庆祝上市 全新改版

【文摘发布】聚合物微囊控制药物释放的模型:辅料及混合物的影响

Title:A mechanistic model of controlled drug release from polymer millirods: Effects of excipients and complex binding

Author:Fangjing Wanga, Gerald M. Saidela, , and Jinming Gaob

Resource:Journal of Controlled Release ,119,(1), 111-120

Abstract:
The incorporation of different cyclodextrin (CD) excipients such as HPβ–CD, β–CD, γ–CD or α–CD into polymer millirods for complexing β-lapachone (β-lap), a potent anti-cancer drug, significantly improved the drug release kinetics with various drug release patterns. However, such a complex system requires a mechanistically based model in order to provide a quantitative understanding of the many molecular events and processes that are essential for the rational development of millirod implants. This study focuses on mathematical modeling of drug release from PLGA cylindrical millirods. This millirod system incorporates multiple components: a PLGA matrix; excipient in free and complex forms; drug in free, bound, and crystalline forms. The model characterizes many dynamic transport and complexation processes that include radial diffusion, excipient complexation and crystalline drug dissolution. Optimal estimates of the model parameters were obtained by minimizing the difference between model simulation and experimentally measured drug release kinetics. The effects of different drug loadings on the drug release rate were simulated and compared with other data to validate this model. Whereas our model can simulate all the experimental data, the Higuchi model can simulate only some of them. Furthermore, our model incorporates mechanisms by which the processes underlying drug release from a polymer matrix can be quantitatively analyzed. These processes include drug entrapment/dissolution in the matrix, drug recrysallization, and supersaturation. This modeling study shows that complex binding capacity, which affects drug initial conditions, drug–polymer interactions, and bound drug behavior in aqueous solution, is crucial in controlling drug release kinetics.

PMID:17379347

【文摘发布】文摘类新闻投稿格式专贴
>

感觉Title翻译的不好
本人已认领该文编译,48小时后若未提交译文,请其他战友自由认领。
Title:A mechanistic model of controlled drug release from polymer millirods: Effects of excipients and complex binding
标题:聚合物微囊药物控释模型:辅料及复合包合的影响
Author:Fangjing Wanga, Gerald M. Saidela, , and Jinming Gaob
作者:Fangjing Wanga, Gerald M. Saidela, , and Jinming Gaob

Resource:Journal of Controlled Release ,119,(1), 111-120
文章来源:Journal of Controlled Release药物控释杂志,119,(1), 111-120
Abstract:
The incorporation of different cyclodextrin (CD) excipients such as HPβ–CD, β–CD, γ–CD or α–CD into polymer millirods for complexing β-lapachone (β-lap), a potent anti-cancer drug, significantly improved the drug release kinetics with various drug release patterns.
摘要:
不同类型的环糊精如HPβ–CD, β–CD, γ–CD or α–CD,与抗癌药物β-lapachone (β-lap)包合形成聚合物微囊,可通过各种不同的药物释放模式明显改善药物的释放动力学行为。
However, such a complex system requires a mechanistically based model in order to provide a quantitative understanding of the many molecular events and processes that are essential for the rational development of millirod implants.
然而,这种包合系统需要一个机械理论模型来对各种分子间的相互作用和过程提供一种量化解释,这对微囊埋植剂的合理发展是必要的。
This study focuses on mathematical modeling of drug release from PLGA cylindrical millirods. This millirod system incorporates multiple components: a PLGA matrix; excipient in free and complex forms; drug in free, bound, and crystalline forms.
这项研究集中在药物从PLGA圆筒型微囊中释放的数学模型。这个微囊系统包括多种成分:PLGA基质;单一和复合型赋形剂;游离、结合和结晶型药物。
The model characterizes many dynamic transport and complexation processes that include radial diffusion, excipient complexation and crystalline drug dissolution. Optimal estimates of the model parameters were obtained by minimizing the difference between model simulation and experimentally measured drug release kinetics.
模型利用径向扩散,辅料络合作用和晶体药物的溶出度来表征多个动力学运输和络合过程。对模型参数的最佳评价通过最小化模型模拟和实验测定间的药物释放动力学差别来获得。

