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Mucoadhesive tablets for controlled release of acyclovir
Roberto Ruiz-Caro1, Manuel Gago-Guillan, Francisco Javier Otero-Espinar
1Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040-Madrid, Spain.
Chemical & Pharmaceutical Bulletin
|August 7, 2012
Summary
Chitosan (CS) and hydroxypropyl-methylcellulose (HPMC) tablets enhance acyclovir (ACV) oral bioavailability. CS tablets provide rapid ACV release, making chitosan ideal for gastroretentive drug delivery formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biomaterials
Background:
- Improving oral bioavailability of drugs like acyclovir (ACV) is crucial for effective treatment.
- Gastric drug delivery systems aim to prolong drug residence time in the stomach.
- Mucoadhesive polymers offer potential for enhanced gastric drug retention.
Purpose of the Study:
- To develop and evaluate mucoadhesive tablets of acyclovir (ACV) using chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) for improved oral bioavailability.
- To investigate the in vitro behavior of these tablets in acidic media simulating fed and fasted gastric states.
- To assess the suitability of CS and HPMC as excipients for gastroretentive drug delivery.
Main Methods:
- Formulation of mucoadhesive tablets containing acyclovir (ACV) with chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC).
- In vitro swelling, bioadhesion, and dissolution studies conducted in acidic media (pH 1.5 and 4).
- Drug release kinetics analyzed using the Hopfenberg model.
Main Results:
- All CS and/or HPMC tablets exhibited good mucoadhesive properties on gastric mucosa.
- In vitro ACV dissolution was significantly influenced by polymer swelling behavior.
- CS/HPMC tablets showed sustained release for 24 hours, while CS-only tablets released ACV completely within 4 hours at pH 1.5.
- Drug release data fitted the Hopfenberg model, indicating heterogeneous erosion.
Conclusions:
- Chitosan (CS) and hydroxypropyl-methylcellulose (HPMC) are effective mucoadhesive polymers for gastric drug delivery of acyclovir (ACV).
- CS-only tablets demonstrate rapid and complete drug release, suitable for immediate gastric release.
- Chitosan (CS) is a promising excipient for developing gastroretentive formulations due to its gastric compatibility and drug release characteristics.
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