Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
Pharm Dev Technol. 2013 Jul-Aug;18(4):821-7. doi: 10.3109/10837450.2012.700930. Epub 2012 Jul 4.
Oral peptide and protein drug delivery still remain the area of challenges for pharmaceutical scientists due to their low stability and permeability in gastrointestinal (GI) tract. In this study phospholipid vesicle-bound lysozyme were prepared and assessed for their physicochemical properties, secondary structure, and permeation across Caco-2 cells.
Lysozyme was found to be substantially bound onto negatively charged vesicles via electrostatic interaction as evidenced by zeta potential measurements regardless of cholesterol content. In contrast, the size of phospholipid vesicle-bound lysozyme became larger with the increasing cholesterol content. The secondary structure of vesicle-bound lysozyme examined by FTIR was unchanged compared to that in buffer solution. The apparent permeability of vesicle-bound lysozyme across Caco-2 cells monolayer was significantly enhanced with a size dependent manner compared to that of solution.
The permeation across Caco-2 cell monolayers of phospholipid vesicle-bound lysozyme was demonstrated to be significantly enhanced with a size-dependent manner.
由于在胃肠道中稳定性和通透性低，口腔肽和蛋白类药物的传递仍然是药物科学家面临的挑战领域。在这项研究中，制备了带负电荷的磷脂囊泡结合溶菌酶，并评估了它们的理化性质、二级结构和跨 Caco-2 细胞的渗透作用。
通过zeta 电位测量，证明溶菌酶通过静电相互作用与带负电荷的囊泡大量结合，而与胆固醇含量无关。相比之下，带负电荷的磷脂囊泡结合溶菌酶的粒径随着胆固醇含量的增加而增大。通过 FTIR 检查的囊泡结合溶菌酶的二级结构与在缓冲溶液中的结构相同。与溶液相比，囊泡结合溶菌酶在 Caco-2 细胞单层中的表观渗透作用以尺寸依赖性的方式显著增强。
磷脂囊泡结合溶菌酶在 Caco-2 细胞单层中的渗透作用被证明是以尺寸依赖性的方式显著增强。
