通过破坏稳定胶束中的 π-π 堆积区域探索释放机制,Journal of Materials Chemistry B

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通过破坏稳定胶束中的 π-π 堆积区域探索释放机制
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2023-09-07 , DOI: 10.1039/d3tb01388j
Fusheng Zhang ₁ , Gongcui Pei ₁ , Baihao Huang ₁ , Jianchang Xu ₂ , Lijuan Zhang ₁

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π-π堆叠策略可以增强递送平台的稳定性能，但即使有交联策略的帮助，也常常受到药物释放性能不完全的限制。因此，通过破坏 π-π 堆积区域（结构重排）来增强药物释放性能引起了人们极大的兴趣。在此，我们合成了聚(3-(异丁氧基)-2-氧代苯甲酸丙酯)-b-聚(甲基丙烯酸2-羟丁酯)-共-聚((乙二醇)甲醚甲基丙烯酸酯)[PBOOPMA- b -P(HBMA- co - PEGMA)、PHB]并揭示了基于PHB的胶束的药物释放机制。研究表明，利用胶束溶解，交联策略产生的结构重排可将早期释放性能提高 43-55%。此外，酯酶响应策略被阐明可诱导77-79%尺寸变化的重组，强化结构重排，这也与交联策略具有协同作用。基于改善药物释放性能的优点，酯酶响应策略被认为是增强后期释放性能的有希望的候选者。同时，人们相信π-π堆积区域的这种响应性调制（交联、酯酶响应）对于后续研究将非常有前景。最后，还验证了PHB-EDE@CPT在400 mg L ^-1下95.81%的生物安全性和IC ₅₀ ≈ 2.5 mg L ^-1的药物细胞毒性，证实了基于PHB的交联胶束的广阔应用前景。

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Exploring release mechanisms by disrupting π–π stacking regions in stable micelles

π–π stacking strategies can enhance the stability performance of delivery platforms but are often restricted by incomplete drug release performance, even with the help of crosslinking strategies. Therefore, there has been considerable interest in enhancing the drug release performance by disrupting the π–π stacking region (structural rearrangements). Herein, we synthesized poly(3-(isobutyloxy)-2-oxopropyl benzoate)-b-poly(2-hydroxybutyl methacrylate)-co-poly((ethylene glycol)methylether methacrylate) [PBOOPMA-b-P(HBMA-co-PEGMA), PHB] and revealed the drug release mechanism of PHB-based micelles. The structural rearrangements derived from the crosslinking strategy were revealed to improve the early release performance by 43–55% using micellar dissolutions. Moreover, the esterase-responsive strategy was elucidated to induce reassembly with 77–79% size variation, intensifying the structural rearrangements, which was also synergistic with the crosslinking strategy. Based on the advantages of improving drug release performance, the esterase-responsive strategy was considered a promising candidate for enhancing late release performance. Meanwhile, it is believed that such responsive modulation (crosslinking, esterase-responsive) in the π–π stacking region will become highly promising for subsequent research. Finally, the biosafety of 95.81% at 400 mg L⁻¹ and drug cytotoxicity of IC₅₀ ≈ 2.5 mg L⁻¹ of PHB-EDE@CPT were also validated, confirming the broad application prospects of PHB-based crosslinked micelles.

更新日期：2023-09-07

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