Prostaglandin-lipid formulations

Details Prostaglandin-lipid formulations Prostaglandin-lipid formulations

1992-01-16

1993-11-16

Bell, Mark L.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

4284022, 436829, 264 43, 264 46, A61K 3722

Patent

active

052621685

ABSTRACT:
A liposome composition and methods for making same are disclosed, such compositions comprise an arachidonic acid metabolite such as a prostaglandin, preferably prostaglandin E.sub.1, a lipid, and a drying protectant such as a saccharide. The liposomes may be loaded with prostaglandin passively, or using a transmembrane concentration gradient, preferably using a transmembrane pH gradient. Using this transmembrane loading technique, trapping efficiencies of 50% to 100% are achieved, and the release rate of the prostaglandin from the liposomes is reduced. The liposome size is maintained after lyophilization and reconstitution.

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Moncada et al., "Prostaglandins, Prostacyclin, and Thromboxane A.sub.2 " The Pharmacol Basis of Therapeutics, MacMillan Pub., Inc., N.Y. pp. 668-676 no date.
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Hoshi et al., "Prostaglandin E, Incorporated in Lipid Microspheres in the Treatment of Peripheral Vascular Diseases and Diabetic Neuropathy" 1986; Drugs Exptl. Clin. Res. XII(8):681.
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