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A pamam-based targeted drug delivery carrier and preparation method thereof

A technology of targeted drug delivery and carrier, applied in the field of biomedicine, can solve problems such as reducing the anti-tumor effect of drugs, reducing drug release, etc., and achieve the effects of reducing cytotoxicity and hemolytic toxicity, reducing uptake, and prolonging circulation time.

Inactive Publication Date: 2017-02-15
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, it is worth noting that the carrier modified by PEGylation will reduce the release of the drug to a certain extent. Liu Dan et al. have reported that DOX can be rapidly released from PAMAM, and the release rate can reach 80% in 48 hours. However, after PEGylation, the release rate in PAMAM-PEG is only 40%, which will greatly reduce the antitumor effect of the drug

Method used

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  • A pamam-based targeted drug delivery carrier and preparation method thereof
  • A pamam-based targeted drug delivery carrier and preparation method thereof
  • A pamam-based targeted drug delivery carrier and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040]Dissolve 10 mg of PAMAM (generation 4) in 1.5 mL of methanol solution, add 1.75 mg of SPDP and 10 μL of triethylamine, and stir at 30 °C for 5 h in the dark to generate the PAMAM-NH-SPDP intermediate; In the PAMAM-NH-SPDP intermediate, the molar ratios of PAMAM and SPDP are 1:8, respectively. Add 28 mg of HS-(CH 2 CH 2 O) 112 -CH 2 OCH 3 , stirred overnight, the resulting product was transferred to a dialysis bag (MW: 8000-14000), dialyzed in water for 2 days, and freeze-dried for 3 days to obtain a white solid, which is the targeted drug delivery carrier PAMAM-SS-PEG 8 , protected from light; generate PAMAM-SS-PEG 8 In the product, the molar ratio of PAMAM and PEG is 1:8.

Embodiment 2

[0042] Dissolve 10 mg of PAMAM (generation 4) in 1.5 mL of methanol solution, add 3.5 mg of SPDP and 10 μL of triethylamine, and stir at 30 °C for 5 h in the dark to generate a PAMAM-NH-SPDP intermediate; -In the NH-SPDP intermediate, the molar ratio of PAMAM to SPDP is 1:16. Add 56 mg of HS-(CH 2 CH 2 O) 112 -CH 2 OCH 3 , stirred overnight, the resulting product was transferred to a dialysis bag (MW: 8000-14000), dialyzed in water for 2 days, and freeze-dried for 3 days to obtain a white solid, which is the targeted drug delivery carrier PAMAM-SS-PEG 16 , protected from light; generated PAMAM-SS-PEG 16 In the product, the molar ratios of PAMAM and PEG are 1:16, respectively.

Embodiment 3

[0044] Dissolve 10 mg of PAMAM (4th generation) in 1.5 mL of methanol solution, add 7 mg of SPDP and 10 μL of triethylamine, and stir for 5 h at 30 °C in the dark to generate PAMAM-NH-SPDP intermediate; In the NH-SPDP intermediate, the molar ratio of PAMAM to SPDP is 1:32. Add 112 mg of HS-(CH 2 CH 2 O) 112 -CH 2 OCH 3 , stirred overnight, the resulting product was transferred to a dialysis bag (MW: 8000-14000), dialyzed in water for 2 days, and freeze-dried for 3 days to obtain a white solid, which is the targeted drug delivery carrier PAMAM-SS-PEG 32 , protected from light; generated PAMAM-SS-PEG 32 In the product, the molar ratio of PAMAM to PEG is 1:32.

[0045] The synthetic product of embodiment 3 is carried out nuclear magnetic analysis, the result is as follows figure 1 Shown, PAMAM-SS-PEG 32 The characteristic proton peaks are assigned as follows: δ = 2.25, 2.45, 2.65, 3.05-3.15 ppm is the characteristic proton peak on PAMAM; δ =3.23 ppm (s, OCH 3 ), ...

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Abstract

The invention discloses a targeted drug delivery carrier based on PAMAM (polyamide amine). A structural formula is described in the specification. A preparation method of the targeted drug delivery carrier based on PAMAM comprises the step of connecting PAMAM having pH sensitivity with hydrophilic polyethylene glycol by virtue of a reduction-sensitive disulfide bond, so that a size-controlled reduction and pH sensitive nano drug delivery carrier is formed. The targeted drug delivery carrier based on PAMAM can obviously reduce cytotoxicity and hemolysis toxicity which are caused by high algebraic PAMAM and also can reduce intake of a reticuloendothelial system and prolong retention time in blood, so that the drug is effectively conveyed to tumour tissues;the disulfide bond in the targeted drug delivery carrier based on PAMAM breaks under high reducing environment and at low pH value in a tumour cell, and an inner core of PAMAM is opened, so that the drug can be rapidly and effectively released, and the aims of improving treatment effect of an anti-tumour drug and reducing toxic and side effects are achieved.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to a targeted drug delivery carrier and a preparation method thereof, in particular to a PAMAM-based reduction and pH-sensitive targeted drug delivery carrier and a preparation method thereof. Background technique [0002] Malignant tumors have become one of the most serious diseases that threaten human health after cardiovascular diseases. Chemotherapy is one of the important methods for clinical treatment of tumors today. Although small molecule chemotherapeutics have strong anti-tumor effects in vitro, they are After administration, due to the lack of tumor targeting, chemotherapy drugs have a strong killing effect on normal tissues while killing tumor cells, resulting in prominent toxic and side effects, and it is difficult for patients to adhere to treatment. Therefore, increasing the concentration of drugs in the tumor site, enhancing the efficacy, reducing the distribution o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61P35/00C08G81/00
Inventor 程亮胡文程丽芳陈大为
Owner SUZHOU UNIV
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