title: Methylated N-(4-N,N-dimethylaminobenzyl) chitosan coated liposomes for oral protein drug delivery.
abstract: In the present study, methylated N-(4-N,N-dimethylaminobenzyl) chitosan (TM(56)Bz(42)CS) was synthesised and investigated for oral protein drug delivery by combining it with liposomes entrapped with fluorescein isothiocyanate-conjugated bovine serum albumin (FITC-BSA), a model protein. Liposomes (LPs) composed of 10:2 molar ratios of egg yolk phosphatidylcholine (EPC) and sodium oleate (NaO) were prepared by a thin film hydration method and coated with TM(56)Bz(42)CS. BSA-loaded, TM(56)Bz(42)CS-coated liposomes (TM(56)Bz(42)CS-coated FITC-BSA-LP) were evaluated for their protein transport efficiencies and cytotoxicities in Caco-2 cells. Moreover, the in vitro stabilities of the TM(56)Bz(42)CS-coated LP-BSA were determined by examining the degradation of the protein in simulated intestinal fluid containing 1% w/v pancreatin porcine pancreas. The mean particle size and zeta-potential of the TM(56)Bz(42)CS-coated LP-BSA were 128 ± 15 nm and 5.38 ± 1.66 mV, respectively. Additionally, the initial FITC-BSA to lipid ratio (2.5% w/w) showed the highest entrapment efficiency percentage (50.13%) and FITC-BSA content (8.08 mg/g of lipid) overall. The results of the FITC-BSA transport showed that the TM(56)Bz(42)CS-coated FITC-BSA-LP enhanced protein permeability across the Caco-2 cell monolayers with low cytotoxicity. In addition, these liposomes protected against protein degradation in pancreatin. Our studies demonstrated that TM(56)Bz(42)CS-coated liposomes have the potential to be used in oral protein drug delivery methods.
authors: Pharmaceutical Development of Green Innovations Group, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.
authors: Jariya
authors: J
authors: Kowapradit
authors: Auayporn
authors: A
authors: Apirakaramwong
authors: Tanasait
authors: T
authors: Ngawhirunpat
authors: Theerasak
authors: T
authors: Rojanarata
authors: Warayuth
authors: W
authors: Sajomsang
authors: Praneet
authors: P
authors: Opanasopit
mesh_terms: D000284:Administration, Oral; D001692:Biological Transport; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism; D016650:Fluorescein-5-isothiocyanate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption; D008081:Liposomes; D012710:Serum Albumin, Bovine / Q000008:administration & dosage* / Q000378:metabolism
chemical_list: D008081:Liposomes; C039217:fluorescein isothiocyanate bovine serum albumin; C539634:methylated N-(4-N,N-dimethylaminobenzyl)chitosan; D012710:Serum Albumin, Bovine; D048271:Chitosan; D016650:Fluorescein-5-isothiocyanate