Papers by Keyword: Mucoadhesion

Abstract: Film-forming systems (FFSs) were developed by using Eudragit^® E100 as a film former. Kaempferia parviflora (black ginger) extract was used as an anti-inflammatory agent for aphthous ulcers. The FFS could rapidly form a thin film in only 5 s when it was applied to a wet surface e.g. an aphthous ulcer. When the FFS was applied to a dry surface, the FFS without extract could form a film in 2-4 min. The incorporation of this extract contributed to delaying the film-formation time in the dry state; hence, the film-forming time increased to 6-8 min. The mucoadhesive property of FFSs was verified with the wash-off method. To simulate oromucosal conditions, the FFSs were applied on a cellophane membrane coated with mucin and washed by phosphate buffer of pH 6.8. The formulations without mucoadhesive polymers could not withstand flushing with a medium for more than 8 min without dislodging. Therefore, three different mucoadhesive agents were trialed: PVP K90, HPMC E15 LV, and HPC SL. The highest adhesion results were obtained when HPMC was added at 5%(w/w) as well as, the residence time was 22 min. In vitro release of black ginger extract from FFS showed a gradual release for 2 h. This study indicated that the FFS with HPMC E15 LV was an appropriate alternative formulation as a local delivery system for an aphthous ulcer.

Abstract: The local drug delivery based on mucoadhesion is an effective medical treatment. The mucoadhesive property relies on the formulated gel having optimized rheology. The addition of the drug also showed a major influence towards the sol-gel transition. In this study, compositional effect of Eudragit E100^® base polymer, various mucoadhesive polymers, and the black ginger extract on the rheological property of the formulated sol-gel was assessed. It was found that gelling point and gel strength could be tuned mainly based on the concentration of Eudragit E100 limited at 40% w/w due to the viscosity. At Eudragit E100 of 30% w/w, 0.5% w/w herbal extract, and 1%w/w polyvinyl alcohol, the solution reached the gel point at 286 s (tan δ=1) with the gel strength of 1 kPa (G’=G”). For all the formulated sol-gels, the rheological property became better (faster gelling point with the gel strength varying from 100-700 kPa at low strain) a simulated saliva environment.

Abstract: Topical oral dosage form for anti-inflammation in the oral cavity provides convenience and patient compliance. Formulations of orabase gels composed of poloxamer 407, PVP, PVA, SCMC and/or white petrolatum (WP) and hydrocarbon gel (HG) were investigated for in vitro swelling and mucoadhesion for incorporation of melatonin. The highest detachment time of 18 h with an optimized swelling ratio of 1.3 was obtained from a gel with 55% of WP and HG in the presence of poloxamer 407 and PVP 90. In conclusion, an optimum balancing ratio between hydrocarbons and bioadhesive polymer parts is required to obtain mucoadhesive characteristics of the oral gel.

Abstract: The aim of this study is to prepare mucoadhesive chitosan microspheres for protein drug to deliver to intestine through oral administration. The thiolated Eudragit was synthesized by reaction between L-cysteine hydrochloride and Eudragit® L-100. About 8 mol-% of cysteine was introduced to the Eudragit-cysteine conjugate. The conjugate was used to coat bovine serum albumin (BSA)-loaded chitosan microspheres. The average particle sizes of BSA-loaded thiolated Eudragit-coated chitsoan microspheres (TECMs) were 4.06±0.74 .m and the uniform sizedistribution was shown. The in vitro release of BSA from BSA-loaded TECMs was pH-dependent. Our results indicated that thiolated Eudragit might be a good candidate as a coating material for oral delivery of protein drug owing to mucoadhesive and pH-sensitive properties.