Friday, August 26, 2011

Transdermal Drug Delivery, Transdermal Patches

Drug delivery technologies are now receiving considerable attention from pharmaceutical companies. The main purpose of developing alternative drug delivery technologies is to increase efficiency and safety of drug delivery and provide more convenience for the patient. Substantial research conducted during the past several years has lead to the development of technologies that meet the requisite criteria for delivering the drug through a non-invasive route. One of such technologies is transdermal drug delivery.

kerdi membrane

Transdermal drug delivery is the non-invasive delivery of medications from the surface of the skin - the largest and most accessible organ of the human body - through its layers, to the circulatory system. Medication delivery is carried out by a patch that is attached to the body surface. Transdermal patch is a medicated adhesive pad that is designed to release the active ingredient at a constant rate over a period of several hours to days after application to the skin. It is also called skin patch. A skin patch uses a special membrane to control the rate at which the drug contained within the patch can pass through the skin and into the bloodstream.

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The first transdermal patch was approved by the FDA in 1979. It was a patch for the treatment of motion sickness. In the mid-1980s, the pharmaceutical companies started the development of a nicotine patch to help smokers quit smoking, and within a few months at the end of 1991 and beginning of 1992 the FDA approved four nicotine patches.

Today drugs administered through skin patches include scopolamine (for motion sickness), estrogen (for menopause and to prevent osteoporosis after menopause), nitroglycerin (for angina), lidocaine to relieve the pain of shingles (herpes zoster). Non-medicated patches include thermal and cold patches, weight loss patches, nutrient patches, skin care patches (therapeutic and cosmetic), aroma patches, and patches that measure sunlight exposure.

Advantages and disadvantages of transdermal drug delivery

Transdermal drug delivery systems offer several important advantages over more traditional approaches, including:
longer duration of action resulting in a reduction in dosing frequency Increased convenience to administer drugs which would otherwise require frequent dosing improved bioavailability more uniform plasma levels reduced side effects and improved therapy due to maintenance of plasma levels up to the end of the dosing interval flexibility of terminating the drug administration by simply removing the patch from the skin Improved patient compliance and comfort via non-invasive, painless and simple application

Some of the greatest disadvantages to transdermal drug delivery are:

possibility that a local irritation at the site of application Erythema, itching, and local edema can be caused by the drug, the adhesive, or other excipients in the patch formulation
The main components of a transdermal patch are:

Transdermal patch may include the following components:

Liner - Protects the patch during storage. The liner is removed prior to use. Drug - Drug solution in direct contact with release liner Adhesive - Serves to adhere the components of the patch together along with adhering the patch to the skin Membrane - Controls the release of the drug from the reservoir and multi-layer patches Backing - Protects the patch from the outer environment
Types of transdermal patches

There are four main types of transdermal patches:

Single-layer Drug-in-Adhesive

In this system the drug is included directly within the skin-contacting adhesive. In this type of patch the adhesive layer is responsible for the releasing of the drug, and serves to adhere the various layers together, along with the entire system to the skin. The adhesive layer is surrounded by a temporary liner and a backing.

Multi-layer Drug-in-Adhesive

The Multi-layer Drug-in-Adhesive is similar to the Single-layer Drug-in-Adhesive in that the drug is incorporated directly into the adhesive. The multi-layer system adds another layer of drug-in-adhesive, usually separated by a membrane. This patch also has a temporary liner-layer and a permanent backing.

Reservoir

The Reservoir transdermal system design includes a liquid compartment containing a drug solution or suspension separated from the release liner by a semi-permeable membrane and adhesive. The adhesive component of the product can either be as a continuous layer between the membrane and the release liner or as a concentric configuration around the membrane.

Matrix

The Matrix system has a drug layer of a semisolid matrix containing a drug solution or suspension, which is in direct contact with the release liner. The adhesive layer in this patch surrounds the drug layer partially overlaying it.

The future of transdermal drug delivery

Transdermal drug delivery is theoretically ideal for many injected and orally delivered drugs, but many drugs cannot pass through the skin because of skin's low permeability. Pharmaceutical companies develop new adhesives, molecular absorption enhancers, and penetration enhancers that will enhance skin permeability and thus greatly expand the range of drugs that can be delivered transdermally.

Two of the better-known technologies that can help achieve significant skin permeation enhancement are iontophoresis and phonophoresis (sonophoresis). Iontophoresis involves passing a direct electrical current between two electrodes on the skin surface. Phonophoresis uses ultrasonic frequencies to help transfer high molecular weight drugs through the skin.

A newer and potentially more promising technology is micro needle-enhanced delivery. These systems use an array of tiny needle-like structures to open pores in the stratum corneum and facilitate drug transport. The structures are small enough that they do not reach the nerve endings, so there is no sensation of pain. These systems have been reported to greatly enhance (up to 100,000 fold) the permeation of macromolecules through skin.

Transdermal Drug Delivery, Transdermal Patches

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