Transmucosal drug delivery refers to the route of drug administration where the drug molecules enter specific tissues through or across the mucosal membrane. These include routes such as buccal, nasal, vaginal, rectal, ocular, sublingual route etc.
What is transmucosal route of drug delivery?
For example, the transmucosal route has been studied as one of the primary methods of delivery in the oral cavity. This approach utilizes the oral mucosa as a means of introducing systemic agents,1 and can be distinguished from mucosal drug delivery, as the latter aims to deliver drugs locally, rather than systemically.1
What are the advantages of transmucosal delivery?
Transmucosal drug delivery may allow dental teams to offer minimal sedation and more comfortable local injections. It also requires less equipment than some delivery methods, making it a cost-effective alternative. Yet, while there are advantages to this modality, there are also restrictions to developing drugs for transmucosal delivery.
Can the oral cavity be used for transmucosal drug delivery?
The oral cavity can be utilized for transmucosal delivery, and the challenges of limited surface area and salivary action can be overcome with efficient agents and appropriate administration. 1. Transmucosal drug delivery may allow dental teams to offer minimal sedation and more comfortable local injections.
What are the advantages of oral mucosal drug delivery?
Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods. Because the oral mucosa is highly vascularised, drugs that are absorbed through the oral mucosa directly enter the systemic circulation, bypassing th …
What is TR146 cell lineage?
The cell lineage known as TR146 was created from buccal mucosa of a squamous cell carcinoma and was originally developed as an in vitro model for buccal mucosa.1 The barrier function of this cell lineage was noted to be less than that of porcine or human tissues.1 Some similarities between TR146 and porcine mucosa have been reported during in vitro research utilizing nicotine.6 More recently, metoprolol has shown similarities in porcine buccal mucosa and TR146, as noted by teams conducting in vitro and in vivo porcine studies.1 These discoveries suggest cell culture models may be an innovative approach in the development of transmucosal drug delivery.1,5
What is the oral cavity?
As noted, the oral cavity consists of various structures (Figure 1), such as the oral mucosa or lining within the oral cavity, which includes sublingual, buccal, labial, palatal, and gingival tissues. 3 Compared to the skin or gastrointestinal tract, the surface area of the oral mucosa is small, yet it is highly vascularized—and this allows agents direct access to systemic circulation via venous and capillary systems. 3 The sublingual and buccal gingiva are the primary focus for transmucosal drug delivery because they are the most permeable. 3 Intraoral mucosa possess different permeability based on cellular thickness and the quantity of keratinized epithelium. 4
What are the limitations of transmucosal delivery?
Another consideration with transmucosal delivery is that certain agents have an onset of action similar to IV drugs.3 One limitation of this method is the variability in absorption, as the oral mucosa is an effective barrier to certain drugs breaching into the environment. Consequently, only high-potency drugs are good candidates for this delivery method. Certain disease states, such as mucositis or blisters, may affect the integrity of the oral mucosa, and when conditions like this are present, transmucosal drug administration may not be appropriate.3 This paper will explore key properties of the oral cavity, various methods of delivery, and prospects for dental applications.
What is the thickness of the sublingual mucosa?
Like the buccal mucosa, the sublingual mucosa is nonkeratinized. One distinguishing feature is the epithelial thickness. The sublingual mucosa is 100 µm to 200 µm, compared to the buccal’s 500 µm to 600 µm.1 The thinness of the sublingual mucosa makes it relatively more permeable,1 and in terms of blood flow, the sublingual mucosa receives less than the buccal mucosa.
What are the tissues that make up the gingiva and palate?
Gingival and Palatal Tissues: The tissues that make up the gingiva and palate are keratinized, and have a thickness of 250 µm and 200 µm, respectively.1 They are less permeable than the buccal and sublingual tissues. At this point, it should be noted that saliva plays a crucial role in the success of transmucosal drug delivery. Saliva is a water-rich environment with a mucus component. The major composition of mucus is mucin, which is mainly composed of glycoprotein. Salivary flow helps determine the amount of time a drug is released into the oral cavity, thus, “saliva washout” can occur, depending on the flow rate.1 Little research has been done to see if this concept affects the efficiency of oral transmucosal drug delivery.2
What is transmucosal delivery?
Transmucosal drug delivery provides an alternative to traditional enteral, intravenous, or intramuscular routes of medication administration.
How effective is benzocaine gel?
