Eltayb Esra Kamal, Aleanizy Fadilah Sfouq, Alqahtani Fulwah Y, Alkahtani Hamad M, Ansari Siddique Akber, Alsarra Ibrahim
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 22452, Riyadh 11495, Saudi Arabia.
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Saudi Pharm J. 2022 Jul;30(7):946-953. doi: 10.1016/j.jsps.2022.05.008. Epub 2022 May 23.
Recently, the focus has been shifting toward Quorum sensing inhibitors which reduce Pseudomonas aeruginosa virulence factors, alleviating infections. In this work, me-ta-bromo-thiolactone (mBTL), a potent quorum and virulence inhibitor for the strains, were formulated in calcium alginate nanoparticles (CANPs). Alginate is used as nutrients and as backbone virulence aspect for Pseudomonas and therefore was chosen. mBTL-loaded-CANPs were characterized for particle size, polydispersity index, zeta potential, morphology visualized by Transmission Electron Microscopy (TEM) and drug release profile. Chemical and physical analysis of formulated mBTL-loaded-CANPs were evaluated using Fourier transform infrared Spectroscopy (FTIR) and differential scanning calorimetry (DSC) and Physical stability of mBTL-loaded-CANPs assessed at various temperature 25 ± 1 °C, 4 ± 0.5 °C and -30° ± 1 °C over a period of 4 and 9 months. Synthesized CANPs showed nano-size particles ranging from 140 to 200 nm with spherical particles for plain CANPS and irregular shape for mBTL-loaded-CANPs with a sustainable release profile over 48hrs. FTIR showed stable structure of loaded-mBTL and DSC displayed no interaction between mBTL and polymer. State of released mBTL from CANPs kept at 25 °C, 4 °C and -30 °C over 4 and 9 months showed stable formula at room temperature which kept as a goal of nanoparticles storage. The findings of this study revealed successful preparation of mBTL-loaded-CANPs.
最近，研究重点已转向群体感应抑制剂，这类抑制剂可降低铜绿假单胞菌的毒力因子，减轻感染。在这项研究中，间溴硫内酯（mBTL）作为该菌株的一种有效的群体感应和毒力抑制剂，被制备在海藻酸钙纳米颗粒（CANPs）中。海藻酸盐被用作营养物质以及假单胞菌毒力方面的骨架，因此被选用。对负载mBTL的CANPs进行了粒径、多分散指数、zeta电位、通过透射电子显微镜（TEM）观察的形态以及药物释放曲线等方面的表征。使用傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）对制备的负载mBTL的CANPs进行化学和物理分析，并在25±1°C、4±0.5°C和-30°±1°C的不同温度下评估负载mBTL的CANPs在4个月和9个月期间的物理稳定性。合成的CANPs显示纳米颗粒尺寸在140至200纳米之间，普通CANPs为球形颗粒，负载mBTL的CANPs为不规则形状，且具有可持续48小时的释放曲线。FTIR显示负载mBTL的结构稳定，DSC显示mBTL与聚合物之间无相互作用。在4个月和9个月期间，将CANPs置于25°C、4°C和-30°C下时，mBTL的释放状态表明该配方在室温下稳定，这也是纳米颗粒储存的目标。本研究结果表明成功制备了负载mBTL的CANPs。
