Particles incorporating surfactants for pulmonary drug delivery

Details Particles incorporating surfactants for pulmonary drug delivery Particles incorporating surfactants for pulmonary drug delivery

1997-01-16

1999-01-05

Kishore, Gollamudi S.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424499, 424501, 424502, 424 43, 424 45, 424 46, 424434, A61K 914, A61K 916

Patent

active

058559132

ABSTRACT:
Aerodynamically light particles incorporating a surfactant on the surface thereof for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of a biodegradable material and have a tap density less than 0.4 g/cm.sup.3 and a mass mean diameter between 5 .mu.m and 30 .mu.m. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of poly(lactic acid) or poly(glycolic acid) or copolymers thereof. Alternatively, the particles may be formed solely of the drug or diagnostic agent and a surfactant. Surfactants can be incorporated on the particle surface for example by coating the particle after particle formation, or by incorporating the surfactant in the material forming the particle prior to formation of the particle. Exemplary surfactants include phosphoglycerides such as L-.alpha.-phosphatidylcholine dipalmitoyl. The aerodynamically light particles incorporating a therapeutic or diagnostic agent and a surfactant may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide a variety of therapeutic agents.

REFERENCES:
patent: 4161516 (1979-07-01), Bell
patent: 4272398 (1981-06-01), Jaffe
patent: 4590206 (1986-05-01), Forrester et al.
patent: 4741872 (1988-05-01), De Luca et al.
patent: 4818542 (1989-04-01), De Luca et al.
patent: 4855144 (1989-08-01), Leong et al.
patent: 4857311 (1989-08-01), Domb et al.
patent: 4865789 (1989-09-01), Castro et al.
patent: 4904479 (1990-02-01), Illum
patent: 5069936 (1991-12-01), Yen
patent: 5160745 (1992-11-01), De Luca et al.
patent: 5169871 (1992-12-01), Hughes et al.
patent: 5384133 (1995-01-01), Boyes et al.
patent: 5456917 (1995-10-01), Wise et al.
patent: 5607695 (1997-03-01), Ek et al.
patent: 5612053 (1997-03-01), Baichwal
Adjei and Garren, "Pulmonary Delivery of Peptide Drugs: Effect of Particle Size on Bioavailability of Leuprolide Acetate in Healthy Male Volunteers," J. Pharm. Res.,7: 565-569 (1990).
Altschuler et al., "Aerosol deposition in the human respiratory tract," Am. Med. Assoc. Arch. Indust. Health 15:293-303 (1957).
Anderson et al., "Effect of Cystic Fibrosis on Inhaled Aerosol Boluses," Am. Rev. Respir. Dis., 140: 1317-1324 (1989).
Barrera et al., "Synthesis and RGD Peptide Modification of a New Biodegradable Copolymer: Poly(lactic acid-co-lysine)," J. Am. Chem. Soc., 115:11010 (1993).
Benita et al., "Characterization of drug-loaded poly(d,l-lactide) microspheres," J. Pharm. Sci. 73, 1721-1724 (1984).
Blackett and Buckton, "A Microcalorimetric Investigation of the Interaction of Surfactants with Crystalline and Partially Crystalline Salbutamol Sulphate in a Model Inhalation Aerosol System," Pharmaceutical Research 12(11):1689-1693 (1995).
**Brain, "Physiology and Pathophysiology of Pulmonary Macrophages," in The Reticuloendothelial System, Reichard and Filkins, Eds, Plenum Press, New York, pp. 315-327 (1985).
Byron, "Determinants of drug and polypeptide bioavailability from aerosols delivered to the lung," Adv. Drug. Del. Rev., 5: 107-132 (1990).
Clark and Egan, "Modeling the deposition of inhaled powdered drug aerosols," J. Aerosol Sci., 25:175-186 (1994).
Clay et al., "Effect of aerosol particle size on bronchodilation with nebulized terbutaline in asthmatic subjects," Thorax 41:364-368 (1986).
Cohen et al., "Controlled Delivery Systems for Proteins Based on Poly(Lactic/Glycolic Acid) Microspheres," Pharm. Res., 8(6): 713-720 (1991).
Colthorpe et al., "The Pharmacokinetics of Pulmonary-Delivered Insulin: A Comparison of Intratracheals and Aerosol Administration to the Rabbit," Pharm. Res. 9:764 (1992).
Daly et al., "The Preparation of N-Carboxyanhydrides of .alpha.-Amino Acids Using Bis(Trichloromethyl)Carbonate," Tetrahedron Lett., 29:5859 (1988).
Damms and Bains, "The Cost of Delivering Drugs without Needles,", J. Controlled Release, 8-11 (1996).
Davies et al., "Breathing of half-micron aerosols. I. Experimental.," J. Appl. Physiol. 32:591-600 (1972).
