scholarly journals Sublingual route for systemic drug delivery

2018 ◽  
Vol 8 (6-s) ◽  
pp. 340-343
Author(s):  
Poonam P Pawar ◽  
Hemant S Ghorpade ◽  
Bhavana A. Kokane

Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a rapid onset of action and better patient compliance than orally ingested tablets. Sublingual literally meaning is “under the tongue”, administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability.  Sublingual technology is convenient for dosing in geriatric, pediatric and psychiatric patients with dysphagia. Sublingual drug delivery shows fast therapeutic action than orally ingested drugs with fewer side effects. This review highlights advantages, disadvantages, different sublingual Gland, sublingual formulation such as tablets, films drops, sprays etc, evaluation parameters. Keywords: Sublingual delivery, dysphagia, sublingual gland, improved bioavailability, evaluations.

Author(s):  
Rohit S. Nikam ◽  
Smita P Borkar ◽  
Prakash D Jadhav ◽  
Vishal D. Yadav ◽  
Apurva V Jadhav

Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a useful when rapid onset of action is desired with better patient compliance than oraly ingested tablets. In terms of permeability, the sublingual area of the oral cavity (i.e. the floor of the mou) is more permeable than the buccal (cheek) area, which in turn is more permeable than the palatal (roof of the mouth) area. A rapid onset of pharmacological effect is often desired for some drugs, especially those used in the treatment of acute disorders. Sublingual tablets disintegrate rapidly and the small amount of saliva present is usually sufficient for achieving disintegration of the dosage form coupled with better dissolution and increased bioavailability.


Author(s):  
Rohit S. Nikam ◽  
Rahul P. Jadhav ◽  
Dr. Prakash D. Jadhav ◽  
Vishal D. Yadav

<p>Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a rapid onset of action and better patient compliance than orally ingested tablets. Sublingual literally meaning is 'under the tongue', administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. Peroral administration of drug has disadvantages such as Hepatic first pass metabolism and enzymatic degradation within the GI tract that limits oral administration of certain classes of drug like peptides and proteins. So, other absorptive mucosa is considered as potential sites for drug administration. Trans-mucosal routes of drug delivery (i.e. the mucosal linings of the nasal, rectal, vaginal, ocular, and oral cavity) offer several advantages over peroral administration for systemic delivery. This review highlights the sublingual dosage forms for the treatment of migraine, advantages, Disadvantages, various evaluation parameters and commercially available sublingual dosage forms.</p>


2012 ◽  
Vol 18 (3) ◽  
Author(s):  
Anthony Giovinazzo ◽  
Nathan Bryson ◽  
Timothy Tankosic

This article addresses the strategic application of systemic oral transmucosal* (i.e., sublingual and buccal) drug delivery. Circumvention of first-pass hepatic metabolism in the gut, rapid onset of action, easy access via the oral cavity, easy administration for patients with dysphagia and a high level of patient acceptance are the principal advantages of the oral transmucosal route. Key clinical and commercial strategies driving the development of oral transmucosal formulations are addressed. A case study of Cynapsus Therapeutics' APL-130277, a sublingual apomorphine formulation in clinical development for Parkinson's disease exemplifies the scientific, clinical and commercial considerations for systemic oral transmucosal drug delivery. *Note: In this article, oral transmucosal delivery refers to systemic drug delivery through the sublingual or buccal mucosa. Local delivery to the oral mucosa is not included.


Author(s):  
Puja Saha ◽  
Sushma Verma ◽  
Pratik Swarup Das

Sublingual literally meaning is “under the tongue”, refers to a method of administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. Sublingual route is a useful when rapid onset of action is desired with better patient compliance than orally ingested tablets. Drugs that are given sublingually reach directly in to the systemic circulation through the ventral surface of the tongue and floor of the mouth. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability. As nowadays most of the people need effective relief within a short period of time so sublingual is the most suitable form of administration. New sublingual technologies address many pharmaceutical and patient needs, ranging from enhanced life‐cycle management to convenient dosing for paediatric, geriatric, and psychiatric patients with dysphagia.


Author(s):  
AHMED M. AGIBA ◽  
AHMED B. ELDIN

Among the various routes of administration, the oral route remains the most convenient and commonly employed route for drug delivery. The oral conventional drug delivery systems have some drawbacks, such as possibility of gastrointestinal destruction of labile molecules, low absorption of macromolecules, slow onset of action, and unavoidable fluctuation in the concentration of drugs which can either lead to under- or over medication with concomitant adverse effects, especially for drugs with small therapeutic index. Therefore, it became essential to design novel oral drug delivery systems to achieve quick dissolution, absorption, rapid onset of action and reduction of drug dose. Among those novel drug delivery systems are oral disintegrating tablets (ODTs). The purpose of this review article is to report the recent advances in ODT systems with emphasis on their preparations, characterizations and applications.


