The Benefits of Sublingual Delivery – How Manufacturers Are Meeting Demand

Sublingual drug delivery, where a drug is positioned under the tongue for absorption, offers various advantages over the conventional oral route. Manufacturers are actively innovating to meet the growing demand for this beneficial delivery method.

Benefits of Sublingual Delivery

  • Quick Onset of Action
    The region under the tongue is highly vascular, meaning drugs absorbed here bypass the gastrointestinal tract and liver, reaching the bloodstream directly. This results in a much quicker onset of therapeutic effects, which is crucial in cases requiring immediate relief.
  • Evading First-Pass Metabolism
    Swallowed drugs pass through the liver before entering the systemic circulation. The liver enzymes break down most of the drug, lowering its bioavailability and potency. Sublingual administration bypasses this process, leading to increased bioavailability and allowing for lower doses to produce the desired effect.
  • Better Bioavailability
    Because first-pass metabolism is avoided and drugs are absorbed directly into the bloodstream, a larger proportion of the drug reaches its site of action, leading to better bioavailability.
  • Convenience and Patient Compliance
    • No Swallowing Involved: This is beneficial for patients who have difficulty swallowing, such as children, the elderly, or those with specific medical conditions.
    • No Water Required: Sublingual drugs can be taken anytime, anywhere, without the need for water, offering great convenience.
    • Non-Invasive and Painless: Compared to injections, sublingual delivery is painless and non-invasive, improving patient compliance.
  • Less Gastrointestinal Irritation
    Since the medication bypasses the stomach, there is less chance of gastrointestinal upset or interactions with food and other drugs.
  • Potential for Dose Reduction
    Due to enhanced bioavailability, a lesser dose of the drug can be effective, potentially reducing side effects.

How Manufacturers Are Addressing Demand

Pharmaceutical and nutraceutical manufacturers are meeting the demand for sublingual delivery through advances in formulation and manufacturing.

  • Advanced Formulations
  • Patient-Centric Design
    Focusing on patient compliance, manufacturers are emphasizing the creation of palatable formulations with good mouthfeel. This includes addressing taste masking for bitter drugs.
  • Research and Development
    Ongoing research is being conducted to identify more drugs suitable for sublingual delivery, study the factors influencing absorption, and develop new models for permeation to enhance formulation development. This also includes exploring the potential for sublingual vaccines.

The trend toward patient-centric healthcare, combined with the natural benefits of bypassing the gastrointestinal tract and liver, is driving substantial innovation and investment in sublingual drug delivery technologies.

Zeon Lifesciences' Role in Sublingual Delivery

Zeon Lifesciences is actively involved in developing and manufacturing sublingual sprays for the nutraceutical market, both through their own offerings and in collaboration with international partners. These sprays are designed for rapid absorption of key nutrients and are positioned as innovative solutions for addressing daily nutrient requirements.

References

https://www.sciencedirect.com/science/article/abs/pii/S1773224719300401 

Hua, S. (2019). Advances in nanoparticulate drug delivery approaches for sublingual and buccal administration. Frontiers in Pharmacology, 10. https://doi.org/10.3389/fphar.2019.01328 

Ahmad, A., Akhtar, J., Ahmad, M., Wasim, R., & Khan, M. I. (2025). Drug delivery approaches for buccal and sublingual administration. Drug Research. https://doi.org/10.1055/a-2560-9884 

Rawas-Qalaji, M., Thu, H. E., & Hussain, Z. (2022).Oromucosal delivery of macromolecules: Challenges and recent developments to improve bioavailability. Journal of Controlled Release, 352, 726–746. https://doi.org/10.1016/j.jconrel.2022.10.059 

Pratap-Singh, A., Guo, Y., Baldelli, A., & Singh, A. (2023). Concept for a Unidirectional Release Mucoadhesive Buccal Tablet for Oral Delivery of Antidiabetic Peptide Drugs Such as Insulin, Glucagon-like Peptide 1 (GLP-1), and their Analogs. Pharmaceutics, 15(9), 2265. https://doi.org/10.3390/pharmaceutics15092265https://pubmed.ncbi.nlm.nih.gov/28323100/ 

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