Compositions and methods for enhancing receptor-mediated cellular internalization
First Claim
1. A method for delivering an agent to cells at a site where uptake is desired comprising (a) administering to the cells at the site where uptake is desired a composition that includes a viscous material and the agent to be delivered, wherein the composition has an apparent viscosity between 10 and 2000 Poise and has approximately the same apparent viscosity, at a shear stress of between approximately 1 and 200 Pascal at a strain rate approximately that of endocytosis, as the cytosolic fluid of the cell to which the agent is to be delivered, and (b) administering an enhancer in an amount effective to enhance expression of or binding to receptors eliciting receptor-mediated endocytosis on the cells at the site where uptake is desired, wherein the enhancer and the agent to be delivered are the same or different compounds.
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Abstract
Compositions and methods for improving cellular internalization of one or more compounds are disclosed. The compositions include a compound to be delivered and a biocompatible viscous material, such as a hydrogel, lipogel, or highly viscous sol. The composition also include, or are administered in conjunction with, an enhancer in an amount effective to maximize expression of or binding to receptors and enhance RME of the compound into the cells. This leads to high transport rates of compounds to be delivered across cell membranes, facilitating more efficient delivery of drugs and diagnostic agents. Compositions are applied topically orally, nasally, vaginally, rectally, and ocularly. The enhancer is administered with the composition or separately, either systemically or preferably locally. The compound to be delivered can also be the enhancer.
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Citations
27 Claims
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1. A method for delivering an agent to cells at a site where uptake is desired comprising
(a) administering to the cells at the site where uptake is desired a composition that includes a viscous material and the agent to be delivered, wherein the composition has an apparent viscosity between 10 and 2000 Poise and has approximately the same apparent viscosity, at a shear stress of between approximately 1 and 200 Pascal at a strain rate approximately that of endocytosis, as the cytosolic fluid of the cell to which the agent is to be delivered, and (b) administering an enhancer in an amount effective to enhance expression of or binding to receptors eliciting receptor-mediated endocytosis on the cells at the site where uptake is desired, wherein the enhancer and the agent to be delivered are the same or different compounds.
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19. A composition for delivering an agent to cells at a site where uptake is desired comprising:
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a viscous fluid, the agent to be delivered, and an enhancer in an amount effective to enhance expression of or binding to receptors on the cells eliciting receptor-mediated endocytosis, thereby to enhance receptor mediated endocytosis of the agent into the cells, wherein the composition has an apparent viscosity between 10 and 2000 Poise and has approximately the same apparent viscosity, at a shear stress of between approximately 1 and 200 Pascal at a strain rate approximately that of endocytosis, as the cytosolic fluid of the cell to which the agent is to be delivered.
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26. A kit for delivering an agent to cells comprising:
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a first composition comprising a viscous fluid and the agent to be delivered, wherein the composition has an apparent viscosity between 10 and 2000 Poise and has approximately the same apparent viscosity, at a shear stress of between approximately 1 and 200 Pascal at a strain rate approximately that of endocytosis, as the cytosolic fluid of the cell to which the agent is to be delivered, and a second composition comprising an enhancer in an amount effective to enhance expression of receptors eliciting receptor-mediated endocytosis on the cells, thereby to enhance receptor mediated endocytosis of the agent into the cells.
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Specification