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Surface-enhanced Resonance Raman Scattering Nanoprobe Ratiometry for Detecting Microscopic Ovarian Cancer via Folate Receptor Targeting
Published on: March 25, 2019
Investigation of Gold Nanoparticle Naproxen-Derived Conjugations in Ovarian Cancer
Cansu Umran Tunc1,2, Gizem Kursunluoglu1, Munevver Akdeniz1,3
1Nanothera Lab, Drug Application and Research Center (ERFARMA), Erciyes University, Kayseri 38039, Turkey.
Abstract:
Ovarian cancer, which is one of the most diagnosed cancer types among women, maintains its significance as a global health problem. Several drug candidates have been investigated for the potential treatment of ovarian cancer. Nonsteroidal anti-inflammatory drugs (NSAIDs) demonstrated anti-cancer activity through the inhibition of cyclooxygenase 2 (COX-2) and by inhibiting COX-2-dependent prostaglandin (PG) production. Naproxen is one of the most used NSAIDs and Naproxen-derived compounds (NDCs) may show potential treatment effects on cancer as chemotherapeutic drugs. Although there are successful drug development studies, the lack of solubility of these drug candidates in aqueous media results in limited bioavailability and high variability of patient responses during treatment. Low aqueous solubility is one of the main problems in the pharmaceutical industry in terms of drug development. Nanotechnology-based strategies provide solutions to hydrophobic drug limitations by increasing dispersion and improving internalization. In this study, two different NDCs (NDC-1 and NDC-2) bearing a thiosemicarbazide/1,2,4-triazole moiety were synthesized and tested for chemotherapeutic effects on ovarian cancer cells, which have a high COX-2 expression. To overcome the limited dispersion of these hydrophobic drugs, the drug molecules were conjugated to the surface of 13 nm AuNPs. Conjugation of drugs to AuNPs increased the distribution of drugs in aqueous media, and NDC@AuNP conjugates exhibited excellent colloidal stability for up to 8 weeks. The proposed system demonstrated an increased chemotherapeutic effect than the free drug counterparts with at least 5 times lower IC50 values. NDC@AuNP nanosystems induced higher apoptosis rates, which established a simple and novel way to investigate activity of prospective drugs in drug discovery research.
Insights
Naproxen-derived compounds (NDCs) conjugated to gold nanoparticles (AuNPs) enhanced chemotherapy for ovarian cancer by improving drug solubility and efficacy, showing significantly lower IC50 values and increased apoptosis.
Area of Science:
- Nanomedicine and Drug Delivery
- Oncology
- Materials Science
Background:
- Ovarian cancer remains a significant global health challenge, necessitating novel therapeutic strategies.
- Nonsteroidal anti-inflammatory drugs (NSAIDs), like Naproxen-derived compounds (NDCs), show anti-cancer potential via cyclooxygenase-2 (COX-2) inhibition.
- Poor aqueous solubility of hydrophobic drugs limits their bioavailability and therapeutic efficacy in cancer treatment.
Purpose of the Study:
- To synthesize and evaluate two novel Naproxen-derived compounds (NDCs) for their chemotherapeutic effects on ovarian cancer cells.
- To enhance the aqueous dispersion and bioavailability of hydrophobic NDCs using nanotechnology.
- To investigate the potential of drug-conjugated gold nanoparticles (AuNPs) as an improved drug delivery system for ovarian cancer.
Main Methods:
- Synthesis of two Naproxen-derived compounds (NDCs) with a thiosemicarbazide/1,2,4-triazole moiety.
- Conjugation of synthesized NDCs to 13 nm gold nanoparticles (AuNPs) to create NDC@AuNP nanosystems.
- Evaluation of chemotherapeutic effects, including IC50 values and apoptosis rates, on ovarian cancer cells expressing high COX-2.
Main Results:
- NDC@AuNP conjugates demonstrated excellent colloidal stability in aqueous media for up to 8 weeks.
- The nanosystems significantly increased drug distribution and exhibited enhanced chemotherapeutic effects compared to free NDCs.
- NDC@AuNP treatment resulted in at least 5-fold lower IC50 values and induced higher rates of apoptosis in ovarian cancer cells.
Conclusions:
- Conjugating NDCs to AuNPs effectively overcomes limitations of poor aqueous solubility, enhancing anti-cancer activity.
- The developed NDC@AuNP nanosystems represent a promising strategy for improving ovarian cancer chemotherapy.
- This approach offers a simple and novel method for investigating prospective drug candidates in drug discovery research.
