Patented Topicon™ Transdermal Delivery Technology

The patented Topicon™ platform technology offers a convenient and painless alternative to frequent injections, using a completely passive formulation with no needles or microneedles. It was initially designed to be the first thermosensitive drug patch (ThermoMatrix™) capable of maintaining the stability of a perishable large molecule drug in a solid matrix at room temperature. Upon application to the skin, the formulation melts into a dermoadhesive gel that serves as a drug reservoir capable of maintaining continuous and consistent transdermal delivery to achieve drug bioavailability and a therapeutic response comparable to that of subcutaneous needle injection. Topicon™ can be used as a gel for local topical delivery of drugs to treat skin conditions including fungal nail infections. We are testing Topicon drops for drug delivery into the eye or ear canal.

Topicon™ is predicted to be a versatile technology with many potential applications including the delivery of therapeutic hormones, growth factors, cytokines, or antibodies. Treatment for bacterial, viral, or parasitic infections will only require self-application of a patch that will deliver drugs continuously and consistently for the prescribed period of time. No more missed pills (or pill bottles). Patch delivery of drugs is ideal for children and adults. Imagine treatment, prevention, or eradication of malaria with simple and convenient extended-wear Truepatch™ products. Fixed-dose combination drug delivery may be possible, which will simplify complex chronic drug regimens to treat TB and HIV, or to manage cardiovascular, psychiatric, neurologic, or neurodegenerative conditions. Our scientists have already considered the possibility of modifying Topicon formulations for use as a chemical penetration retardant for use as a counter measure against exposure to toxins from chemical spills or protection during chemical warfare. The growing field of space medicine may benefit from patch administration in general as an alternative to current injectable drugs. Specific applications may include a once weekly TruePatch™ to protect against the effects of chronic space radiation exposure would address a significant health concern during prolonged missions and deep space exploration and colonization.

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TruePatch™ for Insulin Therapy

The first TruePatch™ product is a needle-free multi-day basal insulin patch that will provide a simple, convenient, and affordable alternative to daily needle injection that allows for fine dose adjustment and achieves continuous and consistent insulin therapy. Reducing the complexity and frequency of administration by subcutaneous needle injection by converting to a convenient TruePatch™ to provide all basal insulin requirements is expected to improve medication adherence, reduce complications, and improve clinical outcomes and quality of life for people with diabetes. Prometheon is developing its flagship basal insulin TruePatch™ product as the first of an entire TopiconDM™ Diabetes Therapy product line for transdermal delivery of drugs to treat type 1 and type 2 diabetes mellitus, including a pre-meal rapid-acting bolus insulin TruePatch™. 

Drug Delivery Across Other Physical Barriers

Our patented Topicon formulation may have broader applications beyond once weekly needle-free passive transdermal drug delivery of peptide/protein drugs for systemic therapy. Topicon may have the ability to deliver many classes of drugs both large and small. Some TruePatch™ products may be able to provide super extended-wear (up to 2-3 weeks) needs to achieve prolonged therapeutic blood levels with a single convenient patch. We are exploring the ability of Topicon™ gel formulations applied as drops to deliver drugs passively across physical barriers other than skin to treat localized diseases. These include eye drops (transcorneal delivery), ear drops (transtympanic delivery), and finger and toe nail drops (transungual delivery). Tissue and animal models already exist that will allow us to generate proof-of-concept to support Topicon™-mediated delivery of drug therapy across such barriers. 

 

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HeatWave™ for Extreme Temperatures

Lack of access to refrigerated transport and storage—a major problem in developing countries as well as during emergencies and power failures in developed countries—causes perishable drugs to become heat-inactivated, resulting in the loss of costly injectable drugs for disease prevention or therapy such as vaccines and antibiotics administered as intravenous solutions. Perishable peptide drugs such as insulin must be kept within an appropriate temperature range (typically refrigerated at 4 °C) in order to maintain therapeutic effectiveness. Equatorial regions of the world have mean annual average temperatures that exceed 32 ° with temperature spikes that are much higher. In the case of insulin, using vials that have become inactivated by exposure to direct heat or sunlight can result in ineffective blood glucose control and diabetic complications. To eliminate this cold chain issue, Prometheon is developing a heat-resistant patch (HeatWave™) that will maintain the stability and therapeutic effectiveness of a perishable drug until it is activated just before application to the skin.

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Future Directions

Obesity has reached epidemic proportions globally and is a major contributor to the global burden of chronic disease and disability. Often coexisting in developing countries with under-nutrition, obesity affects virtually all ages and socioeconomic groups. To address the global pandemic of obesity and associated type 2 diabetes, Prometheon’s Novel Drug Discovery and Development Program is developing a new class of anti-obesity drugs based on discoveries made by a research team led by Dr. Stephen Hsu and co-published in Nature Medicine with collaborators at the Joslin Diabetes Center (Harvard Medical School) and other international research teams. Dr. Hsu continues to lead this effort using a variety of approaches.