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DC cell targeted carrier, nanometer corpuscle and preparation method

A cell-targeting and carrier technology, which is applied in the direction of pharmaceutical formulations, antibody medical ingredients, and medical preparations of non-active ingredients, etc., can solve problems such as increased use costs, inactivation of antigenic peptides and proteins, and complicated preparation processes. Safety, controllable conditions, and good penetrability

Inactive Publication Date: 2011-01-19
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when mannose is directly coupled to the surface of antigenic peptides and proteins, it is necessary to use chemical methods to react to complete the coupling. This process can easily inactivate antigenic peptides and proteins, and the preparation process is complicated, which increases the overall cost of use.

Method used

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  • DC cell targeted carrier, nanometer corpuscle and preparation method
  • DC cell targeted carrier, nanometer corpuscle and preparation method
  • DC cell targeted carrier, nanometer corpuscle and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of DC cell-targeting carrier of the present invention

[0039] 1. Preparation of PCL-PEG diblock copolymer

[0040] Under nitrogen protection, 1 gram of polyethylene glycol monomethyl ether (MPEG, molecular weight 1000), 49 grams of caprolactone (ε-CL), and 0.2 gram of stannous octoate were added to the ampoule, heated to 130 ° C, and reacted After 1 hour, the temperature was raised to 180° C., and the reaction was continued for 2-11 hours, and then the reaction was continued for 0.5-3 hours under vacuum conditions (pressure lower than 200 Pa), and the viscosity of the system increased rapidly. Then it was naturally cooled to room temperature under the protection of nitrogen. The resulting copolymer was purified by a dissolution / precipitation method, and dried in a vacuum oven at a low temperature to a constant weight, thus obtaining a PCL-PEG diblock copolymer with a molecular weight of 50,000. NMR results indicated that the obtained product was...

Embodiment 2

[0047] Example 2 Preparation of DC cell-targeting carrier of the present invention

[0048] 1. Preparation of PCL-PEG-PCL (PCEC) triblock copolymer

[0049] Synthesize PCL-PEG-PCL tri-block copolymer with reference to the method of Example 1, the difference is that dihydroxypolyethylene glycol is used instead of polyethylene glycol monomethyl ether, and the ratio of PEG to ε-CL is controlled to control the molecular weight of PCEC . The synthetic reaction schedule is shown in the figure below. The molecular weight of the PCEC synthesized in this embodiment is a PCL-PEG-PCL (PCEC) copolymer with Mn=45,000 and Mw=78,000 (the molecular weight is the result of GPC gel chromatography). By adjusting the molecular weight of MPEG, and the mass ratio of MPEG to ε-CL, the molecular weight of the obtained PCEC copolymer can be adjusted. The molecular weight of the PCEC synthesized by this patent is 3000-1000000.

[0050] The reaction equation is as follows:

[0051]

[0052] NMR ...

Embodiment 3

[0063] Example 3 Preparation of DC cell-targeting carrier nanoparticles of the present invention

[0064] Take by weighing 30mg PCEC or MAN-PCEC copolymer, be dissolved in the ethyl acetate, total volume is 2ml, then this solution is added in the aqueous solution containing SDS (sodium dodecyl sulfate) (SDS concentration is 0.3mg / ml ), stirring at a high speed of 10000rpm for 5-10 minutes, then rotating the obtained emulsion in a rotary evaporator for 40 minutes, and finally adding water to fix the solution to 4ml, and storing the obtained nanoparticle suspension at 4°C.

[0065] The DC cell-targeting nanoparticles prepared by the present invention have an average particle size of less than 200nm detected by a Malvern particle size analyzer, which meets the requirements and has good uniformity. For detailed results, see the attached Figure 4 .

[0066] Nanoparticles were prepared by using PCL-PEG or MAN-PCL-PEG by the above method, and the particle size of the obtained nanop...

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Abstract

The invention belongs to the pharmaceutical high polymer material field, in particular relates to a dendritic cell (DC cell) targeting carrier, a nano particle, and a preparation method thereof. The DC cell targeting carrier of the invention is a compound which is obtained from a mannan covalence hyperbranched polyester-polyethylene glycol copolymer. Simultaneously, the invention also provides the nano particle which is obtained by preparing the DC cell targeting carrier and a medicine composition which is formed by preparing the effective elements of the encapsulated medicine of the DC cell targeting carrier. At the same time, the invention also provides the preparation method and the purpose of the product. The targeting efficiency of the product of the invention is good, the effect is remarkable, and the security is good; the steps of the method of the invention are simple, the cost is inexpensive, the condition is controllable, and the product is suitable for the mass production.

Description

Technical field: [0001] The invention belongs to the field of medicinal polymer materials, and in particular relates to a DC cell targeting carrier, nanoparticles and a preparation method. Background technique: [0002] Pharmaceutical targeting carriers have always been a hot spot in the field of pharmacy research, among which targeted nanoparticle delivery systems (NDDS) such as liposomes, nanoparticles, microemulsions, and polymer micelles are the current field of molecular biopharmaceuticals. focus of research. Polyester-polyethylene glycol copolymers, which have good biocompatibility and whose degradation rate can be controlled by adjusting the ratio, molecular weight, and crystallinity of the hydrophilic and hydrophobic segments of the copolymer, are commonly used drug release carriers. However, the existing polyester-polyethylene glycol copolymer has the disadvantage of poor targeting. However, the targeting of drug release can not only reduce the toxic and side effec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K47/48A61K39/00A61K9/14A61K9/00A61P35/00C08G81/00A61K47/61
Inventor 钱志勇魏于全黄媚娟杨莉
Owner SICHUAN UNIV
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