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Cellular uptake of bioactive agents

a bioactive agent and cellular technology, applied in the field of can solve the problems of epithelial tissue atrophy, limited effectiveness further limited effect of amino acid supplementation, so as to increase the cellular uptake of bioactive agents, reduce the absolute solubility of bioactive agents, and increase the transport (absorption) of bioactive agents.

Inactive Publication Date: 2006-06-08
JOHNSON MATTHEY PLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention provides a way to increase the uptake of small molecules, such as bioactive compounds, into mammalian cells. This is done by combining a solution containing a bioactive compound and a carbohydrate that reduces the solubility of the compound in water. The solution can be administered in various ways, such as through toothpaste or chewing gum, and can be used to treat various physiological disorders involving damaged tissue. The invention also provides a pharmaceutical dosage composition and kits for easy preparation of the solution.

Problems solved by technology

Depletion of glutamine results in atrophy of epithelial tissue, with associated bacterial translocation.
The effectiveness of amino acid supplementation has been limited in some individuals due to aging or disease.
Effective supplementation with certain amino acids is further limited to varying degrees by the low aqueous solubility and limited cellular uptake of some amino acids.
Transport of small molecules into various cell types is controlled by alternate transport systems, making it more difficult to devise methods for increasing cellular uptake into particular cell types.

Method used

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  • Cellular uptake of bioactive agents
  • Cellular uptake of bioactive agents
  • Cellular uptake of bioactive agents

Examples

Experimental program
Comparison scheme
Effect test

example 1

Evaluation of Cellular Uptake of Glutamine in Combination With Sucrose and Sorbitol

[0062] 1. Materials and Methods

[0063] Distilled, deionized water (107 ml) was added to 207 grams of a mixture of sucrose, sorbitol, and glutamine with excipients (Aesgen-14) as listed in Table 1.

TABLE 1Aesgen-14 (AES-14)L-glutamine240.0Kg57.94 w %* 50.00% w / v**Sucrose144.0Kg34.77 w % 30.00% w / v Crystalline Sorbitol13.44Kg3.24 w %2.80% w / vGlycerin14.0Kg2.92 w %2.52% w / vSodium Phosphate2.6Kg0.63 w %0.54% w / vMonobasic (Anhydrous)Avicel Cellulose Gel874.0g0.18 w %0.17% w / vType CL-611Citric Acid (Anhydrous)280.0g0.07 w %0.06% w / vXanthan Gum230.0g0.05 w %0.04% w / vCarrageenan230.0g0.05 w %0.04% w / vArtificial Flavor230.0g0.05 w %0.04% w / vMethylparaben207.0g0.04 w %0.04% w / vPotassium Sorbate Powder180.0g0.04 w %0.04% w / v30% Simethicone Emulsion115.0g0.02 w %0.02% w / v

*Weight percents are expressed as percent of total weight of dry ingredients for reconstitution with water in a 240 ml bottle.

**Weight / volum...

example 2

Effect of AES-14 on Drug Uptake and Permeability

[0072] The cellular uptake and permeability enhancing effect of a pharmaceutical vehicle on four model drugs (L-glutamine, L-asparagine, glycylsarcosine, acyclovir, along with half saturation L-glutamine) across Caco-2 cell monolayers were measured in this experiment. Uptake and permeability of each compound was measured in the apical-to-basolateral direction, with and without vehicle.

Methods

[0073] Materials. Two amino acids (L-glutamine, L-asparagine), a dipeptide (glycylsarcosine), and a therapeutic agent (and acyclovir) with low permeability were studied. Each compound was tritiated. 14C-mannitol was used as an evaluation of monolayer / cell integrity (i.e. as a low uptake / permeability marker).

[0074] Uptake and Permeability Assessments. Compound cellular uptake into and permeability across Caco-2 monolayers was measured. Caco-2 monolayers were grown using a recently developed, rapid culture system, that requires 4 days rather th...

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Abstract

Provided is a composition and a method for increasing cellular uptake of bioactive agents, particularly those compounds termed “small molecules” into the cells of mammalian tissue, such as the epithelial cells of the mucosa.

Description

RELATED APPLICATIONS [0001] This application continuation of U.S. patent application Ser. No. 10 / 796,261, filed Mar. 9, 2004, which is a divisional of U.S. patent application Ser. No. 09 / 993,465, filed Nov. 14, 2001, now U.S. Pat. No. 6,734,170, which is a continuation under 37 CFR §1.53(b) of PCT Application Serial No. PCT / US00 / 13260, filed May 15, 2000 and published as WO 00 / 69470 on Nov. 23, 2000, which claimed priority from provisional U.S. Patent Application No. 60 / 134,442, filed May 17, 1999, which applications and publications are incorporated herein by reference.BACKGROUND OF THE INVENTION [0002] Absorption of biomolecules, such as amino acids and proteins, is critical to cellular function. About 75 percent of the solids in the mammalian body are proteins, including enzymes, polypeptides such as cytokines, nucleoproteins, transport proteins, and structural proteins. The principal functional constituents of these proteins, amino acids, polypeptides and isolated amino acids, a...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/198A61K9/68C12N5/07A23L1/305A61K9/00A61K9/08A61K31/525A61K31/711A61K47/10A61K47/26A61K47/36A61P1/04A61P3/02A61P17/02A61P31/12C12N5/071
CPCA23L1/3051A61K9/0014A61K9/0095A61K31/197A61K31/198A61K47/26A23L33/175A61P1/02A61P1/04A61P17/02A61P29/00A61P3/02A61P31/12Y02A50/30
Inventor PETIT, ROBERT G. IISHINAL, EDWARD C.
Owner JOHNSON MATTHEY PLC
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