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聚 N-丙烯酰基-(l-苯丙氨酸甲酯)空心核纳米胶囊促进免疫调节药物的持续释放,并具有佐剂特性。

Poly-N-acryloyl-(l-phenylalanine methyl ester) hollow core nanocapsules facilitate sustained delivery of immunomodulatory drugs and exhibit adjuvant properties.

机构信息

School of Engineering Science and Technology, University of Hyderabad, Prof. C. R. Rao Road, 500046, Hyderabad, Telangana, India.

出版信息

Nanoscale. 2017 Sep 28;9(37):14006-14014. doi: 10.1039/c7nr03724d.

Abstract

Polymeric hollow nanocapsules have attracted significant research attention as novel drug carriers and their preparation is of particular concern owing to the feasibility to encapsulate a broad range of drug molecules. This work presents for the first time the synthesis and development of novel poly-N-acryloyl l-phenylalanine methyl ester hollow core nanocapsules (NAPA-HPNs) of avg. size ca. 100-150 nm by the mini-emulsion technique. NAPA-HPNs are biocompatible and capable of encapsulating sodium nitroprusside (SNP) at a rate of ∼1.3 μM per mg of capsules. These NAPA-HPNs + SNP nano-formulations maintained homeostasis of macrophages which carry and facilitate the action of various drug molecules used against various diseases. These NAPA-HPNs also facilitate the prolonged release of a low level of nitric oxide (NO) and enhance the metabolic activities of pro-inflammatory macrophages, which are important for the action of various drugs in body fluids. NAPA-HPN mediated skewing of naïve macrophages toward the M1 phenotype potentially demonstrates its adjuvant action on the innate immune system. These results potentially suggested that NAPA-HPNs can serve both as a carrier of drugs as well as an adjuvant for the immune system. Thus, these nanocapsules could be used for the effective management of various infectious or tumor diseases where immune-stimulation is paramount for treatment.

摘要

聚合物中空纳米胶囊作为新型药物载体引起了广泛的研究关注,其制备受到特别关注,因为可以封装广泛的药物分子。本工作首次通过微乳液技术合成和开发了新型聚-N-丙烯酰基-L-苯丙氨酸甲酯中空核纳米胶囊(NAPA-HPN),平均粒径约为 100-150nm。NAPA-HPN 具有生物相容性,能够以约 1.3μM/毫克胶囊的速率封装硝普钠(SNP)。这些 NAPA-HPN+SNP 纳米制剂维持了巨噬细胞的内环境平衡,巨噬细胞携带并促进各种用于治疗各种疾病的药物分子的作用。这些 NAPA-HPN 还促进了低水平一氧化氮(NO)的延长释放,并增强了促炎巨噬细胞的代谢活性,这对于体液中各种药物的作用很重要。NAPA-HPN 介导的幼稚巨噬细胞向 M1 表型的倾斜可能表明其对先天免疫系统具有佐剂作用。这些结果可能表明,NAPA-HPN 可以作为药物载体和免疫系统的佐剂。因此,这些纳米胶囊可用于有效治疗各种感染或肿瘤疾病,其中免疫刺激对于治疗至关重要。

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