Polypeptide HM-3 nanometer particles and preparation method thereof

A nanoparticle, HM-3 technology, applied in pharmaceutical formulations, peptide/protein components, medical preparations with non-active ingredients, etc., can solve problems such as toxic side effects, blood drug concentrations approaching or exceeding poisoning levels, etc., and achieve the preparation method. Simple, increase the encapsulation efficiency and drug loading, and prolong the half-life effect

Pending Publication Date: 2020-07-31
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The sudden release at the initial stage of administration may cause the blood drug concentration to approach or exceed the toxic level, resulting in obvious toxic side effects

Method used

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  • Polypeptide HM-3 nanometer particles and preparation method thereof
  • Polypeptide HM-3 nanometer particles and preparation method thereof
  • Polypeptide HM-3 nanometer particles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Weigh about 100mg of PLGA (50:50), dissolve in 4ml of dichloromethane as the organic phase; take another 5mg of HM-3, dissolve in 200μL of 0.1% sodium alginate as the inner water phase, and mix the two phases Ultrasonic (150w, 1min) after the probe, fully emulsified and injected into 16ml mixed solution (continuing filtrate of 1% PVA, 4% chitosan solution + 5% calcium chloride mixed solution), stirred at room temperature to evaporate the organic solvent, and stirred at a low speed of 5000rpm 20min, washed 3 times with water, and freeze-dried. Obtain the PLGA nanoemulsion modified by sodium alginate and chitosan with uniform particle size and round shape, see figure 1 .

Embodiment 2

[0038] Embodiment 2: dissolution test

[0039] Two PLGA nanoparticles loaded with the same concentration of HM-3 were dissolved in saline and placed in an ultrafiltration tube, placed in a shaker (37°C, 75rpm), and centrifuged regularly (4°C, 7000rpm, 20min) to collect 1ml Ultrafiltrate, while supplementing an equal amount of release medium. Agilent high performance liquid chromatography was used to measure the content of HM-3 in the ultrafiltrate, and then the cumulative release rate at different time points was calculated. The experimental results are shown in image 3 .

Embodiment 3

[0040] Embodiment 3: in vivo anti-tumor test

[0041] Establishment of xenograft tumor model in black mice: Inoculate murine melanoma cells into the subcutaneous axillary of C57BL / 6 black mice, and the inoculation volume of each black mouse is 2×10 6 cells / 0.1mL, when the tumor grows to a certain size, dissect the black mouse to take out the tumor tissue, cut it into pieces and grind it, pass it through a cell sieve, absorb and centrifuge the filtered cell solution, and re-mix it in the blank medium to make the cells The concentration is 2×10 7 individual / mL. Begin to inoculate the cells in the skin of the right armpit of black mice, and the inoculation volume of each black mouse is 1×10 6 indivual. When the tumor tissue grows to 70-90mm 3 The diameter of the tumor tissue was measured with a vernier caliper. There were 16 mice in the negative control group and 10 mice in the treatment group. The black mice were selected to ensure uniform tumor volume and good growth statu...

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Abstract

The invention provides polypeptide HM-3 nanometer particles and a preparation method thereof. The polypeptide HM-3 nanometer particles are characterized by consisting of polypeptide HM-3, sodium alginate, chitosan, a polylactic acid-amino-oxyacetic acid copolymer (PLGA), an emulsifying agent, a pharmaceutic adjuvant and the like. According to the polypeptide HM-3 nanometer particles provided by the invention, the polypeptide HM-3 is packed in an inner aqueous phase, so that the stability of the polypeptide HM-3 is improved, the release of the polypeptide HM-3 is controlled, and the plasma half-life is prolonged. The polypeptide HM-3 nanometer particles provided by the invention can be applied to treatment of diseases associated with blood vessel regeneration, such as tumors, age-related macular degeneration and the like.

Description

technical field [0001] The invention relates to HM-3 nanoparticles and a preparation method thereof, and mainly relates to a preparation method of HM-3 nanoparticles. Background technique [0002] The anti-tumor polypeptide drug HM-3 is an integrin blocker. The polypeptide sequence is: Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala-Val-Pro-Gly-Gly-Gly-Gly-Arg-Gly -Asp, which contains the integrin ligand sequence (Gly-Gly-Gly-Gly-Arg-Gly-Asp) and neovascularization inhibitory sequence (Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala -Val-Pro), wherein the integrin ligand sequence contains the RGD sequence (Arg-Gly-Asp), the integrin blocker polypeptide sequence can effectively bind to the tumor-specifically expressed integrin subtype, and in this sequence Contains angiogenesis inhibitory sequence, thereby inhibiting tumor angiogenesis, thereby achieving the effect of inhibiting tumor growth and metastasis. Previous studies have shown that its targets are integrin αvβ3 and α5β1, but the main bindi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/10A61K9/51A61K47/34A61K47/36A61K47/32A61P35/00A61P27/02
CPCA61K38/10A61K9/5153A61K9/5161A61K9/5138A61P35/00A61P27/02
Inventor 薛建鹏徐寒梅李则青李应锋袁松涛王瑱李铎谢可人
Owner CHINA PHARM UNIV
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