Effect of Lipid Composition of Liposomes on Biodisposition of Indomethacin in Arthritic Rats

Authors: Srinath P.1; Vyas S.P.2; Diwan P.V.1

Source: Pharmacy and Pharmacology Communications, Volume 5, Number 5, May 1999 , pp. 339-344(6)

Publisher: Pharmaceutical Press

Key:
Free Content - Free Content
New Content - New Content
Subscribed Content - Subscribed Content
Free Trial Content - Free Trial Content

Abstract:

A series of liposomes of indomethacin using various phospholipids (phosphatidyl choline (PC), phosphatidyl ethanolamine (PE), phosphatidyl glycerol (PG), stearylamine (SA) and cholesterol (CH)) was prepared. The effect of lipid composition on biodisposition of indomethacin was studied in arthritic rats.

The greatest encapsulation efficiency (32% ) was achieved with PCratioCHratioSA (1ratio0·5ratio0·1 molar ratio) liposomes. Inclusion of cholesterol did not increase encapsulation of indomethacin in the liposomes. As indomethacin is an acidic drug, inclusion of stearyl-amine, a cationic lipid, might have improved encapsulation because of electrostatic interactions.

The concentration of free indomethacin in blood, liver, spleen, kidney, brain and paw, after intravenous administration, was measured at various time points. Cmax in the liver was achieved 1 h after the administration of free drug but was delayed for up to 4 h with the encapsulated form. Localization in the liver was greatest with a PCratioCHratioPG (1ratio0·5ratio0·2 molar ratio) liposome formulation. Detectable concentrations of the drug in the inflammatory tissue were found for up to just 2 h with free indomethacin. With liposomal formulations detectable levels of the drug were observed even after 24 h and liposomes comprising PCratioCHratioPG (1ratio0·5ratio0·2) showed the greatest localization in the inflammatory tissue.

The results suggest that PCratioCHratioPG (1ratio0·5ratio0·2) is the optimum liposome composition for targeting arthritic joints.

Language: English

Document Type: Research article

Affiliations: 1: Pharmacology Division, Indian Institute of Chemical Technology, Hyderabad–500 007, diwan@iict.ap.nic.in 2: Department of Pharmaceutical Sciences, Dr H. S. Gour Vishwavidyalaya, Sagar – 470 003, India *

The full text electronic article is available for purchase. You will be able to download the full text electronic article after payment.

$38.49 plus tax      Refund Policy

 

OR

Back to top

Key:
Free Content - Free Content
New Content - New Content
Subscribed Content - Subscribed Content
Free Trial Content - Free Trial Content
Share this item with others: These icons link to social bookmarking sites where readers can share and discover new web pages.
Page Help Click here for Page Help
Shopping cart
Tools
Sign in






Need to register?
Sign up here
Text size: A | A | A | A