Subsequent research by Hersch et al11 tested benzocaine gel delivery in two concentrations (10% and 20%) to evaluate efficacy and tolerability in relieving acute toothaches. The team reported that while both concentrations provided temporary relief, the 20% formulation was most effective.
What is oral mucosal delivery?
Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods. Because the oral mucosa is highly vascularised, drugs that are absorbed through the oral mucosa directly enter the systemic circulation, bypassing the gastrointestinal tract ...
Why is oral mucosal delivery important?
Because the oral mucosa is highly vascularised, drugs that are absorbed through the oral mucosa directly enter the systemic circulation, bypassing th …. Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods.
What is the most common drug delivered through the oral mucosa?
Nitroglycerin is one of the most common drugs delivered through the oral mucosa. Research on other cardiovascular drugs, such as captopril, verapamil and propafenone, has proven promising. Oral transmucosal delivery of analgesics has received considerable attention.
Is midazolam a sedative?
Oral mucosal delivery of sedatives such as midazolam, triazolam and etomidate has shown favourable results with clinical advantages over other routes of administration. Oral mucosal delivery of the antinausea drugs scopolamine and prochlorperazine has received some attention, as has oral mucosal delivery of drugs for erectile dysfunction.
Is transmucosal delivery available?
Although many drugs have been evaluated for oral transmucosal delivery, few are commercially available. The clinical need for oral transmucosal delivery of a drug must be high enough to offset the high costs associated with developing this type of product.
Does sublingual testosterone increase muscle mass?
In clinical studies, sublingual testosterone has been shown to result in increases in lean muscle mass and muscle strength, improvement in positive mood parameters, and increases in genital responsiveness in women.
Can you administer a drug through the mucosa?
Not all drugs, however , can be administered through the oral mucosa because of the characteristics of the oral mucosa and the physicochemical properties of the drug. Several cardiovascular drugs administered transmucosally have been studied extensively.
Mucosa of The Oral Cavity
Patches and Other Delivery Vehicles
- In dentistry, transmucosal drug delivery is mostly utilized in the patch form. In fact, adhesive patches have been developed to overcome the disadvantages of other forms of delivery. Advantages of the patch include rapid onset, sustained release, and a rapid decrease in the drug when the patch is released. The tissues in the oral cavity are immobil...
Evaluation of Transmucosal Drug Delivery
- In the late 1960s, researchers developed a method for measuring oral absorption known as the “swirl and spit” test,1 during which subjects are given a known volume of a specific drug concentration and asked to swirl it for an allotted time. Next, the subject expectorates the drug and rinses with a specific volume of a buffer solution. The expelled drug solution and rinse are a…
Current Usage
- Buccal and sublingual drug formulations have been created and are being used in some dental applications. Midazolam, a popular drug used for sedation, can be administered via an oral mucosal solution. A 2002 analysis demonstrated high bioavailability (74.5%) and consistent plasma concentration following the buccal administration of 5 mg midazolam.3 In 2011, investiga…
Conclusions
- Giannola et al12 proposed that transmucosal drug delivery should be considered a slow IV infusion, with the drug allowed to enter systemic circulation through the capillaries. This allows drugs to have higher bioavailability.1 The transmucosal route is noninvasive and does not require specialized equipment or technical skills. The oral cavity can be utilized for transmucosal deliver…
References
- Sattar M, Sayed OM, Lane ME. Oral transmucosal drug delivery — current status and future prospects. Int J Pharm. 2014;471:498–505.
- Patel VF, Liu F, Brown MB. Advances in oral transmucosal drug delivery. J Control Release. 2011;153:106–116.
- Zhang H, Zhang J, Streisand JB. Oral mucosal drug delivery — clinical pharmacokinetics an…
- Sattar M, Sayed OM, Lane ME. Oral transmucosal drug delivery — current status and future prospects. Int J Pharm. 2014;471:498–505.
- Patel VF, Liu F, Brown MB. Advances in oral transmucosal drug delivery. J Control Release. 2011;153:106–116.
- Zhang H, Zhang J, Streisand JB. Oral mucosal drug delivery — clinical pharmacokinetics and therapeutic applications. Clin Pharmacokinet. 2002;41:661–680.
- Satheesh Madhav NV, Semwal R, Semwal DK, Semwal RB. Recent trends in oral transmucosal drug delivery systems: an emphasis on the soft palatal route. Expert Opin Drug Deliv. 2012;9:629–647.
