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Development of gelatin microspheres loaded with diclofenac sodium for intra-articular administration.
J Drug Target. 2011 Feb; 19(2):96-103.JD

Abstract

We have previously reported on the targeting of diclofenac sodium in joint inflammation using gelatin magnetic microspheres. To overcome complications in the administration of magnetic microspheres and achieve higher targeting efficiency, the present work focuses on the formulation of gelatin microspheres for intra-articular administration. Drug-loaded microspheres were prepared by the emulsification/cross-linking method, characterized by drug loading, size distribution, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gas chromatography, and in vitro release studies. The targeting efficiency of microspheres was studied in vivo in rabbits. The microspheres showed drug loading of 9.8, 18.3, and 26.7% w/w with an average size range of 37-46 µm, depending upon the drug-polymer ratio. They were spherical in nature and free from surface drug as evidenced by the SEM photographs. FT-IR, DSC, and XRD revealed the absence of drug-polymer interaction and amorphous nature of entrapped drug. Gas chromatography confirms the absences of residual glutaraldehyde. The formulated microspheres could prolong the drug release up to 30 days in vitro. About 81.2 and 43.7% of administered drug in the microspheres were recovered from the target joint after 1 and 7 days of postintra-articular injection, respectively, revealing good targeting efficiency.

Authors+Show Affiliations

Medicine and Health Sciences, Monash University, Selangor Darul Ehsan, Malaysia. msaravanan72@hotmail.comNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20380621

Citation

Saravanan, Muniyandy, et al. "Development of Gelatin Microspheres Loaded With Diclofenac Sodium for Intra-articular Administration." Journal of Drug Targeting, vol. 19, no. 2, 2011, pp. 96-103.
Saravanan M, Bhaskar K, Maharajan G, et al. Development of gelatin microspheres loaded with diclofenac sodium for intra-articular administration. J Drug Target. 2011;19(2):96-103.
Saravanan, M., Bhaskar, K., Maharajan, G., & Pillai, K. S. (2011). Development of gelatin microspheres loaded with diclofenac sodium for intra-articular administration. Journal of Drug Targeting, 19(2), 96-103. https://doi.org/10.3109/10611861003733979
Saravanan M, et al. Development of Gelatin Microspheres Loaded With Diclofenac Sodium for Intra-articular Administration. J Drug Target. 2011;19(2):96-103. PubMed PMID: 20380621.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of gelatin microspheres loaded with diclofenac sodium for intra-articular administration. AU - Saravanan,Muniyandy, AU - Bhaskar,Kesavan, AU - Maharajan,Gomathinayagam, AU - Pillai,Kalathil Sadasivan, Y1 - 2010/04/12/ PY - 2010/4/13/entrez PY - 2010/4/13/pubmed PY - 2011/4/1/medline SP - 96 EP - 103 JF - Journal of drug targeting JO - J Drug Target VL - 19 IS - 2 N2 - We have previously reported on the targeting of diclofenac sodium in joint inflammation using gelatin magnetic microspheres. To overcome complications in the administration of magnetic microspheres and achieve higher targeting efficiency, the present work focuses on the formulation of gelatin microspheres for intra-articular administration. Drug-loaded microspheres were prepared by the emulsification/cross-linking method, characterized by drug loading, size distribution, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gas chromatography, and in vitro release studies. The targeting efficiency of microspheres was studied in vivo in rabbits. The microspheres showed drug loading of 9.8, 18.3, and 26.7% w/w with an average size range of 37-46 µm, depending upon the drug-polymer ratio. They were spherical in nature and free from surface drug as evidenced by the SEM photographs. FT-IR, DSC, and XRD revealed the absence of drug-polymer interaction and amorphous nature of entrapped drug. Gas chromatography confirms the absences of residual glutaraldehyde. The formulated microspheres could prolong the drug release up to 30 days in vitro. About 81.2 and 43.7% of administered drug in the microspheres were recovered from the target joint after 1 and 7 days of postintra-articular injection, respectively, revealing good targeting efficiency. SN - 1029-2330 UR - https://www.unboundmedicine.com/medline/citation/20380621/Development_of_gelatin_microspheres_loaded_with_diclofenac_sodium_for_intra_articular_administration_ L2 - http://www.tandfonline.com/doi/full/10.3109/10611861003733979 DB - PRIME DP - Unbound Medicine ER -