Abstract
Fluvastatin sodium (FVS) is a cholesterol lowering agent (HMG-CoA reductase inhibitor) which undergoes extensive hepatic first pass metabolism causing an absolute bioavailability of ~30%. The aim of this work was to formulate a buccoadhesive disc of FVS to be applied to the buccal mucosa, releasing the drug in a unidirectional manner, in order to improve the bioavailability of the drug and lower the dose-dependent side effects. The bioadhesive discs were prepared by direct compression method using several polymers such as: guar gum, sodium alginate, sodium carboxymethyl cellulose, carbopol 934P, and hydroxypropylmethyl cellulose. Impermeable ethyl cellulose was applied as the backing layer. Different permeation enhancers such as bile salts, surfactants, fatty acids, chitosan, dimethyl sulfoxide, and polyethylene glycol 6000 (PEG 6000) were tested to improve the permeability of buccal mucosal membranes. The optimized formulation contained FVS, guar gum, PEG 6000, and sodium deoxycholate (permeation enhancer, 4%). It showed a drug release of 95.4% in 80 min, drug permeation through chicken pouch membrane (flux (Jss) = 3.74 mg cm-2 h-1), ex vivo bioadhesion strength of 2.543 g, along with satisfactory bioadhesion time of 4.87 h. Physicochemical characteristics of the buccal discs such as drug content uniformity, disc thickness, disc hardness, surface pH, and swelling index were also evaluated.
Highlights
Oral drug administration is the most suitable and widely acceptable route for the delivery of most therapeutically active agents
Permeation enhancers may be utilized to overcome the permeability barrier in which they act by increasing the retention time of drug around the buccal mucosa, interaction with the buccal mucosal protein and intercellular lipid, and/or enhancing the drug partitioning across the buccal mucosa (Meher et al, 2012)
The maximum duration for buccal drug delivery is usually limited to approximately 4–6 h, since meal intake and/or drinking may require dosage form removal (Neelagiri et al, 2013)
Summary
Oral drug administration is the most suitable and widely acceptable route for the delivery of most therapeutically active agents. The most important determinant of buccal delivery is the degree of permeability of the mucosa since the therapeutic efficacy of a drug mainly depends on its ability to penetrate the tissue fast enough to provide the required effective plasma concentrations (De Caro et al, 2009). Drug absorption through the oral mucosal membranes requires that the drug dissolves sufficiently in a very small volume of saliva, which may represent an obstacle for poorly soluble drugs (Turunen et al, 2011)
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