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Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
Raj Kumar Thapa1, Ju Yeon Choi1, Bijay Kumar Poudel1
1College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongsanbuk-do, South Korea.
Abstract:
Cancer is one of the leading causes of death worldwide. Although different chemotherapeutic agents have been developed to treat cancers, their use can be limited by low cellular uptake, drug resistance, and side effects. Hence, targeted drug delivery systems are continually being developed in order to improve the efficacy of chemotherapeutic agents. The main aim of this study was to prepare folic acid (FA)-conjugated polyvinyl pyrrolidone-functionalized graphene oxides (GO) (FA-GO) for targeted delivery of sorafenib (SF). GO were prepared using a modified Hummer's method and subsequently altered to prepare FA-GO and SF-loaded FA-GO (FA-GO/SF). Characterization of GO derivatives was done using ultraviolet/visible spectroscopy, Fourier transform infrared spectroscopy, X-ray diffraction, atomic force microscopy, zeta potential measurements, and determination of in vitro drug release. Hemolytic toxicity, in vitro cytotoxicity, cellular uptake, and apoptotic effects of FA-GO/SF were also investigated. The results revealed that GO was successfully synthesized and that further transformation to FA-GO improved the stability and SF drug-loading capacity. In addition, the enhanced SF release under acidic conditions suggested possible benefits for cancer treatment. Conjugation of FA within the FA-GO/SF delivery system enabled targeted delivery of SF to cancer cells expressing high levels of FA receptors, thus increasing the cellular uptake and apoptotic effects of SF. Furthermore, the photothermal effect achieved by exposure of GO to near-infrared irradiation enhanced the anticancer effects of FA-GO/SF. Taken together, FA-GO/SF is a potential carrier for targeted delivery of chemotherapeutic agents in cancer.
Insights
This study developed folic acid-conjugated graphene oxide nanoparticles for targeted cancer therapy. These nanoparticles effectively deliver sorafenib to cancer cells, enhancing drug efficacy and reducing side effects.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Cancer Therapeutics
Background:
- Cancer remains a leading global cause of death, with chemotherapy efficacy often limited by poor drug uptake, resistance, and side effects.
- Targeted drug delivery systems are crucial for improving the effectiveness of chemotherapeutic agents.
- Folic acid receptors are overexpressed on many cancer cells, making them a viable target for drug delivery.
Purpose of the Study:
- To prepare and characterize folic acid (FA)-conjugated polyvinyl pyrrolidone-functionalized graphene oxides (GO) for targeted delivery of sorafenib (SF).
- To evaluate the potential of FA-GO/SF as a nanocarrier for enhanced cancer treatment, including targeted delivery and photothermal effects.
Main Methods:
- Graphene oxides (GO) were synthesized using a modified Hummer's method.
- GO was functionalized with folic acid (FA) to create FA-GO, and then loaded with sorafenib (SF) to form FA-GO/SF.
- Characterization involved spectroscopy, diffraction, microscopy, zeta potential, in vitro drug release, hemolytic toxicity, cytotoxicity, cellular uptake, and apoptosis assays.
Main Results:
- Successful synthesis and characterization of GO and FA-GO, demonstrating improved stability and drug-loading capacity.
- FA-GO/SF exhibited enhanced sorafenib release under acidic conditions, beneficial for tumor microenvironments.
- Targeted delivery to FA receptor-expressing cancer cells increased cellular uptake and induced apoptosis, amplified by near-infrared-triggered photothermal effects.
Conclusions:
- FA-GO/SF nanoparticles show promise as an effective system for targeted cancer therapy.
- The combination of targeted drug delivery and photothermal therapy offers a synergistic approach to enhance anticancer efficacy.
- This nanocarrier system represents a potential advancement in delivering chemotherapeutic agents more effectively in cancer treatment.
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