International Center for Chemical and Biological Sciences, H.E.J Research Institute of Chemistry, University of Karachi, Karachi, Pakistan.
School of Environmental and Biological Engineering, Nanjing University of Science and Technology, Nanjing, PR China.
Chem Phys Lipids. 2021 Sep;239:105115. doi: 10.1016/j.chemphyslip.2021.105115. Epub 2021 Jul 9.
The increase in antimicrobial resistance has created a crisis that has become top priority for global policy and public health. Antibiotics are constantly being rendered in-effective due to the emergence of bacterial resistance; therefore, novel strategies for improving therapeutic efficacies of existing drugs must be focused. Advancements in nanotechnology have opened up new avenues for enhancing therapeutic efficacy of existing drugs via construction of intelligent and efficient delivery systems. This study reports the synthesis of Dapsone based nonionic surfactant and its utilization as delivery system for Ceftriaxone sodium. The synthesized nonionic surfactant was characterized via mass spectrometry and H NMR and IR spectroscopic techniques. The drug loaded vesicles of newly synthesized sulfur based nonionic were formed through thin film hydration method and characterized for drug entrapment efficiency, vesicles size, zeta potential, morphology using UV-vis spectrometry, dynamic light scattering (DLS) and atomic force microscopic (AFM) techniques. The biocompatibility of newly synthesized surfactant was assessed using blood hemolysis and in-vitro cells cytotoxicity. Antibacterial potential of drug loaded vesicles was assessed in gram positive and gram negative bacterial cultures. The spectroscopic results confirm successful synthesis of novel sulfur based nonionic surfactant that formed spherical shaped drug loaded vesicles with an average size of 97.95 ± 3.45 nm and 56.3 ± 3.15 % entrapment of the model drug (Ceftriaxone sodium). The vesicles displayed negative surface charge of -16.8 ± 3.72 mV and released the entrapped drug in a controlled way in-vitro drug release. The drug loaded vesicular formulation showed enhanced cellular uptake and greater antibacterial potentials when compared with control. Results of this study show that the Dapsone based surfactant is safe, biocompatible, non-toxic and can be used as promising vesicular carrier for enhancing therapeutic efficacy of antibacterial drug, Ceftriaxone sodium.
抗菌药物耐药性的增加造成了一场危机,成为全球政策和公共卫生的首要关注点。由于细菌耐药性的出现,抗生素的疗效不断降低;因此,必须集中精力研究提高现有药物治疗效果的新策略。纳米技术的进步为通过构建智能和高效的给药系统来提高现有药物的治疗效果开辟了新途径。本研究报告了基于磺胺嘧啶的非离子表面活性剂的合成及其作为头孢曲松钠给药系统的应用。通过质谱、1H NMR 和 IR 光谱技术对合成的非离子表面活性剂进行了表征。通过薄膜水化法形成了新合成的基于硫的非离子载药囊泡,并通过紫外-可见分光光度法、动态光散射(DLS)和原子力显微镜(AFM)技术对载药囊泡的药物包封效率、囊泡粒径、Zeta 电位和形态进行了表征。采用血液溶血和体外细胞毒性实验评估了新合成表面活性剂的生物相容性。评估了载药囊泡对革兰氏阳性和革兰氏阴性细菌培养物的抗菌潜力。光谱结果证实成功合成了新型基于硫的非离子表面活性剂,该表面活性剂形成了平均粒径为 97.95 ± 3.45nm 的球形载药囊泡,模型药物(头孢曲松钠)的包封率为 56.3 ± 3.15%。囊泡显示出-16.8 ± 3.72mV 的负表面电荷,并在体外药物释放中以受控方式释放包封的药物。与对照相比,载药囊泡制剂显示出增强的细胞摄取和更大的抗菌潜力。这项研究的结果表明,基于磺胺嘧啶的表面活性剂安全、生物相容、无毒,可用作增强抗菌药物头孢曲松钠治疗效果的有前途的囊泡载体。