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Targeted delivery of diclofenac sodium via gelatin magnetic microspheres formulated for intra-arterial administration.
J Drug Target. 2008 Jun; 16(5):366-78.JD

Abstract

In the present work, we have attempted to deliver diclofenac sodium to a target site by intra-arterial injection of gelatin magnetic microspheres and subsequent localization using an external magnet. Drug-loaded magnetic microspheres were prepared by emulsification/cross-linking method, characterized by drug loading, magnetite content, size distribution, optical microscopy, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) analysis, differential scanning calorimetry (DSC), X-ray diffraction (XRD), absence of glutaraldehyde by gas chromatography, and in vitro release studies. The targeting efficiency and the therapeutic efficacy of microspheres were studied in vivo in rabbits. The microspheres showed drug loading of 9.1, 18.7, 24.9% w/w, magnetite content of 27.8-28.9% w/w with an average size range of 25-30.6 mum, depending upon the drug-polymer ratio. They were spherical in nature as evidenced by optical microscopy and SEM. FT-IR, DSC, and XRD studies revealed the absence of drug-polymer interaction. Gas chromatography confirmed the absence of residual glutaraldehyde. The microspheres were able to prolong the drug release over 24-30 days and the application of sonication during in vitro release study has slightly increased the release rate. After intra-arterial administration of microspheres, 77.7% of injected dose was recovered at the target site which revealed good targeting efficiency. The microspheres effectively reduced joint swelling, but lesser extent than the oral diclofenac sodium in high dose, in antigen induced arthritic rabbits without producing gastric ulceration which was observed in rabbits treated with oral diclofenac sodium.

Authors+Show Affiliations

School of Pharmacy, Faculty of Medical Sciences, University of West Indies, St Augustine, Trinidad, Tobago. msaravanan72@hotmail.comNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18569281

Citation

Saravanan, Muniyandy, et al. "Targeted Delivery of Diclofenac Sodium Via Gelatin Magnetic Microspheres Formulated for Intra-arterial Administration." Journal of Drug Targeting, vol. 16, no. 5, 2008, pp. 366-78.
Saravanan M, Anbu J, Maharajan G, et al. Targeted delivery of diclofenac sodium via gelatin magnetic microspheres formulated for intra-arterial administration. J Drug Target. 2008;16(5):366-78.
Saravanan, M., Anbu, J., Maharajan, G., & Pillai, K. S. (2008). Targeted delivery of diclofenac sodium via gelatin magnetic microspheres formulated for intra-arterial administration. Journal of Drug Targeting, 16(5), 366-78. https://doi.org/10.1080/10611860802046224
Saravanan M, et al. Targeted Delivery of Diclofenac Sodium Via Gelatin Magnetic Microspheres Formulated for Intra-arterial Administration. J Drug Target. 2008;16(5):366-78. PubMed PMID: 18569281.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Targeted delivery of diclofenac sodium via gelatin magnetic microspheres formulated for intra-arterial administration. AU - Saravanan,Muniyandy, AU - Anbu,Jayaraman, AU - Maharajan,Gomathinayagam, AU - Pillai,Kalathil Sadasivan, PY - 2008/6/24/pubmed PY - 2008/10/9/medline PY - 2008/6/24/entrez SP - 366 EP - 78 JF - Journal of drug targeting JO - J Drug Target VL - 16 IS - 5 N2 - In the present work, we have attempted to deliver diclofenac sodium to a target site by intra-arterial injection of gelatin magnetic microspheres and subsequent localization using an external magnet. Drug-loaded magnetic microspheres were prepared by emulsification/cross-linking method, characterized by drug loading, magnetite content, size distribution, optical microscopy, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) analysis, differential scanning calorimetry (DSC), X-ray diffraction (XRD), absence of glutaraldehyde by gas chromatography, and in vitro release studies. The targeting efficiency and the therapeutic efficacy of microspheres were studied in vivo in rabbits. The microspheres showed drug loading of 9.1, 18.7, 24.9% w/w, magnetite content of 27.8-28.9% w/w with an average size range of 25-30.6 mum, depending upon the drug-polymer ratio. They were spherical in nature as evidenced by optical microscopy and SEM. FT-IR, DSC, and XRD studies revealed the absence of drug-polymer interaction. Gas chromatography confirmed the absence of residual glutaraldehyde. The microspheres were able to prolong the drug release over 24-30 days and the application of sonication during in vitro release study has slightly increased the release rate. After intra-arterial administration of microspheres, 77.7% of injected dose was recovered at the target site which revealed good targeting efficiency. The microspheres effectively reduced joint swelling, but lesser extent than the oral diclofenac sodium in high dose, in antigen induced arthritic rabbits without producing gastric ulceration which was observed in rabbits treated with oral diclofenac sodium. SN - 1029-2330 UR - https://www.unboundmedicine.com/medline/citation/18569281/Targeted_delivery_of_diclofenac_sodium_via_gelatin_magnetic_microspheres_formulated_for_intra_arterial_administration_ L2 - http://www.tandfonline.com/doi/full/10.1080/10611860802046224 DB - PRIME DP - Unbound Medicine ER -