Evaluation of liposomes coated with a pH responsive polymer.
Liposomes have been coated with the pH responsive polymer, Eudragit S100, and the formulation's potential for lower gastrointestinal (GI) targeting following oral administration assessed. Cationic liposomes were coated with the anionic polymer through simple mixing. The evolution of a polymer coat was studied using zeta potential measurements and laser diffraction size analysis. Further evidence of an association between polymer and liposome was obtained using light and cryo scanning electron microscopy. Drug release studies were carried out at pH 1.4, pH 6.3 and pH 7.8, representing the pH conditions of the stomach, small intestine and ileocaecal junction, respectively. The polymer significantly reduced liposomal drug release at pH 1.4 and pH 6.3 but drug release was equivalent to the uncoated control at pH 7.8, indicating that the formulation displayed appropriate pH responsive release characteristics. While the coating layer was not able to withstand the additional challenge of bile salts this reinforces the importance of evaluating these types of formulations in more complex media.
Barea
M J
MJ
Centre for Formulation Engineering, School of Chemical Engineering, University of Birmingham, Edgbaston, Birmingham B15 2TT, UK. mjb246@bham.ac.uk
Jenkins
M J
MJ
Gaber
M H
MH
Bridson
R H
RH
D000284:Administration, Oral; D001647:Bile Acids and Salts / Q000378:metabolism; D002412:Cations; D003106:Colon / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D041981:Gastrointestinal Tract / Q000378:metabolism; D006863:Hydrogen-Ion Concentration; D008081:Liposomes; D008855:Microscopy, Electron, Scanning / Q000379:methods; D011109:Polymethacrylic Acids / Q000737:chemistry*; D014805:Vitamin B 12 / Q000008:administration & dosage / Q000737:chemistry
D001647:Bile Acids and Salts; D002412:Cations; D004337:Drug Carriers; D008081:Liposomes; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D014805:Vitamin B 12