Alotaibi Nasser H, Munir Muhammad Usman, Alruwaili Nabil K, Alharbi Khalid Saad, Ihsan Ayesha, Almurshedi Alanood S, Khan Ikram Ullah, Bukhari Syed Nasir Abbas, Rehman Mubashar, Ahmad Naveed
Department of Clinical Pharmacy, College of Pharmacy, Jouf University, Sakaka 72388, Saudi Arabia.
Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72388, Saudi Arabia.
Pharmaceutics. 2022 Apr 30;14(5):975. doi: 10.3390/pharmaceutics14050975.
The continuing growth of bacterial resistance makes the top challenge for the healthcare system especially in bone-infections treatment. Current estimates reveal that in 2050 the death ratio caused by bacterial infections can be higher than cancer. The aim of this study is to provide an alternative to currently available bone-infection treatments. Here we designed mesoporous hydroxyapatite nanocarriers functionalized with citrate (Ctr-mpHANCs). Amoxicillin (AMX) is used as a model drug to load in Ctr-mpHANCs, and the drug loading was more than 90% due to the porous nature of nanocarriers. Scanning electron microscopy shows the roughly spherical morphology of nanocarriers, and the DLS study showed the approximate size of 92 nm. The Brunauer-Emmett-Teller (BET) specific surface area and pore diameter was found to be about 182.35 m/g and 4.2 nm, respectively. We noticed that almost 100% of the drug is released from the AMX loaded Ctr-mpHANCs (AMX@Ctr-mpHANCs) in a pH-dependent manner within 3 d and 5 d at pH 2.0 and 4.5, respectively. The sustained drug release behaviour was observed for 15 d at pH 7.4 and no RBCs hemolysis by AMX@Ctr-mpHANCs. The broth dilution and colony forming unit (CFU) assays were used to determine the antimicrobial potential of AMX@Ctr-mpHANCs. It was observed in both studies that AMX@Ctr-mpHANCs showed a significant reduction in the bacterial growth of , , and as compared to Ctr-mpHANCs with no bacteria-killing. Thus, we proposed that Ctr-mpHANCs can be used as a drug carrier and a treatment option for bone infections caused by bacteria.
细菌耐药性的持续增长成为医疗系统面临的最大挑战，尤其是在骨感染治疗方面。目前的估计显示，到2050年，由细菌感染导致的死亡率可能高于癌症。本研究的目的是为目前可用的骨感染治疗方法提供一种替代方案。在此，我们设计了用柠檬酸盐功能化的介孔羟基磷灰石纳米载体（Ctr-mpHANCs）。阿莫西林（AMX）用作模型药物负载于Ctr-mpHANCs中，由于纳米载体的多孔性质，药物负载率超过90%。扫描电子显微镜显示纳米载体呈大致球形形态，动态光散射研究表明其近似尺寸为92 nm。发现Brunauer-Emmett-Teller（BET）比表面积和孔径分别约为182.35 m/g和4.2 nm。我们注意到，负载AMX的Ctr-mpHANCs（AMX@Ctr-mpHANCs）中几乎100%的药物分别在pH 2.0和4.5时于3天和5天内以pH依赖的方式释放。在pH 7.4时观察到AMX@Ctr-mpHANCs持续15天的药物释放行为，且未导致红细胞溶血。采用肉汤稀释法和菌落形成单位（CFU）测定法来确定AMX@Ctr-mpHANCs的抗菌潜力。在两项研究中均观察到，与无杀菌作用的Ctr-mpHANCs相比，AMX@Ctr-mpHANCs对金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌的细菌生长有显著抑制。因此，我们提出Ctr-mpHANCs可作为药物载体和治疗由细菌引起的骨感染的一种选择。
