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二元混合普朗尼克系统对温度依赖性自组装过程和药物溶解度的协同作用。

Synergistic Effect of Binary Mixed-Pluronic Systems on Temperature Dependent Self-assembly Process and Drug Solubility.

作者信息

Lee Chin-Fen, Tseng Hsueh-Wen, Bahadur Pratap, Chen Li-Jen

机构信息

Department of Chemical Engineering, National Taiwan University, Taipei 10617, Taiwan.

Department of Chemistry, Veer Narmad South Gujarat University, Surat 395007, India.

出版信息

Polymers (Basel). 2018 Jan 22;10(1):105. doi: 10.3390/polym10010105.

DOI:10.3390/polym10010105
PMID:30966142
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6415020/
Abstract

Mixed Pluronic micelles from very hydrophobic and very hydrophilic copolymers were selected to scrutinize the synergistic effect on the self-assembly process as well as the solubilization capacity of ibuprofen. The tendency of mixing behavior between parent copolymers was systematically examined from two perspectives: different block chain lengths at same hydrophilicity (L92 + F108, +F98, +F88, and +F68), as well as various hydrophobicities at the same PPO moiety (L92 + F88, +F87, and +P84). Temperature-dependent micellization in these binary systems was clearly inspected by the combined use of high sensitivity differential scanning calorimeter (HSDSC) and dynamic light scattering (DLS). Changes in heat capacity and size of aggregates at different temperatures during the whole micellization process were simultaneously observed and examined. While distinction of block chain length between parent copolymers increases, the monodispersity of the binary Pluronic systems decreases. However, parent copolymers with distinct PPO moieties do not affirmatively lead to non-cooperative binding, such as the L92 + P84 system. The addition of ibuprofen promotes micellization as well as stabilizes aggregates in the solution. The partial replacement of the hydrophilic Pluronic by a more hydrophobic Pluronic L92 would increase the total hydrophobicity of mixed Pluronics used in the system to substantially enhance the solubility of ibuprofen. The solubility of ibuprofen in the 0.5 wt % L92 + 0.368 wt % P84 system is as high as 4.29 mg/mL, which is 1.4 times more than that of the 0.868 wt % P84 system and 147 times more than that in pure water at 37 °C.

摘要

选择由极疏水和极亲水共聚物组成的混合普朗尼克胶束,以研究其对自组装过程的协同作用以及布洛芬的增溶能力。从两个角度系统地研究了母体共聚物之间的混合行为趋势:相同亲水性下不同的嵌段链长度(L92 + F108、+F98、+F88和+F68),以及相同聚丙二醇(PPO)部分下的各种疏水性(L92 + F88、+F87和+P84)。通过联合使用高灵敏度差示扫描量热仪(HSDSC)和动态光散射(DLS),清晰地检测了这些二元体系中温度依赖性胶束化过程。同时观察并研究了整个胶束化过程中不同温度下聚集体的热容和尺寸变化。虽然母体共聚物之间嵌段链长度的差异增加,但二元普朗尼克体系的单分散性降低。然而,具有不同PPO部分的母体共聚物并不会肯定地导致非协同结合,例如L92 + P84体系。布洛芬的加入促进了胶束化,并稳定了溶液中的聚集体。用疏水性更强的普朗尼克L92部分替代亲水性普朗尼克会增加体系中所用混合普朗尼克的总疏水性,从而显著提高布洛芬的溶解度。布洛芬在0.5 wt% L92 + 0.368 wt% P84体系中的溶解度高达4.29 mg/mL,是0.868 wt% P84体系的1.4倍,是37℃纯水中溶解度的147倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/54079db8c9b8/polymers-10-00105-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/7f1331130b54/polymers-10-00105-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/09c8b9c20721/polymers-10-00105-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/bcfbc7b2cd4e/polymers-10-00105-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/f3f9bbe7a7ef/polymers-10-00105-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/0419a3ef5df5/polymers-10-00105-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/372140615643/polymers-10-00105-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/9d711b12a970/polymers-10-00105-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/d6318b2df6e0/polymers-10-00105-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/54079db8c9b8/polymers-10-00105-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/7f1331130b54/polymers-10-00105-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/09c8b9c20721/polymers-10-00105-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/bcfbc7b2cd4e/polymers-10-00105-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/f3f9bbe7a7ef/polymers-10-00105-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/0419a3ef5df5/polymers-10-00105-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/372140615643/polymers-10-00105-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/9d711b12a970/polymers-10-00105-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/d6318b2df6e0/polymers-10-00105-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df15/6415020/54079db8c9b8/polymers-10-00105-g009.jpg

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