Complex Coacervates between a Lactose-Modified Chitosan and Hyaluronic Acid as Radical-Scavenging Drug Carriers,Biomacromolecules

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Complex Coacervates between a Lactose-Modified Chitosan and Hyaluronic Acid as Radical-Scavenging Drug Carriers
Biomacromolecules ( IF 5.5 ) Pub Date : 2018-09-11 00:00:00 , DOI: 10.1021/acs.biomac.8b00863
Federica Vecchies ₁ , Pasquale Sacco ₁ , Eva Decleva ₁ , Renzo Menegazzi ₁ , Davide Porrelli ₂ , Ivan Donati ₁ , Gianluca Turco ₂ , Sergio Paoletti ₁ , Eleonora Marsich ₂

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Complex coacervation of two oppositely charged polysaccharides, namely a lactose-modified chitosan (CTL) and hyaluronan (HA), was investigated in this study. Coacervates of the two polysaccharides were prepared by drop-by-drop injection of HA into CTL. Transmittance and dynamic light scattering (DLS) measurements in combination with TEM analyses demonstrated the formation of spheroidal colloids in the nano-/microsize range showing good homogeneity. Strikingly, the presence of 150 mM supporting NaCl did not hamper the colloid formation. Stability studies on selected formulations demonstrated that HA/CTL coacervates were stable up to 3 weeks at 37 °C and behaved as pH-responsive colloids since transition from entangled to disentangled chains was attained for a proper pH range. The possibility of freeze-drying the coacervates for storage purposes and the ability of encapsulating selected payloads were investigated as well, for two values of the fraction of the lactitol side-chain substitution (F_L). Finally, biological tests using human neutrophils were undertaken at acidic pH value (pH = 6.0): under such experimental conditions, akin to those frequently occurring in the inflammatory microenvironment, coacervates scavenged reactive oxygen species (ROS) generated by these cells in basal conditions. Given the well documented bioactivity of CTL with respect to chitosan toward cartilage regeneration, these findings point to a possible application of HA/CTL-based colloids as scavenging and bioactive carriers for the delivery of therapeutic molecules at confined inflamed sites such as knee joints.

中文翻译：

乳糖修饰的壳聚糖和透明质酸之间的复合凝聚层作为清除自由基的药物载体

在这项研究中，研究了两种带相反电荷的多糖，即乳糖修饰的壳聚糖（CTL）和透明质酸（HA）的复合凝聚。通过将HA逐滴注射到CTL中来制备两种多糖的凝聚层。透射率和动态光散射（DLS）测量与TEM分析相结合，证明了在纳米级/微米级范围内球形胶体的形成，显示出良好的均质性。令人惊讶的是，150 mM的支持NaCl的存在并不妨碍胶体的形成。对选定制剂的稳定性研究表明，HA / CTL凝聚层在37°C下可稳定长达3周，并且可作为pH响应胶体，因为在适当的pH范围内可实现从缠结链到解缠链的过渡。_L）。最后，在酸性pH值（pH = 6.0）下使用人嗜中性白细胞进行生物学测试：在这种实验条件下，类似于在炎症性微环境中经常发生的那些，凝聚层清除了这些细胞在基础条件下产生的活性氧（ROS）。考虑到CTL对壳聚糖对软骨再生的生物活性的充分记录，这些发现表明基于HA / CTL的胶体作为清除剂和生物活性载体的可能应用，可用于在狭窄的发炎部位（如膝关节）递送治疗性分子。

更新日期：2018-09-11

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