Ostacolo Luisanna, Russo Paola, De Rosa Giuseppe, La Rotonda Maria Immacolata, Maglio Giovanni, Nese Giuseppe, Spagnuolo Gianrico, Rengo Sandro, Oliva Adriana, Quaglia Fabiana
Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy.
Macromol Biosci. 2008 Jul 7;8(7):682-9. doi: 10.1002/mabi.200700303.
The production of PEEA microspheres with potential as carriers for protein oral delivery is described. PEEAs with different hydrophilicity were synthesized and characterized. Experiments showed that an increase in copolymer hydrophilicity gave particles less prone to cell interaction. BSA release profiles from PEEA microspheres demonstrated that an increase in polymer hydrophilicity was useful in limiting protein burst and modulating drug delivery rate by increasing PEEA degradability. These results show that fine-tuning of the hydrophilic/hydrophobic properties of PCL is essential for the formulation protein-loaded microspheres with specific properties.
本文描述了具有作为蛋白质口服递送载体潜力的聚(乙交酯-乙交酯-乙交酯)(PEEA)微球的制备。合成并表征了具有不同亲水性的PEEA。实验表明,共聚物亲水性的增加使颗粒与细胞相互作用的倾向降低。PEEA微球的牛血清白蛋白(BSA)释放曲线表明,聚合物亲水性的增加有助于通过提高PEEA的降解性来限制蛋白质的突释并调节药物递送速率。这些结果表明,对聚己内酯(PCL)亲水/疏水性质的微调对于制备具有特定性质的载蛋白微球至关重要。