Self-assembled nanoparticles of PLGA-conjugated glucosamine as a sustained transdermal drug delivery vehicle

Abstract

Glucosamine (GlcN), an amino-monosaccharide, is known to be a safe and efficient drug for the treatment of various. inflammatory diseases, including osteoarthritis and rheumatoid arthritis. In this current study, the main issues of high hydrophilicity and poor permeability of GlcN for its use as a transdermal delivery system were overcome by conjugation with the hydrophobic polymer poly(D,L-lactic-co-glycolic acid) (PLGA) and its self-assembly into nanostructures containing nanoparticles (NPs). The self-assembly of the PLGA-GlcN nanostructure was facilitated by probe sonication, which was based on the cavitation and nucleation concept, followed by reversible locking. Hydrophobic PLGA assembly onto the outer surface and hydrophilic GlcN into the inner core helps the nanostructure more flexibly permeate through the skin lipid membrane and release GlcN in a sustained manner for 48 h. Ex vivo transdermal permeation of PLGA-GlcN nanostructures through human cadaver skin exhibited a better permeation profile, which demonstrated the shortest lag time with a higher flux value than the other formulations, such as the GlcN solution, GlcN NPs and PLGA-GlcN solution. Polymer Journal (2013) 45, 202-209; doi:10.1038/pj.2012.103; published online 13 June 2012