Preparation and characterization of quercetin-loaded polymethyl methacrylate microcapsules using a polyol-in-oil-in-polyol emulsion solvent evaporation method.
Flavonoids and related compounds exhibit a wide range of useful pharmacological properties but present challenges related to their stability and solubility in commonly available solvents. In this study, polymethyl methacrylate (PMMA) microcapsules were prepared using a novel polyol-in-oil-in-polyol (P/O/P) emulsion solvent evaporation method as a means of stabilizing the flavonoids, using quercetin as a model flavonoid drug. The morphology of the microcapsules was evaluated using a scanning electron microscope, revealing a spherical shape with a smooth surface. The cross-section image of the PMMA microcapsules prepared with an amphiphilic polymer in the inner polyol phase showed that the microcapsule was filled with several submicron microspheres. The mean diameter varied from 1.03+/-0.12 microm to 2.39+/-0.42 microm, and the encapsulation efficiency ranged from 12.7% to 26.9%. When free quercetin was stored at 42 degrees C, the residual quercetin content gradually decreased to 18% over 28 days as a result of oxidation. However, when encapsulated in PMMA microcapsules with an amphiphilic polymer in the inner polyol phase, the residual quercetin content decreased to just 82%. In-vitro release studies indicated a sustained release pattern throughout the 36-h study. The release kinetics of the microcapsules with an amphiphilic polymer followed a diffusion-controlled mechanism and the microcapsule without amphiphilic polymer followed an anomalous diffusion behaviour. This study suggests that the novel P/O/P emulsion solvent evaporation method can be applied to the encapsulation of flavonoids.
Lee
Dong-Hwan
DH
R & D Center, Hanbul Cosmetics Co., 72-7, Yongsung-ri, Samsung-myun, Umsung-kun, Chungbuk 369-834, Republic of Korea.
Sim
Gwan-Sub
GS
Kim
Jin-Hwa
JH
Lee
Geun-Soo
GS
Pyo
Hyeong-Bae
HB
Lee
Bum-Chun
BC
D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry; D005419:Flavonoids / Q000737:chemistry; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D019904:Polymethyl Methacrylate / Q000737:chemistry*; D011794:Quercetin / Q000737:chemistry*; D012996:Solutions; D012997:Solvents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods*; D014835:Volatilization; D014867:Water / Q000737:chemistry
D002214:Capsules; D004655:Emulsions; D005419:Flavonoids; D009821:Oils; D012996:Solutions; D012997:Solvents; D014867:Water; D019904:Polymethyl Methacrylate; D011794:Quercetin