Bioadhesive drug delivery system of diltiazem hydrochloride for improved bioavailability in cardiac therapy

Purpose: To prepare and evaluate bioadhesive buccal films of diltiazem hydrochloride (a L-type calcium channel blocker) for overcoming the limitations of frequent dosing, low bioavailability and gastrointestinal discomfort of oral delivery. Methods: Buccal films were prepared by solvent casting technique using sodium carboxymethylcellulose, polyvinyl pyrrolidone K-30 and polyvinyl alcohol. The films were evaluated for weight, thickness, surface pH, swelling index, in vitro residence time, folding endurance, in vitro release, ex-vivo permeation (across porcine buccal mucosa) and drug content uniformity. Results: The drug content of the formulations was uniform with a range of 18.94 ± 0.066 (F2) to 20.08 ± 0.07 mg per unit film (F1). The films exhibited controlled release ranging from 58.76 ± 1.62 to 91.45 ± 1.02 % over a period > 6 h. The films containing 20 mg diltiazem hydrochloride, polyvinyl alcohol (10 %) and polyvinyl pyrrolidone (1 % w/v) i.e. formulation F5, showed moderate swelling, convenient residence time and promising drug release, and thus can be selected for further development of a buccal film for potential therapeutic uses. Conclusion: The developed formulation is a potential bioadhesive buccal system for delivering diltiazem directly to systemic circulation, circumventing first-pass metabolism, avoiding gastric discomfort and improving bioavailability at a minimal dose.

Influence of factors in the oral mucosa maturation pattern: a cross-sectional study applying multivariate analyses

Aim: To evaluate the association between oral health status, socio-demographic and behavioral factors with the pattern of maturity of normal epithelial oral mucosa. Methods: Exfoliative cytology specimens were collected from 117 men from the border of the tongue and floor of the mouth on opposite sides. Cells were stained with the Papanicolaou method and classified into: anucleated, superficial cells with nuclei, intermediate and parabasal cells. Quantification was made by selecting the first 100 cells in each glass slide. Sociodemographic and behavioral variables were collected from a structured questionnaire. Oral health was analyzed by clinical examination, recording decayed, missing and filled teeth index (DMFT) and use of prostheses. Multivariable linear regression models were applied. Results: No significant differences for all studied variables influenced the pattern of maturation of the oral mucosa except for alcohol consumption. There was an increase of cell surface layers of the epithelium with the chronic use of alcohol. Conclusions: It is appropriate to use Papanicolaou cytopathological technique to analyze the maturation pattern of exposed subjects, with a strong recommendation for those who use alcohol - a risk factor for oral cancer, in which a change in the proportion of cell types is easily detected.