Combination Therapy in Cancer Treatment: The Role of Artemisinin as an Adjuvant and the Integration of Nanotechnology for Enhanced E

Location

Suwanee, GA

Start Date

6-5-2025 1:00 PM

End Date

6-5-2025 4:00 PM

Description

INTRODUCTION: Artemisinin is a sesquiterpene lactone derived from Artemisia annua L, a Chinese herb commonly used in traditional medicine. It is known mainly for its use as an anti-malarial; however, recent studies have shown that it is helpful as an adjuvant for delivering cancer treatment via the use of nanoparticles. Artemisinin contains an endoperoxide bridge that forms reactive oxygen species in the presence of iron. Artemisinin derivatives have also been shown to demonstrate anti-tumor effects. However, low bioavailability and solubility limit the effects of artemisinin and its derivatives. In cancer therapy, the target delivery of chemotherapeutic medications to cancer cells improves efficacy and safety by limiting systemic toxicity and drug resistance. Nanoparticles are drug delivery systems demonstrating better cell targeting to improve cancer therapy.

OBJECTIVES: The primary aim of this review is to explore the use of artemisinin as a cancer treatment adjuvant and compare the effectiveness of different nanoparticle carriers used in delivering artemisinin and its derivatives to enhance the anti-tumor effects.

METHODS: Information was derived via databases such as PubMed, NIH, and EBSCO, and references were cited to select articles. Keywords used to choose the references include “nanotechnology,” “nanoparticles,” “artemisinin,” “adjuvant,” and “cancer.” Each article was then categorized based on the type of nanotechnology used. The articles selected were published in the year 2000 and above.

RESULTS: The result shows that artemisinin-loaded nanoparticles significantly inhibit tumor growth in various cancer models, including breast, ovarian, lung, and liver cancers.

Various nanoformulations of artemisinin and its derivatives showed improved drug delivery, bioavailability, solubility, and enhanced cytotoxicity effects in cancer. Formulations include polymer-, lipid-, metal-, and carbon-based nanoparticles with and without surface modifications, such as ligands, peptides, and antibodies for cell targeting. A smaller-sized nanoparticle has demonstrated increased surface area for drug loading and more accumulation into the leaky vasculature of tumor cells that support their growth and proliferation. Of the artemisinin-nanoformulations reviewed, lipid nanoparticles were used in more studies than other nanoformulations. The results indicated significant higher cellular uptake, enhanced anticancer activity, and prolonged circulation time than the drug-derivative alone with less toxicity. Artemisinin and its derivatives release from nanoparticles into the target cells have demonstrated a pH-dependent manner with more drug release seen in acidic pH (>5). Cancer cell death has been attributed to G1 cell cycle arrest and downregulation of pRb and cyclin D via artemisinin and its derivatives endoperoxide bridge to induce free radical generation. Cytotoxic effects are dose- and cell-line dependent, with more potent results demonstrated by artemisone than artemisinin and other derivatives in a lipid nanoformulation.

CONCLUSION: Limitations to artemisinin and its derivatives are its poor water solubility and bioavailability; however, incorporating various nanotechnology systems such as liposomes, micelles, polymeric, and metal nanoparticles has shown to overcome these limitations. These nanocarriers allow artemisinin to be delivered directly to their treatment site to prevent damage to nearby tissue and normal cells. Although pre-clinical research has increased, there is limited research on clinical trials of artemisinin nanoparticles due to low drug loading, high cost, and toxicity from preparation.

Embargo Period

5-19-2025

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May 6th, 1:00 PM May 6th, 4:00 PM

Combination Therapy in Cancer Treatment: The Role of Artemisinin as an Adjuvant and the Integration of Nanotechnology for Enhanced E

Suwanee, GA

INTRODUCTION: Artemisinin is a sesquiterpene lactone derived from Artemisia annua L, a Chinese herb commonly used in traditional medicine. It is known mainly for its use as an anti-malarial; however, recent studies have shown that it is helpful as an adjuvant for delivering cancer treatment via the use of nanoparticles. Artemisinin contains an endoperoxide bridge that forms reactive oxygen species in the presence of iron. Artemisinin derivatives have also been shown to demonstrate anti-tumor effects. However, low bioavailability and solubility limit the effects of artemisinin and its derivatives. In cancer therapy, the target delivery of chemotherapeutic medications to cancer cells improves efficacy and safety by limiting systemic toxicity and drug resistance. Nanoparticles are drug delivery systems demonstrating better cell targeting to improve cancer therapy.

OBJECTIVES: The primary aim of this review is to explore the use of artemisinin as a cancer treatment adjuvant and compare the effectiveness of different nanoparticle carriers used in delivering artemisinin and its derivatives to enhance the anti-tumor effects.

METHODS: Information was derived via databases such as PubMed, NIH, and EBSCO, and references were cited to select articles. Keywords used to choose the references include “nanotechnology,” “nanoparticles,” “artemisinin,” “adjuvant,” and “cancer.” Each article was then categorized based on the type of nanotechnology used. The articles selected were published in the year 2000 and above.

RESULTS: The result shows that artemisinin-loaded nanoparticles significantly inhibit tumor growth in various cancer models, including breast, ovarian, lung, and liver cancers.

Various nanoformulations of artemisinin and its derivatives showed improved drug delivery, bioavailability, solubility, and enhanced cytotoxicity effects in cancer. Formulations include polymer-, lipid-, metal-, and carbon-based nanoparticles with and without surface modifications, such as ligands, peptides, and antibodies for cell targeting. A smaller-sized nanoparticle has demonstrated increased surface area for drug loading and more accumulation into the leaky vasculature of tumor cells that support their growth and proliferation. Of the artemisinin-nanoformulations reviewed, lipid nanoparticles were used in more studies than other nanoformulations. The results indicated significant higher cellular uptake, enhanced anticancer activity, and prolonged circulation time than the drug-derivative alone with less toxicity. Artemisinin and its derivatives release from nanoparticles into the target cells have demonstrated a pH-dependent manner with more drug release seen in acidic pH (>5). Cancer cell death has been attributed to G1 cell cycle arrest and downregulation of pRb and cyclin D via artemisinin and its derivatives endoperoxide bridge to induce free radical generation. Cytotoxic effects are dose- and cell-line dependent, with more potent results demonstrated by artemisone than artemisinin and other derivatives in a lipid nanoformulation.

CONCLUSION: Limitations to artemisinin and its derivatives are its poor water solubility and bioavailability; however, incorporating various nanotechnology systems such as liposomes, micelles, polymeric, and metal nanoparticles has shown to overcome these limitations. These nanocarriers allow artemisinin to be delivered directly to their treatment site to prevent damage to nearby tissue and normal cells. Although pre-clinical research has increased, there is limited research on clinical trials of artemisinin nanoparticles due to low drug loading, high cost, and toxicity from preparation.