Formulation of monolayered films with drug and polymers of opposing solubilities

• Published in: International journal of pharmaceutics 2008-06, Vol.358 (1), p.184-191
• Main Authors: Perumal, V.A., Lutchman, D., Mackraj, I., Govender, T.
• Format: Article
• Language: English
• Subjects: Acrylic Resins - chemistry; Adrenergic beta-Antagonists - administration & dosage; Adrenergic beta-Antagonists - chemistry; Biological and medical sciences; Buccal; Chemistry, Pharmaceutical; Chitosan - chemistry; Drug Compounding; Drug release; Excipients - chemistry; General pharmacology; Half-Life; Hardness; Hydrogen-Ion Concentration; Kinetics; Medical sciences; Pharmaceutical Preparations - administration & dosage; Pharmaceutical Preparations - chemistry; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Physicochemical/mechanical characterisation; Propranolol - administration & dosage; Propranolol - chemistry; Reproducibility of Results; Solubility; Surface Properties; Tissue Adhesives
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2008.03.005

The aim of this study was to prepare and characterise monolayered multipolymeric films (MMFs) comprising of a hydrophilic drug (Propranolol HCl) (PHCl) and polymers of opposing solubilities. Films were prepared by emulsification and casted by a new approach using a silicone-molded tray with individual wells. MMFs comprising of PHCl with Eudragit ® 100 (EUD100) and Chitosan (CHT), i.e. films with drug and polymers of opposing solubilities were successfully prepared (PHCl:EUD100:CHT; 1:10:0.5) and demonstrated uniform and reproducible drug content (100.71 ± 2.66%), thickness (0.442 ± 0.030 mm), mucoadhesivity (401.40 ± 30.73 mN) and a controlled drug release profile. Drug release followed Higuchi's square-root model. Maximum swelling of the films occurred after 1 h and 28.26% of the films eroded during the 8-h test period. Mechanical testing revealed that the MMFs displayed a greater abrasion resistance, were more elastic and also required more energy to break, rendering them tougher and more suitable for buccal delivery than the monopolymeric PHCl:EUD100 film. The inclusion of CHT to the film led to a more porous surface morphology. The surface pH of the films remained constant at neutral pH. This study confirmed the potential of the above MMFs as a promising candidate for buccal delivery of PHCl.