In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene.
Poor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. A long-acting preparation may address these limitations. The aim of this paper was to further investigate the in vitro characteristics and in viv...
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2015-01-01
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| Series: | PLoS ONE |
| Online Access: | https://doi.org/10.1371/journal.pone.0125953 |
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| author | Xiangyang Xie Wen Lin Chuanfeng Xing Yanfang Yang Qiang Chi Hui Zhang Ying Li Zhiping Li Yang Yang Zhenbo Yang Mingyuang Li |
| author_facet | Xiangyang Xie Wen Lin Chuanfeng Xing Yanfang Yang Qiang Chi Hui Zhang Ying Li Zhiping Li Yang Yang Zhenbo Yang Mingyuang Li |
| author_sort | Xiangyang Xie |
| collection | DOAJ |
| description | Poor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. A long-acting preparation may address these limitations. The aim of this paper was to further investigate the in vitro characteristics and in vivo performances of nalmefene microspheres. Nalmefene was blended with poly (lactide-co-glycolide) (PLGA) to prepare the target microspheres by an O/O emulsification solvent evaporation method. The prepared microspheres exhibited a controlled release profile of nalmefene in vitro over 4 weeks, which was well fitted with a first-order model. In vitro degradation study showed that the drug release in vitro was dominated by both drug diffusion and polymer degradation mechanisms. Pharmacokinetics study indicated that the prepared microspheres could provide a relatively constant of nalmefene plasma concentration for at least one month in rats. The in vivo pharmacokinetics profile was well correlated with the in vitro drug release. Pharmacodynamics studies revealed that the drug loaded microspheres could produce a long-acting antagonism efficacy on rats. These results demonstrated the promising application of injectable PLGA microspheres containing nalmefene for the long-term treatment of alcohol dependence. |
| format | Article |
| id | doaj-art-ab3fceb144724a27bf91e56c97fa2d8d |
| institution | OA Journals |
| issn | 1932-6203 |
| language | English |
| publishDate | 2015-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj-art-ab3fceb144724a27bf91e56c97fa2d8d2025-08-20T02:34:10ZengPublic Library of Science (PLoS)PLoS ONE1932-62032015-01-01105e012595310.1371/journal.pone.0125953In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene.Xiangyang XieWen LinChuanfeng XingYanfang YangQiang ChiHui ZhangYing LiZhiping LiYang YangZhenbo YangMingyuang LiPoor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. A long-acting preparation may address these limitations. The aim of this paper was to further investigate the in vitro characteristics and in vivo performances of nalmefene microspheres. Nalmefene was blended with poly (lactide-co-glycolide) (PLGA) to prepare the target microspheres by an O/O emulsification solvent evaporation method. The prepared microspheres exhibited a controlled release profile of nalmefene in vitro over 4 weeks, which was well fitted with a first-order model. In vitro degradation study showed that the drug release in vitro was dominated by both drug diffusion and polymer degradation mechanisms. Pharmacokinetics study indicated that the prepared microspheres could provide a relatively constant of nalmefene plasma concentration for at least one month in rats. The in vivo pharmacokinetics profile was well correlated with the in vitro drug release. Pharmacodynamics studies revealed that the drug loaded microspheres could produce a long-acting antagonism efficacy on rats. These results demonstrated the promising application of injectable PLGA microspheres containing nalmefene for the long-term treatment of alcohol dependence.https://doi.org/10.1371/journal.pone.0125953 |
| spellingShingle | Xiangyang Xie Wen Lin Chuanfeng Xing Yanfang Yang Qiang Chi Hui Zhang Ying Li Zhiping Li Yang Yang Zhenbo Yang Mingyuang Li In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene. PLoS ONE |
| title | In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene. |
| title_full | In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene. |
| title_fullStr | In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene. |
| title_full_unstemmed | In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene. |
| title_short | In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene. |
| title_sort | in vitro and in vivo evaluations of plga microspheres containing nalmefene |
| url | https://doi.org/10.1371/journal.pone.0125953 |
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