Skip to main content

Sublingual Route of Drug Delivery

  • Living reference work entry
  • First Online:
The ADME Encyclopedia
  • 56 Accesses

Overview on the Sublingual Drug Administration

Sublingual drug administration is the process of placing a dosage form (usually tablets, lozenges, or strips) under the tongue where it dissolves completely, allowing the drug to directly reach systemic blood circulation upon absorption. Sublingual drops and sprays are also administered via this route. Many small- and macromolecules have been successfully absorbed following their sublingual administration [1,2,3]. Sublingual administration is commonly used for both local and systemic drug treatments [4]. Protection of drugs against destruction by the gastric acid and the intestinal and hepatic enzymes is achieved by this route. The delivery of a drug through the sublingual route is favorable due to the substantially rich blood and lymphatic vessel supply.

As with other routes of administration, drug delivery and absorption from this route depend on the drug permeability across the sublingual mucosa, the drug physicochemical properties, and...

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Institutional subscriptions

References

  1. Shotan A, Brill Z, Matetzky S, Shachar A, Feigenberger Z, Hod H, et al. Pain scoring – a method for assessing acute antianginal therapy comparison of the response to acute sublingual administration of an isosorbide dinitrate tablet, isosorbide dinitrate spray and nitroglycerin spray in unstable angina. Cardiology [Internet]. 1998 Mar [cited 2020 Jun 17];89(3):163–9. Available from: http://www.ncbi.nlm.nih.gov/pubmed/9570429.

  2. Ripamonti C, Bruera E. Rectal, buccal, and sublingual narcotics for the management of cancer pain. J Palliat Care [Internet]. 1991 [cited 2020 Jun 17];7(1):30–5. Available from: http://www.ncbi.nlm.nih.gov/pubmed/2045992.

  3. Miller BE, De Souza MJ, Slade K, Luciano AA. Sublingual administration of micronized estradiol and progesterone, with and without micronized testosterone: effect on biochemical markers of bone metabolism and bone mineral density. Menopause [Internet]. 2000 [cited 2020 Jun 17];7(5):318–26. Available from: http://www.ncbi.nlm.nih.gov/pubmed/10993031.

  4. Thompson IO, van der Bijl P, van Wyk CW, van Eyk AD. A comparative light-microscopic, electron-microscopic and chemical study of human vaginal and buccal epithelium. Arch Oral Biol [Internet]. 2001 Dec [cited 2020 Jun 16];46(12):1091–8. Available from: http://www.ncbi.nlm.nih.gov/pubmed/11684027.

  5. Hua S. Advances in nanoparticulate drug delivery approaches for sublingual and buccal administration. Front Pharmacol [Internet]. 2019 [cited 2020 Jun 17];10:1328. Available from: http://www.ncbi.nlm.nih.gov/pubmed/31827435.

  6. MA A, MA T. Salivary gland emergencies. Emerg Med Clin North Am [Internet]. 2013 [cited 2020 Jun 15];31(2). Available from: https://pubmed.ncbi.nlm.nih.gov/23601484/

  7. Jensen Steven D, Cao D. Oral PH and buffering capacity modifiers. Vol. 2011. PCT/US2O11/030067, 2011.

    Google Scholar 

  8. Khan AB, Kingsley T, Caroline P. Sublingual tablets and the benefits of the sublingual route of administration [Internet]. 16, J Pharm Res. Krupanidhi College of Pharmacy; 2017 [cited 2020 Jun 17];257–267. Available from: http://52.172.159.94/index.php/kpc/article/view/118766/81984

  9. Gibbins HL, Yakubov GE, Proctor GB, Wilson S, Carpenter GH. What interactions drive the salivary mucosal pellicle formation? Colloids Surf B Biointerfaces. 2014;120:184–92.

    Article  CAS  Google Scholar 

  10. Kullaa-Mikkonen A, Mikkonen M, Kotilainen R. The pH of stimulated and resting saliva in different morphologic forms of the tongue surface in a young population. Oral Surg Oral Med Oral Pathol. 1982;53(5):466–8.

    Article  CAS  Google Scholar 

  11. Walton RP. Absorption of drugs through the oral mucosa. III. Fat-water solubility coefficient of alkaloids. Exp Biol Med [Internet]. 1935 Jun 1 [cited 2020 Jun 20];32(9):1488–92. Available from: http://ebm.sagepub.com/lookup/doi/10.3181/00379727-32-8147C

  12. Beckett AH, Moffat AC. Correlation of partition coefficients in n-heptane-aqueous systems with buccal absorption data for a series of amines and acids. J Pharm Pharmacol [Internet]. 1969 Dec [cited 2020 Jul 5];21:Suppl:144S+. Available from: http://www.ncbi.nlm.nih.gov/pubmed/4391148.