The effects of different drug loadings on the drug release rate were simulated and compared with other data to validate this model. Whereas our model can simulate all the experimental data, the Higuchi model can simulate only some of them.
模拟不同载药量对药物释放速率的影响并与其它数据进行比较,以此来验证此模型。然而,我们的模型可以模拟所有的实验数据,而Higuchi模型仅模拟其中某些数据。
Furthermore, our model incorporates mechanisms by which the processes underlying drug release from a polymer matrix can be quantitatively analyzed. These processes include drug entrapment/dissolution in the matrix, drug recrysallization, and supersaturation.
另外,我们的模型整合机制使药物从聚合物基质中释放的过程可以被定量分析。这些过程包括药物在基质中的包埋/溶出,药物再结晶和过饱和。

This modeling study shows that complex binding capacity, which affects drug initial conditions, drug–polymer interactions, and bound drug behavior in aqueous solution, is crucial in controlling drug release kinetics.
此模型研究显示复合包合容量影响药物原始状态、药物-聚合物间相互作用及水溶液中结合型药物的行为,其在药物控释动力学中起决定性作用。
PMID:17379347
编译:

聚合物微囊药物控释模型:辅料及复合包合的影响


不同类型的环糊精如HPβ–CD, β–CD, γ–CD or α–CD,与抗癌药物β-lapachone (β-lap)包合形成聚合物微囊,可通过各种不同的药物释放模式明显改善药物的释放动力学行为。但对于发展微囊埋植剂,需要为这种包合系统建立一个机械理论模型来对各种分子间的相互作用和过程进行量化解释。对此Fangjing Wanga等人进行了相关研究。(Journal of Controlled Release ,119,(1), 111-120)
此项研究集中在药物从PLGA圆筒型微囊中释放的数学模型。这个微囊系统包括多种成分:PLGA基质;单一和复合型赋形剂;游离、结合和结晶型药物。模型利用径向扩散,辅料络合作用和晶体药物的溶出度来表征多个动力学运输和络合过程。通过将模型模拟和实验测定间药物释放动力学差别最小化来获得对模型参数的最佳评价。模拟不同载药量对药物释放速率的影响并与其它数据进行比较,以此来验证此模型。然而研究人员制备的模型可以模拟所有的实验数据,而Higuchi模型仅可以模拟其中某些数据。另外,研究用模型整合机制使药物从聚合物基质中的释放过程可以被定量分析。其中包括药物在基质中的包埋/溶出,药物再结晶和过饱和。此模型研究显示复合包合容量影响药物原始状态、药物-聚合物间相互作用及水溶液中结合型药物的行为,其在药物控释动力学中起决定性作用。(丁香)

中文字符:484
上面的战友辛苦了,但我有一点点意见,提出来仅供参考。

The incorporation of different cyclodextrin (CD) excipients such as HPβ–CD, β–CD, γ–CD or α–CD into polymer millirods for complexing β-lapachone (β-lap), a potent anti-cancer drug, significantly improved the drug release kinetics with various drug release patterns. 将不同类型的环糊精如HPβ–CD, β–CD, γ–CD or α–CD,与抗癌药物β-lapachone (β-lap)包合形成聚合物微囊,可通过各种不同的药物释放模式明显改善药物的释放动力学行为。
many molecular events and processes 各种分子间的相互作用和过程
The model characterizes many dynamic transport and complexation processes that include radial diffusion, excipient complexation and crystalline drug dissolution.模型利用径向扩散,辅料络合作用和晶体药物的溶出度来表征多个动力学运输和络合过程。 characterizes 表征 radial diffusion 径向扩散
The effects of different drug loadings on the drug release rate were simulated and compared with other data to validate this model.模拟不同载药量对药物释放速率的影响并与其它数据进行比较,以此来验证此模型。 drug loadings 载药量
drug entrapment/dissolution in the matrix 药物在基质中的包埋/溶出
十分感谢xxb_6410 的细心指导。
您是专家,偶是菜鸟。~0~ 偶要不断努力学习和进步。
希望xxb_6410 经常指导。^-^
ginnyran战友客气了,哪敢妄谈指导,大家一起学习,一起进步,一同提高。同时也希望能够得到战友的帮助。
您的位置:医学教育网 >> 医学资料