title: A novel nanoparticulate system for sustained delivery of acid-labile lansoprazole.
abstract: In the present study, an effort was made to develop the Eudragit RS100 based nanoparticulate system for sustained delivery of an acid-labile drug, lansoprazole (LPZ). LPZ-loaded Eudragit RS100 nanoparticles (ERSNPs) were prepared by oil-in-water emulsion-solvent evaporation method. The effects of various formulation variables such as polymer concentration, drug amount and solvent composition on physicochemical performance of nanoparticles and in vitro drug release were investigated. All nanoparticles were spherical with particle size 198.9 ± 8.6-376.9 ± 5.6 nm and zeta potential +35.1 ± 1.7 to +40.2 ± 0.8 mV. The yield of nanoparticles was unaffected by change of these three variables. However, the drug loading and encapsulation efficiency were affected by polymer concentration and drug amount. On the other hand, the particle size of nanoparticles was significantly affected by polymer concentration and internal phase composition due to influence of droplet size during emulsification process. All nanoparticles prolonged drug release for 24h which was dominated by a combination of drug diffusion and polymer chain relaxation. The fastest and the slowest release rates were observed in C2-1002-10/0 and C8-4001-10/0, respectively, based on the release rate constant (k). Thus, the developed nanoparticles possessed a potential as a nano-carrier to sustain drug delivery for treatment of acid related disorders.
authors.affiliation: Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, National Taiwan University, Taipei 100, Taiwan.
authors.forename: Milind Sadashiv
authors.initials: MS
authors.lastname: Alai
authors.affiliation: Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, National Taiwan University, Taipei 100, Taiwan. Electronic address: wjlin@ntu.edu.tw.
authors.forename: Wen Jen
authors.initials: WJ
authors.lastname: Lin
mesh_terms: D000143:Acids / Q000737:chemistry*; D000180:Acrylic Resins; D002152:Calorimetry, Differential Scanning; D016503:Drug Delivery Systems; D007700:Kinetics; D064747:Lansoprazole / Q000494:pharmacology*; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D012996:Solutions; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D000143:Acids; D000180:Acrylic Resins; D011108:Polymers; D012996:Solutions; D012997:Solvents; D064747:Lansoprazole; C050528:Eudragit RS
keywords: Acid-labile drug; Eudragit RS100; Lansoprazole; Nanoparticles; Sustained release