Putta Chandra Lekha, Rahman Syed Nazrin Ruhina, Chakraborty Payel, Shunmugaperumal Tamilvanan
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research Guwahati, Sila Katamur (Halugurisuk), Changsari, India.
Department of Biomedical Engineering, Indian Institute of Technology Hyderabad, Sangareddy, India.
J Microencapsul. 2023 Nov;40(7):517-533. doi: 10.1080/02652048.2023.2244094. Epub 2023 Aug 11.
The aims of this study were to systematically optimise a formula for eugenol emulsions via face-centered central composite design and to assess the activity against two-different bacterial strains ( and ) present at planktonic and biofilm forms. The molecular interaction of excipients, mean particle size (MPS) including zeta potential (ZP), drug entrapment efficiency (DEE) and drug release of optimised emulsions was done using FT-IR, Malvern Zetasizer, ultracentrifugation technique and membrane-free dissolution model, respectively. The emulsions consisted of 151.3 ± 1.45 nm MPS, -21.3 ± 1.25 mV ZP and 93.98 ± 1.41% DEE values. On storage of emulsions at 25 °C for 3 months, the value of DEE was found to be 72.12 ± 2.82%. The Tween 80 emulsifier film coverage onto the dispersed eugenol droplets of emulsions delayed significantly the drug release (12%-19%) compared to the drug release occurred from pure eugenol. The treatment of planktonic and with diluted eugenol emulsions showed the minimum inhibitory concentration and minimum bactericidal concentration values at 1.25-2.5 mg/ml whereas it occurred at 10 mg/ml for pure eugenol. Treating the biofilms with eugenol emulsions (1-2 mg/ml) yielded 59-70% minimum biofilm eradication concentration but 10 mg/ml pure eugenol showed 60%. Hence, the eugenol emulsions displayed antibacterial activity and could be projected as an antibiofilm or biofilm disruption agent.
本研究的目的是通过面心中央复合设计系统优化丁香酚乳剂的配方，并评估其对浮游态和生物膜态两种不同细菌菌株（和）的活性。分别使用傅里叶变换红外光谱仪（FT-IR）、马尔文粒度分析仪、超速离心技术和无膜溶出模型对辅料的分子相互作用、包括zeta电位（ZP）的平均粒径（MPS）、药物包封率（DEE）以及优化乳剂的药物释放情况进行研究。所制备的乳剂平均粒径为151.3±1.45 nm，zeta电位为-21.3±1.25 mV，药物包封率为93.98±1.41%。将乳剂在25℃储存3个月后，药物包封率为72.12±2.82%。与纯丁香酚的药物释放相比，吐温80乳化剂在乳剂分散的丁香酚液滴上形成的薄膜显著延迟了药物释放（12%-19%）。用稀释的丁香酚乳剂处理浮游态的和，其最低抑菌浓度和最低杀菌浓度值为1.25-2.5 mg/ml，而纯丁香酚的最低抑菌浓度和最低杀菌浓度值为10 mg/ml。用丁香酚乳剂（1-2 mg/ml）处理生物膜，其最低生物膜根除浓度为59-70%，而10 mg/ml的纯丁香酚最低生物膜根除浓度为60%。因此，丁香酚乳剂具有抗菌活性，可作为抗生物膜或生物膜破坏剂。
