The amphipathic bioactive compounds curcumin, resveratrol, and mitomycin C, which have similar solubility parameter component distributions, have been studied for encapsulation under batch conditions into core–shell nanocarriers composed of external hydrophobically functionalized polyelectrolytes and an inner matrix of polyesters or polyester blends: poly(l-lactide), poly(lactide-co-glycolide), and/or poly(ethylene succinate). Our contribution comprises determining the influence of process parameters on the properties and quality of the final products, namely core–shell nanoparticles loaded with appropriate drugs, according to process analysis technologymanagement. The crucial roles of the organic phase dosing rates and process temperatures were carefully investigated. Moreover, a technically feasible method of removing organic solvents from aqueous dispersions─stripping with inert gas─was employed and evaluated via FT-IR studies. The experiments were supported by the calculation and analysis of solubility parameters (δ) and dispersion (δ_d), polar (δ_p), and hydrogen bond (δ_h) components utilizing HSPiP software. The payload locus and sample morphology were studied via atomic force microscopy and X-ray photoelectron spectroscopy analyses with Ar⁺ sputtering. It was demonstrated that dosing rates of organic phases not exceeding ca. 0.5 mL/min per 1 L of aqueous dispersion of hydrophobically functionalized polyelectrolytes made it possible to obtain core–shell nanoparticles of ca. 100–150 nm with a very narrow polydispersity (PdI < 0.2). The locus of amphipathic payloads in nanocarriers, mostly within the core polymeric structure, was in good agreement with the results of solubility parameter component studies: water-insoluble polyesters with both polar and nonpolar interactions between chains serve as good host materials for amphipathic drugs.

中文翻译：

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批量条件下两亲性药物在核壳聚合物纳米颗粒中的包埋 - 控制和溶解度参数的作用


两亲性生物活性化合物姜黄素、白藜芦醇和丝裂霉素 C 具有相似的溶解度参数组分分布，已经研究了在批量条件下封装到核壳纳米载体中，这些载体由外部疏水官能化聚电解质和聚酯或聚酯混合物的内部基质组成：聚（L-丙交酯）、聚（丙交酯-CO）-乙交酯）和/或聚（琥珀酸乙二醇酯）。我们的贡献包括确定工艺参数对最终产品性能和质量的影响，即根据工艺分析技术管理，载有适当药物的核壳纳米颗粒。仔细研究了有机相加样速率和工艺温度的关键作用。此外，采用了一种技术上可行的方法，即从水性分散体中去除有机溶剂——用惰性气体剥离——并通过 FT-IR 研究进行了评估。利用 HSPiP 软件计算和分析溶解度参数 （δ） 和分散度 （δ_d）、极性 （δ_p） 和氢键 （δ_h） 组分，为实验提供支持。通过原子力显微镜和 Ar⁺ 溅射的 X 射线光电子能谱分析研究了有效载荷轨迹和样品形态。结果表明，疏水官能化聚电解质的水分散体中有机相的加样速率不超过每 1 L 水分散体约 0.5 mL/min，使得获得具有非常窄多分散性 （PdI < 0.2） 的约 100-150 nm 的核壳纳米颗粒成为可能。 纳米载体中两亲性有效载荷的位点，主要在核心聚合物结构内，与溶解度参数成分研究的结果非常一致：链之间具有极性和非极性相互作用的水不溶性聚酯是两亲性药物的良好宿主材料。