Predicting the Loading Capability of mPEG‐PDLLA to Hydrophobic Drugs Using Solubility Parameters†,Chinese Journal of Chemistry

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Predicting the Loading Capability of mPEG‐PDLLA to Hydrophobic Drugs Using Solubility Parameters†
Chinese Journal of Chemistry ( IF 5.5 ) Pub Date : 2020-03-06 , DOI: 10.1002/cjoc.202000078
Jiali Sun _{1,

2} , Qi Wei _{1,

2} , Na Shen ₁ , Zhaohui Tang _{1,

2} , Xuesi Chen ₁

Affiliation

Physical encapsulation of drugs into polymer micelles is a common method of loading hydrophobic drugs. Methoxy polyethylene glycol‐poly(D ,L ‐lactide) (mPEG‐PDLLA) is one of the most commonly used drug carrier. At present, whether a carrier is suitable for the loading of a certain drug is determined by drug loading experiments. This process costs a lot of time. Therefore, an efficient predicting method to avoid time‐consuming tests is critical. In this study, we prepared mPEG_5k‐PDLLA_5k and used it to load a series of drugs. Three parameters were used to test the miscibility of mPEG_5k‐PDLLA_5k with drugs, including absolute difference in Hildebrand solubility parameters (|Δδ |), Flory–Huggins interaction parameter (χ ) and the distance (D value) calculated from the two‐dimensional solubility parameters. We found the two‐dimensional solubility parameters obtained from JB2013 group contribution (GC) method was useful. By comparing the drug loading content (DLC) with the D value, we found that when the D value was less than 5.0 (MJ/m³)^1/2, the miscibility of drug and mPEG_5k‐PDLLA_5k was good and drug loading capability was high; when the D value was more than 8.0 (MJ/m³)^1/2, the drug was barely loaded. Thus, this work provided a rationale to qualitatively predict the loading capability of mPEG_5k‐PDLLA_5k for hydrophobic drugs.

中文翻译：

使用溶解度参数预测mPEG-PDLLA对疏水性药物的负载能力†

将药物物理包封到聚合物胶束中是装载疏水性药物的常用方法。甲氧基聚乙二醇-聚（D，L-丙交酯）（mPEG-PDLLA）是最常用的药物载体之一。目前，通过载药实验来确定载体是否适合载药。该过程花费大量时间。因此，避免浪费时间的测试的有效预测方法至关重要。在本研究中，我们制备了mPEG _5k- PDLLA _5k并用于装载一系列药物。使用三个参数测试mPEG _5k -PDLLA _5k与药物的混溶性，包括Hildebrand溶解度参数的绝对差异（|Δδ |），Flory-Huggins相互作用参数（χ）和从二维溶解度参数计算出的距离（D值）。我们发现从JB2013基团贡献（GC）方法获得的二维溶解度参数很有用。通过将载药量（DLC）与D值进行比较，我们发现当D值小于5.0（MJ / m ³）^1/2时，药物与mPEG _5k -PDLLA _5k的混溶性好，载药量能力高；当D值大于8.0（MJ / m ³）^1/2时，药物几乎没有装。因此，这项工作为定性预测mPEG _5k- PDLLA _5k对疏水性药物的负载能力提供了依据。

更新日期：2020-03-06

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