Department of Pharmaceutics, College of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.
Department of Chemistry, University of Education, Lahore 54000, Pakistan.
Molecules. 2022 Apr 14;27(8):2532. doi: 10.3390/molecules27082532.
In the current study, nitrofurazone- (NFZ) and lidocaine-loaded (LD) silica microspheres were fabricated to address pathological indications of skin infections. The microspheres were prepared by the sol-gel method applying the Box-Behnken design and evaluated for size distribution, morphology, zeta potential, physico-chemical compatibility, XRD, thermogravimetric analysis, antibacterial and cytotoxicity activities. The comparative in vitro drug release study of microspheres revealed a 30% release of NFZ and 33% of LD after 8 h. The microspheres showed 81% percentage yield (PY) and 71.9% entrapment efficiency. XRD patterns confirmed the entrapment of NFZ-LD in silica microspheres with a significant reduction in crystallinity of the drugs. Thermal and FTIR studies proved the absence of any profound interactions of the formulation ingredients. The smooth spherical microspheres had a -28 mV zeta potential and a 10-100 µm size distribution. In vitro antibacterial activities of the NFZ-LD microspheres showed an increased zone of inhibition compared to pure drug suspensions. The in vivo efficacy tested on rabbits showed a comparatively rapid wound healing with complete lack of skin irritation impact. The cytotoxicity studies revealed more acceptability of silica microspheres with negligible harm to cells. The study suggests that the NFZ- and LD-loaded silica microspheres would be an ideal system for accelerating and promoting rapid healing of various acute and chronic wounds.
在本研究中，制备了载有硝呋太尔（NFZ）和利多卡因（LD）的二氧化硅微球，以解决皮肤感染的病理指征。通过溶胶-凝胶法，应用 Box-Behnken 设计制备了微球，并对其粒径分布、形态、Zeta 电位、物理化学相容性、XRD、热重分析、抗菌和细胞毒性活性进行了评价。微球的比较体外药物释放研究表明，NFZ 和 LD 在 8 小时后分别释放了 30%和 33%。微球的产率（PY）为 81%，包封效率为 71.9%。XRD 图谱证实 NFZ-LD 被包封在二氧化硅微球中，药物的结晶度显著降低。热重和 FTIR 研究证明了配方成分之间没有任何深刻的相互作用。光滑的球形微球具有-28 mV 的 Zeta 电位和 10-100 µm 的粒径分布。NFZ-LD 微球的体外抗菌活性显示，与纯药物混悬液相比，抑菌圈增大。在兔子身上进行的体内疗效研究表明，伤口愈合较快，完全没有皮肤刺激的影响。细胞毒性研究表明，二氧化硅微球的可接受性更高，对细胞的危害可以忽略不计。该研究表明，载有 NFZ 和 LD 的二氧化硅微球将是加速和促进各种急性和慢性伤口快速愈合的理想体系。
