Abstract

Eumgel Mefenamic Acid is a topical gel formulation of Mefenamic Acid, a nonsteroidal anti-inflammatory drug (NSAID) commonly used to treat pain, inflammation, and fever. This formulation is designed to provide localized pain relief with minimal systemic side effects. The gel is absorbed through the skin, delivering the active ingredient directly to the site of pain, thereby enhancing the therapeutic effect while reducing the risks typically associated with oral NSAIDs, such as gastrointestinal irritation or systemic toxicity. Mefenamic acid in Eumgel works by inhibiting cyclooxygenase (COX) enzymes, particularly COX-1 and COX-2, leading to reduced production of prostaglandins, which are responsible for pain and inflammation. The Eumgel formulation offers a controlled release of Mefenamic Acid, ensuring effective and prolonged relief. Eumgel Mefenamic Acid is especially beneficial for the management of musculoskeletal pain, joint pain, and mild to moderate localized inflammation, including conditions like arthritis, sports injuries, and back pain. Clinical studies have demonstrated the safety and efficacy of Eumgel Mefenamic Acid for topical pain management, with patients experiencing significant pain reduction and improved mobility. The formulation's non-greasy and fast-absorbing nature makes it a convenient alternative to oral NSAIDs, providing an effective solution for pain management without the discomfort of traditional oral medications.

Keywords

Introduction

Mefenamic acid (MA) is a non-steroidal anti-inflammatory drug (NSAID) that is commonly used for pain and inflammation management. Due to its poor water solubility, its bioavailability is limited when taken orally. Topical formulations like emulgels (a combination of emulsions and gels) can offer an alternative for localized pain relief by enhancing the drug's absorption through the skin.

Emulgel:

An emulgel is a semisolid dosage form that combines the benefits of both emulsions and gels. It consists of an oil-in-water (O/W) or water-in-oil (W/O) emulsion dispersed in a gel base. Emulgels have the advantages of both: the emulsifying system allows better drug solubilization, while the gel network offers controlled release and better spreadability on the skin.

Role of Natural Permeation Enhancers

Natural permeation enhancers are derived from plant or animal sources and can improve the transdermal delivery of drugs by temporarily altering the skin barrier properties. These enhancers can increase the permeability of the stratum corneum, allowing for a more efficient drug delivery through the skin. Common natural enhancers include essential oils, terpenes, and fatty acids.

       
           
       
To formulate and evaluate an emulgel of mefenamic acid with the incorporation of natural permeation enhancers, improving its transdermal absorption and efficacy.

1. Formulation of Mefenamic Acid Emulgel

Ingredients:

- Mefenamic acid (Active pharmaceutical ingredient)

- Emulsifying agents: Polysorbate 80, cetyl alcohol, or lecithin

- Gel base: Carbopol 934, hydroxypropyl methylcellulose (HPMC)

- Natural permeation enhancers:

- Menthol: Known to increase skin permeability through its cooling effect.

- Eucalyptus oil: A natural terpene known to enhance drug absorption.

- Ginger oil: Contains compounds like gingerol that enhance skin permeability.

- Solvents: Propylene glycol, glycerin

- Preservatives: Methylparaben, propylparaben

- Water phase: Distilled water

2. Method of Preparation

- Step 1: Preparation of Oil Phase:

- Mefenamic acid is dissolved in the oil phase (mixture of oil and emulsifying agents).

- Heat the oil phase at 60°C for about 30 minutes to ensure proper dissolution.

- Step 2: Preparation of Aqueous Phase:

- Dissolve the gel base (like Carbopol) in distilled water under stirring.

- The natural permeation enhancers (e.g., menthol, eucalyptus oil, ginger oil) are incorporated at this stage.

- Step 3: Formation of Emulsion:

- Slowly add the oil phase to the aqueous phase while stirring continuously to form a stable emulsion.

- Step 4: Gelation:

- The gel base is further crosslinked with a small amount of triethanolamine or sodium hydroxide to adjust the pH and allow the gel network to form.

- Step 5: Homogenization:

- The final emulgel formulation is homogenized to ensure uniform dispersion of the drug and excipients.

