Stancheva Rumena, Damyanova Tsvetozara, Paunova-Krasteva Tsvetelina, Veleva Ralitsa, Topouzova-Hristova Tanya, Ivanova Viktoria, Trendafilova Antoaneta, Dimitrov Ivaylo, Rangelov Stanislav, Haladjova Emi
Institute of Polymers, Bulgarian Academy of Sciences, Akad. G. Bonchev St, Bl. 103A, 1113 Sofia, Bulgaria.
Centre of Competence "Sustainable Utilization of Bio-Resources and Waste of Medicinal and Aromatic Plants for Innovative Bioactive Products" (BIORESOURCES BG), 1000 Sofia, Bulgaria.
Pharmaceutics. 2025 Jun 19;17(6):800. doi: 10.3390/pharmaceutics17060800.
Nanosized polymeric micelles (PMs) with an average size of about 80 nm and moderately positive ζ potential, based on an amphiphilic poly(4-methyl-piperazin-1-yl)-propenone)-b-polylactide (PMPP-PLA) block copolymer, were prepared. They were used as platforms for the delivery of bioactive sesquiterpene lactones from L. root extract. The PMs were characterized with good encapsulation efficiency as a maximum value of 72% was reached at a polymer-to-extract mass ratio of 10:1. The loaded micelles exhibited good colloidal stability. An in vitro release was performed showing a burst release profile. The biocompatibility of the resulting PMs was confirmed by assessing their cytotoxic effect on human keratinocytes in vitro by colorimetric assay and flow cytometry. : The systems demonstrated the capability to reduce the biomass of pre-formed Gram-positive and Gram-negative bacterial biofilms. The obtained data clearly determine a trend for a strong combined effect between the PMs and the root extract, distinguishing them with an excellent anti-biofilm potential and prospects for future applications in medical practice.
制备了基于两亲性聚(4-甲基-哌嗪-1-基)-丙烯酮)-b-聚丙交酯(PMPP-PLA)嵌段共聚物、平均尺寸约为80nm且ζ电位呈适度正值的纳米级聚合物胶束(PMs)。它们被用作从L.根提取物中递送生物活性倍半萜内酯的平台。对PMs进行了表征,其具有良好的包封效率,在聚合物与提取物质量比为10:1时达到最大值72%。负载的胶束表现出良好的胶体稳定性。进行了体外释放实验,显示出突释曲线。通过比色法和流式细胞术评估所得PMs对人角质形成细胞的细胞毒性作用,证实了其生物相容性。:该系统显示出降低预先形成的革兰氏阳性和革兰氏阴性细菌生物膜生物量的能力。获得的数据清楚地确定了PMs与根提取物之间存在强烈联合效应的趋势,使其具有优异的抗生物膜潜力以及在医学实践中的未来应用前景。