Poloxamer 407 microspheres for orotransmucosal drug delivery. Part I: formulation, manufacturing and characterization.
The two-part article aimed to investigate poloxamer 407-based microspheres as a novel platform for enhancing and controlling the delivery of atenolol across the oromucosal tissue. In the Part I of the work, atenolol-loaded poloxamers 407 microparticles were prepared by the solvent free spray congealing technology. This approach was feasible upon the high viscosity of the systems allowing for high loaded (20% w/w) non-aggregated microspheres. Several formulations were studied and the results demonstrated that the drug release patterns, solubility data, mucoadhesion to buccal tissue and gelling properties in saliva could be modified by adding different amount of an amphiphilic polymer-lipid excipient (Gelucire(®) 50/13) to poloxamer 407. Particularly, microspheres based only on poloxamer 407 exhibited very high solubility, mucoadhesive strength and gelling behaviour. To assess their potential as matrix for buccal application, the gelling property and the drug release from tablets obtained from direct compression of the microparticles were further evaluated. The microspheres were then characterized by differential scanning calorimetry, X-ray powder diffraction and Fourier transform-infrared spectra analysis. No solid state modifications and chemical interactions were detectable in the microspheres after manufacturing and during storage, suggesting their stability and use as orotransmucosal delivery systems.
Albertini
B
B
Department of Pharmaceutical Sciences, University of Bologna, Bologna, Italy. beatrice.albertini@unibo.it
Passerini
N
N
Di Sabatino
M
M
Monti
D
D
Burgalassi
S
S
Chetoni
P
P
Rodriguez
L
L
D000284:Administration, Oral; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D006801:Humans; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009061:Mouth Mucosa / Q000378:metabolism*; D010316:Particle Size; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry*; D033362:Powder Diffraction; D012463:Saliva / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013607:Tablets; D014783:Viscosity; D014961:X-Ray Diffraction
D004337:Drug Carriers; D004364:Pharmaceutical Preparations; D013607:Tablets; D020442:Poloxamer