Potential of Cyclodextrin Complexation and Liposomes in Topical Delivery of Ketorolac: In Vitro and In Vivo Evaluation

The objective of this investigation was to evaluate the effect of delivery strategies such as cyclodextrin complexation and liposomes on the topical delivery of ketorolac acid (KTRA) and ketorolac tromethamine. Ketorolac acid–hydroxypropyl-β-cyclodextrin solid dispersions (KTRA-CD) were prepared by...

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Bibliographic Details
Published in:AAPS PharmSciTech 2008, Vol.9 (4), p.1165-1170
Main Authors: Nagarsenker, M. S., Amin, L., Date, Abhijit A.
Format: Article
Language:English
Subjects:
2-Hydroxypropyl-beta-cyclodextrin
Administration, Topical
Animals
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
beta-Cyclodextrins - chemistry
Biochemistry
Biological Availability
Biomedical and Life Sciences
Biomedicine
Biotechnology
Cricetinae
Drug Carriers
In Vitro Techniques
Ketorolac - administration & dosage
Ketorolac - chemistry
Ketorolac - pharmacokinetics
Liposomes
Pharmacology/Toxicology
Pharmacy
Research Article
Skin Absorption
Spectrophotometry, Ultraviolet
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Summary:The objective of this investigation was to evaluate the effect of delivery strategies such as cyclodextrin complexation and liposomes on the topical delivery of ketorolac acid (KTRA) and ketorolac tromethamine. Ketorolac acid–hydroxypropyl-β-cyclodextrin solid dispersions (KTRA-CD) were prepared by kneading method. The liposomes containing ketorolac tromethamine (KTRM) and KTRA-CD were prepared. The in vitro permeation of KTRM solution, KTRA solution, KTRA-CD, and liposomes containing KTRM or KTRA-CD through guinea pig skin was evaluated. The anti-inflammatory activity of the topically applied KTRA-CD gel (containing 1% w/w KTRA) was compared to that of orally delivered KTRM solution. The KTRA-CD demonstrated significantly higher transdermal transport of ketorolac as compared to all other systems whereas liposomes significantly reduced the transport of ketorolac. The anti-inflammatory activity of the topically applied KTRA-CD gel was similar to that of the orally administered KTRM. Thus, cyclodextrin complexation enabled effective transdermal delivery of the ketorolac.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-008-9157-2