  13. De Boer AG, De Leede LGJ, Breimer DD. Drug absorption by sublingual and rectal routes. Br J Anaesth. 1984;56(1):69–82.

    Article  Google Scholar 

  14. Yu ASL. Paracellular transport as a strategy for energy conservation by multicellular organisms? [Internet]. Tissue Barriers. Taylor and Francis Inc. 2017 [cited 2020 Dec 4];5. Available from: https://pubmed.ncbi.nlm.nih.gov/28452575/

  15. Muheem A, Shakeel F, Jahangir MA, Anwar M, Mallick N, Jain GK, et al. A review on the strategies for oral delivery of proteins and peptides and their clinical perspectives [Internet]. Saudi Pharm J. Elsevier B.V.; 2016 [cited 2020 Aug 9];24:413–28. Available from: https://pubmed.ncbi.nlm.nih.gov/27330372/

  16. Senel S, Kremer M, Katalin N, Squier C. Delivery of bioactive peptides and proteins across oral (buccal) mucosa. Curr Pharm Biotechnol [Internet]. 2005 Mar 25 [cited 2020 Dec 4];2(2):175–86. Available from: https://pubmed.ncbi.nlm.nih.gov/11480421/

  17. Agarwal V, Khan MA. Intestinal transport of insulin. Evidence of active transport for. Pharm. Technol [Internet]. 2001;25(10):76–90. Available from: www.pharmtech.com

    CAS  Google Scholar 

  18. Supervía A, Pedro-Botet J, Nogués X, Echarte JL, Mínguez S, Iglesias ML, et al. Piroxicam fast-dissolving dosage form vs diclofenac sodium in the treatment of acute renal colic: a double-blind controlled trial. Br J Urol [Internet]. 1998 Jan 1 [cited 2020 Jul 6];81(1):27–30. Available from: http://www.ncbi.nlm.nih.gov/pubmed/9467472.

  19. Takada K. Quick-absorbable sublingual pharmaceutical for psychotropic agent. JP21596892A, 1992.

    Google Scholar 

  20. Rachid O, Rawas-Qalaji M, Simons FER, Simons KJ. Dissolution testing of sublingual tablets: a novel in vitro method. AAPS PharmSciTech [Internet]. 2011 [cited 2020 Aug 1];12(2):544–52. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3134647/

  21. Al-Ghananeem AM, Malkawi AH, Crooks PA. Effect of pH on sublingual absorption of oxycodone hydrochloride. AAPS PharmSciTech [Internet]. 2006 Mar 10 [cited 2020 Aug 4];7(1):E163. Available from: http://www.aapspharmscitech.org

  22. Bayrak Z, Tas C, Tasdemir U, Erol H, Ozkan CK, Savaser A, et al. Formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers: in vitro and in vivo evaluation. Eur J Pharm Biopharm [Internet]. 2011;78(3):499–505. Available from: https://doi.org/10.1016/j.ejpb.2011.02.014

  23. Kenny. United States patent (19) 11 patent number: 5,348,136. 1993. p. 1992–5.

    Google Scholar 

  24. Zhu C, Estrada M, White J, Lal M. Heat-stable sublingual oxytocin tablets as a potential needle-free approach for preventing postpartum hemorrhage in low-resource settings. Drug Deliv Transl Res [Internet]. 2018 Feb 12 [cited 2020 Aug 4];8(3):853–6. Available from: https://doi.org/10.1007/s13346-017-0471-7.

  25. Repka MA, Battu SK, Upadhye SB, Thumma S, Crowley MM, Zhang F, et al. Pharmaceutical applications of hot-melt extrusion: Part II. Drug Dev Ind Pharm [Internet]. 2007 Jan 25 [cited 2020 Aug 4];33(10):1043–57. Available from: https://pubmed.ncbi.nlm.nih.gov/17963112/#:~:text=Hot%2Dmelt%20extrusion%20is%20an,modified%2C%20and%20targeted%20drug%20delivery.

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Tarek A. Ahmed .

Section Editor information

Rights and permissions

Reprints and permissions

Copyright information

© 2021 Springer Nature Switzerland AG

About this entry

Check for updates. Verify currency and authenticity via CrossMark

Cite this entry

Ahmed, T.A., El-Say, K.M. (2021). Sublingual Route of Drug Delivery. In: The ADME Encyclopedia. Springer, Cham. https://doi.org/10.1007/978-3-030-51519-5_95-1

Download citation

  • DOI: https://doi.org/10.1007/978-3-030-51519-5_95-1

  • Received:

  • Accepted:

  • Published:

  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-030-51519-5

  • Online ISBN: 978-3-030-51519-5

  • eBook Packages: Springer Reference Biomedicine and Life SciencesReference Module Biomedical and Life Sciences

Publish with us

Policies and ethics