Linker Microemulsions as a Transdermal Drug Delivery Vehicle
Project Number
1452
Description
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:
- Lecithin (extracted from soybean or other source),
- A lipophilic additive such as long chain alcohol (C10 or higher) or long chain fatty acid, monoglyceride, or sorbitol ester
- A hydrophilic additive containing C6 – C9 fatty acids partially saponified
- A C8 – C20 fatty acid ester; and
- 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.
