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Formulation and evaluation of mucoadhesive buccal films of enalapril maleate.

Semalty A, Semalty M, Nautiyal U - Indian J Pharm Sci (2010)

Bottom Line: In the present study ten formulations of mucoadhesive drug delivery system of enalapril maleate were prepared as buccal films, by solvent casting technique.Sodium carboxymethylcellulose, hydroxylpropylmethylcellulose, hydroxyethylcellulose and polyvinyl pyrrolidone K-90 were used as mucoadhesive polymers.It was concluded that the films containing 20 mg of enalapril maleate in sodium carboxymethylcellulose 2% w/v and hydroxyethyl cellulose 2% w/v (formulation F5), showed good swelling, a convenient residence time and promising controlled drug release, thus can be selected for the development of buccal film for effective therapeutic uses.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar (Garhwal)-246 174, India.

ABSTRACT
Enalapril maleate is used in the treatment of hypertension and angina pectoris. It shows low bioavailability due to high hepatic first pass metabolism. Hence the present work was undertaken to formulate mucoadhesive buccal films of enalapril maleate with an objective to improve therapeutic efficacy, patient compliance and the bioavailability. In the present study ten formulations of mucoadhesive drug delivery system of enalapril maleate were prepared as buccal films, by solvent casting technique. Sodium carboxymethylcellulose, hydroxylpropylmethylcellulose, hydroxyethylcellulose and polyvinyl pyrrolidone K-90 were used as mucoadhesive polymers. Prepared films were evaluated for their weight, thickness, surface pH, swelling index, drug content uniformity, in vitro residence time, folding endurance in vitro release and permeation studies. Films exhibited controlled release over more than 10 h in permeation studies. It was concluded that the films containing 20 mg of enalapril maleate in sodium carboxymethylcellulose 2% w/v and hydroxyethyl cellulose 2% w/v (formulation F5), showed good swelling, a convenient residence time and promising controlled drug release, thus can be selected for the development of buccal film for effective therapeutic uses.

No MeSH data available.


Related in: MedlinePlus

Ex vivo permeation studies of selected mucoadhesive buccal films of enalaprilPermeation studies in pH 7.4 phosphate buffer of formulations F5 (—■—) containing SCMC 2% w/v and HEC 2% w/v and F6 (—▲—) containing PVP K-90 5 % w/v and SCMC 2 % w/v with 20 mg enalapril in each film.
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Figure 2: Ex vivo permeation studies of selected mucoadhesive buccal films of enalaprilPermeation studies in pH 7.4 phosphate buffer of formulations F5 (—■—) containing SCMC 2% w/v and HEC 2% w/v and F6 (—▲—) containing PVP K-90 5 % w/v and SCMC 2 % w/v with 20 mg enalapril in each film.

Mentions: It was also concluded that formulation F5 (containing SCMC and HEC) and F6 (containing SCMC and PVP K-90) showed good swelling, a convenient residence time as well as promising drug release. On the basis of release pattern, swelling and residence time, F5 and F6 formulations were chosen for ex vivo study. In ex vivo study, drug permeation through the porcine buccal mucosa was determined for formulation F5 and F6 (Fig. 2). The drug permeation was found to be 82.48 % and 90.86 % in F5 and F6 after 10 h. The drug permeation decreased in ex vivo study in comparison of in vitro release. This decrease in drug diffusion observed from ex vivo study compared to in vitro, may be due to the lesser permeability of porcine mucosa and also the presence of a backing membrane in the ex vivo study, which make the release unidirectional. The backing membrane restricting the contact of the film with the receptor fluid to one side alone slows down the water uptake, swelling and disruption of the matrix in turn releasing lesser amount of drug in specified time, compared to the one without the backing membrane. The correlation coefficient values were found to be 0.9852 and 0.9667 for F5 and F6, respectively showing good correlation. It may be concluded that the release kinetics followed zero order. The Higuchi Plots of F5 and F6 were found to be almost linear with correlation coefficient values of 0.9310 and 0.9748. This proves that the drug permeation followed the matrix diffusion process.


