Effect of novel mucoadhesive buccal patches of carvedilol on isoprenaline-induced tachycardia

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Abstract

The main aim of the study was designed to develop bioadhesive buccal patches of carvedilol (CR) and evaluate for isoprenaline-induced tachycardia. Buccal patches of carvedilol were prepared by using chitosan (CH), sodium salt of carboxy methyl cellulose (NaCMC), and polyvinyl alcohol (PVA) as mucoadhesive polymers. The solvent evaporation method was used for the preparation of buccal patches. The patches were evaluated for their physical characteristics like patch thickness, weight variation, content uniformity, folding endurance, surface pH, residence time, in vitro drug release, and in vivo pharmacodynamic study. The swelling index of the patches was found to be proportional to the polymer concentration, whereas surface pH of all the formulated bioadhesive patches was found to lie between neutral ranges. In-vitro release study shows that 94.75% drug was release in 8 hours from the patch, which containing 2% w/v chitosan. The folding endurance result shows good elasticity in all the patches. Application of buccal patches on buccal mucosa of rabbit shows a significant result in % inhibition of isoprenaline-induced tachycardia. Prepared buccal patches of chitosan, NaCMC, and PVA containing Carvedilol meet the ideal requirement for the delivery of cardiovascular drugs and inhibit the isoprenaline tachycardia.

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Most cited references 42

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Mucoadhesive drug delivery system: An overview

Bindu M. Boddupalli, Zulkar Mohammed, Ravinder Nath … (2010)

Mucoadhesive drug delivery systems interact with the mucus layer covering the mucosal epithelial surface, and mucin molecules and increase the residence time of the dosage form at the site of absorption. The drugs which have local action or those which have maximum absorption in gastrointestinal tract (GIT) require increased duration of stay in GIT. Thus, mucoadhesive dosage forms are advantageous in increasing the drug plasma concentrations and also therapeutic activity. In this regard, this review covers the areas of mechanisms and theories of mucoadhesion, factors influencing the mucoadhesive devices and also various mucoadhesive dosage forms.

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Orotransmucosal drug delivery systems: a review.

N.V. Madhav, Ashok Shakya, Pragati Shakya … (2009)

Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods and also enhances drug bioavailability because the mucosal surfaces are usually rich in blood supply, providing the means for rapid drug transport to the systemic circulation and avoiding, in most cases, degradation by first-pass hepatic metabolism. The systems contact with the absorption surface resulting in a better absorption, and also prolong residence time at the site of application to permit once or twice daily dosing. For some drugs, this results in rapid onset of action via a more comfortable and convenient delivery route than the intravenous route. 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. 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. Transmucosal products are a relatively new drug delivery strategy. Transmucosal drug delivery promises four times the absorption rate of skin. Drugs considered for oral transmucosal delivery are limited to existing products, and until there is a change in the selection and development process for new drugs, candidates for oral transmucosal delivery will be limited. The present papers intend to overview a wide range of orotransmucosal routes being potentially useful for transmucosal drug delivery and remind us of the success achieved with these systems and the latest advancement in the field.

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Drug permeation enhancement via buccal route: possibilities and limitations.

Sevda Senel, A.Atilla Hıncal (2001)

Over the last decade, there has been a particular interest in delivering drugs, especially peptides and proteins via the buccal route. It provides direct entry into the systemic circulation thus avoiding the hepatic first-pass effect and degradation in the gastrointestinal tract, ease of administration, and the ability to terminate delivery when required. However membrane permeation can be a limiting factor for many drugs administered via the buccal route, and the epithelium that lines the oral mucosa is a very effective barrier to the absorption of drugs. In order to deliver broader classes of drugs across the buccal mucosa, reversible methods of reducing the barrier potential of this tissue must be employed. This requisite has fostered the study of penetration enhancers that will safely alter the permeability restrictions of the buccal mucosa. It has been shown that buccal penetration can be improved by using various classes of transmucosal and transdermal penetration enhancers such as bile salts, surfactants, fatty acids and derivatives, chelators, cyclodextrins and chitosan. Among these chemicals used for the drug permeation enhancement, bile salts are most common. The first part of this paper focuses on work related to the elucidation of mechanisms of action of bile salts in buccal permeation enhancement of various drugs and mucosal irritation. In the second part, results showing the enhancing effect of chitosan on buccal permeation of hydrocortisone, a commonly used topical oral anti-inflammatory agent, and transforming growth factor beta (TGF-beta), which is a bioactive peptide to which the oral mucosa is relatively impermeable is presented.

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Author and article information

Journal

Journal ID (nlm-ta): J Adv Pharm Technol Res

Journal ID (iso-abbrev): J Adv Pharm Technol Res

Journal ID (publisher-id): JAPTR

Title: Journal of Advanced Pharmaceutical Technology & Research

Publisher: Medknow Publications & Media Pvt Ltd (India )

ISSN (Print): 2231-4040

ISSN (Electronic): 0976-2094

Publication date (Print): Apr-Jun 2014

Volume: 5

Issue: 2

Pages: 96-103

Affiliations

[1]Department of Pharmacy, IFTM University, Moradabad, Uttar Pradesh, India

[1 ]Defence Research Laboratory, DRDO, Tezpur, Assam, India

Author notes

Address for correspondence: Dr. Navneet Verma, Department of Pharmacy, IFTM University, Moradabad, Uttar Pradesh, India. E-mail: navneet28jan@ 123456yahoo.com

Article

Publisher ID: JAPTR-5-96

DOI: 10.4103/2231-4040.133436

PMC ID: 4065471

SO-VID: 994e57dc-fa61-40e0-8bc8-bd694380d8ca

License:

This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Effect of novel mucoadhesive buccal patches of carvedilol on isoprenaline-induced tachycardia

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Herbal Medicines Journal (Herb Med J)

Most cited references 42

Mucoadhesive drug delivery system: An overview

Orotransmucosal drug delivery systems: a review.

Drug permeation enhancement via buccal route: possibilities and limitations.

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