Dorries and Valberg, "Heterogeneity of phagocytosis for inhaled versus instilled material," Am. Rev. Resp. Disease, 146: 831-837 (1991).
**Doubrow, Ed., "Microcapsules and Nanoparticles in Medicine and Pharmacy," CRC Press, Boca Raton, 1992.
Eldridge et al., "Biodegradable microspheres as a vaccine delivery system," Mol. Immunol., 28: 287-294 (1991).
Findeisen, "Uber das Absetzen kleiner in der Luft suspendierter Teilchen in der menshlichen Lunge bei der Atmung," Pflugers Arch. D. Ges. Physiol. 236:367-379 (1935).
French, Edwards, and Niven, "The influence of formulation on emission, deaggregation and deposition of dry powders for inhalation," J. Aerosol Sci., 27: 769-783 (1996).
Ganderton, "The generation of respirable clouds from coarse powder aggregates," J. Biopharmaceutical Sciences, 3:101-105 (1992).
Edwards, "The macrotransport of aerosol particles in the lung: Aerosol depostion phenomena,"J. Aerosol Sci., 26:293-317 (1995).
Gehr et al., "Surfactant and inhaled particles in the conducting airways: Structural, stereological, and biophysical aspects," Microscopy Res. and Tech., 26: 423-436 (1993).
Gerrity et al., "Calculated deposition of inhaled particles in the airway generations of normal subjects," J. Appl. Phys., 47:867-873 (1979).
Gonda, "Aerosols for delivery of therapeutic and diagnostic agents to the respiratory tract," Critical Reviews in Therapeutic Drug Carrier Systems 6:273-313 (1990).
Gonda, "Preface. Major issues and future prospects in the delivery of therapeutic and diagnostic agents to the respiratory tract," Adv. Drug Del. Rev., 5: 1-9 (1990).
Gonda, "Physico-chemical principles in aerosol delivery," in Topics in Pharmaceutical Sciences 1991, Crommelin, D.J. and K.K. Midha, Eds., Medpharm Scientific Publishers, Stuttgart, pp. 95-117, 1992.
Gonda, "Targeting by deposition," in Pharmaceutical Inhalation Aerosol Technology (ed. A.J. Hickey), Marcel Dekkar Inc., New York, 1992.
Heyder et al., "Mathematical models of particle deposition in the human respiratory tract," J. Aerosol Sci., 17:811-825 (1984).
Heyder and Rudolf, "Mathematical models of particle deposition in the human respiratory tract," J. Aerosol Sci., 15:697-707 (1986).
Heyder et al., "Total Deposition of Aerosol Particles in the Human Respiratory Tract for Nose and Mouth Breathing," J. Aerosol Sci., 6:311-328 (1975).
Hickey et al., "Use of particle morhphology to influence the delivery of drugs from dry powder aerosols," J. Biopharmaceutical Sci., 2(1/2):107-113 (1992).
Hirano et al., "Pulmonary clearance and Toxicity of Zinc Oxide Instilled into the Rat Lung," Toxicology 63:336-342 (1989).
Illum, "Microspheres as a Potential Controlled Release Nasal Drug Delivery System," Delivery Systems for Peptide Drugs, NY: Plenum, 1986.
Johnson et al., "Delivery of Albuterol and Ipratropiumbromide from Two Nebulizer Systems in Chronic Stable Asthma," Chest, 96, 6-10, 1989.
Kassem and Ganderton, "The Influence of Carrier Surface on the Characteristics of Inspirable Powder Aerosols," J. Pharm. Pharmacol., 42:11 (1990).
Kawaguchi et al., "Phagocytosis of latex particles by leukocytes. I. Dependence of phagocytosis on the size and surface potential of particles," Biomaterials 7: 61-66 (1986).
Kobayashi et al., "Pulmonary Delivery of Salmon Calcitonin Dry Powders Containing Absorption Enhancers in Rats," Pharm. Res., 13(1): 80-83 (1996).
Komada et al., "Intratracheal Delivery of Peptide and Protein Agents: Absorption from Solution and Dry Powder by Rat Lung," J. Pharm. Sci. 83(6):863-867 (Jun., 1994).
Krenis and Strauss, "Effect of Size and Concentration of Latex Particles on Respiration of Human Blood Leucocytes," Proc. Soc. Exp. Med., 107:748-750 (1961).
Lai et al., "Sustained bronchodilation with isoproterenol poly(glycolide-co-lactide) microspheres," Pharm. Res., 10(1) 119-125 (1993).
Landahl, "On the removal of air-borne droplets by the human respiratory tract: I. The lung," Bull. Math. Biophys., 12:43-56 (1950).
Langer, "New Methods of Drug Delivery," Sci

Affiliated with

Also associated with

Rating

Particles incorporating surfactants for pulmonary drug delivery does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Particles incorporating surfactants for pulmonary drug delivery, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Particles incorporating surfactants for pulmonary drug delivery will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-859873