Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone
The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax)...
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| Format: | Article |
| Language: | English |
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Sciendo
2016-12-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2016-0047 |
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| author | Gu Fugen Ma Weina Meng Gendalai Wu Chunzhi Wang Yi |
| author_facet | Gu Fugen Ma Weina Meng Gendalai Wu Chunzhi Wang Yi |
| author_sort | Gu Fugen |
| collection | DOAJ |
| description | The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax′, cmax and AUC of oral and nasal routes were significantly different (p < 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0 %. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible. |
| format | Article |
| id | doaj-art-bdd30ca33e8a4ace960fef1b5d56e208 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2016-12-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-bdd30ca33e8a4ace960fef1b5d56e2082025-02-02T09:57:54ZengSciendoActa Pharmaceutica1846-95582016-12-0166455556210.1515/acph-2016-0047acph-2016-0047Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidoneGu Fugen0Ma Weina1Meng Gendalai2Wu Chunzhi3Wang Yi4Department of Pharmaceutics Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050 , ChinaSchool of Pharmacy, Inner Mongolia Medical University, Hohhot 010110, ChinaDepartment of Pharmaceutics Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050 ChinaDepartment of Pharmaceutics Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050, ChinaDepartment of Pharmaceutics Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050, ChinaThe aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax′, cmax and AUC of oral and nasal routes were significantly different (p < 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0 %. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible.https://doi.org/10.1515/acph-2016-0047risperidonenasal gelformulationpharmacokineticsbioavailabilityciliotoxicity |
| spellingShingle | Gu Fugen Ma Weina Meng Gendalai Wu Chunzhi Wang Yi Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone Acta Pharmaceutica risperidone nasal gel formulation pharmacokinetics bioavailability ciliotoxicity |
| title | Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone |
| title_full | Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone |
| title_fullStr | Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone |
| title_full_unstemmed | Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone |
| title_short | Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone |
| title_sort | preparation and in vivo evaluation of a gel based nasal delivery system for risperidone |
| topic | risperidone nasal gel formulation pharmacokinetics bioavailability ciliotoxicity |
| url | https://doi.org/10.1515/acph-2016-0047 |
| work_keys_str_mv | AT gufugen preparationandinvivoevaluationofagelbasednasaldeliverysystemforrisperidone AT maweina preparationandinvivoevaluationofagelbasednasaldeliverysystemforrisperidone AT menggendalai preparationandinvivoevaluationofagelbasednasaldeliverysystemforrisperidone AT wuchunzhi preparationandinvivoevaluationofagelbasednasaldeliverysystemforrisperidone AT wangyi preparationandinvivoevaluationofagelbasednasaldeliverysystemforrisperidone |