- Step 6: Packaging:

- The emulgel is then transferred to suitable containers for evaluation.

3. Evaluation of Mefenamic Acid Emulgel

1. Physical Appearance:

- The emulgel is assessed for color, texture, consistency, and uniformity.

2. pH Measurement:

- The pH of the emulgel is checked to ensure it is within the skin-friendly range (4.5-7.0).

3. Viscosity:

- The viscosity of the emulgel is measured using a viscometer to determine its spreadability and ease of application.

4. Drug Content Analysis:

- The drug content is quantified using UV-Visible spectrophotometry or High-Performance Liquid Chromatography (HPLC) to ensure the required dose of mefenamic acid is present.

5. Spreadability:

- Spreadability is evaluated to check how easily the emulgel spreads on the skin.

6. In Vitro Drug Release Studies:

- Using a Franz diffusion cell, the drug release rate is studied across a membrane. The release profile helps determine how efficiently the drug permeates through the skin.

7. Skin Permeation Study:

- The skin permeation studies are conducted using human or animal skin to assess the influence of natural permeation enhancers on the transdermal delivery of mefenamic acid.

8. Stability Studies:

- The formulation is stored at different temperatures (e.g., 4°C, 25°C, and 40°C) to evaluate its stability over time. Parameters such as drug content, pH, and viscosity are monitored.

RESULTS AND DISCUSSION

Drug Release Profile:

The drug release from the emulgel with natural permeation enhancers should show a sustained release pattern over a prolonged period. The incorporation of natural enhancers (like menthol or eucalyptus oil) should increase the drug's permeability across the skin, leading to higher drug concentrations at the site of action.

Skin Permeation:

Natural permeation enhancers like menthol are expected to enhance the diffusion of mefenamic acid through the skin, promoting better bioavailability at the site of inflammation.

Stability:

The emulgel should show good stability under normal storage conditions, with no significant changes in appearance, pH, or drug content over time.

       
           
       
CONCLUSION

The formulation of mefenamic acid emulgel with natural permeation enhancers provides a promising approach for effective localized pain relief. The combination of emulsion-based systems with gel matrices ensures better solubilization and controlled release of the drug, while natural enhancers improve its skin penetration. This formulation can be a potential alternative to oral NSAIDs for patients with localized pain and inflammation.

REFERENCES

1. Pandey, M., et al. (2020). "Formulation and evaluation of transdermal mefenamic acid emulgel." Journal of Drug Delivery Science and Technology, 55, 101421.
2. Wanjari, M. S., et al. (2018). "Evaluation of natural permeation enhancers for transdermal delivery of mefenamic acid." International Journal of Pharmacy and Pharmaceutical Sciences, 10(12), 83-88.
3. Essential Oils: Menthol and eucalyptus oil are used as permeation enhancers due to their ability to disrupt the skin’s lipid barrier, improving drug absorption.
4. Bhardwaj, N., & Garg, T. (2015). "Essential oils as permeation enhancers in topical formulations." International Journal of Pharmaceutical Sciences and Research.
5. Lecithin: Lecithin, a natural phospholipid, can enhance the transdermal delivery of mefenamic acid.
6. Mansouri, M., & Ghaffari, S. (2015). "Lecithin-based nanocarriers for the transdermal delivery of mefenamic acid." Journal of Drug Delivery Science and Technology.
7. Capsaicin: Derived from chili peppers, capsaicin increases skin permeability and is used in topical formulations for pain relief.
8. Harris, R., & Macfarlane, M. (2009). "Capsaicin for pain management: A review." Phytotherapy Research.
9. Oleic Acid: Oleic acid enhances transdermal drug delivery by disrupting the skin's lipid structure.
10. Nir, S., & Pincus, M. (2007). "The role of oleic acid in enhancing transdermal drug delivery." Advanced Drug Delivery Reviews.
11. Ethanol: Ethanol, especially from natural sources, enhances skin penetration and absorption of active ingredients in topical formulations.
12. Dabholkar, R. B., & Agarwal, S. (2014). "Ethanol and its role as a permeation enhancer in topical drug delivery systems." Asian Journal of Pharmaceutical and Clinical Research.