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Chitosan based nanocarriers for indomethacin ocular delivery.
- Source :
-
Archives of pharmacal research [Arch Pharm Res] 2008 Aug; Vol. 31 (8), pp. 1040-9. Date of Electronic Publication: 2008 Sep 12. - Publication Year :
- 2008
-
Abstract
- Two different chitosan (CS) nanocarriers namely nanoparticles and nanoemulsion were developed to prolong Indomethacin (IM) precorneal residence time and to improve its ocular bioavailability the main limitations in its management of post-operative inflammation and intraocular irritation after cataract extraction. CS-nanoparticles were developed by modified ionic gelation of CS with tripolyphosphate while nanoemulsion was prepared by spontaneous emulsification technique. Transmission electron microscopy revealed regular well-identified spherical shape. The nanoparticles had a mean size of 280 nm, a zeta potential of + 17 mV and high loading efficiency of 84.8 % while the mean size of nanoemulsion was affected by the nature of the surfactant used and varies between 220-690 nm. In vitro release studies, performed under sink conditions, revealed small initial burst release during the first hour followed by slow gradual drug release of 76 and 86% from nanoparticles and nanoemulsion respectively during a 24 h period. In vivo studies and histopathological examination revealed that eyes of rabbits treated with nanoemulsion showed clearer healing of corneal chemical ulcer with moderate effective inhibition of polymorph nuclear leukocytic infiltration (PMNLs) compared with nanoparticles preparation. Moreover, following topical instillation of CS-nanoemulsion to rabbits, it was possible to achieve therapeutic concentration of IM in the cornea through out the duration of the study and fairly high IM level in inner ocular structure, aqueous humor. These levels were significantly higher than those obtained following instillation of IM solution. Therefore, CS nanocarriers developed in this study were able to contact intimately with the cornea providing slow gradual IM release with long-term drug level thereby increasing delivery to both external and internal ocular tissues.
- Subjects :
- Animals
Anti-Inflammatory Agents, Non-Steroidal pharmacology
Anti-Inflammatory Agents, Non-Steroidal therapeutic use
Aqueous Humor metabolism
Area Under Curve
Chemical Phenomena
Chemistry, Physical
Cornea metabolism
Drug Delivery Systems
Drug Stability
Emulsions
Excipients
Indomethacin pharmacokinetics
Indomethacin therapeutic use
Keratitis drug therapy
Keratitis pathology
Male
Microscopy, Electron, Transmission
Ophthalmic Solutions
Particle Size
Powders
Rabbits
Reference Standards
Solutions
Anti-Inflammatory Agents, Non-Steroidal administration & dosage
Chitosan chemistry
Indomethacin administration & dosage
Nanoparticles administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 0253-6269
- Volume :
- 31
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Archives of pharmacal research
- Publication Type :
- Academic Journal
- Accession number :
- 18787795
- Full Text :
- https://doi.org/10.1007/s12272-001-1266-6