Formulation and evaluation of mucoadhesive buccal films of enalapril maleate.

Semalty A, Semalty M, Nautiyal U - Indian J Pharm Sci (2010)

Ex vivo permeation studies of selected mucoadhesive buccal films of enalaprilPermeation studies in pH 7.4 phosphate buffer of formulations F5 (—■—) containing SCMC 2% w/v and HEC 2% w/v and F6 (—▲—) containing PVP K-90 5 % w/v and SCMC 2 % w/v with 20 mg enalapril in each film.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3116300&req=5

Figure 2: Ex vivo permeation studies of selected mucoadhesive buccal films of enalaprilPermeation studies in pH 7.4 phosphate buffer of formulations F5 (—■—) containing SCMC 2% w/v and HEC 2% w/v and F6 (—▲—) containing PVP K-90 5 % w/v and SCMC 2 % w/v with 20 mg enalapril in each film.
Mentions: It was also concluded that formulation F5 (containing SCMC and HEC) and F6 (containing SCMC and PVP K-90) showed good swelling, a convenient residence time as well as promising drug release. On the basis of release pattern, swelling and residence time, F5 and F6 formulations were chosen for ex vivo study. In ex vivo study, drug permeation through the porcine buccal mucosa was determined for formulation F5 and F6 (Fig. 2). The drug permeation was found to be 82.48 % and 90.86 % in F5 and F6 after 10 h. The drug permeation decreased in ex vivo study in comparison of in vitro release. This decrease in drug diffusion observed from ex vivo study compared to in vitro, may be due to the lesser permeability of porcine mucosa and also the presence of a backing membrane in the ex vivo study, which make the release unidirectional. The backing membrane restricting the contact of the film with the receptor fluid to one side alone slows down the water uptake, swelling and disruption of the matrix in turn releasing lesser amount of drug in specified time, compared to the one without the backing membrane. The correlation coefficient values were found to be 0.9852 and 0.9667 for F5 and F6, respectively showing good correlation. It may be concluded that the release kinetics followed zero order. The Higuchi Plots of F5 and F6 were found to be almost linear with correlation coefficient values of 0.9310 and 0.9748. This proves that the drug permeation followed the matrix diffusion process.

Bottom Line: In the present study ten formulations of mucoadhesive drug delivery system of enalapril maleate were prepared as buccal films, by solvent casting technique.Sodium carboxymethylcellulose, hydroxylpropylmethylcellulose, hydroxyethylcellulose and polyvinyl pyrrolidone K-90 were used as mucoadhesive polymers.It was concluded that the films containing 20 mg of enalapril maleate in sodium carboxymethylcellulose 2% w/v and hydroxyethyl cellulose 2% w/v (formulation F5), showed good swelling, a convenient residence time and promising controlled drug release, thus can be selected for the development of buccal film for effective therapeutic uses.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar (Garhwal)-246 174, India.

ABSTRACT
Enalapril maleate is used in the treatment of hypertension and angina pectoris. It shows low bioavailability due to high hepatic first pass metabolism. Hence the present work was undertaken to formulate mucoadhesive buccal films of enalapril maleate with an objective to improve therapeutic efficacy, patient compliance and the bioavailability. In the present study ten formulations of mucoadhesive drug delivery system of enalapril maleate were prepared as buccal films, by solvent casting technique. Sodium carboxymethylcellulose, hydroxylpropylmethylcellulose, hydroxyethylcellulose and polyvinyl pyrrolidone K-90 were used as mucoadhesive polymers. Prepared films were evaluated for their weight, thickness, surface pH, swelling index, drug content uniformity, in vitro residence time, folding endurance in vitro release and permeation studies. Films exhibited controlled release over more than 10 h in permeation studies. It was concluded that the films containing 20 mg of enalapril maleate in sodium carboxymethylcellulose 2% w/v and hydroxyethyl cellulose 2% w/v (formulation F5), showed good swelling, a convenient residence time and promising controlled drug release, thus can be selected for the development of buccal film for effective therapeutic uses.

No MeSH data available.


Related in: MedlinePlus