Permeability of Buccal Mucosa

The buccal mucosa provides an alternative route of drug delivery that can be more beneficial compared to other administration routes. Although numerous studies and reviews have been published on buccal drug delivery, an extensive review of the permeability data is not available. Understanding the buccal mucosa barrier could provide insights into the approaches to effective drug delivery and optimization of dosage forms. This paper provides a review on the permeability of the buccal mucosa. The intrinsic permeability coefficients of porcine buccal mucosa were collected. Large variability was observed among the published permeability data. The permeability coefficients were then analyzed using a model involving parallel lipoidal and polar transport pathways. For the lipoidal pathway, a correlation was observed between the permeability coefficients and permeant octanol/water partition coefficients (Kow) and molecular weight (MW) in a subset of the permeability data under specific conditions. The permeability analysis suggested that the buccal permeation barrier was less lipophilic than octanol. For the polar pathway and macromolecules, a correlation was observed between the permeability coefficients and permeant MW. The hindered transport analysis suggested an effective pore radius of 1.5 to 3 nm for the buccal membrane barrier.

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FORMULATION AND EVALUATION OF MUCOADHESIVE BUCCAL TABLETS CANTANING IVABRADINE HYDROCHLORIDE BY USING NATURAL POLYMERS

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v8i2.588 ◽

2019 ◽

Vol 8 (2) ◽

Author(s):

Manoj Premi ◽

Manish Kumar Gupta ◽

Bannaruvari Phanindra

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Buccal Mucosa ◽

The Body ◽

Angle Of Repose ◽

Natural Polymers ◽

Buccal Tablet ◽

Buccal Drug Delivery ◽

Buccal Tablets

The buccal mucosa is moderately permeable, strong when match up with the other mucosal tissues and is more tolerant to potential allergens which have a compact affinity to unalterable irritation or harm. Mucoadhesive buccal drug delivery system offers a control release system; it entails the administration of required drug through the buccal mucosal membrane lining of the oral cavity. The Bioadhesive was resulting from the need to limit drugs at a definite site in the body. Significantly at the absorption site, enhance the degree of drug absorption is restricted by the residence time of the drug. The API, blend of excipients and drug were prepared at the ratio of 1:1, filled in closed vials and kept in accelerated environmental conditions (40°C/75% RH) for a period of 1 month. Excipients were employed here to assess the compatibility issue with the active ingredient. The possible drug and polymer interaction studies were assessed by using FTIR. Calibration curve of ivabradine HCl was constructed by dissolving pure drug of ivabradine HCl (100 mg) in 100 mL of phosphate buffer (pH 6.8) to give 1mg/mL concentration and designed as stock solution-1. The angle of repose was determined by fixed funnel method. The prepared mucoadhesive buccal tablets were estimated for post compression factors such as thickness, friability, drug content and hardness. The surface pH study was conducted on ivabradine HCl mucoadhesive buccal tablets, carried out to predict the comfort of the buccal formulation into the possibility of any side effects in buccal mucosa environment. F1 and F5 possessed the best results among all the formulations in terms of in vitro release of drug. However, F2 formulation shows highest mucoadhesive and swelling index than other formulation. Therefore, from the data, it may be concluded that F2 formulation might be considered as promising mucoadhesive buccal tablet formulation for a suitable sustained drug delivery system for ivabradine. Keywords: Ivabradine Hydrochloride, Buccal tablet, Mucoadhesive, Natural Polymers.

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Chemical Enhancers in Buccal and Sublingual Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.1.3 ◽

2011 ◽

Vol 4 (1) ◽

pp. 1307-1319

Author(s):

Naveen C ◽

Kiran kumar Y ◽

Venkateshwar Rao P ◽

T. Rama Rao

Keyword(s):

