Use of chitosan as pharmaceutical excipient in ocular drug delivery systems: Sterilization and pharmacokinetics

The use of chitosan as a pharmaceutical excipient in the ocular field is already established. Nevertheless, some aspects related to its ocular administration, such as sterilization and excipient's pharmacokinetics, remain unclear. So, in this study, we evaluated those two relevant aspects, rela...

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Bibliographic Details
Published in:Journal of biomedical materials research. Part B, Applied biomaterials Applied biomaterials, 2020-07, Vol.108 (5), p.2227-2237
Main Authors: Franca, Juçara R., Fuscaldi, Leonardo L., Ribeiro, Tatiana G., Foureaux, Giselle, Cesar, Aina L. A., Castilho, Rachel O., Cronemberger, Sebastião, Ferreira, Anderson J., Fernandes, Simone O. A., Cardoso, Valbert N., Faraco, André A. G.
Format: Article
Language:English
Subjects:
Animal models
Biomedical materials
Casting inserts
Chitosan
Degradation products
Drug delivery
Drug delivery systems
excipient
Eye
Growth media
Inoculation
Inserts
Materials research
Materials science
Medical imaging
ocular drug delivery
Pharmaceuticals
Pharmacokinetics
Pharmacology
Rodents
Sterilization
Technetium
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Summary:The use of chitosan as a pharmaceutical excipient in the ocular field is already established. Nevertheless, some aspects related to its ocular administration, such as sterilization and excipient's pharmacokinetics, remain unclear. So, in this study, we evaluated those two relevant aspects, related to chitosan administration in eye. We used chitosan‐based ocular inserts (CI) as formulation model. CI were produced by solvent/casting method and sterilized by saturated steam. Sterilization was confirmed by direct inoculation of inserts in suitable microbiological growth media. Physicochemical characterization of inserts before and after sterilization was performed. Results suggested that, although steam sterilization changed the arrangement of the matrix, the heat and the humidity did not modify the structure of the main polymeric chain. Pharmacokinetics of CI radiolabeled with technetium‐99m (99mTc) was assessed by scintigraphic images and ex vivo biodistribution study, after ocular administration in male Wistar rats. Scintigraphic and images analysis and ex vivo biodistribution study showed that the insert remained mainly in the eye until 6 hr after administration and its degradation products began to migrate to the abdominal cavity after 18 hr. Together, these data represent an important step forward the manufacturing and the clinical application of CI in the ophthalmic field.
ISSN:1552-4973
1552-4981
DOI:10.1002/jbm.b.34560