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Precision-engineered Carrageenan Gels: Boosting the Efficacy, Selectivity, and Release of Celecoxib for Lung Cancer
Akanksha Bhatt1, Priyank Purohit2, Magda H Abdellattif3
1Department of Pharmacy, Graphic Era Hill University Dehradun, Dehradun, 28008, India.
Background:
Lung cancer is one of the most widespread malignancies among all types of cancers. There is uncertainty in its treatment because of the selectivity. The investigation is aimed to enhance therapeutic efficacy through targeted improvements in drug selectivity and reduced toxicity by analyzing well-accepted cyclooxygenase (COX)-2, which is an enzyme target and a known therapeutic target for anti-inflammatory and antitumor agents.
Objective:
The objective of the present research was to identify the most suitable counterpart for celecoxib, which would produce synergistic effects and improve the selectivity index, safety, and efficacy of targeting cancer cells.
Methods:
The HOPE-62 cancer cell line and noncancerous LLC-MK2 cell line were used to analyze the activity of the prepared formulations. The effectiveness was compared by calculating the half-maximal inhibitory concentration (IC50) values of carrageenan, celecoxib, and celecoxib embedded with carrageenan. The release pattern of celecoxib from the carrageenan matrix was also determined by using a trans-diffusion cell; moreover, the binding sites of carrageenan and celecoxib were also evaluated through in silico molecular docking studies.
Results:
Carrageenan showed promising anticancer activity, with an IC50 value of 17.3±2 μM against the HOPE- 62 cell line. When blended with celecoxib (15.6±2 μM), the combination achieved enhanced efficacy and improved selectivity over celecoxib alone (IC50 of 10.3±1.5 μM). In noncancerous LLC-MK2 cells, the IC50 values were observed to be significantly higher: 1484 ±6 μM in the combined formulation and with IC50 values of 559±3 μM and 878±4 μM, respectively, in celecoxib and carrageenan alone.
Conclusion:
The carrageenan-embedded celecoxib exhibited a significant increase in the selectivity index from 32 to 144, which suggests enhanced anticancer activity with a favorable safety profile. Initially, sustained release of celecoxib from the blend was at a higher rate, but steadily maintained rates were. The In-silico docking studies also supported the synergistic activity of the combined form through separate interaction patterns without interfering with others. These findings underscore the therapeutic potential of excipient-drug blending strategies to achieve synergistic effects, excellent selectivity, and reduced toxicity in cancer treatments.
Insights
This study shows that blending carrageenan with celecoxib enhances its anticancer efficacy and selectivity against lung cancer cells. The combination offers a more favorable safety profile, indicating potential for improved cancer therapies.
Area of Science:
- Oncology
- Pharmacology
- Materials Science
Background:
- Lung cancer remains a leading cause of cancer-related deaths, with treatment challenges stemming from drug selectivity and toxicity.
- Cyclooxygenase-2 (COX-2) is a validated therapeutic target for anti-inflammatory and antitumor agents, offering a potential avenue for improved lung cancer treatment.
Purpose of the Study:
- To identify an optimal counterpart for celecoxib to achieve synergistic effects in targeting cancer cells.
- To enhance the selectivity index, safety, and overall efficacy of cancer cell targeting through drug formulation.
Main Methods:
- Evaluated the anticancer activity of carrageenan, celecoxib, and a carrageenan-celecoxib blend against the HOPE-62 lung cancer cell line and noncancerous LLC-MK2 cells.
- Determined half-maximal inhibitory concentration (IC50) values to compare formulation effectiveness and selectivity.
- Investigated celecoxib release kinetics from the carrageenan matrix and performed in silico molecular docking to assess binding interactions.
Main Results:
- Carrageenan demonstrated significant anticancer activity (IC50: 17.3±2 μM) against HOPE-62 cells.
- The carrageenan-celecoxib blend exhibited enhanced efficacy (IC50: 15.6±2 μM) and improved selectivity compared to celecoxib alone (IC50: 10.3±1.5 μM).
- The combination showed a markedly higher IC50 in noncancerous cells (1484 ±6 μM) versus celecoxib (559±3 μM) or carrageenan (878±4 μM) alone, indicating reduced toxicity.
Conclusions:
- Carrageenan-embedded celecoxib significantly increased the selectivity index from 32 to 144, demonstrating enhanced anticancer activity and a favorable safety profile.
- Sustained release of celecoxib from the carrageenan blend was observed, supporting its therapeutic potential.
- In silico studies confirmed synergistic activity of the combined formulation without interfering interactions, highlighting the value of excipient-drug blending strategies.
