School of Life Sciences, Anhui University, Hefei 230601, Anhui, China; Anhui Key Laboratory of Modern Biomanufacturing, Hefei 230601, Anhui, China; Key Laboratory of Eco-engineering and Biotechnology of Anhui Province, Hefei 230601, Anhui, China.
School of Life Sciences, Anhui University, Hefei 230601, Anhui, China; Key Laboratory of Biomass Chemical Engineering of Ministry of Education, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, China.
Int J Biol Macromol. 2020 Jul 15;155:411-420. doi: 10.1016/j.ijbiomac.2020.03.191. Epub 2020 Mar 26.
Natural polymers like polysaccharides, polypeptides and their derivatives are broadly applied in drug delivery due to excellent biocompatibility and biodegradability. In this study, the dissolving tablets, formed with carboxymethylcellulose/poly-l-lysine/tripolyphosphate (CMC/PLL/TPP) complex, were prepared using metformin hydrochloride (MetHCl) as model drug. Confocal laser scanning microscopy observation manifested that FITC-labeled PLL interacted with CMC and formed a uniform interior microstructure. Scanning electron microscope images showed the drug-loaded tablets had well-formed shapes with smooth surfaces. MetHCl embedded interior the microstructures of the tablets and represented in a crystal form. Thermo-gravimetric analysis and differential scanning calorimetry indicated that the drug-loaded tablets had stable thermal properties with less moisture content (3.52%). Fourier transform infrared spectrometer confirmed that the CMC/PLL/TPP complex was fabricated via the electrostatic interactions between -NH, -COO and -[PO-] groups. The drug-loaded tablets had a high drug loading efficiency of 85.76% and drug encapsulation efficiency of 81.47%, and a shorter wetting time of 2.16 min in SSF (pH 6.8) and lower swelling ratio of 233.34%. The drug loaded in the samples could be released completely within 10 min in simulated saliva fluid (SSF pH 6.8), indicating a rapid drug release and dissolving profile in the environment, which could be developed for dissolving tablets.
天然聚合物如多糖、多肽及其衍生物由于其良好的生物相容性和可生物降解性,被广泛应用于药物传递系统。在本研究中,以盐酸二甲双胍(MetHCl)为模型药物,制备了羧甲基纤维素/聚-L-赖氨酸/三聚磷酸钠(CMC/PLL/TPP)复合物的溶蚀片。激光共聚焦显微镜观察表明,FITC 标记的 PLL 与 CMC 相互作用,形成均匀的内部微观结构。扫描电子显微镜图像显示,载药片具有良好的成型形状和光滑的表面。MetHCl 嵌入片剂的微观结构中,呈结晶形式。热重分析和差示扫描量热法表明,载药片具有稳定的热性能和较低的水分含量(3.52%)。傅里叶变换红外光谱仪证实,CMC/PLL/TPP 复合物是通过-NH、-COO 和-[PO-]基团之间的静电相互作用制备的。载药片具有 85.76%的高载药效率和 81.47%的药物包封效率,在 SSF(pH 6.8)中的润湿时间为 2.16 min,溶胀比为 233.34%。在模拟唾液(SSF pH 6.8)中,样品中负载的药物可在 10 min 内完全释放,表明在环境中具有快速的药物释放和溶解特性,可用于开发溶蚀片。