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Genipin-crosslinked gelatin microspheres as a drug carrier for intramuscular administration: in vitro and in vivo studies.
J Biomed Mater Res A 2003; 65(2):271-82JB

Abstract

Gelatin microspheres have been widely evaluated as a drug carrier. Nevertheless, gelatin dissolves rather rapidly in aqueous environments, making the use of the polymer difficult for the production of long-term delivery systems. This adverse aspect requires the use of a crosslinking agent in forming nonsoluble networks in microspheres. However, the use of crosslinking agents such as formaldehyde and glutaraldehyde can lead to toxic side effects owing to residual crosslinkers. In an attempt to overcome this problem, a naturally occurring crosslinking agent (genipin) was used to crosslink gelatin microspheres as a biodegradable drug-delivery system for intramuscular administration. Glutaraldehyde was used as a control. In the in vitro study, the morphology, dynamic swelling, and antienzymatic degradation of test microspheres were evaluated. In the in vivo study, the biocompatibility and degradability of test microspheres were implanted in the skeletal muscle of a rat model via intramuscular injection. The results obtained in the study suggested that crosslinking of gelatin microspheres with glutaraldehyde or genipin may produce distinct crosslinking structures. The water transport mechanism in both the glutaraldehyde- and genipin-crosslinked gelatin microspheres exhibit anomalous behavior ranging from Fickian to Case-II extremes. The increase of the swelling diameter for the genipin-crosslinked microspheres was significantly less than that observed for the glutaraldehyde-crosslinked microspheres. In the animal study, it was found that the degree in inflammatory reaction for tissues implanted with the genipin-crosslinked microspheres was significantly less than that implanted with the glutaraldehyde-crosslinked microspheres. Additionally, the degradation rate of the genipin-crosslinked microspheres was significantly slower than their glutaraldehyde-crosslinked counterparts. These results indicated that the genipin-crosslinked gelatin microspheres may be used as a long-acting drug carrier for intramuscular administration.

Authors+Show Affiliations

Department of Chemical Engineering, National Tsing Hua University, Hsinchu, Taiwan 300, ROC.No 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

12734822

Citation

Liang, Huang-Chien, et al. "Genipin-crosslinked Gelatin Microspheres as a Drug Carrier for Intramuscular Administration: in Vitro and in Vivo Studies." Journal of Biomedical Materials Research. Part A, vol. 65, no. 2, 2003, pp. 271-82.
Liang HC, Chang WH, Lin KJ, et al. Genipin-crosslinked gelatin microspheres as a drug carrier for intramuscular administration: in vitro and in vivo studies. J Biomed Mater Res A. 2003;65(2):271-82.
Liang, H. C., Chang, W. H., Lin, K. J., & Sung, H. W. (2003). Genipin-crosslinked gelatin microspheres as a drug carrier for intramuscular administration: in vitro and in vivo studies. Journal of Biomedical Materials Research. Part A, 65(2), pp. 271-82.
Liang HC, et al. Genipin-crosslinked Gelatin Microspheres as a Drug Carrier for Intramuscular Administration: in Vitro and in Vivo Studies. J Biomed Mater Res A. 2003 May 1;65(2):271-82. PubMed PMID: 12734822.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Genipin-crosslinked gelatin microspheres as a drug carrier for intramuscular administration: in vitro and in vivo studies. AU - Liang,Huang-Chien, AU - Chang,Wen-Hsiang, AU - Lin,Ko-Jung, AU - Sung,Hsing-Wen, PY - 2003/5/8/pubmed PY - 2003/10/4/medline PY - 2003/5/8/entrez SP - 271 EP - 82 JF - Journal of biomedical materials research. Part A JO - J Biomed Mater Res A VL - 65 IS - 2 N2 - Gelatin microspheres have been widely evaluated as a drug carrier. Nevertheless, gelatin dissolves rather rapidly in aqueous environments, making the use of the polymer difficult for the production of long-term delivery systems. This adverse aspect requires the use of a crosslinking agent in forming nonsoluble networks in microspheres. However, the use of crosslinking agents such as formaldehyde and glutaraldehyde can lead to toxic side effects owing to residual crosslinkers. In an attempt to overcome this problem, a naturally occurring crosslinking agent (genipin) was used to crosslink gelatin microspheres as a biodegradable drug-delivery system for intramuscular administration. Glutaraldehyde was used as a control. In the in vitro study, the morphology, dynamic swelling, and antienzymatic degradation of test microspheres were evaluated. In the in vivo study, the biocompatibility and degradability of test microspheres were implanted in the skeletal muscle of a rat model via intramuscular injection. The results obtained in the study suggested that crosslinking of gelatin microspheres with glutaraldehyde or genipin may produce distinct crosslinking structures. The water transport mechanism in both the glutaraldehyde- and genipin-crosslinked gelatin microspheres exhibit anomalous behavior ranging from Fickian to Case-II extremes. The increase of the swelling diameter for the genipin-crosslinked microspheres was significantly less than that observed for the glutaraldehyde-crosslinked microspheres. In the animal study, it was found that the degree in inflammatory reaction for tissues implanted with the genipin-crosslinked microspheres was significantly less than that implanted with the glutaraldehyde-crosslinked microspheres. Additionally, the degradation rate of the genipin-crosslinked microspheres was significantly slower than their glutaraldehyde-crosslinked counterparts. These results indicated that the genipin-crosslinked gelatin microspheres may be used as a long-acting drug carrier for intramuscular administration. SN - 1549-3296 UR - https://www.unboundmedicine.com/medline/citation/12734822/Genipin_crosslinked_gelatin_microspheres_as_a_drug_carrier_for_intramuscular_administration:_in_vitro_and_in_vivo_studies_ L2 - https://doi.org/10.1002/jbm.a.10476 DB - PRIME DP - Unbound Medicine ER -