+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Efficacies of cyclodextrin-complexed and liposome-encapsulated clarithromycin against Mycobacterium avium complex infection in human macrophages



Efficacies of cyclodextrin-complexed and liposome-encapsulated clarithromycin against Mycobacterium avium complex infection in human macrophages



International Journal of Pharmaceutics (Kidlington) 250(2): 403-414, 16 January



Cyclodextrins and liposomes have been used in recent years as drug delivery vehicles, improving the bioavailability and therapeutic efficacy of many poorly water-soluble drugs. In this study, we used two approaches to enhance the availability of the poorly water-soluble antibiotic, clarithromycin, by inclusion complex formation and by liposome-encapsulation. We examined the efficacies of these formulations against Mycobacterium avium complex (MAC) in human peripheral blood monocyte-derived macrophages. The water solubility of clarithromycin was enhanced by about 700-fold by complexation with cyclodextrin. The use of a rapid radiometric (BACTEC) method for the detection of MAC growth and susceptibility showed identical MICs against MAC for both the free and complexed drug. The anti-MAC efficacy of the cyclodextrin complex of clarithromycin in macrophages was slightly lower than the free drug, probably due to the high stability of the inclusion complex. At higher drug concentrations, Liposome-encapsulated clarithromycin was slightly more effective against intracellular MAC growth than the free drug.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 010568858

Download citation: RISBibTeXText

PMID: 12527166

DOI: 10.1016/s0378-5173(02)00552-5


Related references

Efficacies of liposome-encapsulated clarithromycin and ofloxacin against Mycobacterium avium-M. intracellulare complex in human macrophages. Antimicrobial Agents and ChemoTherapy 38(3): 523-527, 1994

Efficacies of liposome-encapsulated streptomycin and ciprofloxacin against Mycobacterium avium and Mycobacterium intracellulare complex infections in human peripheral blood monocyte/macrophages. Antimicrobial Agents & Chemotherapy 36(12): 2808-2815, 1992

Efficacies of liposome-encapsulated streptomycin and ciprofloxacin against Mycobacterium avium-M. intracellulare complex infections in human peripheral blood monocyte/macrophages. Antimicrobial Agents and ChemoTherapy 36(12): 2808-2815, 1992

Activities of liposome-encapsulated azithromycin and rifabutin compared with that of clarithromycin against Mycobacterium avium-intracellulare complex in human macrophages. International Journal Of Antimicrobial Agents. 4(4): 281-289, 1994

Liposome-Encapsulated Sparfloxacin, Paromomycin, Ciprofloxacin and Clarithromycin for the Therapy of Mycobacterium avium Complex and Mycobacterium tuberculosis in macrophages. Abstracts of the Interscience Conference on Antimicrobial Agents & Chemotherapy 35(0): 86, 1995

Activation with cytokines and infection with Mycobacterium avium complex influence the uptake of clarithromycin by human macrophages. Program & Abstracts of the Interscience Conference on Antimicrobial Agents & Chemotherapy 33(0): 175, 1993

Activity of free and liposome encapsulated streptomycin against Mycobacterium avium complex (MAC) inside peritoneal macrophages. Journal of Antimicrobial ChemoTherapy 28(4): 615-617, 1991

Enhanced effect of liposome encapsulated amikacin on mycobacterium avium and mycobacterium intracellulare complex infection in beige mice. Antimicrobial Agents & Chemotherapy 32(9): 1404-1411, 1988

Comparative mycobactericidal action of free and liposome encapsulated amikacin on mycobacterium avium complex mac in peritoneal macrophages. Abstracts of the Annual Meeting of the American Society for Microbiology 88: 142, 1988

Activities of WIN-57273, minocycline, clarithromycin, and 14-hydroxy-clarithromycin against Mycobacterium avium complex in human macrophages. Antimicrobial Agents and ChemoTherapy 36(10): 2104-2107, 1992

Differential effects of free and liposome encapsulated amikacin on the survival of Mycobacterium avium complex in mouse peritoneal macrophages. Tubercle 71(3): 215-217, 1990

Liposome-encapsulated-gentamicin therapy of Mycobacterium avium complex infection in beige mice. Antimicrobial Agents and ChemoTherapy 34(6): 967-970, 1990