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Amphipathic fluorescence target nano micelle and its preparation method

A nanomicelle, amphiphilic technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problems such as the inability to effectively introduce active end groups and the complex process of synthesizing carriers. , to achieve good biocompatibility and degradability, long-term safe drug release, and uniform distribution.

Inactive Publication Date: 2007-02-28
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The traditional amphiphilic carrier for the preparation of micelles, except that the hydrophobic component is a degradable polymer, the hydrophilic component is mostly polyethylene glycol (PEG), polyoxyethylene (PEO), etc., but the synthetic carrier The process is more complicated and cannot effectively introduce more active end groups to facilitate further functionalization

Method used

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  • Amphipathic fluorescence target nano micelle and its preparation method
  • Amphipathic fluorescence target nano micelle and its preparation method
  • Amphipathic fluorescence target nano micelle and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of PLA-PEI amphiphilic carrier

[0040] (1) PLA:PEI=1:0.4

[0041] Get PLA, N, N-dicyclohexylcarboimide (DCC), N-hydroxysuccinimide (NHS) are dissolved in dichloromethane (DCM), stir at room temperature for 24hr, prepare activated PLA; Take activated PLA Dissolve 1g of PLA in 10ml of DCM (A), 0.0121g of PEI in 5ml of acetone (B); after mixing evenly, slowly add system B to system A with high-speed stirring, and perform aminolysis for 6hr; add the obtained solution to high-speed stirring Precipitate in ice-cold ether; Buchner funnel filtration, vacuum drying to obtain white PLA-PEI powder.

[0042] The obtained PLA-PEI had Mn=6447 g / mol and Mw=16076 g / mol. (See Attachment 1)

[0043] (2) PLA:PEI=1:0.8

[0044] Dissolve PLA, DCC, and NHS in DCM and stir at room temperature for 24 hours to prepare activated PLA; take 1g of activated PLA and dissolve in 10ml of DCM (A), and dissolve 0.0242g of PEI in 5ml of acetone (B); after mixing them unifor...

Embodiment 2

[0049] Embodiment 2: preparation PLA-PEI is the drug-loaded micelle of carrier

[0050] Dissolve 0.5g PLA-PEI in 20ml DCM, dissolve evenly and become an oil phase, and ultrasonically suspend 5-Fu powder in the oil phase; dissolve 1g Tweeen-80 in 100ml water to become a water phase; Add it dropwise into the water phase, continue to stir for 48 hours until the organic solvent evaporates, put it in the refrigerator for 24 hours to further solidify the micelles; centrifuge, rinse with triple distilled water three times, and freeze-dry to obtain nano drug-loaded micelles powder.

[0051] The obtained nanometer drug-loaded micelles have a particle diameter of about 100nm (see accompanying drawing 2), are rounded and spherical, and have uniform sizes. (See Attachment 3)

[0052] The standard curve equation of 5-Fu at 265nm in 0.1M dilute hydrochloric acid is:

[0053] A=0.0567563C+0.000651 (r=0.9999) C is the concentration of 5-Fu (μg / ml), and A is the absorbance.

[0054] ...

Embodiment 3

[0055] Example 3 Preparation of Amphiphilic Targeted Nanomicelles

[0056] The drug-loaded micelles with PLA-PEI as the carrier were suspended in a certain amount of phosphate buffer solution (PBS) with a pH value of 4.0 (C); 0.026g folate and 0.0226g EDAC were dissolved in 5ml DMSO (D ), under magnetic stirring for 3hr; slowly drop system C into D system, keep for 10hr under magnetic stirring, adjust with PBS solution with a pH value of 4.0, and always keep the pH value of the system at 5.0; centrifuge the micellar suspension, three Rinse with distilled water for three times, and freeze-dry for 24 hours to obtain powder targeting nanomicelles.

[0057] Weigh a certain amount of targeting nanomicelle, dissolve it in DMSO, measure the absorbance at 362nm, and substitute it into the standard curve equation:

[0058] PLA: PEI

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Abstract

The invention discloses an amphipathic fluorescent targeting nanometer micelle and preparing method, which comprises the following steps: polymerizing decomposable polyester and multi-ammino polymer to synthesize amphipathic drug carrier, adopting solvent evaporating method to prepare carrier micelle, packing the drug into hydrophobic or little water-soluble tumour prevention drug, grafting targeting molecular folacin on the micelle with ammino, grafting isothiocyanic acid fluorescein on the residual ammino.

Description

technical field [0001] The invention belongs to the technical field of chemical medicines, and in particular relates to an amphiphilic fluorescent targeting nano-micelle and a preparation method thereof. technical background [0002] In recent years, studies have shown that polymeric micelles can be used as potential carriers for drugs that are difficult to dissolve in water. M. Jones et al. have attempted the preparation, characterization and drug application of polymeric micelles. Polymerized micelles provide attractive properties in two main aspects: (1) can dissolve hydrophobic drugs or slightly water-soluble drugs in the hydrophobic core; phagocyte system) uptake. [0003] Although micellar systems appear to be one of the most favorable vehicles for the delivery of poorly water-soluble drugs, their stability in infusion or body fluids remains a problem. X. Zhang et al. reported the use of a diblock copolymer of polylactide and monomethoxypolyethylene glycol (mPEG) as ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K45/00A61K47/30A61P35/00
Inventor 任杰李航袁华
Owner TONGJI UNIV
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