Alginate microparticles for Polymyxin B Peyer's patches uptake: microparticles for antibiotic oral administration.
Microparticles with size less than 3 microm, able to be taken up by M cell of Peyer's patches for the drug delivery to the Gut Associated Limphoid Tissue (GALT), were developed in order to improve oral bioavailability of Polymyxin B (PMB). Less than 3 microm alginate microparticles resistant to gastro-intestinal media were prepared by spray-drying technique and cross-linking by calcium ions and chitosan. The cross-linked microparticles were evaluated for PMB content by spectrophotometric method, alginate/PMB interaction by rheological study, cross-linking degree by EDS analysis and PMB activity by microbiological assay. By modulating the polymer cross-linking degree, cationic PMB interacted on alginate chains leading to a proper PMB loading as well as antibiotic retention in gastric environment and sustained delivery in intestinal fluid. Moreover, the procedure resulted suitable for PMB biological activity preservation.
Coppi
G
G
Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Via Campi, 183, 41100 Modena, Italy. coppi.gilberto@unimore.it
Iannuccelli
V
V
Sala
N
N
Bondi
M
M
D000284:Administration, Oral; D000464:Alginates; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods; D006801:Humans; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010581:Peyer's Patches / Q000378:metabolism*; D011112:Polymyxin B / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012212:Rheology; D013053:Spectrophotometry
D000464:Alginates; D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D011112:Polymyxin B