Arendronic acid modified astragaloside mPEG-PLGA nano-micelle and research on anti-osteoporosis effect of alendronic acid modified astragaloside mPEG-PLGA nano-micelle

An anti-osteoporosis, astragaloside IV technology, applied in the field of pharmaceutical preparations, can solve the problems that the improvement of osteoporosis treatment has not yet been realized, achieve good bone tissue targeting ability, delay internal circulation time, and improve oral bioavailability Effect

Pending Publication Date: 2022-04-12
席焱海
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, prolongation of drug circulation in the body and improvement in the treatment of osteoporosis have not yet been achieved

Method used

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  • Arendronic acid modified astragaloside mPEG-PLGA nano-micelle and research on anti-osteoporosis effect of alendronic acid modified astragaloside mPEG-PLGA nano-micelle
  • Arendronic acid modified astragaloside mPEG-PLGA nano-micelle and research on anti-osteoporosis effect of alendronic acid modified astragaloside mPEG-PLGA nano-micelle
  • Arendronic acid modified astragaloside mPEG-PLGA nano-micelle and research on anti-osteoporosis effect of alendronic acid modified astragaloside mPEG-PLGA nano-micelle

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Synthesis of alendronate-modified mPEG-PLGA (AL-mPEG-PLGA) bone-targeting material in the study of alendronic acid-modified astragaloside IV mPEG-PLGA nanomicelles and its anti-osteoporosis effect:

[0030] MPEG2000-PLGA18000 (50 / 50) compound was dissolved in 2 mL of DMF solution, and CDI (2.5 mg, 0.015 mmol) was added while stirring. Reaction at room temperature for 5h. The reaction was monitored on a TLC plate with a mixture of dichloromethane and methanol. After the two compounds were reacted, the alendronate sodium trihydrate and tetrabutylammonium hydroxide solution (1:2 molar ratio) were stirred, added to the reaction solution, and reacted at 80° C. for 5 h. The reaction was monitored on a TLC plate using a mixture of dichloromethane and methanol. After the reaction, use a rotary evaporator to remove DMF at 70-80°C. The remaining reaction solution was washed with a small amount of water, and excess aluminum sodium and tetrabutylammonium hydroxide (supernatant) ...

Embodiment 2

[0033] Preparation of a kind of alendronic acid-modified astragaloside IV mPEG-PLGA nanomicelle:

[0034] The invention adopts a dialysis method to prepare astragaloside IV mPEG-PLGA nano micelles. Accurately weigh 10mg AL-mPEG-PLGA and dissolve in 10mL distilled water. After ultrasonic probe 30 times, 1.0 mg / mL AL-mPEG-PLGA blank micellar solution was obtained. Then, under magnetic stirring, gradually add 15% ethanol solution of astragaloside IV. After stirring for 10 min, the solution was transferred to a dialysis bag (MWCO 700,000000Da) and dialyzed against double distilled water for 24 h to remove ethanol. The dialysis product was centrifuged at 4000rpm / min for 10min to remove unencapsulated astragaloside IV. After the supernatant was freeze-dried, astragaloside IV mPEG-PLGA nanomicelle solid powder was prepared for follow-up research.

[0035] Physical characterization: After diluting the astragaloside IV mPEG-PLGA nanomicelles prepared in Example 2 with water, a part...

Embodiment 3

[0039] Cytotoxicity Study of Astragaloside IV mPEG-PLGA Nanomicelles in Vitro

[0040] The cytotoxicity of astragaloside IV mPEG-PLGA nanomicelles on MC3T3-E1 cells was detected by MTT assay. After the logarithmic growth phase, MC3T3-E1 cells were seeded in 96-well plates at a density of 5×104 per well, and then incubated at 37°C and 5% carbon dioxide for 24h. After the cells were completely iron-armed, different concentrations (10, 25, 50, 100 and 200 μg / mL) of AL-mPEG-PLGA blank micelles solution, astragaloside IV mPEG-PLGA nanomicelle solution and mPEG-PLGA blank micelles were added solution. At the same time, untreated blank cells were used as the control group, and after continuous culture for 48 hours, 20 μL of MTT solution (5 mg / mL) was added to each well. After continuing to culture in the incubator for 4 hours, discard the supernatant, add DMSO (100 μL) to each well, and shake at constant temperature for 20 minutes. Measure the absorbance at 570nm with a microplate...

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Abstract

The invention discloses an alendronic acid modified astragaloside mPEG-PLGA nano-micelle and an anti-osteoporosis effect research thereof, belongs to the field of pharmaceutical preparations, and aims to provide the astragaloside mPEG-PLGA nano-micelle so as to improve the solubility and oral bioavailability of astragaloside and improve the anti-osteoporosis effect of the astragaloside. The key point of the technical scheme is as follows: the nano-micelle is composed of AL-mPEG-PLGA obtained by synthesis and astragaloside (AS), and is prepared by a dialysis method. The bone targeting material AL-mPEG-PLGA is prepared from an MPEG2000-PLGA 18000 (50 / 50) compound and a mixture of alendronate sodium trihydrate and a tetrabutylammonium hydroxide solution through chemical reaction synthesis. The preparation method comprises the following steps: preparing the bone targeting material AL-mPEG-PLGA; the prepared astragaloside mPEG-PLGA nano-micelle has a relatively small particle size and a relatively high drug encapsulation efficiency, the oral bioavailability is enhanced, and the anti-osteoporosis effect of the astragaloside mPEG-PLGA nano-micelle is enhanced. Therefore, the invention may be a promising strategy for preventing and treating osteoporosis, and provides preliminary information for clinical application of astragaloside and other similar water-insoluble compounds.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a kind of astragaloside IV mPEG-PLGA nanomicelle modified by alendronic acid and research on its anti-osteoporosis effect Background technique [0002] As a systemic bone metabolic disease, osteoporosis can lead to severe complications such as fragility fractures, seriously affecting the quality of life of middle-aged and elderly people, and has become one of the global health problems. In general, women are more prone to osteoporosis than men, possibly because their bones are lighter. It is characterized by disruption of bone homeostasis and loss of bone tissue, leading to fractures and bone pain. The relationship between the destruction of bone microstructure in patients with osteoporosis and bone glass protein (bone glprotein, BGP), tartrate-resistant acid phosphatase 5b (TRACP-5b), type I collagen C-terminal peptide (CTX-1) and inflammatory factor inter...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/60A61K47/69A61K31/7048A61K9/107A61P19/10A61K31/663
Inventor 席焱海蒋廷旺王伟恒
Owner 席焱海
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