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Design and characterization of chitosan/citrate films as carrier for oral macromolecule delivery.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-19 , DOI: 10.1016/j.ejps.2020.105270 Yousif H-E Y Ibrahim 1 , Géza Regdon 2 , Katalin Kristó 2 , András Kelemen 3 , Mohamed E Adam 4 , Elnazeer I Hamedelniel 5 , Tamás Sovány 2
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-19 , DOI: 10.1016/j.ejps.2020.105270 Yousif H-E Y Ibrahim 1 , Géza Regdon 2 , Katalin Kristó 2 , András Kelemen 3 , Mohamed E Adam 4 , Elnazeer I Hamedelniel 5 , Tamás Sovány 2
Affiliation
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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.
中文翻译：
壳聚糖/柠檬酸盐薄膜作为口服大分子载体的设计和表征。
生物药物的口服递送需要包括吸收促进剂，蛋白酶抑制剂和合适的载体系统。与已知的基于乙酸（AA）的薄膜相比，本研究的目的是配制和表征掺入柠檬酸（CA）作为潜在赋形剂的壳聚糖溶液/薄膜。通过溶剂流延法用/不使用甘油（G），丙二醇（PG）和聚乙二醇（PEG-400）作为增塑剂来制备薄膜。研究了所制备溶液的最低成膜温度（MFFT），膜厚，硬度/变形，粘膜粘附性，水分含量，FT-IR光谱和表面自由能（SFE）。据报道，壳聚糖是一种安全有效的亲水大分子旁细胞吸收促进剂，因此，将CA作为溶解度增强剂，渗透增强剂和酶抑制剂并入更合理。CA表现出良好的交联性，理想的增塑性能，并增加了拉伸强度和粘膜粘附性，因此其掺入简化了配方，同时提高了效力。我们得出的结论是，基于CA（3.5、4和5 w / v％）的壳聚糖溶液可以用作新型的涂层/底涂层聚合物，用于口服大分子递送或用作口腔粘膜粘膜。
更新日期：2020-02-20
中文翻译：
壳聚糖/柠檬酸盐薄膜作为口服大分子载体的设计和表征。
生物药物的口服递送需要包括吸收促进剂，蛋白酶抑制剂和合适的载体系统。与已知的基于乙酸（AA）的薄膜相比，本研究的目的是配制和表征掺入柠檬酸（CA）作为潜在赋形剂的壳聚糖溶液/薄膜。通过溶剂流延法用/不使用甘油（G），丙二醇（PG）和聚乙二醇（PEG-400）作为增塑剂来制备薄膜。研究了所制备溶液的最低成膜温度（MFFT），膜厚，硬度/变形，粘膜粘附性，水分含量，FT-IR光谱和表面自由能（SFE）。据报道，壳聚糖是一种安全有效的亲水大分子旁细胞吸收促进剂，因此，将CA作为溶解度增强剂，渗透增强剂和酶抑制剂并入更合理。CA表现出良好的交联性，理想的增塑性能，并增加了拉伸强度和粘膜粘附性，因此其掺入简化了配方，同时提高了效力。我们得出的结论是，基于CA（3.5、4和5 w / v％）的壳聚糖溶液可以用作新型的涂层/底涂层聚合物，用于口服大分子递送或用作口腔粘膜粘膜。
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