Oral delivery systems for microparticles
First Claim
1. A complex for oral delivery of a substance to the circulation or lymphatic drainage system of a host, comprising the substance, a microparticle and a carrier, wherein:
- said substance is entrapped or encapsulated in said microparticle and therein is not deleteriously affected by intestinal digestive substances following oral administration of said complex to the host;
said microparticle is a microsphere or microcapsule having a diameter of 1 nanometer to 150 micrometers and is coupled to said carrier by covalent bond, hydrophobic interaction or both;
said carrier is Vitamin B12 or a Vitamin B12 -analogue that binds Castle'"'"'s intrinsic factor and said carrier is effective to transport said complex via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host, andsaid substance is released from said microparticle into the circulation or lymph after said complex is transported via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host.
3 Assignments
0 Petitions
Accused Products
Abstract
There are disclosed complexes and compositions for oral delivery of a substance or substances to the circulation or lymphatic drainage system of a host. The complexes of the invention comprise a microparticle coupled to at least one carrier, the carrier being capable of enabling the complex to be transported to the circulation or lymphatic drainage system via the mucosal epithelium of the host, and the microparticle entrapping or encapsulating, or being capable of entrapping or encapsulating, the substance(s). Examples of suitable carriers are mucosal binding proteins, bacterial adhesins, viral adhesins, toxin binding subunits, lectins, Vitamin B12 and analogues or derivatives of Vitamin B12 possessing binding activity to Castle'"'"'s intrinsic factor.
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Citations
15 Claims
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1. A complex for oral delivery of a substance to the circulation or lymphatic drainage system of a host, comprising the substance, a microparticle and a carrier, wherein:
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said substance is entrapped or encapsulated in said microparticle and therein is not deleteriously affected by intestinal digestive substances following oral administration of said complex to the host; said microparticle is a microsphere or microcapsule having a diameter of 1 nanometer to 150 micrometers and is coupled to said carrier by covalent bond, hydrophobic interaction or both; said carrier is Vitamin B12 or a Vitamin B12 -analogue that binds Castle'"'"'s intrinsic factor and said carrier is effective to transport said complex via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host, and said substance is released from said microparticle into the circulation or lymph after said complex is transported via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host. - View Dependent Claims (3, 5, 7, 8, 9, 10, 11, 12, 14, 15)
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2. A complex for oral delivery of a substance to the circulation or lymphatic drainage system of a host, comprising the substance, a microparticle and a carrier, wherein:
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said substance can be entrapped or encapsulated in said microparticle and therein is not deleteriously affected by intestinal digestive substances following oral administration of said complex to the host; said microparticle is a microsphere or microcapsule having a diameter of 1 nanometer to 150 micrometers and is coupled to said carrier by covalent bond, hydrophobic interaction or both; said carrier is Vitamin B12 or a Vitamin B12 -analogue that binds Castle'"'"'s intrinsic factor and said carrier can transport said complex via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host, and said microparticle can release said substance into the circulation or lymph after said complex is transported via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host. - View Dependent Claims (6, 13)
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4. A kit for preparing a complex for oral delivery of a substance to the circulation or lymphatic drainage system of a host, comprising:
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(A) at least one microparticle microsphere or microcapsule having a diameter of 1 nanometer to 150 micrometers; (B) a substance entrapped or encapsulated in said microparticle whereby said substance is not deleteriously affected by intestinal digestive substances when said complex is administered orally to a host and said substance is released from said microparticle into the circulation or lymph when said complex enters the circulation or lymphatic drainage system of the host; (C) at least one carrier Vitamin B12 or a Vitamin B12 -analogue molecule that binds Castle'"'"'s intrinsic factor and is effective to transport a complex via the intestinal mucosal epithelium into the circulation or lymphatic drainage system of the host; (D) one or more reagents to couple said microparticle to said carrier by covalent bond, hydrophobic interaction or both to form a complex, wherein said reagents can couple said microparticle to said carrier to form a complex which, upon oral administration, is transported via the intestinal mucosal epithelium into the circulation or lymphatic drainage system and releases said substance into the circulation or lymph of said host.
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Specification