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pH-Responsive Polyion Complex Vesicle with Polyphosphobetaine Shells
Langmuir ( IF 3.7 ) Pub Date : 2018-06-25 00:00:00 , DOI: 10.1021/acs.langmuir.8b00632 Yuki Ohara 1 , Keita Nakai 1 , Sana Ahmed 2 , Kazuaki Matsumura 2 , Kazuhiko Ishihara 3 , Shin-ichi Yusa 1
Langmuir ( IF 3.7 ) Pub Date : 2018-06-25 00:00:00 , DOI: 10.1021/acs.langmuir.8b00632 Yuki Ohara 1 , Keita Nakai 1 , Sana Ahmed 2 , Kazuaki Matsumura 2 , Kazuhiko Ishihara 3 , Shin-ichi Yusa 1
Affiliation
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When a bioactive molecule is taken into cells by endocytosis, it is sometimes unable to escape from the lysosomes, resulting in inefficient drug release. We prepared pH-responsive polyion complex (PIC) vesicles that collapse under acidic conditions such as those inside a lysosome. Furthermore, under acidic conditions, cationic polymer was released from the PIC vesicles to break the lysosome membranes. Diblock copolymers (P20M167 and P20A190) consisting of water-soluble zwitterionic poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) block and cationic or anionic blocks were synthesized via reversible addition–fragmentation chain transfer (RAFT) radical polymerization. Poly(3-(methacrylamidopropyl) trimethylammonium chloride) (PMAPTAC) and poly(sodium 6-acrylamidohexanoate) (PAaH) were used as the cationic and anionic blocks, respectively. The pendant hexanoate groups in the PAaH block are ionized in basic water and in phosphate buffered saline (PBS), while the hexanoate groups are protonated in acidic water. In basic water, PIC vesicles were formed from a charge neutralized mixture of oppositely charged diblock copolymers. At the interface of PIC vesicle and water exists biocompatible PMPC shells. Under acidic conditions, the PIC vesicles collapsed, because the charge balance shifted due to protonation of the PAaH block. After collapse of the PIC vesicles, P20A190 formed micelles composed of protonated PAaH core and PMPC shells, while P20M167 was released as unimers. PIC vesicles can encapsulate hydrophilic nonionic guest molecules into their hollow core. Under acidic conditions, the PIC vesicles can release the guest molecules and P20M167. The cationic P20M167 can break the lysosome membrane to efficiently release the guest molecules from the lysosomes to the cytoplasm.
中文翻译：
具有多磷酸甜菜碱壳的pH响应性聚离子复合物囊泡
当生物活性分子通过内吞作用被带入细胞时，有时无法从溶酶体中逃逸，导致药物释放效率低下。我们准备了在酸性条件下（如溶酶体内部）崩解的pH响应性聚离子复合物（PIC）囊泡。此外，在酸性条件下，阳离子聚合物从PIC囊泡中释放出来，破坏了溶酶体膜。双嵌段共聚物（P 20 M 167和P 20 A 190通过可逆的加成-断裂链转移（RAFT）自由基聚合反应合成了由水溶性两性离子聚（2-甲基丙烯酰氧基乙基磷酰胆碱）（PMPC）嵌段和阳离子或阴离子嵌段组成的）。聚（3-（甲基丙烯酰胺基丙基）三甲基氯化铵）（PMAPTAC）和聚（6-丙烯酰胺基己酸钠）（PAaH）分别用作阳离子和阴离子嵌段。PAaH嵌段中的己酸侧基在碱性水中和磷酸盐缓冲盐水（PBS）中被离子化，而己酸基在酸性水中被质子化。在碱性水中，PIC囊泡是由带相反电荷的二嵌段共聚物的电荷中和后的混合物形成的。在PIC囊泡和水的界面处存在生物相容性PMPC壳。在酸性条件下，PIC囊泡塌陷，因为电荷平衡由于PAaH嵌段的质子化而移动。PIC囊泡塌陷后，P20 A 190形成了由质子化的PAaH核和PMPC壳组成的胶束，而P 20 M 167以单体形式释放。PIC囊泡可将亲水性非离子客体分子包裹到其空心中。在酸性条件下，PIC囊泡可释放客体分子和P 20 M 167。阳离子P 20 M 167可以破坏溶酶体膜，从而有效地将客体分子从溶酶体释放到细胞质中。
更新日期：2018-06-25
中文翻译：
具有多磷酸甜菜碱壳的pH响应性聚离子复合物囊泡
当生物活性分子通过内吞作用被带入细胞时，有时无法从溶酶体中逃逸，导致药物释放效率低下。我们准备了在酸性条件下（如溶酶体内部）崩解的pH响应性聚离子复合物（PIC）囊泡。此外，在酸性条件下，阳离子聚合物从PIC囊泡中释放出来，破坏了溶酶体膜。双嵌段共聚物（P 20 M 167和P 20 A 190通过可逆的加成-断裂链转移（RAFT）自由基聚合反应合成了由水溶性两性离子聚（2-甲基丙烯酰氧基乙基磷酰胆碱）（PMPC）嵌段和阳离子或阴离子嵌段组成的）。聚（3-（甲基丙烯酰胺基丙基）三甲基氯化铵）（PMAPTAC）和聚（6-丙烯酰胺基己酸钠）（PAaH）分别用作阳离子和阴离子嵌段。PAaH嵌段中的己酸侧基在碱性水中和磷酸盐缓冲盐水（PBS）中被离子化，而己酸基在酸性水中被质子化。在碱性水中，PIC囊泡是由带相反电荷的二嵌段共聚物的电荷中和后的混合物形成的。在PIC囊泡和水的界面处存在生物相容性PMPC壳。在酸性条件下，PIC囊泡塌陷，因为电荷平衡由于PAaH嵌段的质子化而移动。PIC囊泡塌陷后，P20 A 190形成了由质子化的PAaH核和PMPC壳组成的胶束，而P 20 M 167以单体形式释放。PIC囊泡可将亲水性非离子客体分子包裹到其空心中。在酸性条件下，PIC囊泡可释放客体分子和P 20 M 167。阳离子P 20 M 167可以破坏溶酶体膜，从而有效地将客体分子从溶酶体释放到细胞质中。
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