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Ibuprofen Topical Science
 
   
     
   
     
 
Transdermal System Enhances Pain Management
 
  Steven Richeimer, M.D.
Director
USC Pain Management, USC Medical Center
Los Angeles, CA, USA


Topical pain relieving drugs are preparations applied to the skin as a cream, ointment, gel, or spray. Topical drug applications are used to help reduce inflammation below the skin surface and alleviate nerve pain. Some of these drugs are available only with a doctor's prescription and others can be purchased over-the-counter (OTC).

In 1980, the first through the skin (TTS) therapeutic, or what is now called a transdermal product, was introduced. Since then scientists around the world continue to develop safer and more expedient methods to deliver drugs, hormones, and supplements into the human body. The administration of medication and health enhancing formulations through the skin is proving to be the "delivery system of the future" (1).

Unlocking Skin Cells

Skin is the largest organ of the human body. It serves as a protective water barrier, regulates temperature, controls fluid loss, and performs many other functions important to homeostasis (healthy internal balance). Skin is composed of many layers supported by an intricate blood supply system. The blood vessels are adjacent to a framework of connective tissue, which is closely connected to bone, muscle, fascia, and fat. In addition, the skin is innervated, which means the skin contains nerve endings. These nerves carry touch, temperature, and pain signals from the skin to the spinal cord.

Scientists have developed compounds that safely expedite the delivery of medicine and other formulations through the layers of skin into the blood supply. It is thought that certain compounds help to penetrate the skin barrier by opening naturally closed channels for a period of time. Some of these compounds actually help the skin to absorb the medicine or formulation (penetration enhancers).

Rapid Dermal Delivery System

IbuCream™ [www.ibucream.com] is a novel topical pain relieving cream available over-the-counter that contains a proprietary compound called ViaDerm FMG™.

ViaDerm FMG™ is a patent-pending non-alcohol rapid dermal delivery system designed to carry active ingredients directly through the skin of the desired part of the body.

ViaDerm FMG™ is comprised of pharmaceutically-acceptable compounds and is thought to penetrate the skin barrier along the naturally occurring epidermal-dermal moisture gradient.

Topical and Transdermal Systems

Spine and pain specialists may recommend the use of a topical pain-reliever to help relieve the symptoms of osteoarthritis, rheumatoid arthritis, neck or low back sprain/strain, whiplash, muscular and joint pain, spasms, and some types of nerve pain.

Advantages:

• Cream base makes application easy and controllable.

• Onset of symptom relief is faster than oral preparations (3-8).

• Symptoms are alleviated at a steady rate and relief may last longer (3-8).

• Drugs delivered topically may need to be applied less frequently and in smaller amounts (3-8).

• Formulations diffuse through the skin and enter into the bloodstream, thereby initially bypassing the liver, stomach, and digestive system (called 'first pass'). Many systemic (whole body) side effects, such as irritated stomach lining, may be diminished or eliminated.

• Studies have shown that when formulations are delivered topically - as much as 95% reach the target cells (e.g. muscle). Results from oral preparations delivered to a targeted site of pain are less than 5% (1).

Uses for ViaDerm FMG™

The future of ViaDerm FMG™'s use in pharmacologic and standardized herbal products is great. Currently used in IbuCream™ (www.ibucream.com) as a skin penetration enhancer for ibuprofen and lidocaine, ViaDerm FMG™ is designed to rapidly deliver drugs and other formulations to treat muscle spasms, tendonitis, myofascitis, intra-articular inflammation, rheumatoid conditions, trigger points and the elusive fibromyalgia.

Initial in vivo anecdotes support the use of ViaDerm FMG™ to reduce oral side effects and dosage, and to increase tolerability and compliance. [Cosmetics enhancement: Genie's Secret Cream]

Summary

Today, patients have a variety of treatment options for managing their pain. Topical pain relief products are not only gaining in popularity, but medical science is discovering innovative ways to broaden their use. Scientists from the University of Strathclyde and University of Glasgow stated (2),

"It is conceivable that the future of the industry may lie in not just striving to make equivalent products to the branded parent medicines, but actually manufacturing improved medicines."

References:

1. Department of Pharmacology, University of Dublin.

2. Uchegbu IF, Schätzlein AG. "Generics Manufacturers Should Exploit Drug Delivery Technologies for Improved Therapeutics." Business Briefing: Pharmagenerics 2002.

3. Kleinbloesem CH, Quwerkerk M, Spitznagel W, Wilkinson FE, Kaiser RR. "Pharmacokinetics and Bioavailability of Percutaneous Ibuprofen." Clin-Pharma Research Ltd., Birsfelden, Switzerland. Arzneimittelforschung. 1995 Oct; 45(10):1117-21.

4. Hadgraft J, Whitefield M. Rosher PH. "Skin Penetration of Topical Formulations of Ibuprofen 5%: An in vitro Comparative Study." NRI, University of Greenwich, Kent, UK. Skin Pharmacol Appl Skin Physiol. 2003 May-Jun; 16(3):137-42.

5. Whitefield M, O'Kane CJ, Anderson S. "Comparative Efficacy of a Proprietary Topical Ibuprofen Gel and Oral Ibuprofen in Acute Soft Tissue Injuries: A Randomized, Double-Blind Study." Dermal Laboratories Ltd., Gosmore, Hitchin, UK. J Clin Pharm Ther. 2002 Dec; 27(6):409-17.

6. Machen J, Whitefield M. "Efficacy of a Proprietary Ibuprofen Gel in Soft Tissue Injuries: A Randomised, Double-Blind, Placebo-Controlled Study." Bancroft, Hitchin, Herts, UK. Int J Clin Pract. 2002 Mar; 56(2):102-6.

7. Rovensky J, Micekova D, Gubzova Z, Fimmers R, Lenhard G, Vogtle-Junkert U, Schreyger F. "Treatment of Knee Osteoarthritis with a Topical Non-Steroidal Anti-Inflammatory Drug. Results of a Randomized, Double-Blind, Placebo-Controlled Study on the Efficacy and Safety of a 5% Ibuprofen Cream." Institute for Rheumatic Diseases, Nabrezie I, Krasku 4, 921 01, Piest'any, Slovak Republic. Drugs Exp Clin Res. 2001; 27(5-6):209-21.

8. Campbell J, Dunn T. "Evaluation of Topical Ibuprofen Cream in the Treatment of Acute Ankle Sprains." Accident and Emergency Department, St. John's Hospital at Howden, Livingston. J Accid Emerg Med. 1994 Sep; 11(3):178-82.
 
     
 
 
     
   
     
  Topically applied NSAIDs have a superior safety profile to oral formulations.” Oral versus topical NSAIDs in rheumatic diseases: a comparison.  
     
 
 
 
 
  The blood levels of topical NSAIDs are extremely low with no systemic side effects, especially no gastric toxicity…” Use of topical non-steroidal anti-inflammatory drugs in aggravated and decompensated arthroses.  
     
 
 
 
 
  In conclusion the percutaneous application of certain NSAIDs has become a well established therapeutic regimen in painful osteoarthrosis and in all other inflammatory degenerative and posttraumatic alterations of soft tissue structures.” Percutaneous therapy of painful arthritis .  
     
 
 
 
 
  CONCLUSION: Topical non-steroidal anti-inflammatory drugs are effective in relieving pain in acute and chronic conditions.” Quantitative systematic review of topically applied non-steroidal anti-inflammatory drugs.  
     
 
 
 
 
 

 
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