Creating systemic oral transmucosal drug delivery strategies: Case study of APL-130277

2012 ◽  
Vol 18 (3) ◽  
Author(s):  
Anthony Giovinazzo ◽  
Nathan Bryson ◽  
Timothy Tankosic
Keyword(s):  
Drug Delivery ◽  
Hepatic Metabolism ◽  
Rapid Onset ◽  
Easy Access ◽  
Patient Acceptance ◽  
Onset Of Action ◽  
Buccal Drug Delivery ◽  
High Level ◽  
Systemic Drug Delivery

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.

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
Keyword(s):  
Drug Delivery ◽  
Blood Vessels ◽  
Psychiatric Patients ◽  
Rapid Onset ◽  
Oral Route ◽  
Sublingual Gland ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Systemic Drug Delivery ◽  
Sublingual Delivery

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.

scholarly journals Nasal Delivery of Acute Medications for Migraine: The Upper Versus Lower Nasal Space

2021 ◽  
Vol 10 (11) ◽  
pp. 2468
Author(s):  
Vincent Martin ◽  
John Hoekman ◽  
Sheena K. Aurora ◽  
Stephen B. Shrewsbury
Keyword(s):  
Acute Treatment ◽  
Drug Efficacy ◽  
Hepatic Metabolism ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Nasal Delivery ◽  
Attractive Alternative ◽  
Gi Tract ◽  
Onset Of Action ◽  
First Pass

The acute treatment of migraine requires effective drugs that are well tolerated and provide rapid and consistent pain relief. Oral tablets are the most commonly used acute treatment for migraine; however, their effectiveness is limited by the rate of gastrointestinal (GI) tract absorption and first-pass hepatic metabolism, and they may not be ideal for patients experiencing GI motility issues. Nasal delivery is an attractive alternative route as it may circumvent GI tract absorption, avoid first-pass metabolism in the liver, and potentially reduce the frequency of GI adverse events. The large surface area and high vascularity within the nose may permit rapid absorption of therapeutics into the systemic circulation, allowing for rapid onset of action. However, the site of drug deposition (upper versus lower nasal cavity) may influence drug pharmacokinetics. Most approved nasal migraine therapies target the lower nasal space where the epithelium is less permeable, and they may be quickly cleared away due to increased ciliary function or dripping from the nose or swallowing, resulting in variable absorption and limited bioavailability. Together with its abundant vascularization, relative mucosal thickness stability, and low clearance rates, the upper nasal space harnesses the benefits of nasal delivery to potentially maximize drug efficacy.

scholarly journals MUCOADHESIVE BUCCAL DRUG DELIVERY SYSTEMS CONTAINING POLYSACCHARIDES

2020 ◽  
Vol 54 (9-10) ◽  
pp. 889-902
Author(s):  
IRINA M. PELIN ◽  
DANA M. SUFLET
Keyword(s):  
Drug Delivery ◽  
Drug Administration ◽  
Drug Delivery Systems ◽  
Enzymatic Degradation ◽  
Low Cost ◽  
Hepatic Metabolism ◽  
Drug Action ◽  
Delivery Systems ◽  
Buccal Drug Delivery ◽  
Systemic Drug

The buccal mucosa is an attractive site for drug administration as it allows avoiding the enzymatic degradation of the drug in the gastrointestinal tract and its hepatic metabolism. For buccal administration, different drug delivery systems with controlled mucoadhesion have been developed and some of them are available on the market. Mucoadhesion makes it possible to obtain prolonged, local or systemic drug action, and this process is highly influenced by several factors, among which, the reactivity of macromolecules from the formulations is very important. Polysaccharides are increasingly studied due to their abundance in natural resources, low-cost availability and easy chemical modification, but also due to their biocompatibility, biodegradability and non-toxicity properties. This review briefly describes the advantages of using the buccal route of drug administration, the influencing factors that are taken into account for obtaining mucoadhesive dosage forms, and the main polysaccharides and their derivatives used for fabrication of buccal drug delivery systems.

scholarly journals A STUDY ON A NOVEL FORMULATION APPROACH TO DELIVER DOXYCYCLINE THROUGH BUCCAL ROUTE

2019 ◽  
Author(s):  
Tanzeena Afroz ◽  
Md. Jasim Uddin ◽  
Md. Shahidul Islam
Keyword(s):  
Drug Delivery ◽  
Release Rate ◽  
Oral Drug Delivery ◽  
Rapid Onset ◽  
Oral Drug ◽  
Onset Of Action ◽  
Drug Degradation ◽  
Wide Range ◽  
Buccal Films

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.

