Investigation of betahistine dihydrochloride biocompatibility and nasal permeability in vitro
| Autor: | Bissera Pilicheva, Plamen Zagorchev, Margarita Kassarova, Milena N Draganova-Filipova |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Drug
Biocompatibility Health Toxicology and Mutagenesis media_common.quotation_subject Biomedical Engineering Pharmacology 030226 pharmacology & pharmacy General Biochemistry Genetics and Molecular Biology Chitosan 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Artificial Intelligence Oral administration medicine Betahistine General Pharmacology Toxicology and Pharmaceutics media_common General Immunology and Microbiology General Neuroscience General Medicine chemistry Drug delivery Toxicity Nasal administration General Agricultural and Biological Sciences 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Journal of Applied Biomedicine. 14:299-305 |
| ISSN: | 1214-0287 1214-021X |
| DOI: | 10.1016/j.jab.2016.06.001 |
| Popis: | Betahistine dihydrochloride, which is widely prescribed for the treatment of symptoms associated with Meniere’s syndrome, is generally administered orally in solid or liquid formulations. There is a strong need of profound investigation of alternative routes of administration of betahistine to overcome difficulties related to oral administration. The aim of this study was to evaluate betahistine cytotoxicity and permeability in vitro and to assess the drug’s relevance for incorporation in drug delivery systems for nasal administration. RPMI epithelial model was used to evaluate drug permeability in vitro. The cytotoxicity of betahistine was assessed by MTT test. Chitosan microspheres were used as a betahistine delivery system. RPMI 2650 formed a thick, impermeable cell layer on the apical side of the filter inserts and developed enough TEER values to confirm confluence. According to the obtained results, BET showed high permeability coefficients (Papp values in the range 2.3 × 10 −5 to 19 × 10 −5 ) and could, therefore, be successfully used in nasal drug delivery formulations. Also, BET exhibited a good safety profile regarding nasal epithelium toxicity. A dose-dependent reduction in cell viability was observed. The microspheres as drug delivery systems affected BET permeation profiles due to the presence of chitosan as an absorption enhancer. |
| Databáze: | OpenAIRE |
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