A REVIEW ON BUCCAL MUCOSAL ROUTE OF DRUG ADMINISTRATION

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (08) ◽  
pp. 5-16
Author(s):  
M Bhatt ◽  
◽  
G Bhatt ◽  
P. Kothiyal ◽  
S. Chaudhary
Keyword(s):  
Drug Administration ◽  
Hepatic Metabolism ◽  
Systemic Circulation ◽  
Oral Route ◽  
Moisture Loss ◽  
Direct Access ◽  
Mucosal Route ◽  
First Pass ◽  
Milling Method ◽  
Buccal Films

Oral route is the most preferred rote of drug administration. In oral route buccal mucosal route is one of the advantageous routes of drug administration. This route provides direct access to systemic circulation through the jugular vein, bypassing the first pass hepatic metabolism, which leads to high bioavailability. The drugs having low bioavailability, shorter half life and those who undergoes extensive first pass metabolism are good candidat for this rote. Various formulations have been developed for this routes, one of which is buccal film. Buccal films were prepared by using methods like solvent casting method, hot-melt extrusion method and direct milling method. Buccal films were evaluated for thickness, swelling property, surface pH, drug content, % moisture loss, etc.

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.

A REVIEW ON BUCCAL FILM: AN INOVATIVE DOSAGE FORM

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (01) ◽  
pp. 5-14
Author(s):  
Menra Muse ◽  
J. S. Dua ◽  
D. N. Prasad ◽  
Keyword(s):  
Cost Effective ◽  
Systemic Circulation ◽  
Dosage Forms ◽  
Sustained Effects ◽  
Buccal Absorption ◽  
Mucosal Route ◽  
First Pass Metabolism ◽  
Evaluation Parameters ◽  
Buccal Films ◽  
Pass Metabolism

Buccal administration of drugs leads to systemic circulation through internal jugular vein, bypassing them from hepatic first pass metabolism and leading to greater bioavailability. Buccal mucosa is most preferred site for both local as well as systemic action. For administration of drug through mucosal route, various types of dosage forms can be prepared. Buccal films can release topical drugs with controlled and sustained effects. Buccal films have the advantage of improved patient compliance because of reduced size with a suitable thickness as compare to other delivery systems. Buccal film can enhance absorption of active medicament as compared to others. Synthetic natural and semi synthetic polymers in low concentration can be used for the preparation of buccal films. Such types of dosage forms are cost effective, non-irritating, easy to handle, elegant, rapidly absorbable and most preferred by consumer. The review describes the anatomy of oral mucosa, mechanism of buccal absorption, methods to increase drug delivery via a buccal route, formulation aspects and evaluation parameters of buccal films.

scholarly journals Overview of Newer Glucocorticosteroid Preparations for Inflammatory Bowel Disease

1990 ◽  
Vol 4 (7) ◽  
pp. 407-414 ◽  
Author(s):  
R Brattsand
Keyword(s):  
Inflammatory Bowel Disease ◽  
Bowel Disease ◽  
Topical Therapy ◽  
Hepatic Metabolism ◽  
Systemic Circulation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Inflammatory Bowel ◽  
Bowel Mucosa ◽  
Pass Metabolism

Because the glucocorticosteroid receptor seems to be uniform in the human body, there is currently no support for a possibility of separating the therapeutic and adverse glucocorticosteroid actions at the receptor level. However, based on a new generation of glucocorticosteroids characterized by a high first pass metabolism in the liver, it seems possible today co reach a more selective topical therapy of inflammatory bowel disease. The properties of three new glucocorticosteroids are presented: the highly potent budesonide, fluticasone propionate and tixocortol pivalate - the latter with only low topical potency. Their properties can be exemplified by budesonide, which is currently the best documented compound. The topical potency of budesonide is 200 and 15 times higher than chose of hydrocortisone and prednisolone, respectively. This means that there is a high potential for anti-inflammatory and immunosuppressive actions on rectal and bowel mucosa. The compound is metabolically stable in the bowel compartment, which allows full retention of glucocorticosteroid activity in the target organ. However, when absorbed and distributed to the liver, there is a 90% first pass hepatic metabolism co metabolites of very low potency. This suggests that after topical application to rectal or bowel mucosa, glucocorticosteroid activity in the systemic circulation is low. This is in contrast to prednisolone, which has a hepatic first pass metabolism of just 20%.

EFFECTS OF ORAL ASPIRIN ON PLATELET AND VASCULAR CYCLOOXYGENASE ACTIVITY IN RATS WITH PORTACAVAL SHUNT

1987 ◽  
Author(s):  
C Cerletti ◽  
M C Gombino ◽  
S Possaghe ◽  
F Bucchi ◽  
Z M Chen ◽  
...  
Keyword(s):  
Inferior Vena ◽  
Vena Cava ◽  
Portacaval Shunt ◽  
Hepatic Metabolism ◽  
Systemic Circulation ◽  
Cyclooxygenase Activity ◽  
First Pass ◽  
Anaesthetized Rats ◽  
Oral Aspirin

