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Positively charged amphiphilic block copolymer as drug carrier and complex thereof with negatively charged drug

A technology of block copolymers and hydrophilic polymers, which is applied in the field of transporting anionic bioactive reagents and polymer micellar drug carriers, and can solve the problems of reducing drug stability and other issues

Inactive Publication Date: 2005-09-28
SAMYANG HLDG CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, since the charged blocks can include several functional groups with charges, when they are incorporated into the molecule by electrostatic binding to drugs with multiple ionic groups, such as peptides or proteins, they can reduce the stability

Method used

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  • Positively charged amphiphilic block copolymer as drug carrier and complex thereof with negatively charged drug
  • Positively charged amphiphilic block copolymer as drug carrier and complex thereof with negatively charged drug
  • Positively charged amphiphilic block copolymer as drug carrier and complex thereof with negatively charged drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0120] Example 1: Amino-containing (-O-C(=O)CHR 1 -NH 3 + Cl - ) Synthesis of methoxypolyethylene glycol-polylactide (mPEG-PLA-O-C(=O)CHR 1 -NH 3 + -Cl - )

[0121] The block copolymer prepared in Preparation 1 and having an -OH group at the chain end of the PLA (B above) block was reacted with an amino acid derivative having a protecting group on the amino group to obtain the title block copolymer.

[0122]

[0123] Dissolve 0.583 g of N-benzyloxycarbonyl-p-hydroxyphenylglycine, 0.575 g of dicyclohexylcarbodiimide (DCC) and 7.0 g of methoxypolyethylene glycol-polylactide (mPEG-PLA, 2000-1765) in 20ml DMF. The resulting solution was reacted at room temperature for 24 hours to obtain N-benzyloxycarbonyl-p-hydroxyphenylglycine methoxypolyethylene glycol-polylactide. Using palladium as a catalyst, the reaction product was hydrogenated to remove the protecting group on the amino group, dissolved in aqueous hydrochloric acid, dialyzed, and then lyophilized to obtain...

Embodiment 2-4

[0124] Embodiment 2-4: the introduction of amino acid group

[0125] In the same manner as in Example 1, each block copolymer prepared in Preparations 2-4 was reacted with an amino acid derivative having a protecting group on the amino group to obtain a copolymer containing an amino acid group. Table 2 below shows the amino acid group-containing block copolymers prepared in Examples 1-4.

[0126] Example

Embodiment 5

[0127] Embodiment 5: Contain aminoethanol (-O-CH 2 CH 2 N + R 3 -Cl - ) Synthesis of methoxypolyethylene glycol-polylactide (mPEG-PLA-O-C(=O)(CH 2 ) Z C(=O)-O-CH 2 CH 2 N + R 3 -Cl - )

[0128] The block copolymer prepared in Preparation 1 was reacted with the diacid chloride to give the carboxylic acid derivative, and then the reaction product was reacted with the 2-aminoethanol derivative to give the title block copolymer.

[0129]

[0130] (where z represents an integer from 0-6)

[0131] 7 g of methoxypolyethylene glycol-polylactide (mPEG-PLA, 2000-1765) and 5 g of excess succinyl dichloride were dissolved in chloroform, 1 ml of pyridine was added thereto, and the mixture was reacted at 60° C. for 12 Hour. The resulting solution was added to diethyl ether to precipitate a block copolymer. The precipitated block copolymer was dissolved in 10 ml of N-methylpyrrolidone, 0.363 g of ethanolamine hydrochloride was added thereto, and the mixture was reacted a...

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Abstract

The present invention provides a cationic group-containing amphiphilic block copolymer that is biocompatible and biodegradable, and when used as a drug carrier for an anionic drug, provides several advantages, such as increased blood concentration and improved stability of the drug.

Description

technical field [0001] The present invention relates to positively charged drug carriers which form complexes with negatively charged drugs. More specifically, the present invention relates to positively charged polymer micellar drug carriers comprising A-B block type copolymers, wherein A is a hydrophilic polymer block, and B is a hydrophobic biodegradable polymer block, and wherein one end of the hydrophobic polymer block (B) is covalently bonded to a cationic group. The positively charged biodegradable block copolymer of the present invention forms complexes with negatively charged drugs by means of electrostatic interactions. The cationic copolymers of the present invention are useful for drug delivery, and in particular for the delivery of anionic bioactive agents. Background of the invention [0002] Biodegradable polymers are attracting attention as drug delivery systems. R. Langer, New Methods of Drug delivery, 249 Science 1527-1533 (1990); B. Jeong et al., Biodeg...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K31/196A61K31/405A61K47/48A61P29/00C08G63/00C08G63/664C08G81/00C08G81/02
CPCC08G63/664C08G81/00C08G63/00A61K31/196A61K31/405A61K38/193A61K38/27A61K47/34A61K9/1075A61P29/00C08G81/02
Inventor 徐敏孝崔仁子曹永薰
Owner SAMYANG HLDG CORP
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