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Bone-targeted nanoparticle delivery system and preparation method thereof

A delivery system and nanoparticle technology, used in bone diseases, powder delivery, drug delivery, etc., can solve the problems of difficult absorption, low bone tissue concentration, short half-life, etc. Effect

Pending Publication Date: 2019-01-22
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In summary, epimedium flavonoids are difficult to absorb, and quickly distribute to tissues after entering the blood (short half-life), most of the drugs are distributed to the liver, and return to the small intestine through metabolism and hepatobiliary circulation, because it is difficult to absorb and excrete, resulting in low concentration in bone tissue

Method used

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  • Bone-targeted nanoparticle delivery system and preparation method thereof
  • Bone-targeted nanoparticle delivery system and preparation method thereof
  • Bone-targeted nanoparticle delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The preparation method of the bone-targeted nanoparticle delivery system is as follows:

[0057] 1. Preparation of nanoparticles

[0058] Dissolve 70mg PLGA into 1mL ethyl acetate, and then add it to 1% polyvinyl alcohol (PVA) aqueous solution, wherein the PVA aqueous solution contains 5mg / mL of small molecule icariin and 0.5mg / mL of dithio Succinimidyl suberate (BS3, can be inserted into the nanocapsule formed by PLGA and PVA, and the active groups at both ends can combine with the amino group of the aspartic acid chain).

[0059] The mixture was continuously sonicated for 2 minutes at room temperature, using a UP200H sonicator (Hielscher Ultrasonics GmbH, Germany) at an amplitude intensity of 40%. After centrifugation, excess solvent was evaporated with constant stirring. The isolated nanoparticles were washed 3 times with PBS and suspended in water. Pressurize with nitrogen, and extrude the nanoparticle suspension with an extruder (LipexTM Extruder), so that the n...

Embodiment 2

[0075] The preparation method of the bone-targeted nanoparticle delivery system is as follows:

[0076] 1. Preparation of nanoparticles

[0077] Dissolve 60 mg of polyhydroxybutyric acid into 1 mL of 1,4-dioxane, and then add it to 0.8% polyvinyl alcohol (PVA) aqueous solution, wherein the PVA aqueous solution contains 3 mg / mL of small molecule icariin and 0.4mg / mL of bisthiosuccinimidyl suberate (BS3, can be inserted into the nanocapsule, and the active groups at both ends can combine with the amino group of the aspartic acid chain).

[0078] The mixture was continuously sonicated for 1 min at room temperature using a UP200H sonicator (Hielscher Ultrasonics GmbH, Germany) at 40% amplitude intensity. After centrifugation, excess solvent was evaporated with constant stirring. The isolated nanoparticles were washed twice with PBS and suspended in water. Pressurize with nitrogen, and extrude the nanoparticle suspension with an extruder (LipexTMExtruder), so that the nanopartic...

Embodiment 3

[0087] The preparation method of the bone-targeted nanoparticle delivery system is as follows:

[0088] 1. Preparation of nanoparticles

[0089] Dissolve 80 mg of polyalkylcyanoacrylate into 1 mL of DMF, and then add it to 1.2% polyvinyl alcohol (PVA) aqueous solution, wherein the PVA aqueous solution contains 8 mg / mL of small molecule puerarin and 0.6 mg / mL of bis Sulfosuccinimidyl suberate (BS3, can be inserted into the nanocapsule, and the active groups at both ends can be combined with alendronate).

[0090] The mixture was continuously sonicated for 1 min at room temperature using a UP200H sonicator (Hielscher Ultrasonics GmbH, Germany) at 40% amplitude intensity. After centrifugation, excess solvent was evaporated with constant stirring. The isolated nanoparticles were washed 3 times with PBS and suspended in water. Pressurize with nitrogen, and extrude the nanoparticle suspension with an extruder (LipexTM Extruder), so that the nanoparticle suspension passes through ...

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Abstract

The invention relates to the field of drug carriers, in particular to a bone-targeted nanoparticle delivery system and a preparation method thereof. The bone-targeted nanoparticle delivery system comprises nanoparticles and bone-targeted functional components. The nanoparticles are monolayer vesicles internally wrapped with pharmaceutical active ingredients, the vesicle membranes of the monolayervesicles are composed of degradable polymers and polyvinyl alcohol, the vesicle membranes are cuttaged with dithiosuccinimide-octyl diacid ester, and the nanoparticles are in conjugated combination with the bone-targeted functional components through the dithiosuccinimide-octyl diacid ester. According to the bone-targeted nanoparticle delivery system, as the monolayer vesicles are wrapped with thepharmaceutical active ingredients, greater drug carrying capacity is achieved, in addition, through detection, stability of vitro release test is good, and drug release is controllable.

Description

technical field [0001] The invention relates to the field of drug carriers, in particular to a bone-targeted nanoparticle delivery system and a preparation method thereof. Background technique [0002] Osteoporosis is a systemic skeletal disease characterized by decreased bone mass and degeneration of bone microstructure, resulting in increased bone fragility and susceptibility to fractures. Head and spine fractures, severe cases fatal. Currently, estrogen replacement therapy, selective estrogen receptor modulators (SERMs, such as tamoxifen), bisphosphonates (such as alendronate), calcium and vitamins are mainly used in the clinical treatment of osteoporosis. D, Western medicines such as human recombinant parathyroid hormone (PTH), but long-term use will have adverse reactions to a certain degree, and the price is expensive, and the clinical application is limited. Therefore, the development of a drug with low toxic and side effects and high biological efficacy has become ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/64A61K47/54A61P19/10A61K31/352A61K31/7048
CPCA61K47/548A61K47/64A61K47/6933A61P19/10A61K31/352A61K31/7048
Inventor 王新峦李玲曹会娟黄翠珊秦岭李志明张蕴
Owner SHENZHEN INST OF ADVANCED TECH
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