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用于难溶性药物PLGA纳米颗粒的表面活性剂介导的加速和区分性体外药物释放方法

Surfactant Mediated Accelerated and Discriminatory In Vitro Drug Release Method for PLGA Nanoparticles of Poorly Water-Soluble Drug.

作者信息

Gupta Ritu, Chen Yuan, Sarkar Mahua, Xie Huan

机构信息

College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.

出版信息

Pharmaceuticals (Basel). 2022 Nov 29;15(12):1489. doi: 10.3390/ph15121489.

DOI:10.3390/ph15121489
PMID:36558940
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9787738/
Abstract

In vitro drug release testing is an important quality control tool for formulation development. However, the literature has evidence that poly-lactide-co-glycolide (PLGA)-based formulations show a slower in vitro drug release than a real in vivo drug release. Much longer in vitro drug release profiles may not be reflective of real in vivo performances and may significantly affect the timeline for a formulation development. The objective of this study was to develop a surfactant mediated accelerated in vitro drug release method for the PLGA nanoparticles (NPs) of a novel chemotherapeutic agent AC1LPSZG, a model drug with a poor solubility. The Sotax USP apparatus 4 was used to test in vitro drug release in a phosphate buffer with a pH value of 6.8. The sink conditions were improved using surfactants in the order of sodium lauryl sulfate (SLS) < Tween 80 < cetyltrimethylammonium bromide (CTAB). The dissolution efficiency (DE) and area under the dissolution curve (AUC) were increased three-fold when increasing the CTAB concentration in the phosphate buffer (pH 6.8). Similar Weibull release kinetics and good linear correlations (R2~0.99) indicated a good correlation between the real-time in vitro release profile in the phosphate buffer (pH 6.8) and accelerated release profiles in the optimized medium. This newly developed accelerated and discriminatory in vitro test can be used as a quality control tool to identify critical formulation and process parameters to ensure a batch-to-batch uniformity. It may also serve as a surrogate for bioequivalence studies if a predictive in vitro in vivo correlation (IVIVC) is obtained. The results of this study are limited to AC1LPSZG NPs, but a similar consideration can be extended to other PLGA-based NPs of drugs with similar properties and solubility profiles.

摘要

体外药物释放测试是制剂研发中一项重要的质量控制工具。然而，文献表明基于聚乳酸-羟基乙酸共聚物（PLGA）的制剂在体外的药物释放比实际体内药物释放要慢。长得多的体外药物释放曲线可能无法反映实际的体内性能，并且可能会显著影响制剂研发的时间线。本研究的目的是为一种新型化疗药物AC1LPSZG（一种溶解度较差的模型药物）的PLGA纳米颗粒（NPs）开发一种表面活性剂介导的加速体外药物释放方法。使用Sotax USP装置4在pH值为6.8的磷酸盐缓冲液中测试体外药物释放。按照十二烷基硫酸钠（SLS）<吐温80<十六烷基三甲基溴化铵（CTAB）的顺序使用表面活性剂改善漏槽条件。当在磷酸盐缓冲液（pH 6.8）中增加CTAB浓度时，溶出效率（DE）和溶出曲线下面积（AUC）增加了三倍。相似的威布尔释放动力学和良好的线性相关性（R2~0.99）表明在磷酸盐缓冲液（pH 6.8）中的实时体外释放曲线与优化介质中的加速释放曲线之间具有良好的相关性。这种新开发的加速且具有区分性的体外测试可作为一种质量控制工具，以识别关键的制剂和工艺参数，确保批次间的一致性。如果获得预测性的体外-体内相关性（IVIVC），它也可作为生物等效性研究的替代方法。本研究结果仅限于AC1LPSZG NPs，但类似的考虑可以扩展到其他具有相似性质和溶解度曲线的基于PLGA的药物NPs。

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