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Tunable Hydrophile-Lipophile Balance for Manipulating Structural Stability and Tumor Retention of Amphiphilic Nanoparticles.

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机构： [1]Huaxi MR Research Center (HMRRC), Functional and Molecular Imaging Key Laboratory of Sichuan Province, Department of Radiology, National Clinical Research Center for Geriatrics, State Key Laboratory of Biotherapy, West China Hospital, and National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, 610041, China. [2]West China School of Medicine, and West China College of Stomatology, Sichuan University, Chengdu, 610041, China. [3]Amgen Bioprocessing Centre, Keck Graduate Institute, CA, 91711, USA.

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Hydrophile-lipophile balance (HLB) has a great influence on the self-assembly and physicochemical properties of amphiphiles, thus affecting their biological effects. It is shown that amphiphilic nanoparticles (NPs) with a moderate HLB value display enhanced stability and highly efficient tumor retention. 2,2-Bis(hydroxymethyl)propionic acid hyperbranched poly(ethylene glycol) (PEG)-pyropheophorbide-a (Ppa) amphiphiles (G320P, G310P, G220P, and G210P) are synthesized with a tunable HLB value from 6.1 to 9.9 by manipulating the number of generation of dendrons (G2 or G3) and the molecular weight of PEG chains (10 or 20 kDa). Molecular dynamics simulations reveal that G320P and G210P with a moderate HLB value (8.0 and 7.8) self-assemble into very stable NPs with a small solvent accessible surface area and high nonbonding interactions. G320P with a moderate HLB value (8.0) and a long PEG chain excels against other NPs in prolonging the blood circulation time of Ppa (up to 13-fold), penetrating deeply into multicellular tumor spheroids and accumulating in tumors, and enhancing the PDT efficacy with a tumor growth inhibition of 96.0%. Rational design of NPs with a moderate HLB value may be implemented in these NP-derived nanomedicines to achieve high levels of retention in tumors. © 2019 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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出版当年[2019]版：

大类 | 1 区

材料科学

小类 | 1 区化学综合 1 区物理化学 1 区纳米科技 1 区材料科学：综合 1 区物理：应用 1 区物理：凝聚态物理

最新[2023]版：

大类 | 1 区

材料科学

小类 | 1 区化学：综合 1 区物理化学 1 区材料科学：综合 1 区纳米科技 1 区物理：应用 1 区物理：凝聚态物理

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第一作者机构： [1]Huaxi MR Research Center (HMRRC), Functional and Molecular Imaging Key Laboratory of Sichuan Province, Department of Radiology, National Clinical Research Center for Geriatrics, State Key Laboratory of Biotherapy, West China Hospital, and National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, 610041, China.

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