Piwowarczyk Ludwika, Kucinska Malgorzata, Tomczak Szymon, Mlynarczyk Dariusz T, Piskorz Jaroslaw, Goslinski Tomasz, Murias Marek, Jelinska Anna
Chair and Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland.
Chair and Department of Toxicology, Poznan University of Medical Sciences, Dojazd 30, 60-631 Poznan, Poland.
Nanomaterials (Basel). 2022 Apr 8;12(8):1274. doi: 10.3390/nano12081274.
Nanoformulations are regarded as a promising tool to enable the efficient delivery of active pharmaceutical ingredients to the target site. One of the best-known and most studied nanoformulations are liposomes-spherical phospholipid bilayered nanocarriers resembling cell membranes. In order to assess the possible effect of a mixture of polyphenols on both the stability of the formulation and its biological activity, two compounds were embedded in the liposomes-(i) curcumin (CUR), (ii) a peracetylated derivative of (-)-epigallocatechin 3--gallate (pEGCG), and (iii) a combination of the aforementioned. The stability of the formulations was assessed in two different temperature ranges (4-8 and 20 °C) by monitoring both the particle size and their concentration. It was found that after 28 days of the experiment, the liposomes remained largely unchanged in terms of the particle size distribution, with the greatest change from 130 to 146 nm. The potential decomposition of the carried substances was evaluated using HPLC. The combined CUR and pEGCG was sensitive to temperature conditions; however its stability was greatly increased when compared to the solutions of the individual compounds alone-up to 9.67% of the initial concentration of pEGCG in liposomes after 28 days storage compared to complete decomposition within hours for the non-encapsulated sample. The potential of the prepared formulations was assessed in vitro on prostate (LNCaP) and bladder cancer (5637) cell lines, as well as on a non-cancerous human lung fibroblast cell line (MRC-5), with the highest activity of IC equal 15.33 ± 2.03 µM for the mixture of compounds towards the 5637 cell line.
纳米制剂被视为一种有前景的工具，可实现活性药物成分向靶部位的高效递送。最知名且研究最多的纳米制剂之一是脂质体——类似于细胞膜的球形磷脂双分子层纳米载体。为了评估多酚混合物对制剂稳定性及其生物活性的可能影响，将两种化合物包封于脂质体中——（i）姜黄素（CUR），（ii）（-）-表没食子儿茶素3-没食子酸酯的全乙酰化衍生物（pEGCG），以及（iii）上述两者的组合。通过监测粒径及其浓度，在两个不同温度范围（4 - 8℃和20℃）评估制剂的稳定性。结果发现，实验28天后，脂质体的粒径分布基本保持不变，最大变化为从130 nm至146 nm。使用高效液相色谱法评估所载物质的潜在分解情况。CUR和pEGCG的组合对温度条件敏感；然而，与单独的各化合物溶液相比，其稳定性大大提高——储存28天后，脂质体中pEGCG的初始浓度高达9.67%，而非包封样品在数小时内就完全分解。在所制备的制剂在前列腺（LNCaP）和膀胱癌（5637）细胞系以及非癌性人肺成纤维细胞系（MRC-5）上进行了体外评估，并发现化合物混合物对5637细胞系的最高IC活性等于15.33±2.03μM。
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