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Method for preparing polymeric micelle containing anionic drug

A technology for anionic drugs and cationic compounds, applied in the directions of drug delivery, pharmaceutical formulations, capsule delivery, etc., can solve problems such as unsuitable delivery, and achieve the effects of increasing stability, easy production, and increasing yield

Active Publication Date: 2018-08-03
SAMYANG HLDG CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although these amphiphilic block copolymers can dissolve hydrophobic and poorly water-soluble drugs in them by forming hydrophobic polymer micelles, negatively charged hydrophilic drugs such as nucleic acids cannot Is embedded in the micellar structure of the polymer, so it is not suitable for the delivery of anionic drugs containing these nucleic acids

Method used

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  • Method for preparing polymeric micelle containing anionic drug
  • Method for preparing polymeric micelle containing anionic drug
  • Method for preparing polymeric micelle containing anionic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-2

[0121] Example 1-2. Preparation of a composition containing siRNA / 1,6-dioTETA / mPEG-PLA-tocopherol (2k-1.7k) / PLANa (1.7k) (preparation of preparation in aqueous phase)

[0122] Dissolve 126 μg of dioTETA in 252 μl of distilled water and place in an ultrasonic cleaner for 10 min to reduce particle size. 5 μg siRNA was dissolved in 4 μl distilled water, and 1 mg mPEG-PLA-tocopherol (2k-1.7k) and 500 μg PLANa (1.7k) were dissolved in 10 μl and 2 μl distilled water, respectively. First siRNA and 1,6-dioTETA were mixed, then mPEG-PLA-tocopherol and PLANa were mixed. Add distilled water to make the volume ratio 1:1. The mixture of siRNA and 1,6-dioTETA and the mixture of mPEG-PLA-tocopherol and PLANa were mixed dropwise under sonication. After holding at 4 °C for 10 min to stabilize the formulation, the mixture was filtered through a 0.45 μm hydrophilic PVDF filter to remove large particles. (Example 1)

Embodiment 1

[0123] In Example 2, according to the method in Example 1, a composition was prepared with 500 μg mPEG-PLA-tocopherol (2k-1.7k) and 100 μg PLANa (1.7k).

[0124] Table 2

[0125]

Embodiment 3

[0126] Example 3. Preparation of compositions containing siRNA / 1,6-dioTETA / mPEG-PLA-tocopherol (2k-1.7k) / PLANa (1.7k) (formation of siRNA / dioTETA nanoparticles in aqueous phase and encapsulation thereof Preparation method in polymer micelles embedded in emulsion)

[0127] 5 μg siRNA was dissolved in 4 μl distilled water, 126 μg dioTETA was dissolved in 126 μl distilled water, and then mixed dropwise under sonication. The mixture was freeze-dried to a powder state, and the powder was dissolved in a solution of 300 µg of PLANa dissolved in 50 µl of ethyl acetate. A solution formed by dissolving 1 mg of mPEG-PLA-tocopherol (2k-1.7k) in 100 μl of distilled water was added dropwise to the mixture of siRNA, dioTETA and PLANa to prepare an emulsion using an ultrasonic generator. The prepared emulsion was placed in a single-necked round-bottomed flask, and was distilled under reduced pressure using a rotary evaporator to selectively remove ethyl acetate to prepare siRNA / 1,6-dioleoylt...

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Abstract

The present invention relates to a preparation method comprising the steps of: producing nanoparticles in an aqueous phase using electrostatic bonding between an anionic drug and a cationic compound,and incorporating the nanoparticles into a polymeric micelle consisting of an amphiphilic polymer and any polylactic acid salt, to thereby increase the yield for preparing a composition for deliveringan anionic drug by raising the anionic drug inclusion rate of the formulation though the increase of electrostatic bonding and hydrophobic bonding.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing anionic drugs for delivering anionic drugs and a preparation method thereof. Background technique [0002] Many diseases arise when the expression of disease-related genes increases due to various factors or exhibits abnormal activity due to mutations. siRNA (short interfering RNA) inhibits the expression of a specific gene in a sequence-specific manner at the post-transcriptional stage, and thus has gained much attention as a gene therapy agent. In particular, due to its high activity and precise gene selectivity, siRNA is expected to be useful as a nucleic acid therapeutic agent capable of solving the problems that existing antisense nucleotides, ribozymes, etc. have. siRNA is a short double-stranded RNA that cleaves the mRNA of a gene having a nucleotide sequence complementary thereto to inhibit the expression of a target gene (McManus and Sharp, Nature Rev. Genet. 3:737 (2002); Elbas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/7088A61K47/14A61K47/30A61K9/00
CPCA61K31/7088A61K9/141A61K9/146A61K9/5115A61K9/5146A61K9/5192A61K9/19A61K9/0019A61K9/1075A61K47/14A61K47/30
Inventor 南惠英金详熹徐敏孝孙智娟
Owner SAMYANG HLDG CORP