Abstract
Purpose: To prepare and characterize buccal transmucosal delivery system of enalapril maleate for overcoming its low bioavailability, and hence provide improved therapeutic efficacy and patient compliance.Methods: Transmucosal drug delivery systems of enalapril maleate were formulated as buccal films by solvent casting technique using polyvinylpyrrolidone K90, hydroxypropyl methylcellulose, sodium carboxymethylcellulose (high viscosity). The films were evaluated for film weight, thickness, folding endurance, drug content uniformity, surface pH, in vitro residence time, in vitro drug release and ex-vivo permeation.Results: All the formulations showed high drug content (96.45 to 98.49 %). Those with good swelling showed good residence time. In vitro drug release was highest for films prepared with high viscosity grade sodium carboxymethylcellulose (SCMC- HV,F2), releasing 92.24 % of drug in 1.5 h) followed by F4 (containing polyvinyl pyrrolidone K-90 1 % w/v and SCMC (HV) 1 % w/v). Ex-vivo drug permeation at the end of 10 h was 82.24 and 89.9 % for F2 and F4, respectively.Conclusion: Prompt drug release was obtained from the formulation (F2) containing SCMC 2 % w/v with 10 mg enalapril. However, on the basis of the highest swelling and residence time, and controlled drug release, formulation F4 (containing PVP K-90 and SCMC HV) would be suitable for the development of buccal film for effective therapy of cardiac diseases.Keywords: Cardiac disease, Transmucosal, Buccal films, Enalapril maleate, Drug release, Ex-vivo permeation
Highlights
In recent years transmucosal drug delivery systems (TMDDSs) have been investigated for delivering the drugs across the various different mucosa for gaining various advantages across the conventional oral dosage forms
The improved bioavailability over the other sites available for TMDDS is the vital factor associated with transmucosal buccal drug delivery
The bubble free drug polymer solution was poured into glass Petri dish placed over a flat surface with Inverted funnel placed over the dish
Summary
In recent years transmucosal drug delivery systems (TMDDSs) have been investigated for delivering the drugs across the various different mucosa (like oral, buccal, nasal, vaginal or rectal) for gaining various advantages across the conventional oral dosage forms These advantages include providing prompt action, preventing the hepatic first pass metabolism, reducing the gastrointestinal irritation and reducing the dosage frequency [1,2]. Various TMDDS like tablets, films, patches, disks, strips, ointments and gels have been investigated [14,15,16,17,18,19,20,21] Out of these transmucosal buccal films have been reported to be more flexible, comfortable with relatively longer residence time (than that of oral gels) on the mucosa. The present study aimed to formulate and characterize transmucosal buccal films of enalapril maleate with the use of mucoadhesive polymers, including sodium carboxymethylcellulose (SCMC), hydroxylpropyl methylcellulose (HPMC), hydroxyethylcellulose (HEC) and polyvinyl pyrrolidone K-90 (PVP K-90)
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.