Potential of cyclodextrin complexation and liposomes in topical delivery of ketorolac: in vitro and in vivo evaluation.

M S Nagarsenker, L Amin, Abhijit A Date
Author Information
  1. M S Nagarsenker: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai 400098, India. mangal_nag511@yahoo.co.in

Abstract

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-beta-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.

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MeSH Term

2-Hydroxypropyl-beta-cyclodextrin
Administration, Topical
Animals
Anti-Inflammatory Agents, Non-Steroidal
Biological Availability
Cricetinae
Drug Carriers
In Vitro Techniques
Ketorolac
Liposomes
Skin Absorption
Spectrophotometry, Ultraviolet
beta-Cyclodextrins

Chemicals

Anti-Inflammatory Agents, Non-Steroidal
Drug Carriers
Liposomes
beta-Cyclodextrins
2-Hydroxypropyl-beta-cyclodextrin
Ketorolac

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