PMID- 16824710
OWN - NLM
STAT- MEDLINE
DCOM- 20061207
LR  - 20181201
IS  - 0378-5173 (Print)
IS  - 0378-5173 (Linking)
VI  - 324
IP  - 2
DP  - 2006 Nov 6
TI  - Novel interpenetrating network chitosan-poly(ethylene oxide-g-acrylamide) 
      hydrogel microspheres for the controlled release of capecitabine.
PG  - 103-15
AB  - This paper describes the synthesis of capecitabine-loaded semi-interpenetrating 
      network hydrogel microspheres of chitosan-poly(ethylene oxide-g-acrylamide) by 
      emulsion crosslinking using glutaraldehyde. Poly(ethylene oxide) was grafted with 
      polyacrylamide by free radical polymerization using ceric ammonium nitrate as a 
      redox initiator. Capecitabine, an anticancer drug, was successfully loaded into 
      microspheres by changing experimental variables such as grafting ratio of the 
      graft copolymer, ratio of the graft copolymer to chitosan, amount of crosslinking 
      agent and percentage of drug loading in order to optimize process variables on 
      drug encapsulation efficiency, release rates, size and morphology of the 
      microspheres. A 2(4) full factorial design was employed to evaluate the combined 
      effect of selected independent variables on percentage of drug release at 5h 
      (response). Regression models were used for the response and data were compared 
      statistically using the analysis of variance (ANOVA). Grafting, interpenetrating 
      network formation and chemical stability of the capecitabine after encapsulation 
      into microspheres was confirmed by Fourier infrared spectra (FTIR). Differential 
      scanning calorimetry (DSC) and X-ray diffractometry (XRD) studies were made on 
      drug-loaded microspheres to investigate the crystalline nature of drug after 
      encapsulation. Results indicated amorphous dispersion of capecitabine in the 
      polymer matrix. Scanning electron microscope (SEM) confirmed spherical shapes and 
      smooth surface morphology of the microspheres. Mean particle size of the 
      microspheres as measured by the laser light scattering technique ranged between 
      82 and 168microm. Capecitabine was successfully encapsulated into semi-IPN 
      microspheres and percentage of encapsulation efficiency varied from 79 to 87. In 
      vitro release studies were performed in simulated gastric fluid (pH 1.2) for the 
      initial 2h, followed by simulated intestinal fluid (pH 7.4) until complete 
      dissolution. The release of capecitabine was continued up to 10h. Release data 
      were fitted to an empirical relationship to estimate the transport parameters. 
      Dynamic swelling studies were performed in the simulated intestinal fluid and 
      diffusion coefficients were calculated by considering the spherical geometry of 
      the matrices.
FAU - Agnihotri, Sunil A
AU  - Agnihotri SA
AD  - Drug Delivery Division, Center of Excellence in Polymer Science, Karnatak 
      University, Dharwad 580 003, India.
FAU - Aminabhavi, Tejraj M
AU  - Aminabhavi TM
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20060603
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Acrylic Resins)
RN  - 0 (Delayed-Action Preparations)
RN  - 0W860991D6 (Deoxycytidine)
RN  - 25852-47-5 (Hydrogel, Polyethylene Glycol Dimethacrylate)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
RN  - 6804DJ8Z9U (Capecitabine)
RN  - 9003-05-8 (polyacrylamide)
RN  - 9012-76-4 (Chitosan)
RN  - U3P01618RT (Fluorouracil)
SB  - IM
MH  - Acrylic Resins
MH  - Calorimetry, Differential Scanning
MH  - Capecitabine
MH  - Chitosan/*administration & dosage
MH  - Delayed-Action Preparations
MH  - Deoxycytidine/administration & dosage/*analogs & derivatives/chemistry
MH  - Diffusion
MH  - Fluorouracil/analogs & derivatives
MH  - Hydrogel, Polyethylene Glycol Dimethacrylate
MH  - *Microspheres
MH  - Polyethylene Glycols
MH  - Solubility
MH  - Spectroscopy, Fourier Transform Infrared
MH  - X-Ray Diffraction
EDAT- 2006/07/11 09:00
MHDA- 2006/12/09 09:00
CRDT- 2006/07/11 09:00
PHST- 2005/11/30 00:00 [received]
PHST- 2006/04/03 00:00 [revised]
PHST- 2006/05/28 00:00 [accepted]
PHST- 2006/07/11 09:00 [pubmed]
PHST- 2006/12/09 09:00 [medline]
PHST- 2006/07/11 09:00 [entrez]
AID - S0378-5173(06)00446-7 [pii]
AID - 10.1016/j.ijpharm.2006.05.061 [doi]
PST - ppublish
SO  - Int J Pharm. 2006 Nov 6;324(2):103-15. doi: 10.1016/j.ijpharm.2006.05.061. Epub 
      2006 Jun 3.