冷冻干燥负载异烟肼聚ε-己内酯纳米颗粒的制备与优化。

IF 4.3 Q2 CHEMISTRY, MEDICINAL
ADMET and DMPK Pub Date : 2025-07-08 eCollection Date: 2025-01-01 DOI:10.5599/admet.2774
Eknath Kole, Yuvraj Pawara, Atul Chaudhari, Aniruddha Chatterjee, Jitendra Naik
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引用次数: 0

摘要

背景:微流控纳米沉淀法之后进行冷冻干燥,可以通过保留其物理化学性质而不影响治疗效果,从而产生尺寸均匀、稳定的纳米颗粒。异烟肼(INH)负载的聚ε-己内酯(PCL)纳米颗粒可以利用微流控技术用于结核病的治疗。实验方法:采用微反应器辅助纳米沉淀法制备负载inh的纳米颗粒,并采用实验设计的析因设计方法进行优化。采用粒径、多分散性指数(PDI)、zeta电位(表面电荷)、傅里叶变换红外光谱、差示扫描量热法、x射线衍射分析和场发射扫描电镜对所得的INH-PCL纳米配方进行了表征。主要结果:优化后的纳米颗粒平均粒径为248.4±5.372 nm,包封效率为82.26±4.36%。热分析和光谱分析证实不存在药物-聚合物相互作用,确保配方的完整性;在加速条件下的稳定性研究表明,在6个月的时间里,颗粒大小、PDI和zeta电位的变化可以忽略不计,表明胶体稳定性很强。扫描电子显微镜研究显示,杆状纳米颗粒表面光滑。冻干(冷冻干燥)提高了长期稳定性,产生易于再分散的粉末(重构指数~1.066)。根据扩散控制动力学,在磷酸盐缓冲盐水(pH 7.4)中的体外药物释放研究显示药物持续释放(48小时内累积释放92.45%)。结论:我们的研究结果证实,负载inh的PCL纳米制剂具有良好的稳定性,高载药量和缓释,是有效治疗结核病的关键属性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Fabrication and optimization of freeze-dried isoniazid-loaded poly-<i>ε</i>-caprolactone nanoparticles.

Fabrication and optimization of freeze-dried isoniazid-loaded poly-<i>ε</i>-caprolactone nanoparticles.

Fabrication and optimization of freeze-dried isoniazid-loaded poly-<i>ε</i>-caprolactone nanoparticles.

Fabrication and optimization of freeze-dried isoniazid-loaded poly-ε-caprolactone nanoparticles.

Background: Microfluidic nanoprecipitation followed by freeze-drying would yield uniformly sized, stable nanoparticles by preserving their physicochemical property without compromising therapeutic performance. The isoniazid (INH)-loaded poly-ε-caprolactone (PCL) nanoparticles could be developed using a microfluidic technique for the management of tuberculosis.

Experimental approach: The INH-loaded nanoparticles were fabricated via a microreactor-assisted nanoprecipitation method and optimization using a design of experiments factorial design approach. The resulting INH-PCL nanoformulation was characterized for particle size, polydispersity index (PDI), zeta potential (surface charge), Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis and field emission scanning electron microscope.

Key results: The optimized nanoparticles exhibited an average particle size (248.4 ± 5.372 nm) and high encapsulation efficiency (82.26 ± 4.36 %). Thermal and spectroscopic analyses confirmed the absence of drug-polymer interactions, ensuring formulation integrity; stability studies under accelerated conditions demonstrated negligible changes in particle size, PDI, and zeta potential over the period of 6 months, indicating robust colloidal stability. A scanning electron microscopy study revealed rod-shaped nanoparticles with smooth surfaces. Lyophilization (freeze-drying) enhanced long-term stability, yielding a readily re-dispersible powder (reconstitution index ~1.066). Following diffusion-controlled kinetics, in vitro drug release studies in phosphate buffer saline (pH 7.4) showed sustained drug release (92.45 % cumulative release over 48 h).

Conclusion: Our results confirm that the INH-loaded PCL nanoformulation combines excellent stability, high drug-loading capacity, and sustained release, key attributes of effective tuberculosis therapy.

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来源期刊
ADMET and DMPK
ADMET and DMPK Multiple-
CiteScore
4.40
自引率
0.00%
发文量
22
审稿时长
4 weeks
期刊介绍: ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study
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