Sublingual Drug Delivery

Sublingual drug delivery, administered under the tongue, offers a pathway for rapid absorption into the systemic circulation, making it especially valuable for treatments requiring immediate effects. This mode of delivery holds promise for individuals with compromised gastrointestinal function or difficulty swallowing, offering a convenient and effective alternative route for drug administration.

Integral BioSystems scientists have expertise in developing sublingual dose forms. Contact us for a discussion.

Mechanism of Drug Absorption via Sublingual Tissue

Sublingual drug delivery is drug administration under the tongue. This mode of delivery refers to a method of administering substances can result in rapid absorption into the systemic circulation. This is especially relevant in indications that necessitate immediate effect upon dosing. Individuals with compromised gastro-intestinal functionality can benefit from this route. Patients with compromised digestion and with difficulty swallowing can benefit from medicines delivered in this route.

What Drugs are Appropriate for Sublingual Drug Delivery

  • Cardiovascular drugs, steroids, some barbiturates and enzymes.
  • Vitamins and Minerals
  • Drug substances with doses < 20 mg
  • No bitter taste
  • Small to moderate molecular weight 
  • Good stability in water and saliva

Factors Affecting Sublingual Absorption of Drugs

  • Lipophilicity of drug: For a drug to be absorbed sublingually, the drug must have higher lipid solubility, with a log P ideally in the range 2-3. 
  • Solubility in Sublingual/ Buccal Fluids: The drug should be soluble in aqueous buccal fluids i.e. biphasic solubility of drug is necessary for absorption.
  • pH-and-pKa of the Saliva: As the mean pH of the saliva is 6.0, this pH favors the absorption of drugs which remain unionized. 
  • Binding-to-oral-mucosa: Systemic availability of drugs that bind to oral mucosa is poor. 
  • Thickness of oral epithelium: As the thickness of sublingual epithelium is 100200 μm which is less as compared to buccal thickness. So the absorption of drugs is faster due to thinner epithelium and also the immersion of drug in smaller volume of saliva. 
  • Oil-to-water-partition coefficient: Compounds with favorable oiltowater partition coefficients are readily absorbed through the oral mucosa. The ideal log P should be ~2-3. 

CRO Services for Sublingual Drug Delivery

Integral BioSystems offers quality contract research organization services in pre-clinical stage pharmaceutical research and development at a competitive price and turnaround time. Learn more about our CRO services > 

Ready to explore the potential of sublingual drug delivery for your therapeutic compounds? Contact Integral BioSystems today to collaborate with our expert team in optimizing drug formulations for rapid and efficient absorption via sublingual tissue. Let’s work together to unlock the benefits of this innovative drug delivery route and enhance patient outcomes. Take the next step towards maximizing therapeutic efficacy with Integral BioSystems as your trusted partner!