Mohamed Ahmad E, Elgammal Walid E, Eid Ahmed M, Dawaba Aya M, Ibrahim Ahmed G, Fouda Amr, Hassan Saber M
Delta Aromatic International Company, First Industrial Zone, 6th of October, Egypt.
Department of Chemistry, Faculty of Science, Al-Azhar University, Nasr City, Cairo, Egypt.
Int J Biol Macromol. 2022 May 15;207:242-253. doi: 10.1016/j.ijbiomac.2022.02.173. Epub 2022 Mar 3.
Recently, chitosan and its derivatives have been gaining more attention due to their high integration into various biomedical applications. Herein, a new chitosan derivative was prepared by linking the chitosan (Cs) with a novel heterocyclic compound, Benzoimidazolyl-thiadiazole (BzimTD) to form Cs-BzimTD. The synthesis of the new chitosan derivative was confirmed by Fourier-Transform Infrared (FT-IR) spectroscopy, proton nuclear magnetic resonance (H NMR), thermogravimetric (TGA-DTG) analysis, elemental analysis, and UV-Visible spectrophotometer. Data showed the high efficacy of functionalized Cs-BzimTD to inhibit the growth of pathogenic microbes, Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans, with inhibition zones of 15.3 ± 0.6 - 9.2 ± 0.3 mm. Also, Cs-BzimTD was applied in a topical gel formulation by using two different polymers, Carbopol 940 (CP) and Carboxymethyl Cellulose (CMC) to form three gel formulations: Cs-BzimTD-CP, Cs-BzimTD-CMC, and Cs-BzimTD-CP-CMC. The new gels were checked for physical appearance, viscosity, Cs-BzimTD release, pH, spread-ability, and drug content. The results showed that all formulations were clear, transparent, and homogeneous with non-irritant pH values for skin (6.4 - 6.8). The spread-ability was found in the range of 7.1 - 9.4 g.cm/s. The Cs-BzimTD-CP formula showed the maximal Cs-BzimTD content percentage (86.5%) and the Cs-BzimTD release varied from 89.9 to 81.6% after 8 h depending on the gel formulation, with a maximum release achieved for Cs-BzimTD-CMC.
近年来，壳聚糖及其衍生物因其在各种生物医学应用中的高度整合而受到越来越多的关注。在此，通过将壳聚糖（Cs）与新型杂环化合物苯并咪唑基噻二唑（BzimTD）连接制备了一种新的壳聚糖衍生物，形成Cs-BzimTD。通过傅里叶变换红外（FT-IR）光谱、质子核磁共振（H NMR）、热重（TGA-DTG）分析、元素分析和紫外可见分光光度计证实了新壳聚糖衍生物的合成。数据显示功能化的Cs-BzimTD对致病性微生物金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌、铜绿假单胞菌和白色念珠菌具有高效抑制作用，抑菌圈为15.3±0.6 - 9.2±0.3毫米。此外，通过使用两种不同的聚合物卡波姆940（CP）和羧甲基纤维素（CMC）将Cs-BzimTD应用于局部凝胶制剂中，形成三种凝胶制剂：Cs-BzimTD-CP、Cs-BzimTD-CMC和Cs-BzimTD-CP-CMC。对新凝胶进行了外观、粘度、Cs-BzimTD释放、pH值、铺展性和药物含量检查。结果表明，所有制剂均清澈、透明且均匀，对皮肤的pH值无刺激性（6.4 - 6.8）。铺展性在7.1 - 9.4 g.cm/s范围内。Cs-BzimTD-CP配方显示Cs-BzimTD含量百分比最高（86.5%），8小时后Cs-BzimTD的释放量根据凝胶制剂的不同在89.9%至81.6%之间变化，Cs-BzimTD-CMC的释放量最大。
