Details

Autor(en) / Beteiligte

• Zheng, Xiuli
• Pan, Dayi
• Chen, Miao
• Dai, Xinghang
• Cai, Hao
• Zhang, Hu
• Gong, Qiyong
• Gu, Zhongwei
• Luo, Kui

Titel

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

Ist Teil von

• Advanced materials (Weinheim), 2019-08, Vol.31 (35), p.e1901586-n/a

Ort / Verlag

Germany: Wiley Subscription Services, Inc

Erscheinungsjahr

2019

Link zum Volltext

Quelle

Wiley Online Library - AutoHoldings Journals

Beschreibungen/Notizen

• 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. Amphiphilic nanoparticles with a moderate hydrophile–lipophile balance display excellent structural stability, a prolonged blood circulation time, enhanced tumor penetration, and retention in tumors, all of which are key components for photodynamic therapy in cancer treatment. It is demonstrated that rational design of nanoparticles with a moderate hydrophile–lipophile balance value may significantly enhance their tumor retention and antitumor effect.