Thailand medical researchers develop new transdermal delivery system for painkiller diclofenac sodium

Thailand Medical: Researchers from Silpakorn University in Nakhon Pathom, Thailand, have made significant strides in improving pain management through the development of a new transdermal delivery system for Diclofenac Sodium (DCFNa). This innovative system utilizes a self-microemulsifying drug delivery system (SMEDDS) embedded in pressure-sensitive adhesive (PSA) patches to enhance the solubility and permeability of DCFNa, a widely used non-steroidal anti-inflammatory drug (NSAID). This Thailand Medical news report delves into how this novel approach could transform pain relief treatments for common ailments like arthritis, muscle strains, and inflammation.


Thailand medical researchers develop new transdermal delivery system for painkiller diclofenac sodium

Diclofenac Sodium is often prescribed for its pain-relieving and anti-inflammatory properties, but it presents challenges when delivered through the skin. The poor solubility of DCFNa in water, coupled with its limited ability to permeate the skin, makes it difficult for the drug to be fully effective when applied topically.
 
The researchers sought to overcome these limitations by developing a more efficient transdermal delivery system, which enhances the drug's solubility and penetration through the skin.
 
The Challenges of Diclofenac Sodium
Diclofenac Sodium is a potent NSAID frequently used for pain management in conditions such as osteoarthritis, rheumatoid arthritis, and acute muscle strains. While it is highly effective in reducing inflammation and pain, the traditional oral and injectable forms of the drug come with a range of side effects, including gastrointestinal irritation and potential harm to the cardiovascular and renal systems. To mitigate these adverse effects, topical formulations of NSAIDs, including gels, creams, and patches, have become a popular alternative.
 
However, DCFNa poses a unique challenge when used in topical applications. Its poor solubility in water means that much of the drug does not dissolve adequately to be absorbed through the skin. As a result, topical formulations often fail to deliver the optimal amount of the drug to the target site, requiring higher doses or more frequent applications. This can result in inadequate pain relief and an increased risk of side effects.
 
A Breakthrough in Transdermal Delivery
To address these challenges, the research team developed a DCFNa-loaded SMEDDS, which was embedded in a PSA patch. SMEDDS is a drug delivery system that forms fine oil-in-water emulsions upon contact with water. By encapsulating DCFNa in these emulsions, the researchers were able to increase its solubility and improve its ability to pass through the lipid-rich layers of the skin. The SMEDDS system consisted of clove oil, Tween® 80 as a surfactant, and propylene glycol as a co-surfactant, optimized to achieve maximum solubility for DCFNa.
 
The development of the transdermal patch itself involved the use of a combination of pectin and polyacrylate, which were selected for their adhesive proper ties and ability to promote drug accumulation in the skin. The patch was carefully designed using a simplex lattice experimental method to ensure optimal adhesion and drug delivery. The researchers conducted a series of tests to measure the patch's tacking and peel strength, ensuring it would remain securely attached to the skin for extended periods without causing irritation.
 
Impressive Study Findings
The study results were promising, demonstrating that the new DCFNa-loaded SMEDDS transdermal patch significantly improved the delivery of the drug compared to traditional topical formulations.
 
Key findings include:
-Enhanced Solubility: The SMEDDS formulation increased the solubility of DCFNa by approximately 18-fold compared to phosphate buffer solutions. The nano-sized droplets formed by the SMEDDS allowed for more effective dispersion of the drug in the skin.
 
-Increased Skin Permeability: The study showed a 9-fold increase in skin permeability of DCFNa when delivered through the SMEDDS patch compared to an aqueous solution. This is a significant improvement, as it allows for better absorption of the drug at the site of pain or inflammation.
 
-Superior Adhesion and Comfort: The PSA patch, containing 20% pectin and 40% polyacrylate, demonstrated excellent adhesion and was able to remain on the skin for up to 24 hours without causing irritation. This is a notable advantage over many commercial patches that may need to be reapplied frequently or cause discomfort after prolonged use.
 
-Improved Drug Accumulation: The SMEDDS-loaded PSA patch delivered twice the amount of DCFNa to the skin compared to commercial patches, offering enhanced pain relief with fewer applications.
 
-No Skin Irritation: Despite the strong adhesive properties of the patch, it did not cause any significant irritation during the study, making it a more comfortable option for patients needing long-term pain relief.
 
A Safer and More Effective Alternative
This new transdermal patch presents several advantages over existing topical formulations. By significantly improving the solubility and skin permeability of DCFNa, the SMEDDS-loaded patch offers a more effective treatment option for patients suffering from pain and inflammation. The controlled release of the drug from the patch reduces the need for frequent reapplication, making it a more convenient solution for patients. Furthermore, the patch's strong adhesion ensures that it remains securely attached to the skin, allowing for continuous drug delivery over 24 hours.
 
The biocompatibility of the materials used in the patch, including pectin and polyacrylate, ensures that it is safe for long-term use without causing irritation or discomfort. The study also highlights the potential of SMEDDS technology to enhance the transdermal delivery of other poorly soluble drugs, paving the way for further advancements in pain management and drug delivery systems.
 
Conclusion
In summary, the research conducted by Silpakorn University represents a significant breakthrough in the field of transdermal drug delivery. The development of a Diclofenac Sodium-loaded SMEDDS embedded in a PSA patch offers a safer, more effective, and patient-friendly alternative to traditional pain relief methods. By addressing the limitations of DCFNa's solubility and skin permeability, this new system has the potential to revolutionize the way pain is managed for conditions like arthritis and muscle strains. The optimized patch provides controlled drug release, superior adhesion, and enhanced patient comfort, making it a promising option for those in need of effective, long-lasting pain relief.
 
The study findings were published in the peer-reviewed Journal of Drug Delivery Science and Technology.
https://www.sciencedirect.com/science/article/abs/pii/S1773224724008645
 
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