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Novel interpenetrating network microspheres of xanthan gum-poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine--in vitro and in vivo evaluation.
Drug Deliv. 2010 Sep-Oct; 17(7):508-19.DD

Abstract

Xanthan gum (XG), a trisaccharide branched polymer and poly vinyl alcohol (PVA), was used to develop pH-sensitive interpenetrating network (IPN) microspheres by emulsion cross-linking method in the presence of glutaraldehyde as a cross-linker to deliver model anti-inflammatory drug, diclofenac sodium (DS) to the intestine. Various formulations were prepared by changing the ratio of XG:PVA, extent of cross-linking in order to optimize the formulation variables on drug encapsulation efficiency, and release rate. Formation of interpenetrating network and the chemical stability of DS after penetration of microspheres was confirmed by Fourier Transform infrared (FTIR) spectroscopy. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis were done on the drug loaded microspheres which confirmed molecular dispersion of DS in the IPN. Microspheres formed were spherical with smooth surfaces, as evidenced by scanning electron microscopy (SEM), and mean particle size, as measured by laser light scattering technique ranged between 310.25-477.10 microm. Drug encapsulation of up to 82.94% was achieved as measured by UV method. Both equilibrium and dynamic swelling studies and in vitro release studies were performed in pH 1.2 and 6.8. Release data indicated a Fickian trend of drug release which depends on the extent of cross-linking and the ratio of XG:PVA present in the microsphere. When subjected to in vivo pharmacokinetic evaluation in rabbits, microparticles show slow and prolonged drug release when compared with DS solution. Based on the results of in vitro and in vivo studies it was concluded that these IPN microspheres provided oral controlled release of water-soluble DS.

Authors+Show Affiliations

Gupta College of Technological Sciences, Ashram More, Asansol-1, West Bengal, India. somasreeray@yahoo.co.inNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20482471

Citation

Ray, Somasree, et al. "Novel Interpenetrating Network Microspheres of Xanthan Gum-poly(vinyl Alcohol) for the Delivery of Diclofenac Sodium to the Intestine--in Vitro and in Vivo Evaluation." Drug Delivery, vol. 17, no. 7, 2010, pp. 508-19.
Ray S, Banerjee S, Maiti S, et al. Novel interpenetrating network microspheres of xanthan gum-poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine--in vitro and in vivo evaluation. Drug Deliv. 2010;17(7):508-19.
Ray, S., Banerjee, S., Maiti, S., Laha, B., Barik, S., Sa, B., & Bhattacharyya, U. K. (2010). Novel interpenetrating network microspheres of xanthan gum-poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine--in vitro and in vivo evaluation. Drug Delivery, 17(7), 508-19. https://doi.org/10.3109/10717544.2010.483256
Ray S, et al. Novel Interpenetrating Network Microspheres of Xanthan Gum-poly(vinyl Alcohol) for the Delivery of Diclofenac Sodium to the Intestine--in Vitro and in Vivo Evaluation. Drug Deliv. 2010 Sep-Oct;17(7):508-19. PubMed PMID: 20482471.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel interpenetrating network microspheres of xanthan gum-poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine--in vitro and in vivo evaluation. AU - Ray,Somasree, AU - Banerjee,Subham, AU - Maiti,Sabyasachi, AU - Laha,Bibek, AU - Barik,Saikat, AU - Sa,Biswanath, AU - Bhattacharyya,Uttam Kumar, PY - 2010/5/21/entrez PY - 2010/5/21/pubmed PY - 2010/12/14/medline SP - 508 EP - 19 JF - Drug delivery JO - Drug Deliv VL - 17 IS - 7 N2 - Xanthan gum (XG), a trisaccharide branched polymer and poly vinyl alcohol (PVA), was used to develop pH-sensitive interpenetrating network (IPN) microspheres by emulsion cross-linking method in the presence of glutaraldehyde as a cross-linker to deliver model anti-inflammatory drug, diclofenac sodium (DS) to the intestine. Various formulations were prepared by changing the ratio of XG:PVA, extent of cross-linking in order to optimize the formulation variables on drug encapsulation efficiency, and release rate. Formation of interpenetrating network and the chemical stability of DS after penetration of microspheres was confirmed by Fourier Transform infrared (FTIR) spectroscopy. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis were done on the drug loaded microspheres which confirmed molecular dispersion of DS in the IPN. Microspheres formed were spherical with smooth surfaces, as evidenced by scanning electron microscopy (SEM), and mean particle size, as measured by laser light scattering technique ranged between 310.25-477.10 microm. Drug encapsulation of up to 82.94% was achieved as measured by UV method. Both equilibrium and dynamic swelling studies and in vitro release studies were performed in pH 1.2 and 6.8. Release data indicated a Fickian trend of drug release which depends on the extent of cross-linking and the ratio of XG:PVA present in the microsphere. When subjected to in vivo pharmacokinetic evaluation in rabbits, microparticles show slow and prolonged drug release when compared with DS solution. Based on the results of in vitro and in vivo studies it was concluded that these IPN microspheres provided oral controlled release of water-soluble DS. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/20482471/Novel_interpenetrating_network_microspheres_of_xanthan_gum_poly_vinyl_alcohol__for_the_delivery_of_diclofenac_sodium_to_the_intestine__in_vitro_and_in_vivo_evaluation_ L2 - http://www.tandfonline.com/doi/full/10.3109/10717544.2010.483256 DB - PRIME DP - Unbound Medicine ER -