Isoliquiritigenin nanosuspension and preparation method and application thereof

A nano-suspension and isoliquiritigenin technology, which is applied in liquid transportation, pharmaceutical formula, emulsion transportation, etc., can solve the problem that the isoliquiritigenin nano-suspension does not meet the expected experimental effect, and achieves the improvement of cumulative dissolution rate , low cost, and the effect of improving the ability of apoptosis

Pending Publication Date: 2020-03-06
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Like the above-mentioned patents, in the present invention, when the inventor prepared the isoliquiritigenin nanosuspension, in order to achieve a better effect, he added a steric stabilizer and a charge stabilizer at the same time, but the prepared isoliquiritigenin nanosuspension The various characterizations of the liquid did not meet the expected experimental results

Method used

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  • Isoliquiritigenin nanosuspension and preparation method and application thereof
  • Isoliquiritigenin nanosuspension and preparation method and application thereof
  • Isoliquiritigenin nanosuspension and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1, preparation of isoliquiritigenin nanosuspension

[0046] Isoliquiritigenin nanosuspension (ISL-NS): Weigh 0.25g of isoliquiritigenin, add it to 50ml of distilled water, and stir magnetically for 15 minutes to obtain a coarse suspension. Before grinding, add 140ml of zirconia grinding beads with a particle size of 0.6-0.8mm into the grinding chamber, and grind for 45 minutes at 2000rpm. sexual charge.

[0047] Isoliquiritigenin Nanosuspension 1 (HPC SSL-SDS-ISL-NS): Weigh 0.05g of hydroxypropyl cellulose, 0.05g of sodium lauryl sulfate, add 50ml of distilled water, and stir to obtain a stabilizer solution. Add 1 g of isoliquiritigenin under a magnetic stirrer, and stir magnetically for 15 minutes to obtain a coarse suspension. Before grinding, add 140ml of yttrium-stabilized zirconia grinding beads with a particle size of 0.6-0.8mm into the grinding chamber, and grind for 45 minutes at a speed of 2000rpm. After the obtained sample is diluted 10 times with...

Embodiment 2

[0053] Example 2, Preparation of Isoliquiritigenin Micro and Nano Suspensions

[0054] Isoliquiritigenin Nanosuspension 2 (HPC SSL-ISL-NS): Weigh 0.1g of hydroxypropyl cellulose (HPC), add 50ml of distilled water, stir evenly to obtain a stabilizer solution, add 0.25g of iso Liquiritigenin, magnetically stirred for 15 minutes to obtain a coarse suspension. Before grinding, add 140ml of yttrium-stabilized zirconia grinding beads with a particle size of 0.6-0.8mm into the grinding chamber, grind at 2000rpm for 45min, and dilute the obtained sample 10 times with purified water to obtain the isoliquiritigenin nanosuspension particles The diameter is 238.1nm, and the potential is -16.83mV.

[0055] Isoliquiritigenin Nanosuspension 3 (PVP K30-ISL-NS): Weigh 0.1g of povidone K30, add 50ml of distilled water, stir evenly to obtain a stabilizer solution, add 0.25g of isoliquiritigenin under magnetic stirring, and magnetically Stir for 15 min to obtain a coarse suspension. Before gri...

Embodiment 3

[0066] Example 3. Freeze-dried powder and characterization of isoliquiritigenin nanosuspension.

[0067] Add 2% lyoprotectant lactose to the isoliquiritigenin nanosuspension, mix well, pre-freeze at -80°C for 12h, transfer to a freeze dryer, freeze at -40°C for 8h, and finally freeze at 12°C Under heating and sublimation for 4 hours, the freeze-dried powder of isoliquiritigenin nanosuspension was obtained. Freeze-dried powder is characterized by scanning electron microscopy, differential scanning calorimeter (DSC), X-ray diffraction (XRD), Fourier transform infrared spectrometer (FTIR) and X-ray photoelectron spectroscopy (XPS), and the results are as follows: figure 1 , 2, 3, 4, 5.

[0068] From figure 1It can be seen from the figure that the isoliquiritigenin API exists in square, columnar and irregular forms, and the form of ISL-MS is small particles, while the form of HPC SSL-ISL-NS and PVP K30-ISL-NS is in the form of irregular The flake-like form exists, and it can be...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to an isoliquiritigenin nanosuspension and a preparation method and application thereof. The isoliquiritigenin nanosuspension is composed of isoliquiritigenin and a space stabilizer with a mass ratio of 1:(0.1-10), wherein the particle size is 200-700 nm, and the electric potential is -30 mV to 20 mV. The space stabilizer is one or more of hydroxypropyl cellulose, povidone K30, hydroxypropyl methyl cellulose, polyethylene glycol 6000, vitamin E polyethylene glycol succinate and croscarmellose sodium. The isoliquiritigenin nanosuspension is high in drug loading capacity and good in stability, and the cumulative dissolution rate and dissolution rate are also remarkably increased. In-vitro cell experiments show that: compared with an isoliquiritigenin raw material medicine, the capacity of inducing lung cancer A549 cell apoptosis is remarkably improved, the capacities of being taken in by tumor cells and inhibiting cancer cell proliferation are also remarkably enhanced, and a new thought is provided for improving the solubility and anti-tumor activity of indissolvable medicines.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an isoliquiritigenin nanosuspension and its preparation method and application. Background technique [0002] Isoliquiritigenin is a flavonoid compound extracted from the root of licorice, which is insoluble in water and has pharmacological activities such as anti-tumor, anti-oxidation and anti-inflammation. It can inhibit the proliferation of various cancer cells, including lung cancer, cervical cancer, breast cancer, pancreatic cancer, etc., by blocking the G0 / G1 phase or G2 / M phase. It can also induce the apoptosis of tumor cells by inducing the increase of cytoplasmic reactive oxygen species (ROS) levels, up-regulating Caspase-3, and down-regulating the expression of Bcl-2, thereby exerting anti-tumor effects. However, due to the poor water solubility and low bioavailability of isoliquiritigenin, at the same time, the method of solubilizing insoluble drugs with exc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/38A61K47/32A61K47/10A61K47/22A61K47/20A61K47/36A61K47/24A61K31/122A61P35/00
CPCA61K9/10A61K47/38A61K47/32A61K47/10A61K47/22A61K47/20A61K47/36A61K47/24A61K31/122A61P35/00
Inventor 杨建宏乔芳霞张万年侯延辉李莉曲卓刘艳华
Owner NINGXIA MEDICAL UNIV
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