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Published on: June 13, 2014
Targeting drug resistant colorectal cancer with apigenin nanoarchitectures
Pouya Goleij1, Saeid Ferdousmakan2, Mohammad Amin Khazeei Tabari3
1USERN Office, Kermanshah University of Medical Sciences, Kermanshah 6715847141, Iran; Department of Genetics, Faculty of Biology, Sana Institute of Higher Education, Sari 4816118761, Iran.
Abstract:
Drug resistance remains a critical obstacle in the treatment of colorectal cancer (CRC), contributing to high mortality rates, particularly in advanced stages. Conventional therapies, including surgery, chemotherapy, and targeted drugs, often face limitations such as systemic toxicity, poor drug selectivity and the development of multi-drug resistance (MDR). Recent studies have explored the use of apigenin, a naturally occurring flavonoid, as a promising therapeutic agent against drug-resistant CRC. This review aims to summarize and critically evaluate current research on the use of apigenin-loaded nanoarchitectures in overcoming drug resistance mechanisms in CRC. Specifically, it examines the efficacy of apigenin when delivered via various nanocarriers, including PLGA nanoparticles, lipid-polymer hybrid nanoparticles and liposomal formulations. These nanoarchitectures enhance the bioavailability, targeted delivery and sustained release of apigenin, improving its therapeutic efficacy. Apigenin-loaded nanoparticles effectively increase cellular uptake, circumvent drug efflux pumps and induce apoptosis in drug-resistant CRC cells. They also inhibit cancer cell proliferation by arresting the cell cycle and suppressing oncogenic pathways, such as PI3K/Akt/mTOR. Furthermore, apigenin disrupts angiogenesis and inflammation, thereby weakening the tumor microenvironment. Synergistic effects with conventional chemotherapy further underscore apigenin's potential as a chemo-sensitizer and in combination therapy, offering a promising avenue for reducing drug resistance in CRC. The findings suggest that apigenin nanoarchitectures could be a powerful strategy for enhancing CRC treatment outcomes, providing a foundation for further clinical development.
Insights
Apigenin nanoarchitectures show promise in overcoming drug resistance in colorectal cancer (CRC). These formulations enhance apigenin delivery, increasing efficacy against resistant CRC cells and offering a new strategy for treatment.
Area of Science:
- Oncology
- Nanotechnology
- Pharmacology
Background:
- Drug resistance is a major challenge in colorectal cancer (CRC) treatment, leading to high mortality.
- Conventional therapies for CRC have limitations including toxicity and multi-drug resistance (MDR).
- Apigenin, a natural flavonoid, is being investigated for its potential against drug-resistant CRC.
Purpose of the Study:
- To review and evaluate the use of apigenin-loaded nanoarchitectures in overcoming drug resistance in CRC.
- To examine the efficacy of apigenin delivered via nanocarriers like PLGA nanoparticles, lipid-polymer hybrid nanoparticles, and liposomes.
- To assess apigenin's impact on cellular mechanisms, tumor microenvironment, and synergistic effects with chemotherapy.
Main Methods:
- Review of current research on apigenin-loaded nanoarchitectures for CRC treatment.
- Analysis of nanocarrier-mediated delivery systems (PLGA nanoparticles, lipid-polymer hybrid nanoparticles, liposomes).
- Evaluation of apigenin's effects on drug-resistant CRC cells, including cellular uptake, apoptosis, cell cycle arrest, and pathway inhibition (PI3K/Akt/mTOR).
Main Results:
- Apigenin nanoarchitectures improve bioavailability, targeted delivery, and sustained release of apigenin.
- Apigenin-loaded nanoparticles enhance cellular uptake, overcome drug efflux pumps, and induce apoptosis in resistant CRC cells.
- Apigenin inhibits proliferation, arrests the cell cycle, suppresses oncogenic pathways, and disrupts angiogenesis and inflammation.
Conclusions:
- Apigenin nanoarchitectures represent a potent strategy to enhance CRC treatment outcomes by overcoming drug resistance.
- Apigenin acts as a chemo-sensitizer and shows potential in combination therapy for CRC.
- Further clinical development of apigenin nanoarchitectures is warranted for improved CRC treatment.
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