scholarly journals Sublingual Tablets : An Overview

2020 ◽  
pp. 333-339
Author(s):  
Rohit S. Nikam ◽  
Smita P Borkar ◽  
Prakash D Jadhav ◽  
Vishal D. Yadav ◽  
Apurva V Jadhav
Keyword(s):  
Drug Delivery ◽  
Oral Cavity ◽  
Mucous Membrane ◽  
Dosage Form ◽  
Rapid Onset ◽  
Oral Route ◽  
Mouth Area ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Oral Mucous Membrane

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.

scholarly journals Sublingual Tablets : An Overview

2019 ◽  
pp. 181-187
Author(s):  
Rohit S. Nikam ◽  
Rahul P. Jadhav ◽  
Dr. Prakash D. Jadhav ◽  
Vishal D. Yadav
Keyword(s):  
Drug Delivery ◽  
Rapid Onset ◽  
Oral Route ◽  
Dosage Forms ◽  
Peroral Administration ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Evaluation Parameters ◽  
Pass Metabolism

<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>

scholarly journals Future Trends in Nebulized Therapies for Pulmonary Disease

2020 ◽  
Vol 10 (2) ◽  
pp. 37 ◽  
Author(s):  
Sean D. McCarthy ◽  
Héctor E. González ◽  
Brendan D. Higgins
Keyword(s):  
Drug Delivery ◽  
Mechanical Ventilation ◽  
Rapid Onset ◽  
Therapeutic Effects ◽  
Aerosol Therapy ◽  
Breathing Patterns ◽  
Onset Of Action ◽  
Therapeutic Drugs ◽  
Patient Variables ◽  
Systemic Side Effects

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.

scholarly journals Nasal Drug Delivery: A Potential Route for Brain Targetting

2015 ◽  
Vol 1 (2) ◽  
pp. 65 ◽  
Author(s):  
Brahmaiah Bonthagarala ◽  
Shabana P. ◽  
Abbaraju Lakshmi Harini ◽  
Varun Dasari
Keyword(s):  
Drug Delivery ◽  
Nasal Mucosa ◽  
Targeted Drug Delivery ◽  
Drug Transport ◽  
Relative Concentration ◽  
Rapid Onset ◽  
Nasal Drug Delivery ◽  
Onset Of Action ◽  
First Pass ◽  
The Brain

Present review highlights the potential of nasal mucosa as an administration route for targeting the centralnervous system, the brain. Targeted drug delivery seeks to concentrate the medication in the tissues ofinterest while reducing the relative concentration of medication in the remaining tissues. Thus improvingefficacy of the drug and reducing side effects. The nasal mucosa when compared to other mucousmembranes is easily accessible and provides a practical entrance portal for small and large molecules.Intranasal administration offers rapid onset of action, no first-pass effect, no gastrointestinal degradationor lung toxicity and non-invasiveness application and also improves bioavailability. It is thought thatolfactory route of drug transport, by pass the blood-brain barrier and allows the direct transport of drugfrom the nose to the brain. This review provides an overview of strategies to improve the drug delivery tobrain via nasal mucosa and recent advances in this field.

scholarly journals Sublingual spray: a new technology oriented formulation with multiple benefits

2019 ◽  
Vol 10 (4) ◽  
pp. 2875-2885 ◽  
Author(s):  
Aravindhanthan V ◽  
Anjali P B ◽  
Arun Radhakrishnan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
New Technology ◽  
Rapid Onset ◽  
Regulatory Agencies ◽  
Onset Of Action ◽  
First Pass ◽  
Delivery Technology ◽  
Pass Metabolism

Sublingual drug delivery system was a well-established platform for delivering the drug that need to exhibit quick action without any first-pass metabolic effect, but various pitfall in the regular sublingual drug delivery systems such as a tablet, capsule etc., that can be overcome by novel sublingual drug delivery technology such as particulate sublingual spray. Sublingual spray for drug administration has gained attention in the market since it proved its propensity to by-pass the first-pass metabolism and to initiate a rapid onset of action due to its atomized micro particulate nature, which is significantly higher than the other sublingual formulations. The approval of sublingual spray by the regulatory agencies may commence further research in this field by subsuming various essential drugs for indications such as cancer pain, cardiovascular issue etc. This article comprises a detailed study on the drawback of conventional sublingual drug delivery system and the approach by which these drawbacks can be overruled by spray technology in the sublingual area and the, in-depth mechanism of drug delivery through sublingual with the help of atomization followed by the entire formulation strategy along with evaluation and industrial perspective of the sublingual spray dosage form as a future tool of patient-friendly drug delivery.

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