Demir Yusuf Kemal, Metin Ayşegül Ülkü, Şatıroğlu Betül, Solmaz Mehmet Ertuğrul, Kayser Veysel, Mäder Karsten
Department of Pharmaceutical Technology, Faculty of Pharmacy, Marmara University, Istanbul 34668, Turkey; Institute of Pharmacy, Martin Luther University Halle-Wittenberg, 06120 Halle (Saale), Germany.
Department of Chemistry, Faculty of Arts and Sciences, Kırıkkale University, Kırıkkale 71450, Turkey.
Eur J Pharm Biopharm. 2017 Aug;117:182-194. doi: 10.1016/j.ejpb.2017.04.018. Epub 2017 Apr 21.
Cross-linking of natural and synthetic polymers is widely explored to achieve the desired material properties (mechanical strength, drug loading capacity, swelling and erosion rates). However, the potential of polymers produced by crosslinking poly (methyl vinyl ether-co-maleic acid) (PMVE/MA) and pectin (PE) in pharmaceutics is mainly unexplored so far. We have investigated the effect of various esterification conditions and pectin content on the physicochemical properties. Materials have been characterized by fourier transform infrared, differential scanning calorimetry and scanning electron microscopy. In addition, swelling and bioadhesive features of PMVE/MA-PE hydrogel systems were investigated. A band shift for the carbonyl group from 1706 to 1776cm, and glass transition (Tg) increased from 55.4±0.9°C to 119.5±0.3°C confirmed the formation of esterification reaction within the cross-linked films. Cross-linked PMVE/MA:PE films with a ratio of 5 demonstrated a superior mass increase when compared to 2.5, 3.125, 3.75, 6.25, and 7.5 ratios of the same hydrogel film. Formulations containing PMVE/MA and pectin with a ratio of 3.75 showed superior bioadhesive features. For the first time, we engineered three-dimensional printing based swell-able microneedle arrays made out of cross-linked PMVE/MA-PE. Microneedle arrays height and aspect ratio were ranged from 702.5±11.9μm to 726±23.3μm and 3.12±0.20 to 3.29±0.21, respectively. Cross-linked PMVE/MA-PE Microneedle arrays (10-2, 24h) indicated the least height loss, 22.33±4.15%, during axial compression test; whilst, transverse failure of cross-linked PMVE/MA-PE Microneedle arrays was varied from 0.15±0.05 to 0.25±0.04N/needle. In conclusion, we obtained a novel cross-linked polymer system with promising features of drug delivery and bio-analytical applications.
天然和合成聚合物的交联被广泛研究,以实现所需的材料性能(机械强度、药物负载能力、溶胀和侵蚀速率)。然而,到目前为止,交联聚(甲基乙烯基醚-马来酸)(PMVE/MA)和果胶(PE)制备的聚合物在制药方面的潜力尚未得到充分探索。我们研究了各种酯化条件和果胶含量对其物理化学性质的影响。通过傅里叶变换红外光谱、差示扫描量热法和扫描电子显微镜对材料进行了表征。此外,还研究了PMVE/MA-PE水凝胶体系的溶胀和生物粘附特性。羰基的谱带从1706cm移动到1776cm,玻璃化转变温度(Tg)从55.4±0.9°C升高到119.5±0.3°C,证实了交联膜中发生了酯化反应。与相同水凝胶膜的2.5、3.125、3.75、6.25和7.5比例相比,比例为5的交联PMVE/MA:PE膜表现出更高的质量增加。含有比例为3.75的PMVE/MA和果胶的制剂表现出优异的生物粘附特性。我们首次制造了由交联PMVE/MA-PE制成的基于三维打印的可溶胀微针阵列。微针阵列的高度和长宽比分别为702.5±11.9μm至726±23.3μm和3.12±0.20至3.29±0.21。交联PMVE/MA-PE微针阵列(10-2,24小时)在轴向压缩试验中显示出最小的高度损失,为22.33±4.15%;同时,交联PMVE/MA-PE微针阵列的横向破坏从0.15±0.05到0.25±0.04N/针不等。总之,我们获得了一种具有药物递送和生物分析应用前景的新型交联聚合物体系。