Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride
Donepezil hydrochloride thermosensitive in situ gel for nasal delivery was prepared by using Poloxamer 407 and Poloxamer 188 as thermoreversible polymers, hydroxypropyl-β-cyclodextrin and ethylparaben as permeation enhancer and preservative, respectively. The gelation temperature and time, pH value...
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| Format: | Article |
| Language: | English |
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Sciendo
2020-09-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2020-0032 |
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| author | Gu Fugen Fan Huimin Cong Zhixin Li Shuang Wang Yi Wu Chunzhi |
| author_facet | Gu Fugen Fan Huimin Cong Zhixin Li Shuang Wang Yi Wu Chunzhi |
| author_sort | Gu Fugen |
| collection | DOAJ |
| description | Donepezil hydrochloride thermosensitive in situ gel for nasal delivery was prepared by using Poloxamer 407 and Poloxamer 188 as thermoreversible polymers, hydroxypropyl-β-cyclodextrin and ethylparaben as permeation enhancer and preservative, respectively. The gelation temperature and time, pH value of the gel formulation were found to meet the requirements for nasal administration. The in vitro erosion and in vitro release tests exhibited obvious drug sustained release behavior. Meantime, main pharmacokinetic parameters such as tmax, cmax and AUC in plasma as well as in brain were significantly different between the nasal gel formulation and intragastric drug solution in rats (p < 0.01). The relative bioavailability and drug targeting efficiency of the gel formulation were calculated to be 385.6 and 151.2 %, respectively. Thus, the drug gel formulation might be a potential new delivery system for treatment of Alzheimer’s disease due to its higher bioavailability and better distribution to brain when compared to oral route. |
| format | Article |
| id | doaj-art-bc29ca7cbf744ae291e13a3dc9568e03 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2020-09-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-bc29ca7cbf744ae291e13a3dc9568e032025-02-02T12:01:39ZengSciendoActa Pharmaceutica1846-95582020-09-0170341142210.2478/acph-2020-0032acph-2020-0032Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochlorideGu Fugen0Fan Huimin1Cong Zhixin2Li Shuang3Wang Yi4Wu Chunzhi5Affiliated Hospital, Inner Mongolia Medical University, Hohhot010050ChinaSchool of Pharmacy, Inner Mongolia Medical University, Hohhot010110ChinaSchool of Pharmacy, Inner Mongolia Medical University, Hohhot010110ChinaSchool of Pharmacy, Inner Mongolia Medical University, Hohhot010110ChinaAffiliated Hospital, Inner Mongolia Medical University, Hohhot010050ChinaAffiliated Hospital, Inner Mongolia Medical University, Hohhot010050ChinaDonepezil hydrochloride thermosensitive in situ gel for nasal delivery was prepared by using Poloxamer 407 and Poloxamer 188 as thermoreversible polymers, hydroxypropyl-β-cyclodextrin and ethylparaben as permeation enhancer and preservative, respectively. The gelation temperature and time, pH value of the gel formulation were found to meet the requirements for nasal administration. The in vitro erosion and in vitro release tests exhibited obvious drug sustained release behavior. Meantime, main pharmacokinetic parameters such as tmax, cmax and AUC in plasma as well as in brain were significantly different between the nasal gel formulation and intragastric drug solution in rats (p < 0.01). The relative bioavailability and drug targeting efficiency of the gel formulation were calculated to be 385.6 and 151.2 %, respectively. Thus, the drug gel formulation might be a potential new delivery system for treatment of Alzheimer’s disease due to its higher bioavailability and better distribution to brain when compared to oral route.https://doi.org/10.2478/acph-2020-0032donepezil hydrochloridethermosensitive in situ gelnasal deliverybioavailabilitybrain targeting |
| spellingShingle | Gu Fugen Fan Huimin Cong Zhixin Li Shuang Wang Yi Wu Chunzhi Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride Acta Pharmaceutica donepezil hydrochloride thermosensitive in situ gel nasal delivery bioavailability brain targeting |
| title | Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride |
| title_full | Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride |
| title_fullStr | Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride |
| title_full_unstemmed | Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride |
| title_short | Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride |
| title_sort | preparation characterization and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride |
| topic | donepezil hydrochloride thermosensitive in situ gel nasal delivery bioavailability brain targeting |
| url | https://doi.org/10.2478/acph-2020-0032 |
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