Phospholipid-based powders for drug delivery
OwnerJeffry G. Weers, Thomas E. Tarara +3inventors
InventorsJeffry G. Weers, Thomas E. Tarara, Luis A. Dellamary, Jean G. Riess, Ernest G. Schutt
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Abstract
Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.
Claims80
A particulate composition for delivery to the pulmonary system, the composition comprising:
- particles comprising an active agent, a saturated phospholipid and a polyvalent cation, wherein the molar ratio of polyvalent cation to phospholipid is at least 0.05 and is sufficiently high to increase the gel-to-liquid crystal transition temperature of the particles compared to particles without the polyvalent cation such that the particles have a gel-to-liquid crystal transition temperature that is greater than room temperature by at least 20° C.
A particulate composition comprising:
- particles comprising an active agent, a saturated phospholipid and a polyvalent cation, wherein the molar ratio of polyvalent cation to phospholipid is at least 0.05 and wherein the particles have a gel-to-liquid transition temperature at least 20° C. higher than room temperature.
A particulate composition for delivery to the pulmonary system, the composition comprising porous particles comprising:
- 20-99.9% of a saturated phospholipid;
- a polyvalent cation;
- and
- 0.1-80% active agent;
- wherein the molar ratio of polyvalent cation to phospholipid is at least 0.05 and is sufficiently high to increase the gel-to-liquid crystal transition temperature of the particles compared to particles without the polyvalent cation such that the particles have a gel-to-liquid crystal transition temperature that is greater than room temperature by at least 20° C.
A method of delivering an active agent to a patient in need thereof, the method comprising:
- administering to the respiratory tract of the patient an effective amount of particles comprising an active agent, a saturated phospholipid and a polyvalent cation, wherein the molar ratio of polyvalent cation to phospholipid is at least 0.05 and is sufficiently high to increase the gel-to-liquid crystal transition temperature of the particles compared to particles without the polyvalent cation such that the particles have a gel-to-liquid crystal transition temperature that is greater than room temperature by at least 20° C.
A particulate composition comprising:
- particles comprising a structural matrix comprising a saturated phospholipid and a polyvalent cation, wherein the molar ratio of polyvalent cation to phospholipid is at least 0.05 and is sufficiently high to increase the gel-to-liquid crystal transition temperature of the particles compared to particles without the polyvalent cation such that the particles have a gel-to-liquid crystal transition temperature that is greater than room temperature by at least 20° C., and wherein the particles further comprise an active agent.
A particulate composition for delivery to the pulmonary system, the composition comprising:
- particles comprising an active agent, a saturated phospholipid and a polyvalent cation, wherein the molar ratio of polyvalent cation to phospholipid is at least 0.05 and less than 2, whereby the gel-to-liquid crystal transition temperature of the particles is higher than particles without the polyvalent cation, and is greater than room temperature by at least 20° C.
A method of making a temperature stable particulate composition for delivery to the pulmonary system, the method comprising:
- (a) forming a feedstock comprising a saturated phospholipid emulsion and an active agent;
- (b) adding a polyvalent cation to the feedstock in an amount sufficient to provide a molar ratio of polyvalent cation to phospholipid in the feedstock that is at least 0.05 and less than 2;
- and
- (c) drying the polyvalent cation containing feedstock to form porous particles having a gel-to-liquid crystal transition temperature that is higher than a storage room temperature of the porous particles by at least about 20° C.
Dependencies are inferred from the claim text.