Design and production of gentamicin/dextrans microparticles by supercritical assisted atomisation for the treatment of wound bacterial infections.
In this work, the supercritical assisted atomisation (SAA) is proposed, for the first time, for the production of topical carrier microsystems based on alginate-pectin blend. Gentamicin sulphate (GS) was loaded as high soluble and hygroscopic antibiotic model with poor flowability. Particularly, different water solutions of GS/alginate/pectin were processed by SAA to produce spherical microparticles (GAP) of narrow size (about 2 μm). GS loading was varied between 20% and 33% (w/w) with an encapsulation efficiency reaching about 100%. The micronised powders also showed high flow properties, good stability and constant water content after 90 days in accelerated storage conditions. The release profiles of the encapsulated drug were monitored using vertical diffusion Franz cells to evaluate the application of GAP microsystems as self-consistent powder formulation or in specific fibres or gels for wound dressing. All formulations showed an initial burst effect in the first 6h of application (40-65% of GS loaded), and in particular GAP4 produced with a GS/alginate/pectin ratio of 1:3:1, exhibited the ability to release GS continuously over 6 days. Antimicrobial tests against Staphylococcus aureus indicated that GS antibiotic activity was preserved at 6 days and higher than pure GS at 12 and 24 days for all SAA formulations, especially for GAP1.
Department of Pharmaceutical and Biomedical Sciences, University of Salerno, via Ponte don Melillo, 84084 Fisciano, SA, Italy.
Rita P
RP
Aquino
Giulia
G
Auriemma
Teresa
T
Mencherini
Paola
P
Russo
Amalia
A
Porta
Renata
R
Adami
Sara
S
Liparoti
Giovanna
G
Della Porta
Ernesto
E
Reverchon
Pasquale
P
Del Gaudio
D000279:Administration, Cutaneous; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001682:Biological Availability; D025924:Chromatography, Supercritical Fluid / Q000295:instrumentation / Q000379:methods*; D003911:Dextrans / Q000008:administration & dosage* / Q000627:therapeutic use; D004337:Drug Carriers / Q000008:administration & dosage / Q000627:therapeutic use; D015195:Drug Design; D004355:Drug Stability; D005839:Gentamicins / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008826:Microbial Sensitivity Tests / Q000379:methods; D010316:Particle Size; D011208:Powders / Q000008:administration & dosage / Q000627:therapeutic use; D013211:Staphylococcus aureus / Q000187:drug effects; D014946:Wound Infection / Q000188:drug therapy*
D000900:Anti-Bacterial Agents; D003911:Dextrans; D004337:Drug Carriers; D005839:Gentamicins; D011208:Powders