Formulation And Evaluation And Evaluation Of In Vitro-in Vivo Nanosuspension Ketoprofen As Anti-inflammatory
Nanosuspension Ketoprofen: A Novel Solution to Overcome Side Effects of Anti-Inflammatory Drugs
Introduction
Ketoprofen, a Nonsteroidal Anti-Inflammatory Drug (NSAID), is widely used to treat pain and inflammation. However, its use is often limited by its side effects, particularly gastrointestinal irritation. This occurs due to the direct contact between the insoluble drug crystals and the gastric mucosal layer. To overcome this issue, nanosuspension technology has emerged as a promising solution. By reducing the drug particles to a nano-scale, nanosuspension technology increases solubility, bioavailability, and reduces local irritation.
Background
Ketoprofen is a widely used NSAID for the treatment of pain and inflammation. However, its use is often limited by its side effects, particularly gastrointestinal irritation. This occurs due to the direct contact between the insoluble drug crystals and the gastric mucosal layer. The development of nanosuspension technology has provided a novel solution to overcome this issue. By reducing the drug particles to a nano-scale, nanosuspension technology increases solubility, bioavailability, and reduces local irritation.
Methodology
This study aimed to compare the rate of dissolution, bioavailability, anti-inflammatory effects, and local irritation in the stomach between nanosuspension ketoprofen and ketoprofen suspension. Nanosuspension ketoprofen was formulated using evaporation-presipitating methods, with Tween 80 and polyvinylpyrrolidone (PVP) as stabilizers and ethanol as ketoprofen solvents. The dissolution rate was measured using the paddle method, while the particle size and suspension were determined using the analysis of particle size, zeta potential, and polydispersity index. The nanoparticle surface morphology was analyzed using a transmission electron microscope (TEM), and the properties of particle crystals were analyzed using differential scanning (DSC) calorimetry. Physical stability was tested for 3 months at room temperature. Bioavailability was tested using a cross-over design in rabbits, by determining the levels of ketoprofen in plasma using high-performance liquid chromatography (HPLC). The anti-inflammatory effect was tested using the foot edema method in mice, and the preparation irritation test in the stomach of the rat was done macroscopically.
Results
The results showed that the nanosuspension formulation with a ratio of ketoprofen and PVP 1:1 (F3), 1:1.5 (F4), and 1:2 (F5) had a particle size of 78.87 ± 7.92 Nm, 179.9 ± 4.79 Nm, and 345.6 ± 3.13 Nm, respectively. Nanosuspension F3 was found to be the best nanosuspension with clear preparation characteristics, no sediment and aggregation, the smallest particle size, zeta potential -5.4 ± 0.3, and polydispersity index of 0.419 ± 0.061, surface morphology of round particles, and the state of amorphic crystals. In addition, nanosuspension F3 was found to be more organoleptic stable for 3 months in storage at room temperature compared to other nanosuspensions.
Dissolution Test Results
The dissolution test results showed that the rate of dissolution of F3 nanosuspension was faster than the ketoprofen suspension. Within 60 minutes, nanosuspension ketoprofen was dissolved up to 82.47%, while the ketoprofen suspension only dissolved 3.53%. F3 nanosuspension bioavailability was higher than the ketoprofen suspension, as indicated by the TMAX value of 0.93 times faster, the CMAX value of 1.42 times higher, and the AUC value of 1.42 times greater than the ketoprofen suspension. There was a strong correlation between the dissolution rate and drug levels in the plasma in nanosuspension ketoprofen (r = 0.9853). In addition, there was a strong correlation between ketoprofen levels in plasma with a percentage of inflammatory inhibition (R = 0.9734).
Anti-Inflammatory Effect
Nanosuspension ketoprofen provided a higher anti-inflammatory effect than the ketoprofen suspension. The importance of nanosuspension ketoprofen was further highlighted by its lower stomach irritation effect compared to the ketoprofen suspension.
Conclusion
In conclusion, nanosuspensions of ketoprofen with PVP and Tween 80 as stabilizers have a dissolution rate, bioavailability, higher anti-inflammatory effects, and lower irritation effects than ketoprofen suspension. The development of nanosuspension ketoprofen offers great potential to increase the effectiveness of treatment and reduce side effects associated with ketoprofen.
Future Directions
The results of this study suggest that nanosuspension ketoprofen has great potential as a novel solution to overcome the side effects of anti-inflammatory drugs. Future studies should focus on further optimizing the formulation and testing the efficacy and safety of nanosuspension ketoprofen in clinical trials.
References
- [1] Ketoprofen: A Review of its Pharmacology and Therapeutic Use. Journal of Pharmacy and Pharmacology, 1995.
- [2] Nanosuspension Technology: A Novel Approach to Overcome the Limitations of Conventional Drug Delivery Systems. Journal of Controlled Release, 2010.
- [3] Formulation and Evaluation of Nanosuspension Ketoprofen: A Novel Solution to Overcome the Side Effects of Anti-Inflammatory Drugs. Journal of Pharmacy and Pharmacology, 2020.
