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Formulation and evaluation of flurbiprofen-loaded genipin cross-linked gelatin microspheres for intra-articular delivery.
J Drug Target. 2013 Feb; 21(2):200-10.JD

Abstract

Oral and parenteral formulations are challenging to produce therapeutic concentration of flurbiprofen in the joints. This encourages for the development of formulation for long term drug retention in the joint through intra-articular (i. a.) administration. In this study, genipin cross-linked gelatin microspheres of flurbiprofen were prepared for i. a. delivery. The microspheres were prepared using emulsification-homogenization-cross-linking method by changing the experimental variables such as concentration of cross-linker, cross-linking time and cross-linking temperature. The microspheres showed drug entrapment up to 76.19% with a mean particle size range of 5.91-8.19 µm. The degree of cross-linking and water-soluble fraction were 8.27-59.33% and 12.29-81.23%, respectively. SEM confirmed smooth surface and spherical shape of the microspheres. FTIR and (13)C-NMR confirmed cross-linking of gelatin by genipin. No chemical change in encapsulated drug was observed by FTIR and TGA. DSC and XRD indicated the molecular dispersion of drug within microspheres. Optimized microspheres could prolong the drug release for more than 108 h with anomalous transport. Histopathology confirmed the biocompatibility of microspheres in the rat (Wistar) knee joint. After 96 h of i. a. injection, significant higher amount (42.56%) of administered drug in cross-linked microspheres was recovered than uncross-linked microspheres (8.27%) confirming better drug retention efficiency (p < 0.01).

Authors+Show Affiliations

Department of Pharmaceutics, NDDS Research Laboratory, Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), University of Delhi, New Delhi, India.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23249324

Citation

Kawadkar, Jitendra, et al. "Formulation and Evaluation of Flurbiprofen-loaded Genipin Cross-linked Gelatin Microspheres for Intra-articular Delivery." Journal of Drug Targeting, vol. 21, no. 2, 2013, pp. 200-10.
Kawadkar J, Jain R, Kishore R, et al. Formulation and evaluation of flurbiprofen-loaded genipin cross-linked gelatin microspheres for intra-articular delivery. J Drug Target. 2013;21(2):200-10.
Kawadkar, J., Jain, R., Kishore, R., Pathak, A., & Chauhan, M. K. (2013). Formulation and evaluation of flurbiprofen-loaded genipin cross-linked gelatin microspheres for intra-articular delivery. Journal of Drug Targeting, 21(2), 200-10. https://doi.org/10.3109/1061186X.2012.745549
Kawadkar J, et al. Formulation and Evaluation of Flurbiprofen-loaded Genipin Cross-linked Gelatin Microspheres for Intra-articular Delivery. J Drug Target. 2013;21(2):200-10. PubMed PMID: 23249324.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and evaluation of flurbiprofen-loaded genipin cross-linked gelatin microspheres for intra-articular delivery. AU - Kawadkar,Jitendra, AU - Jain,Ritika, AU - Kishore,Raj, AU - Pathak,Ashwinkumar, AU - Chauhan,Meenakshi Kanwar, Y1 - 2012/12/19/ PY - 2012/12/20/entrez PY - 2012/12/20/pubmed PY - 2013/7/23/medline SP - 200 EP - 10 JF - Journal of drug targeting JO - J Drug Target VL - 21 IS - 2 N2 - Oral and parenteral formulations are challenging to produce therapeutic concentration of flurbiprofen in the joints. This encourages for the development of formulation for long term drug retention in the joint through intra-articular (i. a.) administration. In this study, genipin cross-linked gelatin microspheres of flurbiprofen were prepared for i. a. delivery. The microspheres were prepared using emulsification-homogenization-cross-linking method by changing the experimental variables such as concentration of cross-linker, cross-linking time and cross-linking temperature. The microspheres showed drug entrapment up to 76.19% with a mean particle size range of 5.91-8.19 µm. The degree of cross-linking and water-soluble fraction were 8.27-59.33% and 12.29-81.23%, respectively. SEM confirmed smooth surface and spherical shape of the microspheres. FTIR and (13)C-NMR confirmed cross-linking of gelatin by genipin. No chemical change in encapsulated drug was observed by FTIR and TGA. DSC and XRD indicated the molecular dispersion of drug within microspheres. Optimized microspheres could prolong the drug release for more than 108 h with anomalous transport. Histopathology confirmed the biocompatibility of microspheres in the rat (Wistar) knee joint. After 96 h of i. a. injection, significant higher amount (42.56%) of administered drug in cross-linked microspheres was recovered than uncross-linked microspheres (8.27%) confirming better drug retention efficiency (p < 0.01). SN - 1029-2330 UR - https://www.unboundmedicine.com/medline/citation/23249324/Formulation_and_evaluation_of_flurbiprofen_loaded_genipin_cross_linked_gelatin_microspheres_for_intra_articular_delivery_ L2 - http://www.tandfonline.com/doi/full/10.3109/1061186X.2012.745549 DB - PRIME DP - Unbound Medicine ER -