Pentravan™

Transdermal delivery involves the passage of therapeutic quantities of drug substances through the skin and into the general circulation for systemic effects. For transdermal drug delivery, it is considered ideal for the drug to migrate through the skin to the underlying blood supply without buildup in the dermal layers.

Transdermal delivery of drugs is effective and used to treat many different conditions. Transdermal drug delivery can be “individualized” for each patient by changing the drugs used, their concentrations, and the formulation. This type of drug delivery is routinely used for delivery of hormones, pain medication, nonsteroidal anti-inflammatory drugs (NSAIDs), antinauseant medications, and many others.

Transdermal delivery may have different advantages over other delivery systems, including:

• Avoids gastrointestinal (GI) drug absorption difficulties caused by GI pH, enzymatic activity and drug interactions with food, drink, and other orally administered drugs.
• A substitute for other routes of administration (e.g. oral administration, intravenous injection) when that route is unsuitable, as with vomiting, swallowing problems, resistant children and diarrhea.
• Avoids the first-pass effect, possibly avoiding the deactivation by digestive and liver enzymes.
• Patient acceptability. Transdermal delivery is noninvasive, avoiding the inconvenience of parenteral therapy.
• Ability to dissolve a wide range of medications with different chemical properties, making combination therapy with one transdermal cream possible.
• Provides extended therapy with a single application, improving compliance.
• Drug therapy may be terminated rapidly by removal of the application from the skin surface.1

For more information about transdermal delivery systems and their advantages, please read the article “Transdermals: the skin as part of a drug delivery system” by Allen, L.V. Jr.*

* Allen LV Jr. Transdermals: the skin as part of a drug delivery system. International Journal of Pharmaceutical compounding. 2011; 15(4): p. 308-315.

Pentravan™ is an oil-in-water emulsion with a liposomal matrix that uses the same penetration enhancing ingredients that enable it to establish a greater rate and extent of absorption of the drug than other transdermal bases. Therefore, more of the drug will become available in a shorter time to establish the effect of the therapy. Besides that, Pentravan™ is a true vanishing cream, leaving no sticky residue and providing a cosmetically elegant skin feel. Therefore, there is no need to cover the area of application to prevent transferring of the cream and to ensure effectiveness of therapy. It is preserved and fragrance-free.

After application on the skin, the drug molecules that are dispersed within the liposomes of Pentravan™ penetrate the stratum corneum through the intercellular channels. Once through the stratum corneum, drug molecules may pass through the deeper epidermal tissues and into the dermis. When the drug reaches the vascularised dermal layer, it becomes available for absorption into the systemic circulation.

A broad range of Pentravan formulations for pain management, BHRT and other therapies are available on request. Please contact Fagron to get access to these formulations.

Description: stiff, yellow cream; slight odor of lecithin.
pH: 4.0-5.5.
Yield value: 40-150 Pa.
Shelf life: 3 years.

An in vitro absorption study* with different APIs shows that Pentravan™ delivers more drug in a shorter amount of time than PLO. Comparing permeation of drugs in Pentravan™ vs. PLO: - The API in Pentravan™ reached peak permeation faster. - The amount of drug in Pentravan™ that is absorbed is pharmacologically higher. - Ketoprofen in Pentravan™ shows a 3.8 higher absorption than in PLO. - Testosterone in Pentravan™ shows a 1.7 higher absorption than in PLO. * Lehman PA, Raney SG. In vitro percutaneous absorption of Ketoprofen and Testosterone: comparison of Pluronic Lecithin Organogel vs. Pentravan cream. International Journal of Pharmaceutical Compounding. 2012; 16(43): p. 248-252.