Drug Delivery ◽

Buccal Mucosa ◽

Oral Delivery ◽

Oral Absorption ◽

Repeated Administration ◽

Therapeutic Agents ◽

Penetration Enhancers ◽

Direct Access ◽

Limiting Factor ◽

Buccal Drug Delivery

Rapid developments in the field of molecular biology and gene technology resulted in generation of many macromolecular drugs with superior pharmacological efficacy, site specificity and devoid of toxic effects. However, the major problem for the oral delivery of these therapeutic agents is their extensive presystemic metabolism, instability in acidic environment resulting into inadequate and erratic oral absorption. Parenteral route of administration is the only established route that overcomes all these drawbacks associated with these orally less/inefficient drugs. But, these formulations are costly, have least patient compliance and require repeated administration. The buccal delivery system found to be most convenient and easily accessible site for the delivery of such therapeutic agents. This route provides direct access to the systemic circulation through the internal jugular vein thus avoiding the hepatic first-pass effect and degradation in the gastrointestinal tract, ease of administration, and the ability to terminate delivery when required. The epithelium that lines the oral mucosa is a very effective barrier that restricts the membrane permeation for many drugs administered via this route, and can be a limiting factor to the absorption of drugs. The use of penetration enhancers is one approach for improving buccal drug delivery. This requisite has fostered the study of penetration enhancers that will safely alter the permeability restrictions of the buccal mucosa. This review describes various classes of transmucosal chemical permeation enhancers such as bile salts, surfactants, fatty acids and their derivatives, chelators, cyclodextrins and chitosan along with their mechanism of action. Even though these enhancers influence drug delivery, further exploration of these compounds is required to understand their modifying action on the properties of buccal mucosa.

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An Updated Overview on Mucoadhesive Buccal Drug Delivery System

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00781 ◽

2021 ◽

pp. 4495-4500

Author(s):

Om M. Bagade ◽

Ashwini R. Mali ◽

Saroja S. Survase ◽

Ankita K. Chaudhari ◽

Priyanka E. Doke

Keyword(s):

Drug Delivery ◽

Buccal Mucosa ◽

Scale Up ◽

Hot Melt Extrusion ◽

Water Soluble ◽

Matrix Tablets ◽

Melt Extrusion ◽

Buccal Drug Delivery ◽

Industrial Manufacture ◽

Hot Melt

Among the various routes of drug delivery, the oral route is an attractive site for the delivery of drugs. The main advantages of these formulations are: drug targeting, sustained release, increased permanence time in the buccal mucosa, increased bioavailability, and decreased potential adverse effects and maintains constant blood levels for extended period of time. The buccal cavity was found to be the most suitable and easily accessible site for the delivery of therapeutic agents for both local and systemic delivery. Buccal mucosa has a tremendous availability, which leads to direct access to systemic circulation through the internal jugular vein bypasses the drug from hepatic first pass metabolism. The main disadvantage of this route is Limited absorption area- the total surface area of the membranes of the oral cavity available for drug absorption is 170 cm2 of which ~50 cm2 represents non-keratinized tissues, including buccal membrane, the barrier function of the skin changes from one site to the other and from one person to other person with age and large dose of drug are difficult to be administered. Melt granulation is emerging technique and this technique used to increase the dissolution rate of poorly water-soluble drugs. Tablet molding technique: Tablets produced by the molding technique are easier to scale up for industrial manufacture than lyophilisation technique. Hot melt extrusion of film method: Hot melt extrusion has been used for the manufacture of controlled release matrix tablets, pellets and granules, as well as oral disintegrating films.

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Plantago Ovata and Locust Bean Gum as a Natural Polymer in Hydrodynamically Balanced Systems: A Review

Journal of Biomedical and Allied Research ◽

10.37191/mapsci-2582-4937-2(1)-015 ◽

2020 ◽

Author(s):

Ghildiyal s

Keyword(s):

Drug Delivery ◽

Locust Bean Gum ◽

Main Role ◽

Natural Polymer ◽

Release Formulation ◽

Sustained Drug Delivery ◽

Modern Drug ◽

Buccal Drug Delivery ◽

Locust Bean ◽

Ceratonia Siliqua L

Hydrodynamically Balanced systems have wide development as they have achieved the parameters of modern drug delivery system, it is a type of system which owes very tremendous and curative benefits for the delivery of oral controlled release dosage forms and have wide properties in many aspects such as its main role is to maintain the effective concentration in the system for longer period of time. To reduce the gastric mucosal irritation due to the presence of synthetic polymers, being a natural polymer incorporation of Plantago ovate (Psyllium Husk) could ease out the mucosal irritation in the gastric region. Due to its properties such as a rate-controlling polymer possessing a very good quality of swelling and good gelling nature, and also incorporated as a matrix-forming agent basically in the modified release formulation. Locust bean gum can be used as sustained-release carriers and release modifiers for the delivery of drugs. It is a neutral plant galactomannan extracted from the seeds (kernels) of the carob tree Ceratonia siliqua L fabaceae. Nowadays it is focussing polymer and a lot of researchers are focussing on exploring the potential in topical drug delivery, colonic drug delivery, oral sustained drug delivery, ocular drug delivery, buccal drug delivery.

