Development of 5-fluorouracil loaded poly(acrylamide-co-methylmethacrylate) novel core-shell microspheres: in vitro release studies.
Novel poly(acrylamide-methylmethacrylate) copolymeric core-shell microspheres crosslinked with N,N'-methylene bisacrylamide have been prepared by free radical emulsion polymerization using varying amounts of acrylamide (AAm), methylmethacrylate (MMA) and N,N'-methylene bisacrylamide (NNMBA). 5-Fluorouracil was loaded into these microspheres during in situ polymerization (method-I) as well as by the absorption and adsorption technique (method-II). The core-shell microspheres have been characterized by differential scanning calorimetry (DSC) and X-ray diffractometry (X-RD) to understand about the drug dispersion in microspheres. Scanning electron microscopy (SEM) was used to assess the surface morphology of particles prepared. In vitro release of 5-fluorouracil has been studied in terms of core-shell composition, amount of crosslinking agent and amount of 5-fluorouracil in the microspheres. Core-shell microspheres with different copolymer compositions have been prepared in yields ranging 80-85%. DSC and X-RD techniques indicated a uniform distribution of 5-fluorouracil particles in core-shell microspheres, whereas SEM suggested the formation of well-defined core-shell structures. The in vitro drug release indicated that particle size and release kinetics depend upon copolymer composition, amount of crosslinking agent used and amount of 5-fluorouracil present in the microspheres. Prolonged and controlled release of 5-fluorouracil was achieved when drug was loaded by method-I instead of method-II.
Babu
V Ramesh
VR
Drug Delivery Division, Center of Excellence in Polymer Science, Karnatak University, Dharwad 580003, India.
Sairam
Malladi
M
Hosamani
Kallappa M
KM
Aminabhavi
Tejraj M
TM
D000042:Absorption; D000178:Acrylamides / Q000737:chemistry / Q000378:metabolism; D000180:Acrylic Resins / Q000737:chemistry*; D000327:Adsorption; D000465:Algorithms; D002152:Calorimetry, Differential Scanning / Q000379:methods; D003432:Cross-Linking Reagents / Q000737:chemistry; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D005472:Fluorouracil / Q000737:chemistry* / Q000493:pharmacokinetics; D007700:Kinetics; D020366:Methylmethacrylate / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning / Q000379:methods; D008863:Microspheres; D053769:Nanocapsules; D010316:Particle Size; D014961:X-Ray Diffraction / Q000379:methods; D000099166:Polyacrylamides
D000178:Acrylamides; D000180:Acrylic Resins; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D005472:Fluorouracil; D020366:Methylmethacrylate; D053769:Nanocapsules; D000099166:Polyacrylamides; C021221:N,N'-methylenebisacrylamide