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Formulation strategies to modulate drug release from poloxamer based in situ gelling systems.
Expert Opinion on Drug Delivery ( IF 6.6 ) Pub Date : 2020-02-23 , DOI: 10.1080/17425247.2020.1731469
Hani Abdeltawab 1 , Darren Svirskis 1 , Manisha Sharma 1
Affiliation  

Introduction: Poloxamer based in situ gelling systems offer numerous advantages in drug delivery; however, their application as prolonged-release delivery platforms is limited mainly due to their weak mechanical properties and the interconnected aqueous network causing fast gel erosion and drug diffusion.Area covered: The focus of this review is to provide an insightful discussion on the formulation strategies that can be employed to sustain/prolong the drug release from poloxamer based in situ gelling systems. The review also outlines the formulation factors, influencing drug release from these systems.Expert opinion: The nature, composition, and concentration of poloxamers are the most critical factors in defining the rate of drug release from an in situ gelling matrix. Hydrophobic gel matrices have compact micellar arrangements resulting in slow diffusion and erosion. Depending on the intended clinical application, gel characteristics can be modulated, either by physical blending or by chemical crosslinking with additive materials, to slow release and improve residence time at the administration site. Incorporating drug-loaded particles into poloxamer gels sustains drug release by creating multiple rate-limiting release barriers. Chemical modification of poloxamers appears to be a promising strategy to obtain prolonged sustained release for parenteral application without compromising the rheological properties of the formulation.

中文翻译:

基于泊洛沙姆的原位胶凝系统调节药物释放的配方策略。

简介:基于泊洛沙姆的原位胶凝系统在药物输送方面具有众多优势;然而,它们作为缓释平台的应用受到限制,主要是由于其较弱的机械性能以及相互连接的水性网络导致快速的凝胶侵蚀和药物扩散。可用于维持/延长基于泊洛沙姆的原位胶凝系统中的药物释放。综述还概述了影响这些系统中药物释放的配方因素。专家意见:泊洛沙姆的性质,组成和浓度是确定原位胶凝基质中药物释放速率的最关键因素。疏水性凝胶基质的胶束排列紧密,导致扩散和侵蚀缓慢。根据预期的临床应用,可以通过物理掺混或通过与添加剂材料的化学交联来调节凝胶特性,以减慢释放并改善在给药部位的停留时间。将载有药物的颗粒掺入泊洛沙姆凝胶中可通过产生多个限速释放屏障来维持药物释放。化学修饰泊洛沙姆似乎是获得延长的肠胃外持续释放而不损害制剂流变性能的有前途的策略。通过物理掺合或通过与添加剂材料的化学交联来减缓释放并改善在给药部位的停留时间。将载有药物的颗粒掺入泊洛沙姆凝胶中可通过产生多个限速释放屏障来维持药物释放。化学修饰泊洛沙姆似乎是获得延长的肠胃外应用持续释放而不损害制剂流变性能的有前途的策略。通过物理掺合或通过与添加剂材料的化学交联来减缓释放并改善在给药部位的停留时间。将载有药物的颗粒掺入泊洛沙姆凝胶中可通过产生多个限速释放屏障来维持药物释放。化学修饰泊洛沙姆似乎是获得延长的肠胃外应用持续释放而不损害制剂流变性能的有前途的策略。
更新日期:2020-04-20
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