Liposome-encapsulated ciprofloxacin

A - Human Necessities – 61 – K

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A61K 31/495 (2006.01) A61K 9/127 (2006.01) A61K 47/28 (2006.01)

Patent

CA 2101241

Despite its potency and broad spectrum antibacterial activity, the therapeutic effectiveness of ciprofloxacin is limited in that it has a short elimination half-life and its potency against some bacteria may be compromised by the ability of some intracellular bacteria to reside and multiply within the human host cells where they are protected from the antibiotic. These problems can be solved by encapsulating the antibiotic within the microscopic lipid vesicles called liposomes, which protect the drug from dilution and elimination from the body. Moreover, the liposome-encapsulated antibiotic is naturally taken up by phagocytic cells which results in the delivery of the drug to intracellular sites of infection.

Malgré sa puissance et son activité anti-infectieuse à large spectre, l'efficacité thérapeutique de la ciprofloxacine est limitée en ce sens qu'elle a une courte demi-vie d'élimination et que sa puissance contre certaines bactéries peut être compromise par la capacité de bactéries intracellulaires qui résident et se multiplient à l'intérieur de cellules hôtes humaines, où elles sont protégées des antibiotiques. Ces problèmes peuvent être résolus par l'encapsulation de l'antibiotique à l'intérieur de vésicules lipidiques microscopiques, appelées liposomes, qui protègent le médicament contre une dilution et une élimination du corps. Cet antibiotique encapsulé est naturellement repris par des phagocytes, ce qui permet au médicament d'être acheminé vers les sites d'infection intracellulaires.

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