Obesity & Glucose-Controlling Agent Transdermal Treatments

Revolutionizing Obesity Treatment with Advanced Transdermal Delivery.

THE OBESITY MARKET

The U.S. Centers for Disease Control and Prevention reports that 2 in 5 U.S. adults have obesity. The numbers are extreme with 41.9% of U.S. adults considered obese, and 9.2% considered highly obese.

OBESITY DRUGS

There are various targets for anti-obesity drugs including GLP-1 (Glucagon like peptide) agonists, CB1 antagonists effecting the CB1 endocannabinoid receptor, and Sodium glucose cotransporter 2 (SGLT-2) inhibitors. Some of the obesity drugs available decrease appetite while others increase insulin secretion to lower blood sugar levels and protein bound glucose or inhibit reabsorption of sugar by the kidneys. A number of obesity medications are delivered subcutaneously (by needle) with newer developments providing oral administration. Current subcutaneous obesity drugs, while effective, are associated with several drawbacks. These include patient discomfort due to frequent injections, potential injection site reactions, and the need for proper storage and handling of injectable medications. Additionally, the invasive nature of subcutaneous administration can lead to reduced patient compliance, potentially compromising treatment efficacy. Oral administration has the drawback of first pass through the liver that can increase toxicity and decreases the concentration of drug in the blood stream. Oral administration also may cause interactions with food in the gut and nausea. Skinvisible has identified a system that can dispense these drugs safely and with reduced toxicity; a transdermal delivery system.

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Drug Development & Delivery

TRANSDERMAL OBESITY AND GLUCOSE-CONTROLLING

PATENTS PENDING

Skinvisible has made major advancements in the treatment of obesity and other conditions requiring glucose-controlling agents. The Company filed a provisional patent application covering its formulations that leverage the Company’s proprietary delivery technology Invisicare for the transdermal administration of obesity drugs, followed by an expansion of the initial patent to cover a greater array of glucose-controlling agents and conditions.

The need for improved administration routes for glucose-regulating medications prompted Skinvisible’s research into transdermal delivery of these therapeutic agents. The purpose of this research and development was to define a transdermal delivery system, capable of high drug throughput of obesity and glucose-controlling agents using modifications of Skinvisible Invisicare polymer delivery system. The Invisicare delivery technology was modified to enhance drug permeation and bioavailability, with permeation enhancers incorporated into the formulation.
Skinvisible’s data revealed substantial permeation of the therapeutic agents. These findings show that Invisicare technology provides non-invasive delivery of anti-obesity drugs, potentially overcoming limitations of subcutaneous and oral administration.

Following successful penetration through the skin barrier, the therapeutic agent enters circulation by the bloodstream, allowing for systemic distribution throughout the body. A transdermal delivery method may be desirable over conventional routes i.e., oral or injection due to the avoidance of systemic side effects from first pass metabolism and greater patient compliance. Transdermal delivery offers a promising alternative to drug delivery, but traditionally faces limitations in drug molecular weight and throughput. Skinvisible has made significant progress in this field with its proprietary Invisicare polymer delivery system. This technology has demonstrated potential in the transdermal administration of glucagon-like peptide-1 (GLP-1) agonists and cannabinoid receptor type 1 (CB-1) antagonists, primarily targeting obesity management and other conditions requiring glucose regulation. Of particular interest is the recent provisional patent application for transdermal obesity and glucose-controlling agents utilizing the Invisicare system. This development represents a promising avenue for non-invasive administration of metabolic regulators.

Skinvisible analyses the potential permeation of these active ingredients through the analytical method: Franz cell diffusion analysis along with long-term stability testing. Franz diffusion cells are utilized to assess the compounds’ ability to penetrate a model membrane, simulating percutaneous absorption. This in-vitro methodology provides valuable insights into the pharmacokinetic properties and potential efficacy of these actives for transdermal administration.

While only small molecules <1000 g/mol can pass through the skin, there are many smaller molecules potentially useful in the treatment of obesity that have molecular weights less than 1000 g/mol which could benefit from a transdermal Invisicare formulation. It is also believed that transdermal systems cannot deliver high drug throughput necessary for therapeutic efficacy. While traditional transdermal systems have faced challenges in delivering high drug throughput necessary for therapeutic efficacy, recent advancements by Skinvisible show very promising results, with a high ratio of release over extended periods of time.

Skinvisible has conducted Franz diffusion cell permeation studies to evaluate the transdermal delivery potential of GLP-1 agonists and cannabinoid receptor type 1 (CB1) antagonists in an Invisicare formulation. The results show a controlled and steady release over six hours resulting in up to 99% of the active delivered. Our novel Invisicare transdermal delivery system therefore has significant potential for the administration of glucose-controlling agents in obesity management, offering a competitive alternative to traditional routes of administration such as injection, oral delivery, patches, and microneedles.

Our Patents
Patent applications include:
  • Transdermal Delivery Composition for Delivery of CB-1 Receptor Antagonists and/or GLP-1 Receptor Agonists, and Method of Delivery
  • Transdermal Delivery Composition for Delivery of at Least One Glucose Controlling Agent, and Method of Delivering at Least One Glucose Controlling Agent.

INVISICARE TRANSDERMAL DELIVERY OF OBESITY AND GLUCOSE-CONTROLING AGENTS

KEY BENEFITS

Due to the emerging prominence of the endocannabinoid system, and the heightened interest in obesity drugs, the Company has modified its Invisicare technology system for transdermal delivery and has demonstrated enhanced drug permeation and increased bioavailability.
It is anticipated that the transdermal delivery of obesity and glucose-controlling agents would have the following benefits:

AVOIDS FIRST PASS / SIDE-EFFECTS

Oral medication must be processed through the GI tract then metabolized by the liver before it reaches systemic circulation. This “first pass metabolism” may result in as low as 15% of active ingredient available for systemic circulation. Transdermal application avoids first pass which may result in less side-effects.

HIGH RATIO RELEASE OVER EXTENDED TIME

Transdermal delivery of active ingredients with Invisicare can result in:

  • Efficient release of drug systemically with higher concentrations than oral delivery;
  • Extended release of drug over time.

IMPROVED PATIENT COMPLIANCE

Transdermal application with a metered dose applicator is a non-invasive delivery of drug for a patient that can be can be easily self-administered. There are no needles to inject and no pills to swallow; therefore greater patient convenience and compliance.