Application of Methylated N-(4-N,N-Dimethylaminocinnamyl) Chitosan for Oral Protein Drug Delivery
In the present study, methylated N-(4-N,N-dimethylaminocinnamyl) chitosan (TM65CM50CS) was synthesized and investigated for oral protein drug delivery by combining with liposomes entrapped bovine serum albumin (FITC-BSA), a model protein. FITC-BSA liposomes composed of egg yolk phosphatidylcholine and sodium oleate in molar ratio of 10:2 were prepared by thin film hydration method. The TM65CM50CS coated liposomal FITC-BSA was evaluated for transport of protein and its cytotoxicity in Caco-2 cells. Moreover, the in vitro stability of BSA in TM65CM50CS coated liposomes was also examined by the degradation of protein from pancreatin. The mean particle size and zeta-potential of liposomes were 101+0.02 nm and -27.44+2.02 mV, respectively. Initial FITC-BSA (2.5% w/w) to lipid showed the highest percentage entrapment efficiency (50.13%) and FITC-BSA content (8.08 mg/g of lipid). The results of FITC-BSA transport showed that TM65CM50CS coated FITC-BSA liposomes enhanced protein permeability across Caco-2 cell monolayers with low cytotoxicity. In addition, these liposomes could protect the degradation of protein from pancreatin. Our studies demonstrated that TM65CM50CS coated liposomes have the potential to be used as an oral protein drug delivery.
J. Kowapradit et al., "Application of Methylated N-(4-N,N-Dimethylaminocinnamyl) Chitosan for Oral Protein Drug Delivery", Advanced Materials Research, Vol. 506, pp. 465-468, 2012