Triantafyllopoulou Efstathia, Perinelli Diego Romano, Forys Aleksander, Pantelis Pavlos, Gorgoulis Vassilis G, Lagopati Nefeli, Trzebicka Barbara, Bonacucina Giulia, Valsami Georgia, Pippa Natassa, Pispas Stergios
Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens (NKUA), Panepistimioupolis Zografou, 15771 Athens, Greece.
School of Pharmacy, University of Camerino, Via Gentile III da Varano, 62032 Camerino, Italy.
Pharmaceutics. 2024 Sep 13;16(9):1204. doi: 10.3390/pharmaceutics16091204.
Despite the appealing properties of random copolymers, the use of these biomaterials in association with phospholipids is still limited, as several aspects of their performance have not been investigated. The aim of this work is the formulation of lipid/random copolymer platforms and the comprehensive study of their features by multiple advanced characterization techniques. Both biomaterials are amphiphilic, including two phospholipids (1,2-dioctadecanoyl-sn-glycero-3-phosphocholine (DSPC), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC)) and a statistical copolymer of oligo (ethylene glycol) methyl ether methacrylate (OEGMA) and 2-(diisopropylamino) ethyl methacrylate (DIPAEMA). We examined the design parameters, including the lipid composition, the % comonomer ratio, and the lipid-to-polymer ratio that could be critical for their behavior. The structures were also probed in different conditions. To the best of the authors' knowledge, this is the first time that P(OEGMA-co-DIPAEMA)/lipid hybrid colloidal dispersions have been investigated from a membrane mechanics, biophysical, and morphological perspective. Among other parameters, the copolymer architecture and the hydrophilic to hydrophobic balance are deemed fundamental parameters for the biomaterial co-assembly, having an impact on the membrane's fluidity, morphology, and thermodynamics. Exploiting their unique characteristics, the most promising candidates were utilized for methotrexate (MTX) loading to explore their encapsulation capability and potential antitumor efficacy in vitro in various cell lines.
尽管无规共聚物具有吸引人的特性，但这些生物材料与磷脂结合使用的情况仍然有限，因为其性能的几个方面尚未得到研究。这项工作的目的是制备脂质/无规共聚物平台，并通过多种先进的表征技术对其特性进行全面研究。这两种生物材料都是两亲性的，包括两种磷脂（1,2 - 二硬脂酰 - sn - 甘油 - 3 - 磷酸胆碱（DSPC）、1,2 - 二油酰 - sn - 甘油 - 3 - 磷酸胆碱（DOPC））以及寡聚（乙二醇）甲基醚甲基丙烯酸酯（OEGMA）和甲基丙烯酸2 - （二异丙基氨基）乙酯（DIPAEMA）的统计共聚物。我们研究了设计参数，包括脂质组成、共聚单体比例以及脂质与聚合物的比例，这些参数可能对它们的行为至关重要。还在不同条件下对结构进行了探测。据作者所知，这是首次从膜力学、生物物理和形态学角度对P（OEGMA - co - DIPAEMA）/脂质混合胶体分散体进行研究。在其他参数中，共聚物结构和亲水 - 疏水平衡被认为是生物材料共组装的基本参数，对膜的流动性、形态和热力学有影响。利用它们的独特特性，最有前景的候选物被用于负载甲氨蝶呤（MTX），以探索其在各种细胞系中的包封能力和体外潜在的抗肿瘤功效。
