Cyclodextrin polymer compositions for use as drug carriers

a technology of cyclodextrin and polymer composition, which is applied in the field of cyclodextrin polymer composition for use as drug carriers, can solve the problems of limited disclosure or suggestion of any cyclodextrin, the pharmacokinetics of many antiviral and anti-cancer drugs and other active agents that penetrate cells are not easily controlled, and the drug carrying capacity is low

Inactive Publication Date: 2001-10-25
KOSAK KENNETH M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] In one embodiment, the water-soluble (or colloidal) cyclodextrin polymers of the instant invention overcome the problem of low carrying capacity of individual cyclodextrins. Also, by complete entrapment of the guest molecules, the problem of losing drug or other active agent by diffusion when diluted in vivo, is solved. In another embodiment, the invention also provides a means for controlled release of the entrapped drug in vivo, which was not possible in the prior art of cyclodextrins.

Problems solved by technology

The pharmacokinetics of many anti-viral and anti-cancer drugs and other active agents that penetrate cells are not easily controlled.
However, because cyclodextrin polymers of the prior art lack any specific release mechanism, many of the advantages of cyclodextrins are limited.
However, Weinshenker makes no disclosures or suggestions for any cyclodextrin polymers and they cannot be made with the synthesis methods disclosed.
Review articles on the pharmaceutical applications of cyclodextrins have identified many problems due to the high turnover rate between inclusion complex formation and dissociation.
They reported on page 1145 that "any attempt to dilute the samples resulted in erratic precipitation" due to competitive displacement factors found in plasma.
Because of these problems, cyclodextrins in the prior art are used for solubilizing and stabilizing certain drugs before or during administration but are not suitable for carrying and delivering drugs in the bloodstream.

Method used

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  • Cyclodextrin polymer compositions for use as drug carriers
  • Cyclodextrin polymer compositions for use as drug carriers
  • Cyclodextrin polymer compositions for use as drug carriers

Examples

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preparation ii

Cyclodextrin Polymer Carrier with Completely Entrapped 2AA

[0215] The purpose is to prepare a water-soluble (or colloidal) cyclodextrin polymer carrier with completely entrapped 2-aminoanthracene (2AA). The procedure was to combine 0.5 ml of 4.4% beta cyclodextrin in water, with 0.02 ml of solution containing 80% 1,4 butanediol diglycidyl ether (BDE), 10% of 0.1 M guest molecule, 2-aminoanthracene in dimethylformamide, and 2.4% 2 N NaOH while mixing vigorously and incubating at 60.degree. C.

[0216] After about 1 hour, 0.2 ml of 0.01 M K.sub.2HPO.sub.4 (K2 buffer, pH 8.6), and 0.02 ml more of BDE was added and mixed to continue the crosslinking. After about one half hour more, the mixture was mixed with 0.1 ml of 1M lysine for about 2.5 hours more. The preparation was then centrifuged for 8 minutes at 2500 rpm and 0.55 ml of supernatant was fractionated on a column of Sephadex.RTM. G-25 (14.times.0.8 cm) equilibrated with K2 buffer.

[0217] The 0.5 ml fractions were then collected and ex...

preparation xiv

Cyclodextrin Catalyst Agent

[0338] A cyclodextrin catalyst agent is a new invention defined herein as a cyclodextrin derivative of an individual cyclodextrin, or dimer, trimer or polymer, wherein the CD derivative host functions as an "artificial enzyme", and certain guest molecules function as chemical substrates. When the chemical substrate comes in contact with the cyclodextrin catalyst agent under appropriate conditions, it is modified to produce a product that is inhibitory or toxic to certain cells, microbes or parasites. In one embodiment, the CD catalyst agent is coupled to a biorecognition molecule for targeting specific infected cells, cancer cells, tissues or disease organisms.

[0339] With suitable derivatization, the CD catalyst agents can be synthesized to bind and modify prodrugs into active drugs and modify other specific substrates. The CD catalyst agent can also catalyze specific reactions such as generate free radicals, including singlet or triplet oxygen that direct...

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Abstract

This invention discloses compositions of cyclodextrin polymers for carrying drugs and other active agents. Compositions are also disclosed of cyclodextrin polymer carriers that release drugs under controlled conditions. The invention also discloses compositions of cyclodextrin polymer carriers that are coupled to biorecognition molecules for targeting the delivery of drugs to their site of action. The advantages of the water-soluble cyclodextrin polymer carrier are: (1) Drugs can be used based on efficacy without solubility or conjugation requirements. (2) Drugs can be delivered as macromolecules and released within the cell. (3) Drugs can be targeted by coupling the carrier to biorecognition molecules. (4) Synthesis methods are independent of the drug to facilitate multiple drug therapies.

Description

RELATED PATENT APPLICATIONS[0001] This is a continuation-in-part of PCT / US99 / 30820, filed Dec. 27, 1999, which is a continuation-in-part of U.S. patent application Ser. No. 09 / 223,055, filed Dec. 30, 1998, now U.S. Pat. No. 6,048,736, issued Apr. 11, 2000. The contents of those applications are incorporated herein.[0002] This invention discloses methods for preparing compositions of cyclodextrin polymers for carrying drugs and other active agents for therapeutic, medical or other uses. Methods are also disclosed for preparing cyclodextrin polymer carriers that release drugs and other active agents under controlled conditions. The invention also discloses methods for preparing compositions of cyclodextrin polymer carriers that are coupled to biorecognition molecules for targeting the delivery of drugs and other active agents to their site of action.DESCRIPTION OF THE PRIOR ART[0003] The pharmacokinetics of many anti-viral and anti-cancer drugs and other active agents that penetrate c...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/51A61K47/48C08B37/16
CPCA61K9/1075A61K9/5161A61K9/5192A61K47/48969B82Y5/00C08B37/0012A61K47/6951
Inventor KOSAK, KENNETH M.
Owner KOSAK KENNETH M
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