<br>确定影响长春瑞滨热敏脂质体制剂体外性能特征的关键参数,Journal of Controlled Release

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确定影响长春瑞滨热敏脂质体制剂体外性能特征的关键参数
Journal of Controlled Release ( IF 10.5 ) Pub Date : 2020-09-04 , DOI: 10.1016/j.jconrel.2020.08.059
Maximilian Regenold ₁ , Jessica Steigenberger ₂ , Elisa Siniscalchi ₃ , Michael Dunne ₁ , Luca Casettari ₄ , Heiko Heerklotz ₂ , Christine Allen ₁

Affiliation

研究证明了通过热敏脂质体进行热触发药物递送治疗局部癌症的优势。当触发血管内药物释放时，传统脂质体系统面临的挑战（例如有限的药物释放和整个感兴趣区域的均匀分布）可能会得到克服。最突出的例子是阿霉素热敏脂质体制剂，称为 ThermoDox®。许多其他药物可能受益于使用热敏脂质体的相同靶向和局部递送方法，因为它可以显着改善治疗指数。长春瑞滨是一种半合成的长春花生物碱，已证明对多种癌症具有活性。已经开发了几种封装长春瑞滨的脂质体制剂作为减少全身药物暴露的手段。本研究采用系统方法探索制剂和载药参数及其对长春瑞滨快速释放热敏脂质体制剂性能特征的影响。更广泛地说，这项研究表明，特定药物（即长春瑞滨）的非热敏脂质体制剂观察到的趋势不能轻易转化为其热敏对应物。还强调了白蛋白的存在对稳定性和体外释放的深远影响。鉴于最近的一些报告在没有生物学相关成分的情况下检查药物释放，这一点具有重要意义。因此，强烈建议对脂质体制剂进行体外彻底挑战，以便更好地了解其体内可能的行为以及未来临床转化的潜力。

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Determining critical parameters that influence in vitro performance characteristics of a thermosensitive liposome formulation of vinorelbine

Studies have demonstrated the advantages associated with heat-triggered drug delivery via thermosensitive liposomes for the treatment of localized cancer. Challenges that traditional liposomal systems face such as limited drug release and homogeneous distribution throughout the region of interest can potentially be overcome when triggering intravascular drug release. The most prominent example is a thermosensitive liposome formulation of doxorubicin known as ThermoDox®. Many other drugs may benefit from the same targeted and localized delivery approach using thermosensitive liposomes as it can result in a significant improvement in the therapeutic index. Vinorelbine is a semi-synthetic vinca alkaloid which has shown to be active in a broad range of cancers. Several liposome formulations encapsulating vinorelbine have been developed as a means to reduce systemic drug exposure. The present study takes a systematic approach in exploring formulation and drug loading parameters and their influence on performance characteristics of a rapidly releasing thermosensitive liposome formulation of vinorelbine. More broadly, this study shows that trends observed for non-thermosensitive liposome formulations of specific drugs (i.e. vinorelbine) can not be easily translated to their thermosensitive counterparts. The profound impact of the presence of albumin on stability and in vitro release is also highlighted. This is of significance given that a number of recent reports examine drug release in the absence of biologically relevant components. As a result, a strong recommendation emanating from this is a thorough challenge of the liposome formulation in vitro in order to gain a better understanding of its likely behaviour in vivo as well as potential for future clinical translation.

更新日期：2020-09-04

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