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BUCCAL DRUG DELIVERY SYSTEM: A TOOL FOR THE EFFECTIVE DELIVERY OF PHARMACEUTICALS

Universal Journal of Pharmaceutical Research ◽

10.22270/ujpr.v2i3.rw2 ◽

2017 ◽

Vol 2 (3) ◽

pp. 20-25

Author(s):

Bhartee Pathak ◽

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

System A ◽

Buccal Drug Delivery ◽

Effective Delivery

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Applied Nanotechnologies in Anticoagulant Therapy: From Anticoagulants to Coagulation Test Performance of Drug Delivery Systems

Applied Nano ◽

10.3390/applnano2020009 ◽

2021 ◽

Vol 2 (2) ◽

pp. 98-117

Author(s):

Yuri B. G. Patriota ◽

Luíse L. Chaves ◽

Evren H. Gocke ◽

Patricia Severino ◽

Mônica F. R. Soares ◽

...

Keyword(s):

Drug Delivery ◽

Anticoagulant Therapy ◽

Test Performance ◽

Vitamin K Antagonists ◽

Oral Anticoagulants ◽

Direct Oral Anticoagulants ◽

Delivery Systems ◽

Reversal Agent ◽

Laboratory Assessment ◽

Administration Routes

Heparin-based delivery systems have been explored to improve their therapeutic efficacy and to reduce toxicity for different administration routes. Regardless of the applied drug delivery system (DDS), the evaluation of anticoagulant performance is instrumental for the development of a suitable DDS. The understanding of the range of anticoagulant assays, together with their key applications and limitations, is essential both within the context of scientific research and for clinical usage. This review provides an overview of the current anticoagulant therapy and discusses the advantages and limitations of currently available anticoagulant assays. We also discuss studies involving low-molecular-weight heparin (LMWH)-based nanocarriers with emphasis on their anticoagulation performance. Conventional anticoagulants have been used for decades for the treatment of many diseases. Direct oral anticoagulants have overcome some limitations of heparins and vitamin K antagonists. However, the lack of an accurate laboratory assessment, as well as the lack of a factor “xaban” (Xa) inhibitor reversal agent, remains a major problem associated with these anticoagulants. LMWHs represent anticoagulant agents with noteworthy efficacy and safety, and they have been explored to improve their outcomes with various nanocarriers through several administration routes. The main problems related to LMWHs have been surmounted, and improved efficiency may be achieved through the use of DDSs.

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The Interplay between Drug and Sorbitol Contents Determines the Mechanical and Swelling Properties of Potential Rice Starch Films for Buccal Drug Delivery

Polymers ◽

10.3390/polym13040578 ◽

2021 ◽

Vol 13 (4) ◽

pp. 578

Author(s):

Bilal Harieth Alrimawi ◽

May Yee Chan ◽

Xin Yue Ooi ◽

Siok-Yee Chan ◽

Choon Fu Goh

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Physicochemical Characteristics ◽

Rice Starch ◽

Swelling Behaviour ◽

Swelling Properties ◽

Buccal Drug Delivery ◽

Swelling Characteristics ◽

Starch Films ◽

Film Development

Rice starch is a promising biomaterial for thin film development in buccal drug delivery, but the plasticisation and antiplasticisation phenomena from both plasticisers and drugs on the performance of rice starch films are not well understood. This study aims to elucidate the competing effects of sorbitol (plasticiser) and drug (antiplasticiser) on the physicochemical characteristics of rice starch films containing low paracetamol content. Rice starch films were prepared with different sorbitol (10, 20 and 30% w/w) and paracetamol contents (0, 1 and 2% w/w) using the film casting method and were characterised especially for drug release, swelling and mechanical properties. Sorbitol showed a typical plasticising effect on the control rice starch films by increasing film flexibility and by reducing swelling behaviour. The presence of drugs, however, modified both the mechanical and swelling properties by exerting an antiplasticisation effect. This antiplasticisation action was found to be significant at a low sorbitol level or a high drug content. FTIR investigations supported the antiplasticisation action of paracetamol through the disturbance of sorbitol–starch interactions. Despite this difference, an immediate drug release was generally obtained. This study highlights the interplay between plasticiser and drug in influencing the mechanical and swelling characteristics of rice starch films at varying concentrations.

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