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Predicting the Loading Capability of mPEG‐PDLLA to Hydrophobic Drugs Using Solubility Parameters †
Author(s) -
Sun Jiali,
Wei Qi,
Shen Na,
Tang Zhaohui,
Chen Xuesi
Publication year - 2020
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.202000078
Subject(s) - solubility , miscibility , chemistry , hildebrand solubility parameter , polyethylene glycol , micelle , flory–huggins solution theory , drug , polymer , chemical engineering , chromatography , aqueous solution , organic chemistry , psychology , psychiatry , engineering
Summary of main observation and conclusion 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 (|Δ δ |), 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/m 3 ) 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/m 3 ) 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.