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).
Advantages:
Topical and Transdermal Systems
• 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 transdermally 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 transdermally - 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).
Summary
Today, patients have a variety of treatment
options for managing their pain. Transdermal
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.
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