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PH-sensitive magnetic targeting hydrogel drug beads as well as preparation method and application thereof

A hydrogel and magnetic targeting technology, which is applied in the fields of pharmaceutical formulation, drug combination, drug delivery, etc., can solve the problems of no pH sensitivity and targeting, inability to release drugs at the lesion site, and high preparation cost, so as to improve the Efficacy and bioavailability, excellent pH sensitivity, simple and fast method

Inactive Publication Date: 2018-02-06
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 201410054357.8 discloses a methotrexate-chitosan temperature-sensitive gel and its application. The preparation process requires the use of pH regulators, solubilizers and isotonic regulators, etc., and continuous ice bath stirring is required. The preparation cost is high and the conditions are high. Harsh, in addition, the methotrexate-chitosan thermosensitive gel of the invention does not effectively target the specificity of the tumor microenvironment, that is, the gel drug delivery system does not have pH sensitivity and targeting, and cannot effectively act on the lesion site. Targeted therapy that cannot be applied to tumors
Shao Xue et al. prepared polyvinyl alcohol / chitosan composite hydrogel with interpenetrating network structure as a carrier of chloramphenicol by cyclic freezing-thawing method combined with genipin cross-linking method. However, the preparation of the composite hydrogel The process is cumbersome and the cost is high, and the obtained hydrogel does not have a definite visual appearance. In the process of drug release, it does not have targeting performance and cannot release the drug to the lesion in a targeted manner (Shao Xue et al. pH sensitive type Swelling and Drug Loading and Release Properties of Polyvinyl Alcohol / Chitosan Interpenetrating Network Hydrogel. Journal of Southwest University for Nationalities, 2015, 582-587.)

Method used

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  • PH-sensitive magnetic targeting hydrogel drug beads as well as preparation method and application thereof
  • PH-sensitive magnetic targeting hydrogel drug beads as well as preparation method and application thereof
  • PH-sensitive magnetic targeting hydrogel drug beads as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of pH-sensitive magnetic targeting hydrogel beads

[0023] In this example, chitosan, polyvinyl alcohol, Fe 3 o 4 And the mass ratio of methotrexate is 8:8:4:1.

[0024] Weigh 400 mg of polyvinyl alcohol and add it to 10 mL of deionized water, heat to 75°C to 85°C, and stir well until it is completely dissolved.

[0025] Weigh 400 mg of chitosan and add it into 20 mL of 2% (v / v) acetic acid solution, and ultrasonically stir for 30 min to form a light yellow colloidal transparent liquid.

[0026] Acetic acid solution of chitosan, 200mg Fe 3 o 4 And 50 mg of methotrexate is added into the aqueous solution of polyvinyl alcohol, and stirred thoroughly at 30-50° C. to obtain a uniform mixed solution.

[0027] The mixed solution was added dropwise into 0.5M NaOH aqueous solution, and after being fully gelled, it was collected by a magnet, and washed with deionized water for several times to obtain pH-sensitive magnetic targeting hydrogel beads.

...

Embodiment 2

[0029] Example 2: Preparation of pH-sensitive magnetic targeting hydrogel beads

[0030] In this example, chitosan, polyvinyl alcohol, Fe 3 o 4 And the mass ratio of methotrexate is 32:16:8:1.

[0031] Weigh 400 mg of polyvinyl alcohol and add it to 10 mL of deionized water, heat to 75°C to 85°C, and stir well until it is completely dissolved.

[0032] Weigh 800 mg of chitosan and add it into 20 mL of 2% (v / v) acetic acid solution, and ultrasonically stir for 30 min to form a light yellow colloidal transparent liquid.

[0033] Acetic acid solution of chitosan, 200mg Fe 3 o 4 And 25 mg of methotrexate was added into the aqueous solution of polyvinyl alcohol, and stirred thoroughly at 30-50° C. to obtain a uniform mixed solution.

[0034] The mixed solution was added dropwise into 1M NaOH aqueous solution, and after being fully gelled, it was collected by a magnet, and washed with deionized water for several times to obtain pH-sensitive magnetic targeting hydrogel beads.

[...

Embodiment 3

[0036] Example 3: Preparation of pH-sensitive magnetic targeting hydrogel beads

[0037] In this example, chitosan, polyvinyl alcohol, Fe 3 o 4 And the mass ratio of methotrexate is 16:8:4:1. Weigh 400 mg of polyvinyl alcohol and add it to 10 mL of deionized water, heat to 75°C to 85°C, and stir well until it is completely dissolved.

[0038] Weigh 800 mg of chitosan and add it into 20 mL of 2% (v / v) acetic acid solution, and ultrasonically stir for 30 min to form a light yellow colloidal transparent liquid.

[0039] Acetic acid solution of chitosan, 200mg Fe 3 o 4 And 50 mg of methotrexate is added into the aqueous solution of polyvinyl alcohol, and stirred thoroughly at 30-50° C. to obtain a uniform mixed solution.

[0040] The mixed solution was added dropwise into 1M NaOH aqueous solution, and after being fully gelled, it was collected by a magnet, and washed with deionized water for several times to obtain pH-sensitive magnetic targeting hydrogel beads.

[0041] The...

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Abstract

The invention discloses pH-sensitive magnetic targeting hydrogel drug beads as well as a preparation method and an application thereof. The pH-sensitive magnetic targeting hydrogel drug beads are prepared after chitosan, polyvinyl alcohol, Fe3O4 nanoparticles and antitumor drug methotrexate are fully mixed and subjected to NaOH aqueous solution gelling. The pH-sensitive magnetic targeting hydrogeldrug bead preparation process is simple, low in cost, green and environmentally friendly, the prepared hydrogel drug beads have excellent biocompatibility, and the Fe3O4 nanoparticles can endow the drug beads with good magnetic targeting performance, so that the drug beads fully gather in focus areas under the guide of external magnetic fields. The prepared pH-sensitive magnetic targeting hydrogel drug beads have excellent magnetic response performance and drug slow-release performance and have great application potentials in the targeted tumor therapy field.

Description

technical field [0001] The invention relates to a pH-sensitive magnetic targeting hydrogel medicinal bead, a preparation method and application thereof, and belongs to the technical field of material preparation. Background technique [0002] Methotrexate is one of the well-known antineoplastic drugs, which can treat malignant tumors such as head and neck cancer, breast cancer, skin cancer, and lung cancer. Methotrexate has a very short plasma half-life and a high efflux rate, requiring high doses of methotrexate for treatment. In addition, when the traditional methotrexate drug is used, the drug cannot fully reach the tumor site, but spreads all over the body, causing toxic and side effects on normal tissues, which limits its clinical application. Delivering anti-tumor drugs to the lesion site through nano-carriers, adjusting drug release according to the nature and strength of a certain stimulus-sensitive signal in the external environment can achieve the purpose of local...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/06A61K47/36A61K47/32A61K47/02A61K31/519A61P35/00
CPCA61K9/0009A61K9/06A61K31/519A61K41/00A61K47/02A61K47/32A61K47/36
Inventor 姜炜吴娟蒋炜沈烨文田仁兵
Owner NANJING UNIV OF SCI & TECH
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