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聚乙二醇化 PAMAM 树枝状聚合物载奥沙利铂,具有延长释放和高载药量而无突释效应。

PEGylated PAMAM dendrimers loading oxaliplatin with prolonged release and high payload without burst effect.

机构信息

Graduate University of Science and Technology, Vietnam Academy of Science and Technology, Hanoi, Vietnam.

Institute of Applied Materials Science, Vietnam Academy of Science and Technology, Ho Chi Minh City, Vietnam.

出版信息

Biopolymers. 2019 Jul;110(7):e23272. doi: 10.1002/bip.23272. Epub 2019 Mar 21.

Abstract

Oxaliplatin (OXA) was coupled to PEGylated polyamidoamine dendrimers of fourth generation (G4-PEG@OXA) in the comparison to PEGylated ones of odd generation (G3.5-PEG@OXA). Proton nuclear magnetic resonance and Fourier-transform infrared spectroscopy were used to confirm the successful incorporation of OXA as well as the synthesis of carrier systems. Both two types of carrier systems exhibited in sphere nanoparticle shape with size of less than 100 nm that was in the range being able to cause toxicity on cancer cells. The average drug loading efficiency (DLE) of G4-PEG@OXA was obtained at 84.63% that was higher than DLE of G3.5-PEG of 75.69%. The release kinetic of G4-PEG@OXA and G3.5-PEG@OXA did not show any burst release phenomenon while free OXA was released over 40% at the first hour. The sustainable release of OXA was achieved when it was encapsulated in these carriers, but the G4 generation liberated OXA (3.4%-6.4%) slower than G3.5 one (11.9%-22.8%). The in vitro cytotoxicities of G4-PEG@OXA were evaluated in HeLa cell lines using resazurin assay and live/dead staining test. Although the free OXA showed a rather moderate killing ability, the G4-PEG@OXA still displayed the low viability of HeLa that was better to the result of G3.5-PEG@OXA due to released OXA amount. The benefit of this system was to overcome the burst release phenomenon to minimize OXA toxicity without compromising its efficiency.

摘要

奥沙利铂(OXA)与第四代聚乙二醇化聚酰胺胺树枝状大分子(G4-PEG@OXA)偶联,与奇数代聚乙二醇化树枝状大分子(G3.5-PEG@OXA)进行比较。质子核磁共振和傅里叶变换红外光谱用于确认 OXA 的成功结合以及载体系统的合成。两种载体系统均表现为小于 100nm 的球形纳米颗粒形状,这是能够对癌细胞产生毒性的范围内。G4-PEG@OXA 的平均药物载量效率(DLE)为 84.63%,高于 G3.5-PEG 的 75.69%。G4-PEG@OXA 和 G3.5-PEG@OXA 的释放动力学没有表现出任何爆发释放现象,而游离 OXA 在第一个小时内释放超过 40%。当 OXA 被包裹在这些载体中时,OXA 可以实现持续释放,但 G4 代释放 OXA(3.4%-6.4%)比 G3.5 代(11.9%-22.8%)慢。通过使用 Resazurin 测定法和活/死染色试验,在 HeLa 细胞系中评估了 G4-PEG@OXA 的体外细胞毒性。尽管游离 OXA 显示出相当温和的杀伤能力,但 G4-PEG@OXA 仍显示出 HeLa 的低存活率,这比 G3.5-PEG@OXA 的结果更好,因为释放的 OXA 量更多。该系统的优势在于克服爆发释放现象,以最小化 OXA 毒性,而不影响其效率。

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