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Updated: May 30, 2025
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Nanoformulation of Spirooxindole and Methods for Treating Hepatocellular Carcinoma
Assem Barakat1, Fardous F El-Senduny2,3, Mohammad Shahidul Islam1
1Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
Abstract:
Objectives: This in vivo study introduces a newly developed spirooxindole derivative that is deemed safe and effective as a potential targeted therapy for various cancers. Methods: Extensive in vivo investigations, including histopathology, immunohistochemistry, and molecular biology, validated its potential for further preclinical and clinical exploration, necessitating comprehensive examinations of its bioavailability, pharmacodynamics, and pharmacokinetics. Additionally, this study involves the development of a commercially viable proniosomal drug delivery system for the compound, facilitating controlled drug release. Results: The data revealed efficacy of spirooxindole derivative in halting the progression of liver cancer, metastasis, and portal vein thrombosis, with potential implications for enhancing regeneration and recovery of early-stage cancer cells in multiple organs, thereby improving recovery rates and remission among cancer patients. The proniosomes, loaded with the compound, exhibited high entrapment efficiency and prolonged drug release rates of up to 12 h in vitro. The optimized formula demonstrated superior drug release percentages and stability compared to conventional niosomes. Further analysis via FTIR and DSC confirmed the absence of chemical interactions and proper entrapment of the compound within the nanovesicles, indicating a stable and effective drug delivery system. Conclusions: This study presents a novel, safe, and effective chemical entity of spirooxindole derivatives for further preclinical and clinical studies.
Insights
A novel spirooxindole derivative shows promise as a safe and effective targeted cancer therapy. Developed proniosomes enhance drug delivery, improving outcomes for liver cancer and metastasis patients.
Area of Science:
- Oncology
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Targeted cancer therapies are crucial for improving patient outcomes.
- Spirooxindole derivatives represent a class of compounds with potential anticancer activity.
- Effective drug delivery systems are needed to enhance the bioavailability and efficacy of novel therapeutics.
Purpose of the Study:
- To introduce and evaluate a newly developed spirooxindole derivative as a potential targeted cancer therapy.
- To develop and characterize a proniosomal drug delivery system for enhanced controlled release of the spirooxindole derivative.
- To assess the in vivo efficacy and safety of the spirooxindole derivative and its proniosomal formulation.
Main Methods:
- In vivo studies including histopathology, immunohistochemistry, and molecular biology.
- Development and optimization of a proniosomal drug delivery system.
- In vitro evaluation of entrapment efficiency and drug release kinetics.
- Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) for formulation analysis.
Main Results:
- The spirooxindole derivative demonstrated efficacy in halting liver cancer progression, metastasis, and portal vein thrombosis.
- Proniosomes exhibited high entrapment efficiency and prolonged in vitro drug release (up to 12 hours).
- The optimized proniosomal formulation showed superior stability and drug release compared to conventional niosomes.
- FTIR and DSC confirmed the compound's stability and entrapment within the nanovesicles.
Conclusions:
- A novel spirooxindole derivative is identified as a safe and effective chemical entity for cancer therapy.
- The developed proniosomal formulation provides a stable and effective drug delivery system.
- The findings support further preclinical and clinical investigation of this spirooxindole derivative for cancer treatment.
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