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Thermo sensitive in situ gel loaded with drug by chemical bonds, and preparation method thereof

An in-situ gel, drug-loading technology, applied in the field of drug-containing polymer gels, can solve the problems of difficult industrialization, harsh preparation conditions, and high production costs, achieve slow and long-lasting drug release, increase drug loading, and prepare simple craftsmanship

Inactive Publication Date: 2012-12-12
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these polymer nanoparticles also have disadvantages, such as targeting, being quickly eliminated from the body with blood circulation, and low drug availability.
Differences in drug types, different application requirements, and limitations in the structure and properties of polyphosphazene make it impossible for a single polyphosphazene-PEG bonded drug in-situ gel system to meet the needs of multiple drug prodrugs. Moreover, polyphosphazene is expensive, the preparation conditions are harsh, the production cost is too high, and it is difficult to industrialize

Method used

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  • Thermo sensitive in situ gel loaded with drug by chemical bonds, and preparation method thereof
  • Thermo sensitive in situ gel loaded with drug by chemical bonds, and preparation method thereof
  • Thermo sensitive in situ gel loaded with drug by chemical bonds, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Polymer and drug ester bond connection:

[0027] Add 1.5g dihydroxy PEG (number average molecular weight 1500Da), 2mLε-caprolactone, 117μl stannous octoate (Sn(Oct) 2 ), evacuated and filled with nitrogen. The reaction was terminated after 6h at 140°C. Dissolve with dichloromethane, precipitate with ether, and obtain polycaprolactone (PCL)-PEG-PCL by vacuum filtration. Put 3.5 g of PCL-PEG-PCL and 0.22 g of succinic anhydride into a dry flask, and evacuate nitrogen. The reactant was reacted at 140° C. for 5 hours, then cooled to room temperature, dissolved in dichloromethane, precipitated with ether, and vacuum filtered to obtain COOH-PCL-PEG-PCL-COOH. Then add 0.35g COOH-PCL-PEG-PCL-COOH, 0.17g paclitaxel (PTX) and 82.52mg dicyclohexylcarbodiimide (DCC) into the dry reaction tube, and then dissolve dimethylformamide (DMF). 48.87 mg of 4-dimethylaminopyridine (DMAP) was added. Vacuum and fill with nitrogen. React at room temperature for 24h. The reaction solution was...

Embodiment 2- Embodiment 13

[0029] According to the method of Example 1, the composition and type of polyethylene glycol, polyester, and drugs were changed to obtain a variety of PEG-polyesters (I-2 to I-13) with different C / BAB / C type bonded drugs and their The specific parameters of the temperature-sensitive in-situ gel are shown in Table 1.

[0030] Table 1 C / B-A-B / C type (ester bond) drug-bonded PEG-polyester block copolymer and its temperature-sensitive in-situ gel

[0031]

[0032]

[0033] M PEG :The number average relative molecular mass of PEG; M PE : Number average relative molecular mass of polyester; N: molar ratio of drug to polyester block; W ABC : Mass ratio of hydrophobic block / hydrophilic block (hydrophobic drug content is included in the mass of the hydrophobic block, and hydrophilic drug content is included in the mass of the hydrophilic block); C gel :The PEG-polyester content of the bonded drug in the in-situ gel system; T gel : Gelation temperature region; PTX: paclitaxel; docetaxe...

Embodiment 14

[0035] Example 14 (II-1)

[0036] Add 1.0g polyethylene glycol monomethyl ether (mPEG) (number average molecular weight 750Da), 3.2mLε-caprolactone, 100μl stannous octoate (Sn(Oct) 2 ), evacuated and filled with nitrogen. The reaction was terminated after 6h at 140°C. It was dissolved in dichloromethane, precipitated with ether, and filtered under vacuum to obtain mPEG-PCL. Put 3.15g mPEG-PCL and 0.11g succinic anhydride into a dry flask, evacuated and ventilated nitrogen. The reactants were reacted at 140°C for 5 hours, then cooled to room temperature, dissolved in dichloromethane, precipitated with ether, and vacuum filtered to obtain mPEG-PCL-COOH. Then add 0.32g mPEG-PCL-COOH, 0.17g paclitaxel (PTX) and 82.52mg dicyclohexylcarbodiimide (DCC), dimethylformamide (DMF) to dissolve in the dry reaction tube, and finally add 48.87mg4 -Dimethylaminopyridine (DMAP). Vacuum and fill with nitrogen. React at room temperature for 24h. The reaction solution was dialyzed in DMF for 2...

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Abstract

The present invention discloses a thermo sensitive in situ gel loaded with a drug by chemical bonds, and a preparation method thereof. The gel is formed by dispersing a drug-bonded polyethylene glycol-polyester block copolymer in a water system, wherein the block copolymer is a C / B-A-B / C copolymer, an A-B / C copolymer, a C / A-B copolymer or a C / A-B / C copolymer, and is formed by a hydrophilic polyethylene glycol block A, a polyester block B, and a drug C. The preparation process comprises that: under a catalytic effect of tin octoate, the polyethylene glycol is adopted as an initiator to carry out a ring-opening polymerization reaction to obtain polyethylene glycol-polyester; a terminal group modification treatment is performed for the polyethylene glycol-polyester; the drug C is bonded to the polyethylene glycol-polyester by the chemical bonds; the drug-bonded polyethylene glycol-polyester copolymer is prepared into lyophilized powder; the lyophilized powder is dispersed in a water media, and the dispersion is transformed into the stagnant in situ gel when the mass concentration of the dispersion is 10-50% and the temperature is 25-60 DEG C. The preparation process of the gel of thepresent invention is simple, and the prepared drug-loaded thermo sensitive in situ gel has a plurality of application prospects of prodrugs.

Description

Technical field [0001] The invention relates to a temperature-sensitive in-situ gel loaded with drugs by chemical bonds and its preparation, and belongs to the technical field of polymer gels containing drugs. Background technique [0002] Nanoparticles formed based on the self-assembly of polyethylene glycol (PEG)-polyester-drug copolymer have the following advantages: (1) Several drug molecules can be connected to each polymer chain to increase drug loading. (2) Amphiphilic polymers can self-assemble to form nanoparticles, which are usually taken up by tumor cells by phagocytosis. (3) Anticancer drugs and polymers are connected by covalent bonds, thereby prolonging blood circulation time and reducing the release of drugs during blood circulation. (4) The drug is connected to the polymer through a pH-sensitive bond, and can be released at a specific pH to improve the availability of the drug. MPEG-PCL / PTX, mPEG-PLA-PTX, PEO-(PCL / DOX) nanoparticles linked by ester linkages, ami...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/48A61K47/34
Inventor 董岸杰蔺晓娜邓联东
Owner TIANJIN UNIV
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