US 9,808,509 B2Granted

Pharmaceutical compositions and methods for enhancing targeting of therapeutic compounds to the central nervous system

AssigneeHealthPartners Research Foundation

InventorsWilliam H. Frey, II, Leah Ranae Bresin Hanson, Shyeilla V. Dhuria

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Abstract

Pharmaceutical compositions and methods for enhancing targeting of therapeutic compounds to, inter alia, the CNS applied via intranasal administration while reducing non-target exposure are provided. In certain embodiments, at least one vasoconstrictor is provided intranasally prior to intranasal administration of at least one therapeutic compound. In other embodiments, the vasoconstrictor(s) and therapeutic compound(s) are combined in a pharmaceutical composition and delivered intranasally. The present invention substantially increases targeting of the therapeutic compound(s) to, inter alia, the CNS while substantially reducing unwanted and potentially harmful systemic exposure. The preferred administration of the invention applies the vasoconstrictor(s) and/or therapeutic compound(s) to the upper third of the nasal cavity, though application to the lower two-thirds of the nasal cavity is also within the scope of the invention.

Claims16

Dependent claims

A method for treating a disease or condition within a patient's brain, with increased targeting efficiency for at least one delivery target related to anatomical structures located in the rostral portion of the patient's brain compared to any delivery targets in the caudal portion of the patient's brain, and increased delivery of at least one therapeutic compound thereto compared with the caudal portion of the patient's brain, comprising:

providing at least an effective amount of at least one therapeutic compound capable of treating the disease or condition;
providing at least an effective amount of at least one vasoconstrictor;
administering the at least an effective amount of the at least one therapeutic compound to the upper third of the patient's nasal cavity;
administering the at least an effective amount of the at least one vasoconstrictor to the upper third of the patient's nasal cavity;
thereby increasing targeting efficiency of the administered amounts of the at least one therapeutic compound to the patient's olfactory epithelium and thereby enabling at least an effective amount of the at least one therapeutic compound to bypass the patient's blood-brain barrier;
delivering an effective amount of the at least one therapeutic compound to at least one target in the rostral portion of the patient's brain, with increased efficiency as compared with the delivery efficiency of the at least one therapeutic compound within the caudal portion of the patient's brain;
minimizing the amount of the at least one therapeutic compound absorbed into the patient's blood and/or peripheral tissues;
and
treating the patient's disease or condition.

6 more elements

A method for treating a disease or condition located within a patient's lymphatic system or meninges, with increased targeting efficiency for targets within the patient's lymphatics or meninges comprising:

providing at least an effective amount of at least one therapeutic compound capable of treating the disease or condition;
providing at least an effective amount of at least one vasoconstrictor;
administering the at least an effective amount of the at least one therapeutic compound to the upper third of the patient's nasal cavity;
administering the at least an effective amount of the at least one vasoconstrictor to the upper third of the patient's nasal cavity;
thereby increasing targeting and delivery efficiency of the administered amounts of the at least one therapeutic compound to the patient's olfactory epithelium and thereby enabling at least an effective amount of the at least one therapeutic compound to bypass the patient's blood-brain barrier;
delivering, with increased targeting and delivery efficiency, an effective amount of the at least one therapeutic compound to the patient's lymphatics or meninges as compared with an administration of the at least one therapeutic agent to the upper third of the patient's nasal cavity without administration of a vasoconstrictor;
minimizing the amount of the at least one therapeutic compound absorbed into the patient's blood and/or peripheral tissues;
and
treating the patient's disease or condition.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application: 12/134,385Filed 6 Jun 2008 · us provisional application
Priority: 8 Jun 2007
Published: US 2008/0305077 A111 Dec 2008
Granted: 7 Nov 2017
Term ends: Not estimatedThe source records don’t support an estimate.

Classification29 codes

A61K 38/2006
Interleukins [IL]: il-1
A61K 9/0043
Galenical forms characterised by the site of application: nose
A61K 31/16
Medicinal preparations containing organic active ingredients: amides, e.g. hydroxamic acids
A61K 33/24
Medicinal preparations containing inorganic active ingredients: heavy metals; Compounds thereof