Fast-Dissolving Freeze Dried Sublingual Wafer as a Novel Drug Delivery System

Currently, active compounds (e.g. pharmaceutical and/or nutraceutical active ingredients) are administered intravenously, intramuscularly or orally. These conventional methods of administration have their own shortcomings. For example, intravenous administration often requires an expensive clinical setting, is invasive, painful and not suitable for individuals who have a phobia of needles. Oral administration (e.g. via the consumption of capsules, tablets, mixtures and suspensions) is also not a suitable method for the delivery of active compounds which are effectively lost during hepatic (first-pass liver metabolism) and/or gastrointestinal metabolism, a process that affects the bioavailability of numerous active compounds when ingested orally. Oral ingestion can also delay the onset of a therapeutic effect by several hours.

The technology is a proprietary wafer formulation that allows pharmaceutical and/or nutraceutical active compounds to be administered sublingually, allowing for these compounds to be delivered safely, rapidly and conveniently into the blood stream. The technology is a superior mode of delivery as it reduces the effects of hepatic and gastrointestinal metabolism. Using the technology, sublingual delivery increases the rate and predictability of already approved drugs, resulting in an increase of new and improved clinical applications.

The technology is a non-invasive proprietary sublingual wafer that was developed to address the sub-optimal characteristics of currently available drug delivery technologies such as the intravenous, intramuscular and oral routes of administration used in the treatment of acute medical conditions or symptoms.  The sublingual wafer, when introduced to the moist environment of the oral cavity, disintegrates rapidly and releases the active compounds for absorption directly into an individual’s systemic circulation via the jugular vein. This allows the active compounds to bypass the “corrosive” gastrointestinal tract and the hepatic first-pass effect.

The nature of the wafer matrix also allows the use of pH control to set the optimum pH for the drug’s absorption, or long-term stability. Other additives to enhance the therapeutic effect can be readily added, allowing great flexibility in the formulation to suit each active.

The sublingual route produces a fast and reliable onset of pharmaceutical and/or therapeutic action of the active compounds, and such rapid and superior absorption characteristics provides a higher bioavailability of the active compounds (achieving blood therapeutic levels similar to IV administration) and has the potential to lower the administered dose and reduce concurrent side effects (lower peak blood concentration, C_max compared to IV administration) in an individual.

Wafer administration has been reported to be tolerable with no after-taste, leaves behind no residue or grittiness under the tongue and hence reduces the urge to swallow. 

The technology may be applied to numerous pharmaceutical and nutraceutical active compounds. (Note: TRL level may be higher for certain actives.)

It is ideal for partners and/or licensees seeking to:

• Enhance the pharmacokinetics and/or pharmacodynamics of their current products;
• Enhance and differentiate their current products from other market competitors by leveraging on our revolutionary delivery platform;
• Administer actives that require fast delivery (comparable to IV administration); and
• Administer actives that cannot otherwise be administered orally (e.g. due to loss during hepatic and/or gastrointestinal metabolism).

The technology is perfectly poised to meet the increasing demand for convenient, painless, efficient and cost-effective delivery of pharmaceutical and nutraceutical active compounds.

Customer benefits include:

• Superior (faster, easier, painless, more convenient and efficient) method of administration;
• Rapid absorption and onset of action;
• Increased bioavailability of active compounds administered sublingually;
• Cost-effective and with a better storage and side-effect profile;
• Protection from counterfeiting (as a result of patent protection and proprietary formulation and manufacturing processes); and
• High level of end-user compliance and preference:

• • For healthcare workers – it will help prevent risks and injuries associated with needle-stick, and would therefore minimize occupational health and safety hazards; and
  • For patients/individuals – would be suitable for individuals who have phobias and inhibitions associated with conventional methods of administration (e.g. patients with a phobia of needles, small children, or ill or aged adults, who are unable to swallow capsules or tablets).
  • Unit-dose system (accurate dose no need to measure an aliquot for a dose) where you can carry/store your medicine in a limited space (handbag, cupboard etc) unlike bulky mixture/suspension bottles (50, 100, 200 or even 500mL, inaccurate dose measurement).