Article

In vitro and in vivo evaluation of buccal bioadhesive films containing salbutamol sulphate.

Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221005, India.
Chemical & pharmaceutical bulletin (impact factor: 1.7). 01/2010; 58(3):307-11. pp.307-11
Source: PubMed

ABSTRACT The aim of present study was to prepare and evaluate buccal bioadhesive films of salbutamol sulphate (SS) for the treatment of asthma. The films were designed to release the drug for a prolonged period of time so as to reduce the frequency of administration of the available conventional dosage forms of SS. The different proportions of sodium carboxymethylcellulose (SCMC) and Carbopol 940P (CP 940P) were used for the preparation of films. Carbopol was used to incorporate the desired bioadhesiveness in the films. The films were prepared by solvent casting method and evaluated for bioadhesion, in vitro drug release and anti asthmatic effect (bronchoprotection) in histamine induced bronchospasm of guinea pigs. In vitro drug release from the film was determined using a modified Franz diffusion cell while bioadhesiveness was evaluated with a modified two-arm balance using guinea pig buccal mucosa as a model tissue. Films containing SCMC : CP 940P ratio of 76 : 24 was found to be the best with moderate swelling along with favorable bioadhesion force and in vitro drug release. The drug release mechanism was found to follow non-Fickian diffusion as release mechanism. The prolonged in vivo effect (bronchoprotection) obtained from the buccal bioadhesive film of SS administered via buccal route may improve the treatment of asthmatic disorders by reducing the frequency of administration which is associated with the tolerance effect of SS. Additionally for the clinical benefit, it is also expected to reduce the major adverse effects of SS such as tachycardia and arrhythmias via buccal absorption.

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    Article: Buccoadhesive films for once-a-day administration of rivastigmine: systematic formulation development and pharmacokinetic evaluation.
    Rishi Kapil, Sanju Dhawan, Sarwar Beg, Bhupinder Singh
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    ABSTRACT: Context: Rivastigmine, an anti-Alzheimer's drug, suffers from major predicaments like low oral bioavailability, severe GI adverse effects related to rapid fluctuations in drug plasma levels, and high frequency of dosing. Objective: The present investigation aims at developing buccoadhesive films capable of delivering the drug in vivo in a sustained manner. Augmentation of drug bioavailability by the avoidance of first-pass effect through the buccal route and reduction in GI side effects would be other key advantages of this system. Methods: Buccoadhesive films of rivastigmine were systematically designed and evaluated for in vitro drug release, ex vivo buccal permeation and ex vivo buccoadhesive strength. Optimal composition of the polymer blends was rationally chosen using a central composite design and overlay plot. In vivo pharmacokinetic studies were carried out in rabbits, and attempts were made to establish in vitro/ in vivo correlations (IVIVC). Results: Besides possessing the requisite drug release regulation, the optimized formulation exhibited excellent buccoadhesion, and buccal permeation. Pharmacokinetic studies indicated extension of plasma drug levels and level A of IVIVC was successfully established. Discussion: Excellent buccal bioadhesion and transmucosal permeation, coupled with drug release control, ratify the potential of the optimized formulation to deliver the drug in a controlled and site-specific manner. Successful establishment of IVIVC substantiated the judicious choice of in vitro dissolution media for simulating the in vivo conditions. Conclusion: Besides unraveling the polymer synergism, the study helped in developing an optimal once-a-day buccoadhesive drug delivery system exhibiting excellent trans-buccal permeation and buccoadhesive characteristics with improved bioavailability potential.
    Drug Development and Industrial Pharmacy 03/2012; · 1.49 Impact Factor
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Keywords

asthmatic effect
 
available conventional dosage forms
 
buccal absorption
 
buccal bioadhesive film
 
buccal bioadhesive films
 
buccal route
 
drug release mechanism
 
favorable bioadhesion force
 
guinea pig buccal mucosa
 
guinea pigs
 
histamine induced bronchospasm
 
major adverse effects
 
model tissue
 
modified Franz diffusion cell
 
modified two-arm balance
 
release mechanism
 
sodium carboxymethylcellulose
 
tolerance effect
 
vitro drug release
 
vivo effect