Enhancement of tobramycin and amikacin activities by co-encapsulation in liposomal-thymoquinone formulation: antibacterial, antibiofilm, and cytocompatibility study.

IF 3.4 Q2 PHARMACOLOGY & PHARMACY

Therapeutic delivery Pub Date : 2026-03-01 Epub Date: 2026-04-10 DOI:10.1080/20415990.2026.2653455

Raghad R Alzahrani, Manal M Alkhulaifi, Abdulkareem M Albekairy, Bahauddeen M Alrfaei, Rizwan Ali, Salleh N Ehaideb, Mohammed A Assiri, Alaa Eldeen B Yassin, Majed A Halwani

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引用次数: 0

Abstract

Background and aim: Aminoglycoside antibiotics (AGAs) are vital but are faced with limited uptake, resistance, and nephrotoxicity. Thymoquinone (THQ) from Nigella sativa has antibacterial and cytoprotective effects but is unstable, posing challenges for formulation. This study co-encapsulated amikacin (AMK) and tobramycin (TOB) with THQ in liposomes to improve antimicrobial activity and renal cytocompatibility.

Methods: Liposomes (Lipo-AMK-THQ and Lipo-TOB-THQ) were prepared and characterized using dynamic light scattering, zeta potential, encapsulation efficiency, Fourier transform infrared spectroscopy, and transmission electron microscopy. Antimicrobial efficacy was evaluated using minimum inhibitory or bactericidal concentrations (MIC-MBC), time-kill, and biofilm inhibition assays. Cytocompatibility was assessed in HK-2 and HEK293T cells.

Results: Formulations exhibited nanoscale size (around 100 nm), low polydispersity (0.1-0.2), and zeta potential around -60 mV. Sustained antibiotic release over 24 h was observed. MIC values were reduced compared to free antibiotics, particularly against resistant MRSA and E. coli isolates (by up to 31-500-fold). Enhanced biofilm inhibition was observed (up to 90-98%) relative to free drugs (38-41%). Cell viability remained at 63-100% (HK-2) and 84-100% (HEK293T).

Conclusion: Co-encapsulation of selected AGAs with THQ in liposomes improved antibacterial and antibiofilm activity while maintaining cytocompatibility, supporting further in vivo evaluation to establish the therapeutic potential and safety.

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脂质体-百里醌共包封增强妥布霉素和阿米卡星活性：抗菌、抗生物膜和细胞相容性研究。

背景和目的：氨基糖苷类抗生素（AGAs）是至关重要的，但面临着有限的吸收，耐药和肾毒性。黑草中的百里醌（THQ）具有抗菌和细胞保护作用，但不稳定，给配方带来了挑战。本研究将阿米卡星（AMK）和妥布霉素（TOB）与THQ共包封在脂质体中，以提高抗微生物活性和肾细胞相容性。方法：制备脂质体（lipoo - amk - thq和lipoo - ob - thq），并利用动态光散射、zeta电位、包封效率、傅里叶变换红外光谱和透射电镜对其进行表征。使用最低抑菌或杀菌浓度（MIC-MBC）、时间杀伤和生物膜抑制试验来评估抗菌效果。在HK-2和HEK293T细胞中评估细胞相容性。结果：该配方具有纳米级尺寸（约100 nm），低多分散性（0.1-0.2），zeta电位约为-60 mV。观察抗生素持续释放超过24 h。与免费抗生素相比，MIC值降低了，特别是对耐药的MRSA和大肠杆菌分离株（高达31-500倍）。与游离药物（38-41%）相比，生物膜抑制作用增强（高达90-98%）。细胞活力维持在63-100% （HK-2）和84-100% （HEK293T）。结论：选定的AGAs与THQ共包埋在脂质体中，可提高抗菌和抗生物膜活性，同时保持细胞相容性，支持进一步的体内评价，以确定治疗潜力和安全性。

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

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.