Kalhapure Rahul S, Mocktar Chunderika, Sikwal Dhiraj R, Sonawane Sandeep J, Kathiravan Muthu K, Skelton Adam, Govender Thirumala
Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa.
Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa.
Colloids Surf B Biointerfaces. 2014 May 1;117:303-11. doi: 10.1016/j.colsurfb.2014.02.045. Epub 2014 Mar 12.
Ion pairing of a fatty acid with an antibiotic may be an effective strategy for formulation optimization of a nanoantibiotic system. The aim of this study was therefore to explore the potential of linoleic acid (LA) as an ion pairing agent to simultaneously enhance encapsulation efficiency and antibacterial activity of triethylamine neutralized vancomycin (VCM) in solid lipid nanoparticles (SLNs). The prepared VCM-LA2 conjugate was characterized by Fourier transform-infrared (FT-IR) spectroscopy, logP and binding energy calculations. The shifts in the FT-IR frequencies of COOH, NH2 and CO functionalities, an increase in logP value (1.37) and a lower interaction energy between LA and VCM (-125.54 kcal/mol) confirmed the formation of the conjugate. SLNs were prepared by a hot homogenization and ultrasonication method, and characterized for size, polydispersity index (PI), zeta potential (ZP), entrapment efficiency (%EE), surface morphology and physical stability. In vitro antibacterial activity studies against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) were conducted. Size, PI and ZP for VCM-LA2_SLNs were 102.7±1.01, 0.225±0.02 and -38.8±2.1 (mV) respectively. SLNs were also stable at 4 °C for 3 months. %EE for VCM-HCl_SLNs and VCM-LA2_SLNs were 16.81±3.64 and 70.73±5.96 respectively, indicating a significant improvement in encapsulation of the drug through ion pairing with LA. Transmission electron microscopy images showed spherical nanoparticles with sizes in the range of 95-100 nm. After 36 h, VCM-HCl showed no activity against MRSA. However, the minimum inhibitory concentration for VCM-HCl_SLNs and VCM-LA2_SLNs were 250 and 31.25 μg/ml respectively against S. aureus, while against MRSA it was 500 and 15.62 μg/ml respectively. This confirms the enhanced antibacterial activity of VCM-LA2_SLNs over VCM-HCl_SLNs. These findings therefore suggest that VCM-LA2_SLNs is a promising nanoantibiotic system for effective treatment against both sensitive and resistant S. aureus infections.
脂肪酸与抗生素的离子配对可能是纳米抗生素系统制剂优化的有效策略。因此，本研究的目的是探索亚油酸（LA）作为离子配对剂在同时提高固体脂质纳米粒（SLN）中三乙胺中和的万古霉素（VCM）的包封效率和抗菌活性方面的潜力。通过傅里叶变换红外（FT-IR）光谱、logP和结合能计算对制备的VCM-LA2缀合物进行表征。COOH、NH2和CO官能团的FT-IR频率发生位移、logP值增加（1.37）以及LA与VCM之间较低的相互作用能（-125.54 kcal/mol）证实了缀合物的形成。通过热均质化和超声处理方法制备SLN，并对其粒径、多分散指数（PI）、zeta电位（ZP）、包封率（%EE）、表面形态和物理稳定性进行表征。对金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌（MRSA）进行了体外抗菌活性研究。VCM-LA2_SLNs的粒径、PI和ZP分别为102.7±1.01、0.225±0.02和-38.8±2.1（mV）。SLN在4℃下也稳定3个月。VCM-HCl_SLNs和VCM-LA2_SLNs的%EE分别为16.81±3.64和70.73±5.96，表明通过与LA离子配对药物包封有显著改善。透射电子显微镜图像显示尺寸在95-100nm范围内的球形纳米颗粒。36小时后，VCM-HCl对MRSA无活性。然而，VCM-HCl_SLNs和VCM-LA2_SLNs对金黄色葡萄球菌的最低抑菌浓度分别为250和31.25μg/ml，而对MRSA分别为500和15.62μg/ml。这证实了VCM-LA2_SLNs比VCM-HCl_SLNs具有更强的抗菌活性。因此，这些发现表明VCM-LA2_SLNs是一种有前景的纳米抗生素系统，可有效治疗敏感和耐药金黄色葡萄球菌感染。
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