Gerayelou Golara, Khameneh Bahman, Malaekeh-Nikouei Bizhan, Mahmoudi Asma, Fazly Bazzaz Bibi Sedigheh
School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Department of Pharmaceutical Control, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Adv Pharm Bull. 2021 Sep;11(4):684-692. doi: 10.34172/apb.2021.077. Epub 2020 Oct 14.
Microbial biofilms are one of the main causes of persistent human infections. Encapsulation of an antibiotic and a biofilm dispersal agent within a nano-carrier has been recognized as a novel approach to combat the problem of biofilm-related infections. Here, we develop the nanoliposomal formulation for delivery of vancomycin in combination with cis-2- decenoic acid (C2DA), to biofilm. The effects of the formulations were studied at two stages: biofilm growth inhabitation and biofilm eradication. Liposomal formulations were prepared by the solvent evaporation dehydration-rehydration method and were evaluated for size, zeta potential, and encapsulation efficacy. The ability of different agents in free and encapsulated forms were assessed to evaluate the anti-biofilm activities. Vancomycin and C2DA were successfully co-encapsulated in the same nanoliposome (liposomal combination). The zeta potential values of the liposomal formulations of vancomycin, C2DA, and the liposomal combination were 37.2, 40.2, 51.5 mV, and the mean sizes of these liposomal formulations were 167.8±1.5, 215.5±8.8, 235.5±0.01, respectively. Encapsulation efficacy of C2DA was 65% and about 40% for vancomycin. The results indicated that liposomal combination exerted strong anti-biofilm activities, slightly exceeding those observed by the free form of a combination of vancomycin and C2DA, but higher than either agent used alone in their free forms. The anti-biofilm activity of formulations followed concentration and time-dependent manner. The combination of vancomycin and C2DA could inhibit biofilm formation. Employing the liposomal combination is a considerable method to remove bacterial biofilm.
微生物生物膜是人类持续性感染的主要原因之一。将抗生素和生物膜分散剂封装在纳米载体中已被认为是解决生物膜相关感染问题的一种新方法。在此,我们开发了用于将万古霉素与顺式 -2- 癸烯酸(C2DA)联合递送至生物膜的纳米脂质体制剂。在两个阶段研究了该制剂的效果:生物膜生长抑制和生物膜根除。通过溶剂蒸发脱水 - 再水化方法制备脂质体制剂,并对其大小、zeta 电位和包封率进行评估。评估了游离形式和封装形式的不同药剂的能力,以评价其抗生物膜活性。万古霉素和 C2DA 成功共封装在同一纳米脂质体中(脂质体组合)。万古霉素、C2DA 和脂质体组合的脂质体制剂的 zeta 电位值分别为 37.2、40.2、51.5 mV,这些脂质体制剂的平均大小分别为 167.8±1.5、215.5±8.8、,235.5±0.01。C2DA 的包封率为 65%,万古霉素约为 40%。结果表明,脂质体组合具有很强的抗生物膜活性,略超过游离形式的万古霉素和 C2DA 组合所观察到的活性,但高于单独使用的任何一种游离形式的药剂。制剂的抗生物膜活性呈浓度和时间依赖性。万古霉素和 C2DA 的组合可抑制生物膜形成。采用脂质体组合是去除细菌生物膜的一种相当有效的方法。