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摘要
We evaluated structural factors characterizing PEG-b-P(Asp-Bzl) micelles including core size, aggregation number (N-agg), and core surface PEG density by means of small- angle X-ray scattering (SAXS), field flow fractionation with multi-angle light scattering (FFF-MALS) analysis, and DLS. Furthermore, we evaluated the stability of PEG-b-P(Asp-Bzl) micelles by means of GPC. This paper reports the correlation between the evaluated micelles' structural factors and the micelles' behaviors including the micelles' in vivo pharmacokinetic behaviors. One micelle PEG(12)-b-P(Asp-Bzl) (PEG= 12,000) exhibited a high core surface density (similar to 0.99 chain/nm(2)). In these circumstances, PEG(12)-b-P(Asp-Bzl) micelles exhibited a highly stretched PEG brush form. However, the evaluated core surface PEG densities could not fully explain the micelles' in vivo pharmacokinetic behaviors. In contrast, GPC will become a strong tool for predicting PEG(12)-b-P(Asp-Bzl) micelles' in vivo behaviors, as well as the micelles' in vitro behaviors. The stability results correlated strongly with the area-under-the-curve (AUC) values of PEG-b-P(Asp-Bzl) micelles' in vivo pharmacokinetics. Finally, we evaluated PEG(12)-b-P(Asp-Bzl) micelles' most effective structural factor for determining the micelles' behaviors, and the micelles' outermost shell surface's PEG density (D-OS,D- (PEG)) correlated with the micelles' behaviors. We revealed that the evaluated D-OS, (PEG) is the most important factor for understanding PEG(12)-b-P(Asp-Bzl) micelles' behaviors.
- 出版日期2015-4-10
- 单位河北医科大学
