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Hypericin Delivery System Based on P84 Copolymeric Micelles Linked with N-(3-Aminopropyl)-2-pyrrolidone for Melanoma-Targeted Photodynamic Therapy
ACS Applied Polymer Materials ( IF 4.4 ) Pub Date : 2020-03-25 , DOI: 10.1021/acsapm.0c00114 R. S. Gonçalves 1 , G. Braga 1 , A. C. V. de Oliveira 1 , G. B. César 2 , T. T. Tominaga 2 , E. H. Zampiere 1 , I. R. Calori 1 , F. A. P. de Morais 1 , E. A. Basso 1 , R. M. Pontes 1 , N. Hioka 1 , W. Caetano 1
ACS Applied Polymer Materials ( IF 4.4 ) Pub Date : 2020-03-25 , DOI: 10.1021/acsapm.0c00114 R. S. Gonçalves 1 , G. Braga 1 , A. C. V. de Oliveira 1 , G. B. César 2 , T. T. Tominaga 2 , E. H. Zampiere 1 , I. R. Calori 1 , F. A. P. de Morais 1 , E. A. Basso 1 , R. M. Pontes 1 , N. Hioka 1 , W. Caetano 1
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A hypericin (HYP) delivery system was developed on the basis of P84 copolymeric micelles linked covalently with N-(3-aminopropyl)-2-pyrrolidone (APP). The higher monomeric amounts of HYP when loaded in different proportions of P84 and P84-APP micelles were predicted by using a chemometric experimental design. Dynamic light scattering (DLS), ζ potential, loading efficiency, and transmission electron microscopy (TEM) were performed for characterizations of the copolymeric micelles. The particle size and low negative ζ potential showed that APP conjugation provides high levels of stability in the aqueous medium of P84 micelles. 1H1H-NOESY spectroscopy and theoretical calculations were applied to provide accurate insight on the preferential interaction sites of HYP-loaded P84 and P84-APP copolymeric micelles. The findings showed that HYP molecules were preferentially located in the core of both P84 and P84-APP micellar nanostructures. Self-assembled HYP molecules (in a more stable “head-to-tail” conformation) were observed when loaded into P84 micelles. In accordance with the chemometric experimental design the optimal ratio of P84/P84-APP (1:1) showed that the most pronounced HYP phototoxicity effect against B16-F10 melanoma cells recorded survival index that reached 18% at 10.0 μmol L–1. The findings pointed out that the high phototoxicity observed is related to the capacity of APP molecules in enhancing the HYP uptake by melanoma cells.
中文翻译：
基于P84胶束与N-（3-氨基丙基）-2-吡咯烷酮连接的金丝桃素递送系统，用于针对黑素瘤的光动力疗法
在与N-（3-氨基丙基）-2-吡咯烷酮（APP）共价连接的P84共聚物胶束的基础上，开发了金丝桃素（HYP）递送系统。通过使用化学计量实验设计，可以预测当以不同比例的P84和P84-APP胶束负载时，HYP的单体含量较高。进行动态光散射（DLS），ζ电位，负载效率和透射电子显微镜（TEM）表征共聚胶束。粒径和较低的负ζ电位表明APP偶联在P84胶束的水性介质中提供了高水平的稳定性。1小时1使用H-NOESY光谱学和理论计算，可以准确了解HYP负载的P84和P84-APP共聚胶束的优先相互作用位点。研究结果表明，HYP分子优先位于P84和P84-APP胶束纳米结构的核心。当装载到P84胶束中时，观察到自组装的HYP分子（处于更稳定的“头到尾”构象）。根据化学计量学实验设计，最佳比例的P84 / P84-APP（1：1）表明，对B16-F10黑色素瘤细胞最明显的HYP光毒性作用记录的生存指数在10.0μmolL –1时达到18％。。研究结果指出，观察到的高光毒性与APP分子增强黑素瘤细胞摄取HYP的能力有关。
更新日期：2020-04-23
中文翻译：
基于P84胶束与N-（3-氨基丙基）-2-吡咯烷酮连接的金丝桃素递送系统，用于针对黑素瘤的光动力疗法
在与N-（3-氨基丙基）-2-吡咯烷酮（APP）共价连接的P84共聚物胶束的基础上，开发了金丝桃素（HYP）递送系统。通过使用化学计量实验设计，可以预测当以不同比例的P84和P84-APP胶束负载时，HYP的单体含量较高。进行动态光散射（DLS），ζ电位，负载效率和透射电子显微镜（TEM）表征共聚胶束。粒径和较低的负ζ电位表明APP偶联在P84胶束的水性介质中提供了高水平的稳定性。1小时1使用H-NOESY光谱学和理论计算，可以准确了解HYP负载的P84和P84-APP共聚胶束的优先相互作用位点。研究结果表明，HYP分子优先位于P84和P84-APP胶束纳米结构的核心。当装载到P84胶束中时，观察到自组装的HYP分子（处于更稳定的“头到尾”构象）。根据化学计量学实验设计，最佳比例的P84 / P84-APP（1：1）表明，对B16-F10黑色素瘤细胞最明显的HYP光毒性作用记录的生存指数在10.0μmolL –1时达到18％。。研究结果指出，观察到的高光毒性与APP分子增强黑素瘤细胞摄取HYP的能力有关。
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