BACKGROUND
Self-Micro Emulsifying Drug Delivery System (SMEDDS) is an advanced lipid-based delivery system composed of an isotropic mixture of surfactants and oils that rapidly and spontaneously assemble into microemulsions (5-150 nm) upon exposure to water with a gentle agitation. These features enable enhanced delivery and quick absorption of hydrophobic bioactive compound through gastrointestinal tract and epithelial tissues. SMEDDS are easy to manufacture, offer high loading capacities, and have a long shelf life.
Biocompatible and fully dilutable SMEDDS are the next generation of SMEDDS that are produced by using natural/plant-based excipients, rather than PEGs and short chain alcohols. However, designing SMEDDS is a challenging task because it requires matching the hydrophobic and polar nature of the active with the surfactant and solvent used.
TECHNOLOGY OVERVIEW
Researchers at the University of Toronto had previously developed alcohol-free lecithin-based microemulsions for a wide range of applications (US9918934B2). The present invention builds upon this initial technology by providing a water-free, fully dilutable SMEDDS that can solubilize and deliver poorly water-soluble polar active ingredients. This delivery system is composed of GRASS and/or FDA-approved ingredients such as lecithin as the main surfactant, a hydrophilic linker, and a carrier oil. The interfacial properties of this microemulsion systems are engineered to achieve larger and/or faster solubilization, absorption/penetration.
This technology platform is designed in three physical forms: liquid concentrate, dry powder, and semi-solid gel for different applications to provide tunable release profiles (immediate, delayed, and controlled release. The technology is backed up by a equation of state (the Net-Average Curvature or NAC) for surfactant-oil-water (SOW) systems that is used to customize the formulation to the active and delivery conditions.
COMPETITIVE ADVANTAGE
- Biocompatible ingredients: All the excipients are designated by FDA either GRAS or additive status without the use PEGs
- Encapsulates water-insoluble bioactive compounds
- Fully dilutable in water and biological fluids (e.g., gastrointestinal fluids)
- Easily and economically scalable
- No need for specialized high shear equipment to load the drug. Mild mixing is sufficient to produce delivery systems.
- Flexible delivery modalities: Topical, transdermal, oral, trans-nasal, buccal, vaginal, subcutaneous, nasal, and ophthalmic routes of administration
- Higher Bioavailability, shorter onset time and partial bypassing 1st hepatic metabolism
APPLICATIONS
- Food and dietary supplements, cosmetics, cannabinoids, agricultural bio-actives, and pharmaceuticals.
INTELLECTUAL PROPERTY STATUS
- PCT Application (June. 2022)
PROJECT STATUS
This novel SMEDDS has been tested/evaluated and used to encapsulate a variety of hydrophobic bioactive compounds including pharmaceuticals (ibuprofen), nutraceuticals (b-carotene), cannabinoids (CBD, THC), terpenes, and supplements (curcumin, melatonin). In vitro studies demonstrated the cumulative transdermal permeation of model drugs through excised pig skin. In vivo studies in rats were demonstrated quick uptake and higher accumulation of ibuprofen and CBD in the plasma.
COMMERCIALIZATION
Through a licensing agreement, the technology has been adopted and marketed by “Micellae Delivery Systems” to enhance the solubility and bioavailability of cannabinoids.
We are seeking similar arrangements for partnerships to commercialize the technology for other pharmaceuticals (type II & IV BCS drugs) and bioactive compounds.
