Restani Rita B, Pires Rita F, Tolmatcheva Anna, Cabral Rita, Baptista Pedro V, Fernandes Alexandra R, Casimiro Teresa, Bonifácio Vasco D B, Aguiar-Ricardo Ana
LAQV, REQUIMTE Departamento de Química, Faculdade de Ciências e Tecnologia Universidade Nova de Lisboa 2829-516 Caparica Portugal.
CQFM/IN and IBB-Institute for Bioengineering and Biosciences, Instituto Superior Técnico Universidade de Lisboa 1049-001 Lisboa Portugal.
ChemistryOpen. 2018 Jul 25;7(10):772-779. doi: 10.1002/open.201800093. eCollection 2018 Oct.
POxylated polyurea dendrimer (PUREOOx)-based nanoparticles were loaded with paclitaxel (PTX) and doxorubicin (DOX) and micronized with chitosan (CHT) by using supercritical CO-assisted spray drying (SASD). Respirable, biocompatible, and biodegradable dry powder formulations (DPFs) were produced to effectively transport and deliver the chemotherapeutics with a controlled rate to the deep lung. In vitro studies performed with the use of the lung adenocarcinoma cell line showed that DOX@PUREOOx nanoparticles were much more cytotoxic than the free drug. Additionally, the DPFs did not show higher cytotoxicity than the respective nanoparticles, and DOX-DPFs showed a higher chemotherapeutic effect than PTX formulations in adenocarcinoma cells.
基于聚氧化聚脲树枝状大分子（PUREOOx）的纳米颗粒负载了紫杉醇（PTX）和阿霉素（DOX），并通过超临界CO₂辅助喷雾干燥（SASD）与壳聚糖（CHT）一起进行微粉化处理。制备出了可吸入、生物相容且可生物降解的干粉制剂（DPF），以有效地将化疗药物以可控速率运输并递送至肺深部。使用肺腺癌细胞系进行的体外研究表明，DOX@PUREOOx纳米颗粒的细胞毒性比游离药物大得多。此外，DPF的细胞毒性并不高于相应的纳米颗粒，并且DOX-DPF在腺癌细胞中的化疗效果比PTX制剂更高。
