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首页> 外文期刊>Journal of drug delivery science and technology >Enhancement of macrophage uptake via phosphatidylserine-coated acetalated dextran nanoparticles
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Enhancement of macrophage uptake via phosphatidylserine-coated acetalated dextran nanoparticles

机译：通过磷脂酰丝氨酸涂覆的乙炔甲醛纳米粒子增强巨噬细胞吸收

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Although vital to the immune system, macrophages can act as reservoirs for pathogens such as tuberculosis and human immunodeficiency virus. Limitations in the treatment of such diseases include targeting therapeutics directly to macrophages and the large systemic dosages needed. The objective of this study is to develop a nanoparticle (NP)-based drug delivery system that can provide targeted delivery into macrophages. Acetalated dextran (Ac-Dex) NP loaded with the lipophilic model compound curcumin (CUR) were synthesized and coated in 1,2-dipalmitoyl-sn-glycero-3-phospho-l-serine (DPPS), a phospholipid that induces phagocytosis in macrophages. DPPS-CUR NP were found to release 67.8% of encapsulated CUR within 24?h at pH 5.35 and exhibited minimal CUR release (6.3%) at pH 7.4. DPPS-CUR NP were uptaken by murine macrophages significantly more than NP without DPPS coating and NP exposure to these macrophages resulted in minimal toxicity to the cells and minimal nitric oxide production. These results suggest that the combination of the DPPS coating and pH-sensitive polymer Ac-Dex can provide a NP delivery system capable of enhanced uptake by macrophages and potential systemic stability to more effectively deliver drugs of interest. As a result, the described DPPS-CUR NP can serve as a viable delivery system for the treatment of macrophage-associated diseases.
机译：虽然对免疫系统至关重要，但巨噬细胞可以作为植物的储层，如结核病和人类免疫缺陷病毒。治疗这种疾病的限制包括将治疗剂直接靶向巨噬细胞和所需的大型全身剂量。本研究的目的是开发纳米颗粒（NP）的药物递送系统，可提供靶向递送到巨噬细胞中。合成含有亲脂性化合物姜黄素（Cur）的乙炔（AC-DEX）NP在1,2-Dipalmitoyl-Sn-甘油-3-磷酸-1-丝氨酸（DPP）中，含有诱导吞噬作用的磷脂巨噬细胞。发现DPPS-Cur NP在pH 5.35的24℃内释放出67.8％的封装强度，并在pH 7.4下发挥最小的Cur释放（6.3％）。 DPPS-Cur NP被鼠巨噬细胞膨胀显着大于NP，没有DPPS涂层，NP暴露于这些巨噬细胞对细胞的毒性最小，并且最小的一氧化氮产生。这些结果表明DPP涂层和pH敏感聚合物AC-DEX的组合可以提供能够通过巨噬细胞增强的NP递送系统，并潜在的系统稳定性，以更有效地提供感兴趣的药物。结果，所描述的DPPS-Cur NP可以作为用于治疗巨噬细胞相关疾病的可行递送系统。

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