FormatPDF

Pages19

Reading Time48 min

AccessFree to download

Background

Materials and Methods

Results

Conclusion

International Journal of Nanomedicine Dovepress Open Access Full Text Article ORIGINAL RESEARCH Improving the Cytotoxic Activity of Hinokitiol from Drug-Loaded Phytosomal Formulation Against Breast Cancer Cell Lines Tarek A Ahmed 1 , 2 , Ghada A Milibary 1 , Alshaimaa M Almehmady 1 , Amerh A Alahmadi 1 , Ehab MM Ali 3 , Khalid M El-Say 1 1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; 2Centre for Artificial Intelligence in Precision Medicine, King Abdulaziz University, Alsulaymanyah, Jeddah, 21589, Saudi Arabia; 3Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, 21589, Saudi Arabia Correspondence: Tarek A Ahmed, Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia, Tel +96626400000 ext 22250, Email [tabdelnapy@kau.edu.sa](tabdelnapy@kau.edu.sa) | Background: This study investigates the influence of various formulation parameters on the characteristics of hinokitiol-loaded phytosomes and evaluates their anticancer potential against breast cancer cells.
Materials and Methods: Phytosomal nanoparticles were prepared and characterized for size, zeta potential, and entrapment efficiency. Morphological analysis was conducted using optical microscopy and transmission electron microscopy (TEM) . The solubility of hinokitiol at different pH levels was determined, and the in vitro release profile of the optimized phytosomes was assessed. Cytotoxicity assays were performed to evaluate the anticancer efficacy against breast cancer cell lines, and apoptosis induction was examined using Annexin V/propidium iodide staining. Cell cycle analysis was conducted to assess the impact on cell cycle progression.
Results: The optimized phytosomes demonstrated a size range of 138.4 ± 7.7 to 763.7 ± 15.4 nm, with zeta potentials ranging from −10.2 ± 0.28 to −53.2 ± 1.06 mV and entrapment efficiencies between 29.161 ± 1.163% and 92.77 ± 7.01% . Morphological characterization confirmed uniformity and spherical morphology. Hinokitiol solubility increased with pH, and the release from the optimized phytosomes exhibited sustained patterns. The formulated phytosomes showed superior cytotoxicity, with lower IC50 values compared to pure hinokitiol. Treatment induced significant apoptosis and cell cycle arrest at the G2/M and S phases.
Conclusion: Hinokitiol-loaded phytosomes demonstrate promising anticancer efficacy against breast cancer cells, highlighting their potential as targeted therapeutic agents for breast cancer therapy.
Keywords: hinokitiol, phytosomes, cytotoxic activity, breast cancer, apoptosis, cell cycle | | --- | | Introduction
Breast cancer is a prevalent disease, impacting the lives of millions of women worldwide, making it one of the most pressing health challenges of our time. Its widespread occurrence underscores the urgent need for innovative and effective therapeutic strategies.1 In 2020, the global burden of breast cancer was staggering, with new cases totaling 2.3 million, accounting for approximately 11.7% of all cancer incidents. Projections based on global demographic trends paint a troubling picture for the future, with anticipated cases and deaths on the rise. Trailing closely behind are lung, colorectal, prostate, and stomach cancers. Despite this shift, lung cancer remains the primary cause of cancer-related deaths, claiming an estimated 1.8 million lives. However, female breast cancer follows closely behind, underscoring the urgent need for continued research, prevention, and treatment efforts to combat this pervasive disease.2,3 By 2040, the worldwide burden of cancer is projected to reach 28.4 million cases, marking a significant 47% increase from the levels observed in 2020.4 The anticipated increase is expected to be particularly pronounced in developing nations, where projections indicate a sharp rise in prevalence from 64% to 95% . In contrast, more dev

FAQs

How were hinokitiol-loaded phytosomes prepared and characterized?

Phytosomal nanoparticles were prepared and characterized for size, zeta potential, and entrapment efficiency, with morphology examined using optical microscopy and TEM. Hinokitiol solubility was measured across different pH levels, and in vitro release of optimized phytosomes was assessed.

What findings demonstrate improved cytotoxicity against breast cancer cells?

The optimized phytosomes exhibited a wide size range, specific zeta potential values, and high entrapment efficiencies. They showed superior cytotoxicity with lower IC50 values compared with pure hinokitiol.

What cellular mechanisms were observed after treatment?

Treatment induced significant apoptosis measured by Annexin V/propidium iodide staining and caused cell-cycle arrest at the G2/M and S phases.

Sep 21, 2026

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