负载壳聚糖的RNA聚合酶抑制剂纳米颗粒增加了……毒素释放的衰减。（原句似乎不完整，“from”后面缺少具体内容）

Chitosan loaded RNA polymerase inhibitor nanoparticles increased attenuation in toxin release from .

作者信息

Yahya Alqahtani Fulwah, Sfouq Aleanizy Fadilah, Alkahtani Hamad M, El Tahir Eram, Akber Ansari Siddique, Alharbi Atheer, Al-Bdrawy Asmaa, Shakeel Faiyaz, Haq Nazrul, Al-Rasheed Lamees S, Alfaraj Rihaf, Alshememry Abdullah K, Alsarra Ibrahim A

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Saudi Pharm J. 2023 Jan;31(1):170-179. doi: 10.1016/j.jsps.2022.11.015. Epub 2022 Nov 25.

DOI:10.1016/j.jsps.2022.11.015

PMID:36685302

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9845126/

Abstract

BACKGROUND

Multidrug-resistant (MDR) bacterial infections have become an emerging health concern around the world. Antibiotics resistance among strains increased recently contributing to increase in incidence of pneumococcal infection. This necessitates the discovery of novel antipnemococcal such as compound C3-005 which target the interaction between RNA polymerase and σ factors. Chitosan nanoparticles (CNPs) exhibited antibacterial activity including . Therefore, the aims of the current investigation were to formulate CNPs loaded with C3-005 and characteristic their antimicrobial properties against

METHODS

The CNPs and C3-005 loaded CNPs were produced utilizing ionic gelation method, and their physicochemical characteristics including particle size, zeta potential, polydispersity index (PDI), encapsulation efficiency (EE%), and release profile were studied. Both differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR) were used for chemical characterization. The synthesized NPs' minimum inhibitory concentration (MIC) was determined using killing assay and broth dilution method, and their impact on bacteria induced hemolysis were also studied.

RESULTS

The NPs encapsulating C3-005 were successfully prepared with particle size of 343.5 nm ± 1.3, zeta potential of 29.8 ± 0.37, and PDI of 0.20 ± 0.03. 70 % of C3-005 were encapsulated in CNPs and sustained release pattern of C3-005 from CNPs was revealed by an release study. CNPs containing C3-005 exhibited higher antipnomcoccal activity with MIC of 30 µg/ml when compared with C3-005 and empty CNPs alone. The prepared C3-CNPs showed a reduction of bacterial hemolysis in a concentration-related (dependent) manner and was higher than C3-005 alone.

CONCLUSIONS

The findings of this study showed the potential for using C3-005 loaded CNPs to treat pneumococcal infection.

摘要

背景

耐多药（MDR）细菌感染已成为全球日益严重的健康问题。近期菌株中的抗生素耐药性增加，导致肺炎球菌感染发病率上升。这就需要发现新型抗肺炎球菌药物，如靶向RNA聚合酶与σ因子相互作用的化合物C3 - 005。壳聚糖纳米颗粒（CNPs）具有抗菌活性，包括……。因此，本研究的目的是制备负载C3 - 005的CNPs，并表征其对……的抗菌性能。

方法

采用离子凝胶法制备CNPs和负载C3 - 005的CNPs，并研究其物理化学特性，包括粒径、zeta电位、多分散指数（PDI）、包封率（EE%）和释放曲线。差示扫描量热法（DSC）和傅里叶变换红外光谱法（FTIR）均用于化学表征。使用杀菌试验和肉汤稀释法测定合成纳米颗粒的最低抑菌浓度（MIC），并研究其对细菌诱导溶血的影响。

结果

成功制备了负载C3 - 005的纳米颗粒，粒径为343.5 nm±1.3，zeta电位为29.8±0.37，PDI为0.20±0.03。70%的C3 - 005被包封在CNPs中，释放研究显示C3 - 005从CNPs中呈缓释模式。与单独的C3 - 005和空CNPs相比，负载C3 - 005的CNPs表现出更高的抗肺炎球菌活性，MIC为30μg/ml。制备的C3 - CNPs以浓度相关（依赖）的方式降低了细菌溶血，且高于单独的C3 - 005。