Synergistic encapsulation of the anti-HIV agent efavirenz within mixed poloxamine/poloxamer polymeric micelles
Synergistic encapsulation of the anti-HIV agent efavirenz within mixed poloxamine/poloxamer polymeric micelles
复制标题
DOI：
10.1016/j.nano.2011.01.017
复制
发表时间：
2011-10-01
影响因子：
5.4
通讯作者：
Sosnik, Alejandro
中科院分区：
文献类型：
--
作者：
Chiappetta, Diego A.;Facorro, Graciela;Sosnik, Alejandro
本研究考察了由线性和支化聚（环氧乙烷）-聚（环氧丙烷）制成的混合聚合物胶束的协同性能，以更有效地包封抗HIV药物依法韦仑。通过动态光散射、浊点和电子自旋共振实验研究了10%的高亲水性泊洛沙姆（Pluronic F127）和更疏水的泊洛沙胺（Tetronic T304和T904）组成的二元体系的共胶束化过程。然后，胶束的协同增溶能力显示。结果显示溶解度从4 μ g/ml急剧增加到超过33 mg/ml，代表8430倍的增加。此外，与纯泊洛沙胺相比，载药混合胶束显示出随时间增加的物理稳定性。总体研究结果证实了泊洛沙姆/泊洛沙胺系统作为特洛伊纳米载体用于药物封装和通过口服途径释放的巨大通用性，并且它们需要对先前技术进行相关增强，以实现更顺应的儿科HIV药物治疗。在本研究中，作者证明了泊洛沙姆/泊洛沙胺系统作为特洛伊纳米载体用于抗-艾滋病毒药物封装和口服释放途径。显示了高度相关的稳定性和溶解度增强，这可能最终导致更顺应性的抗HIV药物治疗。(C)2011 Elsevier Inc. All rights reserved.
This study investigated the synergistic performance of mixed polymeric micelles made of linear and branched poly(ethylene oxide)-poly (propylene oxide) for the more effective encapsulation of the anti-HIV drug efavirenz. The co-micellization process of 10% binary systems combining different weight ratios of a highly hydrophilic poloxamer (Pluronic F127) and a more hydrophobic poloxamine counterpart (Tetronic T304 and T904) was investigated by means of dynamic light scattering, cloud point and electronic spin resonance experiments. Then, the synergistic solubilization capacity of the micelles was shown. Findings revealed a sharp solubility increase from 4 mu g/ml up to more than 33 mg/ml, representing a 8430-fold increase. Moreover, the drug-loaded mixed micelles displayed increased physical stability over time in comparison with pure poloxamine ones. Overall findings confirmed the enormous versatility of the poloxamer/poloxamine systems as Trojan nanocarriers for drug encapsulation and release by the oral route and they entail a relevant enhancement of the previous art towards a more compliant pediatric HIV pharmacotherapy.From the Clinical Editor: In this study, the authors demonstrate the versatility of poloxamer/poloxamine systems as Trojan nanocarriers for anti-HIV drug encapsulation and release by the oral route. A highly relevant stability and solubility enhancement is shown, which may ultimately lead to more compliant anti-HIV pharmacotherapy. (C) 2011 Elsevier Inc. All rights reserved.