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Preparation method for difunctional nanoparticle carrier and preparation method for difunctional nanoparticle preparation
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A nanoparticle and dual-function technology, which can be used in powder delivery, antineoplastic drug delivery, freeze-drying delivery, etc., can solve the problems of limiting the types of drugs to be entrapped, and achieve good cytotoxicity, good performance, and good encapsulation efficiency.
Inactive Publication Date: 2014-08-06
SHANGHAI JIAOTONG UNIV
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Problems solved by technology
However, most of the existing researches use acid-sensitive linkages between polymers and drugs, which greatly limits the types of drugs to be entrapped.
Moreover, the bifunctional nanoparticle carrier PLGA-PEG-Folate (i.e. pH-sensitive folic acid-targeted nanoparticle carrier PLGA-PEG-Folate) with both folic acid and acid-sensitive linking groups has not been reported. The development of the carrier will provide a new idea for the anti-tumor therapy of the nano drug delivery system
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Embodiment 1
[0039] This embodiment relates to a preparation method of a bifunctional nanoparticle carrier PLGA-PEG-Folate;
[0040] The synthesis of bifunctional nanoparticle carrier PLGA-PEG-Folate specifically includes the following steps:
[0041] (1) Using HO-PEG-OH as raw material, NH was synthesized in three steps 2 -PEG-NH 2 , the synthesis process is as figure 1 Shown, NH 2-PEG-NH 2 of 1 HNMR results such as figure 2 shown;
[0042] (2) with CH 2 Cl 2 As a solvent, react the activated PLGA-COOH with p-hydroxybenzaldehyde, and then add the catalyst p-toluenesulfonic acid to undergo a condensation reaction to form a PLGA derivative with a hydrazone bond (-NH-N=CH-), and synthesize Process such as image 3 As shown, the PLGA derivatives with hydrazone bonds 1 HNMR results such as Figure 4 shown;
[0043] (3) After activation of the carboxyl terminal of the PLGA derivative with a hydrazone bond, use DMF as solvent, DCC\NHS as catalyst, and NH 2 -PEG-NH 2 The acylation...
Embodiment 2
[0045] This embodiment relates to a preparation method of a bifunctional nanoparticle preparation loaded with vincristine sulfate;
[0046] The preparation of the bifunctional nanoparticle preparation loaded with vincristine sulfate comprises the following steps:
[0047] (1) Vincristine sulfate was dissolved in Tris-HCl buffer solution at pH 6.8 to form a concentrated solution (referred to as phase I), and PLGA-mPEG and bifunctional nanoparticle carrier PLGA-PEG-Folate (the mass of both ratio of 8:1) dissolved in an organic solvent (dichloromethane or acetone) (called phase II), the volume ratio of Tris-HCl buffer solution to organic solvent is 1: (5-20), vincristine sulfate administration The amount is 10%~15% (w / w);
[0048] (2) Under the condition of ultrasonic ice bath, add phase I dropwise to phase II to obtain colostrum;
[0049] (3) Under the condition of ultrasonic ice bath, add Tris-HCl buffer solution containing 0.6% to 2% PVA (w / v) and pH 5 to 7.4 dropwise into c...
Embodiment 3
[0054] This embodiment relates to a preparation method of PLGA-mPEG nanoparticles;
[0055] The preparation method is the same as in Example 1 and Example 2 to obtain PLGA-mPEG nanoparticle preparation NP1.
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Abstract
The invention discloses a preparation method for a difunctional nanoparticle carrier and a preparation method for a difunctional nanoparticle preparation. The preparation method for the difunctional nanoparticle carrier comprises the following steps of: synthesizing ester with formyl by using poly(lactic-co-glycolic acid)-COOH (PLGA-COOH) and p-hydroxybenzaldehyde as raw materials in the presence of 4-dimethylaminopyridine and a condensing agent; synthesizing a PLGA derivative with an acid-sensitive connecting segment hydrazone bond by using the ester with the formyl and carboxyl phenylhydrazine in the presence of p-toluenesulfonic acid; conjugating NH2-polyethylene glycol (PEG)-NH2 and the PLGA derivative with the acid-sensitive connecting segment hydrazone bond in the presence of N-hydroxysuccinimide (NHS) and the condensing agent; and adding folate, the NHS and the condensing agent, and conjugating again to obtain the difunctional nanoparticle carrier PLGA-PEG-folate. The prepared difunctional nanoparticle carrier shows a good pharmacokinetic behavior in vitro, and has high medicine-loading rate, encapsulation rate and stability.
Description
technical field [0001] The invention relates to a preparation method of a nanoparticle carrier and a nanoparticle preparation, in particular to a preparation method of a bifunctional nanoparticle carrier and a bifunctional nanoparticle preparation. Background technique [0002] Targeted nano drug delivery systems can generally be divided into active targeting and passive targeting nano drug delivery systems. An important direction of active targeted drug delivery system research is to use the principle of specific binding of receptors and ligands to synthesize nanoparticle carriers with active targeting functions. Folate is a commonly used active targeting ligand, and folate receptors are overexpressed on the surface of many tumor cell membranes. Based on this special effect, drug carriers combined with folic acid can be introduced into these tumor cells. An important research direction of passive targeting nano drug delivery system is to develop pH-sensitive drug-loaded n...
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