Linker Microemulsions as a Transdermal Drug Delivery Vehicle
The ChallengeA key challenge in developing an effective transdermal delivery system for hydrophobic compounds, involves the creation of formulations that balance high permeability of the stratum corneum barrier with minimal skin irritation. Because of their small droplet size, high oil solubilization capacity and large interfacial area, microemulsions have demonstrated a greater adsorption/penetration of hydrophobic actives when compared to conventional emulsions. Unfortunately, toxicity issues associated with the types of surfactants and cosurfactants used in the past have limited their application, especially in cosmeceutical formulations.
The Solution
The development of formulations based on low-toxicity and/or natural ingredients represents a clear solution to this problem, especially for longer-term or continual use applications common to the cosmetics industry. We have now developed unique microemulsion formulations based on natural, low-toxicity ingredients that demonstrate superior permeability and delivery of hydrophobic active components.
The Technology
We have developed a novel formulation for biocompatible microemulsions for use as delivery vehicles for active ingredients in transdermal, topical and oral delivery. The formulation is based on five basic ingredients: (1) lecithin (extracted from soybean or other source), a (2) lipophilic additive such as long chain alcohol (C10 or higher) or long chain fatty acid, monoglyceride, or sorbitol ester; (3) a hydrophilic additive containing C6 – C9 fatty acids partially saponified; (4) a C8 – C20 fatty acid ester; and (5) water. Particular combinations of these ingredients, at specific ratios, yield thermodynamically stable microemulsions capable of increasing the solubility (in isotonic solutions) of hydrophobic drugs such as lidocaine, and alpha-tocopherol acetate by more than 20 fold. The increased solubility produces an increase in the absorption and permeation of active ingredients through the epithelial tissue without significant cytotoxic side effects. In addition to superior performance, two important features of this technology are that all compounds used in the present formulation are found on the FDA GRAS list and that (relevant to the cosmetics industry) the formulation produces a transparent microemulsion.
Opportunity
Our technology represents an effective and novel approach to transdermal drug delivery, with many additional benefits. Accordingly we have filed a provisional patent at the USPTO in November 2006. As such, this is the ideal opportunity for companies with both cosmetic and pharmaceutical interests looking for effective differentiated delivery strategies. The Innovations Group at the University of Toronto is seeking a partner to license this IP.
Type of Offer: Licensing
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