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Enhancing Photochemical Internalization of DOX through a Porphyrin-based Amphiphilic Block Copolymer
Biomacromolecules ( IF 6.2 ) Pub Date : 2017-10-31 00:00:00 , DOI: 10.1021/acs.biomac.7b01037
Jia Tian 1 , Lei Xu 1 , Yudong Xue 1 , Xiaoze Jiang 2 , Weian Zhang 1, 2
Affiliation  

Drug resistance is a primary obstacle that seriously reduces the therapy efficiency of most chemotherapeutic agents. To address this issue, the photochemical internalization (PCI) was employed to help the anticancer drug escape from lysosome and improve their translocation to the nucleus. A pH-sensitive porphyrin-based amphiphilic block copolymer (PEG113-b-PCL54-a-porphyrin) was synthesized, which was acted not only as a carrier for the delivery of DOX but also as a photosensitizer for PCI. PEG113-b-PCL54-a-porphyrin as a drug carrier exhibited a higher drug loading capacity, entrapment efficiency, and DOX release content. The PCI effect of PEG113-b-PCL54-a-porphyrin was studied by confocal laser scanning microscopy, and the results showed that most of DOX could be translocated into the nucleus for DOX-loaded PEG113-b-PCL54-a-porphyrin micelles. Moreover, the IC50 of pH-sensitive DOX-loaded PEG113-b-PCL54-a-porphyrin micelles was much lower than that of its counterpart without pH-responsiveness, DOX-loaded PEG113-b-PCL54-porphyrin micelles. Therefore, this drug delivery system based on pH-sensitive porphyrin-containing block copolymer would act as a potential vehicle for overcoming drug resistance in chemotherapy.

中文翻译:

通过基于卟啉的两亲嵌段共聚物增强DOX的光化学内在化

耐药性是严重降低大多数化疗药物治疗效率的主要障碍。为了解决这个问题,采用了光化学内在化(PCI)来帮助抗癌药物从溶酶体中逃逸并改善其向核的转运。pH敏感的卟啉类两亲嵌段共聚物(PEG 113 - b -PCL 54 --卟啉)合成,其作用不仅是作为对DOX的递送的载体,而且作为PCI的光敏剂。PEG 113 - b -PCL 54 - a卟啉作为药物载体表现出较高的载药量,包封率和DOX释放量。PEG的PCI效果113 - b -PCL 54 --卟啉,通过共聚焦激光扫描显微镜观察,结果表明,大多数DOX的可转位到细胞核中用于装载DOX PEG 113 - b -PCL 54 --卟啉微团。此外,pH敏感的负载DOX的PEG 113 - b- PCL 54 - a的IC 50-卟啉胶束比没有pH响应的DOX负载的PEG 113 - b -PCL 54-卟啉胶束要低得多。因此,这种基于pH敏感的含卟啉的嵌段共聚物的药物递送系统将成为克服化学疗法中耐药性的潜在媒介。
更新日期:2017-10-31
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