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Somatostatin receptor mediated tumor-targeted medicament composition

A technology targeting somatostatin receptors and tumors, applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve the problems of increasing curative effect, reducing drug release, hindering liposome fusion and phagocytosis, and achieving simple production Effect

Inactive Publication Date: 2009-05-27
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Doxorubicin stealth liposomes are currently on the market Studies have shown that PEG modification can stabilize liposomes, reduce drug release (and thus reduce drug diffusion), and hinder liposome fusion and phagocytosis to a certain extent. Therefore, although long-circulating liposomes can increase tumor tissue concentration, but the efficacy does not necessarily increase

Method used

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  • Somatostatin receptor mediated tumor-targeted medicament composition
  • Somatostatin receptor mediated tumor-targeted medicament composition
  • Somatostatin receptor mediated tumor-targeted medicament composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Octreotide (OCT)-modified long-circulating liposome OCT-L[CD] simultaneously loaded with CA-4 and doxorubicin

[0059] The formulations of the liposomes are: EPC: CHOL: DSPE-PEG: CA-4 (25: 1.28: 6.24: 2) (unit: mg). Accurately weigh the prescribed amount of EPC, CHOL, DSPE-PEG, DSPE-PEG-OCT (2% molar ratio) and CA-4, put them in a pear-shaped bottle, and add an appropriate amount of chloroform to dissolve. Rotary evaporation under reduced pressure at 37°C formed a uniform transparent film. Add 123mM ammonium sulfate solution, and sonicate in a water bath until blue opalescence appears. A polycarbonate film of 200 nm was extruded 5 times. Pass the prepared liposomes through a Sephadex G50 column, elute with PBS buffer (pH7.4) as the mobile phase, collect the liposome fraction, heat the collected liposomes in a water bath at 40°C, add Adriamycin Incubate the plain powder for 20 minutes and shake it frequently to obtain this product.

Embodiment 2

[0061] Basic physicochemical properties of octreotide (OCT)-modified long-circulating liposome OCT-L[CD] loaded with CA-4 and doxorubicin

[0062] The basic physical and chemical properties of the long-circulating liposome L[CD] and OCT-L[CD] prepared by the present invention, which simultaneously entrap CA-4 and doxorubicin, are compared in Table 1:

[0063] preparation Average particle size (nm) PDI Surface potential (mv)

[0064] L(D) 88.65 0.237 -4.916 OCT-L(D) 86.87 0.169 -5.189 L(CD) 92.70 0.232 -2.198 OCT-L (CD) 91.43 0.199 -4.911

Embodiment 3

[0066] In vitro tumor cell (NCI-H446) growth inhibition test of OCT-modified long-circulating liposome OCT-L[D] loaded with doxorubicin. The results of the study showed that the cytotoxic effect of octreotide OCT-modified liposomes was more obvious than that of non-targeted modified liposomes, which also indicated that the tumor cell-targeting effect of octreotide-modified liposomes could significantly enhance the antitumor drug effect. cellular uptake. For specific results, see figure 1 .

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Abstract

The invention relates to a somatostatin receptor-mediated tumor targeted pharmaceutical composition which adopts a targeted somatostatin receptor functional polypeptide and polyethylene glycol for simultaneously modifying a pharmaceutical carrier, and an anti-tumor drug or / and an anti-angiogenic drug is delivered to the tumor part, thereby enhancing the tumor treatment effect.

Description

Technical field: [0001] The invention relates to a tumor-targeting pharmaceutical composition, in particular to a somatostatin receptor-mediated tumor-targeting pharmaceutical composition. Background technique: [0002] Malignant tumors have always been an important disease that plagues human beings, and there is currently no cure for cancer. The traditional therapy for malignant solid tumors is surgical resection of the tumor followed by chemotherapy with antineoplastic drugs. Most chemotherapeutic drugs are non-selective, and these drugs also have a killing effect on normal cells while killing tumor cells, so they will produce serious side effects, such as the cardiotoxic effect of doxorubicin. Encapsulation of anti-tumor drugs with appropriate carrier systems (such as liposomes, micelles, etc.) can significantly prolong the time of their circulation in the body, which is conducive to the accumulation of anti-tumor drugs in the tumor area, thereby increasing the therapeut...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K45/08A61K47/48A61K9/127A61P35/00A61K31/704A61K47/60A61K47/64
Inventor 张强王坚成张烜张元金武章俊麟
Owner PEKING UNIV
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