Oral aspirin can be extensively hydrolysed to salicylate in stomach and liver before entering the systemic circulation. “Pre-systemic” acetylation of the platelets may thus occur during aspirin absorption. This may result in concomitant sparing of peripheral vascular cyclooxygenase mainly exposed to salicylate. We tested whether the “biochemical selectivity” of oral aspirin as an inhibitor of platelet vs. vascular cyclooxygenase would be reduced by elimination of the “first-pass” hepatic metabolism. A portacaval shunt was inserted in anaesthetized rats by connecting the portal vein to the inferior vena cava through a “Y” heparinized polyethylene PE 60-160 cannula. Sham operated rats acted as controls. 90 min after recovery from anaesthesia rats were given aspirin orally (10 mg/kg) and 45 min later serum TxB2 and 6-keto-PGF la formation by vascular rings were evaluated by radioimmunoassay. Serum TxB2 was completely suppressed in all animals; in contrast, vascular 6-keto-PGF la was significantly reduced (by 40-60* in aorta and vena cava) in rats with portacaval shunt but not in controls. The results in rats with portacaval shunt were similar to those previously obtained after i.v. aspirin. 15 min after aspirin administration, plasma levels of unmetabolized drug measured by HPLC were significantly higher in rats with portacaval shunt (0.56±0.16 μg/ml; n= 5) than in sham operated controls (0.16±0.22 }μg/ml; n= 5). This study directly supports the role of “ first-pass” hepatic metabolism in determining the “biochemical selectivity” of oral aspirin.

Transcending the Cutaneous Barrier Through Nanocarrier Exploration for Passive Delivery of Anti-hypertensive Drugs: A Critical Review

2020 ◽  
Vol 14 (3) ◽  
pp. 193-209
Author(s):  
Lalit Kumar ◽  
Puneet Utreja
Keyword(s):  
Patient Compliance ◽  
Transdermal Delivery ◽  
Antihypertensive Drugs ◽  
Skin Barrier ◽  
Oral Route ◽  
Term Treatment ◽  
New Approaches ◽  
Long Term Treatment ◽  
First Pass ◽  
Transdermal Route

Background: Hypertension comes under the category of chronic disease, which requires long term treatment. Hypertension is usually treated by oral administration of various therapeutic agents. There are several limitations of the oral route, making pharmaceutical scientists to discover an alternative route for drug delivery. Methods: The transdermal route may be a better alternative as it shows various advantages like lack of first-pass effect and high patient compliance. The skin may act as a primary barrier for the transdermal delivery of anti-hypertensive drugs; therefore, new approaches are required to cross this barrier. Nanocarrier systems come under these new approaches to cross the skin barrier. Various nanocarrier systems explored for transdermal delivery of antihypertensive drugs are liposomes, elastic liposomes, ethosomes, transethosomes, oleic acid vesicles, niosomes, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions/microemulsions, and carbon nanotubes. Results: This review summarizes the potential of advanced nanocarrier systems for effective management of hypertension following the transdermal route. The entire literature search regarding the utility of nanocarrier systems in transdermal delivery of antihypertensive drugs was done by using Pubmed and Google Scholar. Conclusion: Nanocarrier systems are capable of reducing various drawbacks of conventional formulations of antihypertensive drugs like excessive first-pass effects, high dosing frequency, and toxicity promoting high patient compliance. However, the clinical efficacy determination of such nanocarrier systems is still a challenge and it will govern their presence in the global pharmaceutical market.

Direct access of drugs to the human brain after intranasal drug administration?

Neurology ◽  
2003 ◽  
Vol 60 (10) ◽  
pp. 1669-1671 ◽  
Author(s):  
P. Merkus ◽  
H.-J. Guchelaar ◽  
D. A. Bosch ◽  
F. W.H.M. Merkus
Keyword(s):  
Human Brain ◽  
Drug Administration ◽  
Direct Access ◽  
Intranasal Drug Administration

Development and Evaluation of Trans Buccal Patches based on Natural and Synthetic Polymers Loaded with Rivastigmine using Solvent Casting Technique

2021 ◽  
pp. 5133-5140
Author(s):  
Prasanta Kumar Mohapatra ◽  
Boddu Pavan Kumar ◽  
Pankaj Singh Patel ◽  
Harish Chandra Verma ◽  
Satyajit Sahoo
Keyword(s):  
Drug Release ◽  
Kinetic Equations ◽  
Moisture Loss ◽  
Release Mechanism ◽  
Solvent Casting ◽  
Casting Technique ◽  
Weight Variation ◽  
Zero Order Release ◽  
Buccal Films

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.

scholarly journals A comprehensive review on buccal patches

2020 ◽  
Vol 13 (1) ◽  
pp. 130-135
Author(s):  
Seema ◽  
Kapil kumar ◽  
Deepak Teotia
Keyword(s):  
Drug Delivery ◽  
Oral Cavity ◽  
Systemic Circulation ◽  
Drug Formulation ◽  
Delivery Method ◽  
Modern Approach ◽  
Comprehensive Review ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal Patches are the type of drug formulation that has normally a different course of administration through the buccal mucosa for drug delivery. The product is placed between upper gingiva (gums) and cheek to treat local and systemic conditions. Buccal patch have good accessibility to the membranes that line the oral cavity. These patches tend to help drug enter directly into the systemic circulation escaping hepatic first pass metabolism. This type of drug delivery method is considered useful for elevating the bioavailability of drugs. This review is a thorough study to apprehend the procedures involved in assessment of buccal patches and the modern approach towards this type of drug delivery. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

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.

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