2021 ◽  
Vol 11 ◽  
Author(s):  
Deepak Sharma ◽  
Dinesh Kumar ◽  
Gurmeet Singh

Background: The delivery of therapeutic agents through the oral route remains the most favorable one as compared to other routes of drug administration. However, numerous disadvantages are encountered in conventional formulations such as low bioavailability, first-pass metabolism, gastric irritation, delayed onset of action, bitter taste, low retention time, frequent dosing, and non-localized drug targeting. All these problems encountered guide the various pharmaceutical industries to manufacture and develop a novel solid oral dosage form called lozenges. Lozenges are solid oral dosage forms of medicament, meant to be dissolved within the mouth or pharynx. It may consist of one or more than one medicinal agent contained in a sweetened and flavored base material. Objective: The present review is focused on various types, compositions, methodologies used to prepare the medicated lozenges and on different evaluation parameters that establish its safety and efficacy. It also put a light on different commercially available and reported medicated lozenges formulation. Method: The various review and research articles reported by different researchers were studied extensively by using the databases of Google Scholar, Pubmed, Scopus, Web of Science and various commercial websites that were also investigated for information regarding new products. Results: Lozenges provides various advantages in terms of patient compliance, rapid onset of action, prolonged retention time, enhancement of bioavailability, ease of manufacturing, localized drug targeting, sustained or controlled effect, and reduced dosing frequency. It has also the ability to incorporate the drugs belong to different therapeutic classes for treating various disorders related to oral cavities like gingivitis, dental plaque, mouth ulcers, throat pain, oral thrush, throat infection, periodontitis, and pharyngitis. However, its applicability is not only limited to localized action, but it has also been employed to deliver the drug systemically for the conditions such as cough, decongestion, runny nose, nausea, vomiting, allergy, low immunity, fever, body ache, the killing of worms and smoking cessation. Conclusion: It was concluded that it has been played an important role in the field of drug delivery and will continue to perform in the same way in the future as well.


Author(s):  
Tanzeena Afroz ◽  
Md. Jasim Uddin ◽  
Md. Shahidul Islam

Recent developments in drug delivery technologies have a great impact on the limitations of traditional oral drug delivery for both the pediatric and geriatric patients. Administration of drug via buccal mucosa is a modern alternative for overcoming low bioavailability, enzymatic inactivation and/or drug degradation in gastrointestinal tract, hence showing rapid onset of action. The aim of the study was to develop doxycycline (antibiotic) loaded buccal films for the treatment of a wide range of systemic and non-systemic bacterial and protozoa infections. The bases of each film were prepared using mucoadhesive polymers, plasticizer, cellulose gums, and instant release film former and penetration enhancer. Optimized films were characterized for weight, width. Length, thickness, surface pH, percentage swelling index, percentage elongation, percentage moisture content, percentage moisture uptake, hydration and in vitro drug release studies. Concentration of different polymers tailored the increase in release rate of doxycycline from the mucoadhesive buccal films. In conclusions, mucoadhesive buccal films can be a substitute route for the delivery of doxycycline as antibacterial or antiprotozoal drug with a faster release rate to reach the site of action.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 870
Author(s):  
Amer S. AlAli ◽  
Mohammed F. Aldawsari ◽  
Ahmed Alalaiwe ◽  
Bjad K. Almutairy ◽  
Ramadan Al-Shdefat ◽  
...  

Sildenafil citrate undergoes first-pass metabolism, resulting in poor oral bioavailability at 25–41% of the administered dose. This study aimed to design and optimize fast-disintegrating tablets for the sublingual delivery of sildenafil citrate to improve bioavailability and facilitate rapid onset of action. The design-of-experiment (DoE) approach using 32 full factorial design was conducted to develop a new formulation of sildenafil fast-disintegrating sublingual tablets (FDSTs) using the fluid-bed granulation technique. The levels of partially pre-gelatinized starch (5–15%) and microcrystalline cellulose (10–60%) were selected as independent formulation variables. The prepared FDSTs were investigated for physical properties. Further, the optimum formulation was chosen for in vivo study in rabbits. Regression analysis showed that independent variables have a significant (p < 0.05) influence on critical attributes of FDSTs. The optimized formulation showed acceptable mechanical strength (friability <1.0%) with very fast disintegration (14.561 ± 0.84 s) and dissolution (94.734 ± 2.76% after 15 min). Further, the optimized formulation demonstrated a significant increase (p < 0.01) in Cmax and AUC0–∞ with short tmax compared to the market product (Viagra®). Based on these results, using the DoE approach, a high level of assurance was achieved for FDSTs’ product quality and performance.


2020 ◽  
Vol 10 (2) ◽  
pp. 37 ◽  
Author(s):  
Sean D. McCarthy ◽  
Héctor E. González ◽  
Brendan D. Higgins

Aerosol therapy is a key modality for drug delivery to the lungs of respiratory disease patients. Aerosol therapy improves therapeutic effects by directly targeting diseased lung regions for rapid onset of action, requiring smaller doses than oral or intravenous delivery and minimizing systemic side effects. In order to optimize treatment of critically ill patients, the efficacy of aerosol therapy depends on lung morphology, breathing patterns, aerosol droplet characteristics, disease, mechanical ventilation, pharmacokinetics, and the pharmacodynamics of cell-drug interactions. While aerosol characteristics are influenced by drug formulations and device mechanisms, most other factors are reliant on individual patient variables. This has led to increased efforts towards more personalized therapeutic approaches to optimize pulmonary drug delivery and improve selection of effective drug types for individual patients. Vibrating mesh nebulizers (VMN) are the dominant device in clinical trials involving mechanical ventilation and emerging drugs. In this review, we consider the use of VMN during mechanical ventilation in intensive care units. We aim to link VMN fundamentals to applications in mechanically ventilated patients and look to the future use of VMN in emerging personalized therapeutic drugs.


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