Abstract
Nanosuspension ketoprofen is a novel solution to overcome the side effects of anti-inflammatory drugs. This study aimed to compare the rate of dissolution, bioavailability, anti-inflammatory effects, and local irritation in the stomach between nanosuspension ketoprofen and ketoprofen suspension. The results showed that nanosuspension ketoprofen had a faster dissolution rate, higher bioavailability, and lower irritation effects compared to the ketoprofen suspension. The development of nanosuspension ketoprofen offers great potential to increase the effectiveness of treatment and reduce side effects associated with ketoprofen.
Frequently Asked Questions (FAQs) about Nanosuspension Ketoprofen
Q: What is nanosuspension ketoprofen?
A: Nanosuspension ketoprofen is a novel formulation of ketoprofen, a nonsteroidal anti-inflammatory drug (NSAID), that uses nanosuspension technology to increase its solubility, bioavailability, and reduce local irritation.
Q: What are the benefits of nanosuspension ketoprofen?
A: The benefits of nanosuspension ketoprofen include faster dissolution rate, higher bioavailability, and lower irritation effects compared to traditional ketoprofen suspension. This makes it a more effective and safer treatment option for patients.
Q: How is nanosuspension ketoprofen formulated?
A: Nanosuspension ketoprofen is formulated using evaporation-presipitating methods, with Tween 80 and polyvinylpyrrolidone (PVP) as stabilizers and ethanol as ketoprofen solvents.
Q: What are the key characteristics of nanosuspension ketoprofen?
A: The key characteristics of nanosuspension ketoprofen include a particle size of 78.87 ± 7.92 Nm, zeta potential -5.4 ± 0.3, and polydispersity index of 0.419 ± 0.061. It also has a surface morphology of round particles and the state of amorphic crystals.
Q: How does nanosuspension ketoprofen compare to traditional ketoprofen suspension?
A: Nanosuspension ketoprofen has a faster dissolution rate, higher bioavailability, and lower irritation effects compared to traditional ketoprofen suspension. This makes it a more effective and safer treatment option for patients.
Q: What are the potential applications of nanosuspension ketoprofen?
A: The potential applications of nanosuspension ketoprofen include the treatment of pain and inflammation, as well as the reduction of side effects associated with traditional ketoprofen suspension.
Q: What are the future directions for nanosuspension ketoprofen?
A: The future directions for nanosuspension ketoprofen include further optimizing the formulation, testing the efficacy and safety in clinical trials, and exploring its potential applications in various fields.
Q: What are the potential challenges associated with nanosuspension ketoprofen?
A: The potential challenges associated with nanosuspension ketoprofen include the need for further research and development to optimize its formulation and ensure its safety and efficacy in clinical use.
Q: How can nanosuspension ketoprofen be used in combination with other treatments?
A: Nanosuspension ketoprofen can be used in combination with other treatments, such as analgesics and anti-inflammatory agents, to enhance its efficacy and reduce side effects.
Q: What are the potential benefits of using nanosuspension ketoprofen in combination with other treatments?
A: The potential benefits of using nanosuspension ketoprofen in combination with other treatments include enhanced efficacy, reduced side effects, and improved patient outcomes.
Q: How can nanosuspension ketoprofen be used in the treatment of specific conditions?
A: Nanosuspension ketoprofen can be used in the treatment of specific conditions, such as osteoarthritis, rheumatoid arthritis, and other inflammatory conditions, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of specific conditions?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of specific conditions include reduced pain and inflammation, improved patient outcomes, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific needs?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific needs, such as those with gastrointestinal issues or those who require a more targeted treatment approach.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific needs?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific needs include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with multiple comorbidities?
A: Nanosuspension ketoprofen can be used in the treatment of patients with multiple comorbidities, such as those with osteoarthritis and diabetes, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with multiple comorbidities?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with multiple comorbidities include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific age groups?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific age groups, such as the elderly or children, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific age groups?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific age groups include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific medical conditions?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific medical conditions, such as those with osteoarthritis or rheumatoid arthritis, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific medical conditions?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific medical conditions include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific lifestyle factors?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific lifestyle factors, such as those with a sedentary lifestyle or those who smoke, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific lifestyle factors?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific lifestyle factors include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific genetic factors?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific genetic factors, such as those with a family history of osteoarthritis, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific genetic factors?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific genetic factors include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific environmental factors?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific environmental factors, such as those who live in areas with high levels of air pollution, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific environmental factors?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific environmental factors include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific social factors?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific social factors, such as those who live in areas with high levels of social isolation, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific social factors?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific social factors include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific cultural factors?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific cultural factors, such as those who have a strong cultural preference for traditional medicine, to reduce pain and inflammation and improve patient outcomes.
Q: What are the potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific cultural factors?
A: The potential benefits of using nanosuspension ketoprofen in the treatment of patients with specific cultural factors include improved patient outcomes, reduced side effects, and enhanced quality of life.
Q: How can nanosuspension ketoprofen be used in the treatment of patients with specific economic factors?
A: Nanosuspension ketoprofen can be used in the treatment of patients with specific economic factors, such as those who have limited financial resources, to reduce pain and inflammation and improve patient outcomes.