Innovative Microencapsulation of Polymyxin B for Enhanced Antimicrobial Efficacy via Coated Spray Drying.

IF 4.5 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Amal Yousfan, Arwa Omar Al Khatib, Afrah M H Salman, Mahmoud H Abu Elella, Glyn Barrett, Nicholas Michael, Mohammed Gulrez Zariwala, Hisham Al-Obaidi
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Abstract

This study aims to develop an innovative microencapsulation method for coated Polymyxin B, utilizing various polysaccharides such as hydroxypropyl β-cyclodextrin, alginate, and chitosan, implemented through a three-fluid nozzle (3FN) spray drying process. High-performance liquid chromatography (HPLC) analysis revealed that formulations with a high ratio of sugar cage, hydroxypropyl β-cyclodextrin (HPβCD), and sodium alginate (coded as ALGHCDHPLPM) resulted in a notable 16-fold increase in Polymyxin B recovery compared to chitosan microparticles. Morphological assessments using fluorescence labeling confirmed successful microparticle formation with core/shell structures. Alginate-based formulations exhibited distinct layers, while chitosan formulations showed uniform fluorescence throughout the microparticles. Focused beam reflectance and histograms from fluorescence microscopic measurements provided insights into physical size analysis, indicating consistent sizes of 6.8 ± 1.2 μm. Fourier-transform infrared (FTIR) spectra unveiled hydrogen bonding between Polymyxin B and other components within the microparticle structures. The drug release study showed sodium alginate's sustained release capability, reaching 26 ± 3% compared to 94 ± 3% from the free solution at the 24 h time point. Furthermore, the antimicrobial properties of the prepared microparticles against two Gram-negative bacteria, Escherichia coli and Pseudomonas aeruginosa, were investigated. The influence of various key excipients on the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values was evaluated. Results demonstrated effective bactericidal effects of ALGHCDHPLPM against both E. coli and P. aeruginosa. Additionally, the antibiofilm assay highlighted the potential efficacy of ALGHCDHPLPM against the biofilm viability of E. coli and P. aeruginosa, with concentrations ranging from 3.9 to 500 μg/m. This signifies a significant advancement in antimicrobial drug delivery systems, promising improved precision and efficacy in combating bacterial infections.

通过涂层喷雾干燥法创新微胶囊化多粘菌素 B 以增强抗菌效力。
本研究旨在通过三流体喷嘴(3FN)喷雾干燥工艺,利用羟丙基 β-环糊精、海藻酸和壳聚糖等多种多糖,开发一种创新的包衣多粘菌素 B 微囊化方法。高效液相色谱(HPLC)分析表明,与壳聚糖微粒相比,糖笼、羟丙基 β-环糊精(HPβCD)和海藻酸钠(代号为 ALGHCDHPLPM)比例较高的制剂可使多粘菌素 B 的回收率显著提高 16 倍。利用荧光标记进行的形态学评估证实,成功形成了具有核/壳结构的微颗粒。藻酸盐配方显示出明显的层次,而壳聚糖配方则在整个微颗粒中显示出均匀的荧光。聚焦光束反射率和荧光显微测量直方图为物理尺寸分析提供了见解,表明尺寸一致为 6.8 ± 1.2 μm。傅立叶变换红外光谱(FTIR)揭示了多粘菌素 B 和微粒结构中其他成分之间的氢键作用。药物释放研究表明,海藻酸钠具有持续释放能力,在 24 小时内,药物释放率为 26 ± 3%,而游离溶液的释放率为 94 ± 3%。此外,还研究了制备的微粒对两种革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)的抗菌特性。评估了各种关键辅料对最低抑菌浓度(MIC)和最低杀菌浓度(MBC)值的影响。结果表明,ALGHCDHPLPM 对大肠杆菌和绿脓杆菌都有有效的杀菌作用。此外,抗生物膜试验突出显示了 ALGHCDHPLPM 对大肠杆菌和铜绿假单胞菌生物膜活力的潜在功效,浓度范围为 3.9 至 500 μg/m。这标志着抗菌药物输送系统取得了重大进展,有望提高抗击细菌感染的精确性和有效性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Molecular Pharmaceutics
Molecular Pharmaceutics 医学-药学
CiteScore
8.00
自引率
6.10%
发文量
391
审稿时长
2 months
期刊介绍: Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development. Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
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