Amphotericin B-incorporated polymeric micelles composed of poly(d,l-lactide-co-glycolide)/dextran graft copolymer.
In this study, we prepared amphotericin B (AmpB)-encapsulated polymeric micelle of poly(d,l-lactide-co-glycolide) (PLGA) grafted-dextran (DexLG) copolymer and characterized its physicochemical properties in vitro. The average particle size of AmpB-encpasulated DexLG polymeric micelles was around 30-150nm while particle size of empty polymeric micelles was below 100nm according to the copolymer composition. The morphology of AmpB-encapsulated polymeric micelle of DexLG copolymer was spherical shapes at transmission electron microscopy (TEM) observation. At 1H NMR study, specific peaks of AmpB and DexLG copolymer was obtained at DMSO but specific peaks characterized to AmpB and PLGA was disappeared at D2O environment. These results indicated that AmpB was encapsulated into the micellar core of polymeric micelle. XRD results also support these results, indicating that specific crystal peaks of AmpB and broad peaks of DexLG copolymer were obtained but specific peaks of AmpB was disappeared at polymeric micelles while physical mixture of AmpB/empty polymeric micelles showed both specific peaks. Drug release rate was decreased according to the increase of drug contents and increase of PLGA component of DexLG copolymer. At the minimal inhibition concentration (MIC) study using Candida albicans, AmpB-encapsulated polymeric micelle showed almost similar effectives on the growth inhibition of microorganisms. These showed that AmpB-encapsulated polymeric micelle of DexLG copolymer can be considered to potential antifungal agent carriers.
Choi
Ki-Choon
KC
Division of Endocrinology and Metabolism, Department of Internal Medicine, College of Medicine, Korea University, Seoul, Republic of Korea.
Bang
Je-Yong
JY
Kim
Pyoung-Il
PI
Kim
Chan
C
Song
Chae-Eun
CE
D000666:Amphotericin B / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D003911:Dextrans; D019344:Lactic Acid; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D014961:X-Ray Diffraction
D000935:Antifungal Agents; D003911:Dextrans; D008823:Micelles; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000666:Amphotericin B