University of Szeged Institute of Pharmaceutical Technology and Regulatory Affairs, Eötvös u. 6. H-6720, Szeged, Hungary; University of Szeged, Department of Applied Informatics, Boldogasszony sgt. 6. H-6725, Szeged, Hungary.
University of Szeged Institute of Pharmaceutical Technology and Regulatory Affairs, Eötvös u. 6. H-6720, Szeged, Hungary.
Eur J Pharm Sci. 2020 Apr 15;146:105270. doi: 10.1016/j.ejps.2020.105270. Epub 2020 Feb 19.
The oral delivery of biopharmaceuticals requires the including of absorption enhancer, protease inhibitor and a suitable carrier system. The aim of the present work was to formulate and characterize chitosan solutions/films incorporating citric acid (CA) as potential excipient in comparison to the well-known acetic acid (AA)-based films as a reference. Films were made by the solvent casting method with/without glycerol (G), propylene glycol (PG) and polyethylene glycol (PEG-400) as plasticizers. The minimum film forming temperature (MFFT) of the prepared solutions, film thickness, hardness/deformation, mucoadhesivity, moisture content, FT-IR spectra and surface free energy (SFE) were investigated. Chitosan has been reported as a safe and effective paracellular absorption enhancer for hydrophilic macromolecules, therefore there would be more rationale for incorporating CA as a solubility enhancer, a permeation enhancer and an enzyme inhibitor. CA shows good cross-linking, an ideal plasticizing property and increases both tensile strength and mucoadhesivity, thus its incorporation simplifies the formulation while improving effectiveness. We concluded that CA (3.5, 4 and 5 w/v %)-based chitosan solution could be used as a novel coating/subcoating polymer for oral macromolecule delivery, or as oral mucoadhesive films.
生物制药的口服给药需要包括吸收增强剂、蛋白酶抑制剂和合适的载体系统。本工作的目的是将柠檬酸（CA）制成壳聚糖溶液/薄膜并进行配方和特性分析，将其与众所周知的基于醋酸（AA）的薄膜作为参比进行比较。薄膜通过溶剂浇铸法制备，其中含有/不含有甘油（G）、丙二醇（PG）和聚乙二醇（PEG-400）作为增塑剂。研究了制备溶液的最低成膜温度（MFFT）、薄膜厚度、硬度/变形、粘膜粘附性、水分含量、傅里叶变换红外光谱（FT-IR）和表面自由能（SFE）。壳聚糖已被报道为亲水分子的安全有效的细胞旁吸收增强剂，因此将 CA 作为增溶剂、渗透增强剂和酶抑制剂加入其中更有意义。CA 具有良好的交联性、理想的增塑特性，可提高拉伸强度和粘膜粘附性，因此其加入简化了配方，同时提高了效果。我们得出结论，基于 CA（3.5、4 和 5 w/v%）的壳聚糖溶液可用于口服大分子给药的新型包衣/次包衣聚合物，或作为口服粘膜粘附性薄膜。
