Development of a polymeric nanoparticulate drug delivery system. In vitro characterization of nanoparticles based on sugar-containing conjugates.
This paper reports the synthesis of polymeric nanoparticles from a sugar-containing conjugate for liver-specific drug delivery. The conjugate was composed of lactobionic acid, diamine-terminated poly(ethylene glycol) and cholic acid (abbreviated as LEC). The conjugate was characterized by (1)H NMR and FT-IR spectroscopy measurements. In aqueous media, the conjugate can self-assemble to form core-shell type nanoparticles, and the formation of a core-shell structure was observed by fluorescence spectroscopy. The critical association concentration (CAC) of the LEC conjugate nanoparticles was determined from fluorescence excitation spectra to be 0.05 g/l. The LEC nanoparticles were mostly spherical with sizes ranging from 10 to 30 nm. Clonazepam (CNZ) was used as a model hydrophobic drug, and was incorporated into the hydrophobic core of the nanoparticles. CNZ was released more slowly at a higher drug loading due to drug crystallization.
Kim
In-Sook
IS
Department of Biological Chemistry, College of Pharmacy, Chosun University, #375 Seosuk-dong, Dong-gu, Gwangju 501-759, Republic of Korea. shkim@mail.chosun.ac.kr
Kim
Sung-Ho
SH
D000927:Anticonvulsants / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D019826:Cholic Acid / Q000737:chemistry; D002998:Clonazepam / Q000737:chemistry; D003460:Crystallization; D003692:Delayed-Action Preparations; D004187:Disaccharides / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D009682:Magnetic Resonance Spectroscopy; D008854:Microscopy, Electron; D036103:Nanotechnology; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers; D013050:Spectrometry, Fluorescence; D017550:Spectroscopy, Fourier Transform Infrared
D000927:Anticonvulsants; D003692:Delayed-Action Preparations; D004187:Disaccharides; D004337:Drug Carriers; D011108:Polymers; D011092:Polyethylene Glycols; D002998:Clonazepam; C005608:lactobionic acid; D019826:Cholic Acid