Sustained-release hydrogen sulfide donor microsphere as well as preparation method and application thereof

A hydrogen sulfide donor and microsphere technology, which is applied in the direction of pharmaceutical formulations, microcapsules, sulfur/selenium/tellurium active ingredients, etc., can solve the problem of large particle size distribution span of porous microspheres, poor delivery effect, poor particle size uniformity, etc. question

Active Publication Date: 2020-03-06
SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Usually, the method of preparing drug-loaded porous microspheres is the emulsification and volatilization method. The biggest problem of this method is that the prepared porous microspheres have a large particle size distribution span and poor particle size uniformity, which leads to poor delivery effect.

Method used

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  • Sustained-release hydrogen sulfide donor microsphere as well as preparation method and application thereof
  • Sustained-release hydrogen sulfide donor microsphere as well as preparation method and application thereof
  • Sustained-release hydrogen sulfide donor microsphere as well as preparation method and application thereof

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preparation example Construction

[0035] The first aspect of the present invention provides a preparation method of slow-release hydrogen sulfide donor microspheres, comprising:

[0036] a) providing a dispersed phase, the dispersed phase being an emulsion comprising a water phase and an oil phase, the oil phase being selected from an organic solution comprising a donor microsphere material and ACS14;

[0037] b) providing a continuous phase;

[0038] c) distributing the dispersed phase provided in step a) in the continuous phase provided in step b) to provide microsphere droplets of the dispersed phase;

[0039] d) solidifying, washing and drying the microsphere droplets provided in step c).

[0040]The preparation method of the sustained-release hydrogen sulfide donor microspheres provided by the present invention may include: providing a dispersed phase, the dispersed phase is an emulsion comprising a water phase and an oil phase, and the oil phase is selected from materials comprising donor microspheres ...

Embodiment 1

[0051] Preparation of microspheres:

[0052] Configure 100 milliliters of polyvinyl alcohol aqueous solution with a mass concentration of 5% (w / v), 50 milliliters of which are sucked into a 50 milliliter syringe, the head of the syringe is connected to one end of the continuous phase capillary, and another 50 milliliters of polyvinyl alcohol aqueous solution is packed into a 100 milliliter crystallizer with a capacity of 100 milliliters. dish for collection.

[0053]Configure 1 ml of ammonium bicarbonate aqueous solution with a mass concentration of 5% (w / v), configure the mass ratio of polylactic acid-glycolic acid and hydrogen sulfide-releasing aspirin to be 2:1 and configure the mass concentration of polylactic acid-glycolic acid to be 3%. (w / v) 3 milliliters of dichloromethane solution, the two were mixed and ultrasonically broken into a homogeneous emulsion, collected with a 5 milliliter syringe, and the head of the syringe was connected to one end of the dispersed phase ...

Embodiment 2

[0059] Biosafety of ACS-14 drug-loaded microspheres:

[0060] CCK-8 kit was used to detect the cell viability of pulmonary artery endothelial cells (HPAECs) incubated with ACS-14 and ACS-14 drug-loaded microspheres at the same concentration and time.

[0061] The experimental steps are as follows:

[0062] 1. Add 100 μl of cell suspension to the cultured HPAECs in a 96-well plate at a cell density of 5000 cells / well.

[0063] 2. Incubate overnight in an incubator.

[0064] 3. Add MSs (75.4mg / L), ACS-14 (50μM) and ACS-14MSs (50μM) respectively to the 96-well plate, the molecular weight of ACS-14 is 388.99g / mol, and the drug loading capacity of the microspheres is 25.8%, so The concentration of microspheres was (50*388.99*10^-3) / 25.8%=75.4mg / L) respectively for 0h, 6h, 12, and 24h.

[0065] 4. Add 10 μl CCK-8 solution to each well and incubate in the incubator for 2 hours.

[0066] 5. Measure the absorbance at 450 nm with a microplate reader.

[0067] The specific experimen...

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Abstract

The invention relates to the field of high polymer materials, in particular to a sustained-release hydrogen sulfide donor microsphere as well as a preparation method and an application thereof. The preparation method of the slow-release hydrogen sulfide donor microspheres comprises the following steps: providing a dispersion phase which is an emulsion comprising a water phase and an oil phase, andselecting the oil phase from an organic solution comprising a donor microsphere material and ACS14; providing a continuous phase; distributing the dispersed phase in the continuous phase to provide microsphere droplets of the dispersed phase; and solidifying, washing and drying the provided microsphere liquid drops. The invention constructs the biodegradable high-molecular polymer microsphere capable of slowly releasing H2S. The prepared drug-loaded porous microspheres are good in particle size monodispersity, uniform in size and good in aerodynamic performance and can be inhaled and administrated through the respiratory tract, the lung targeting property and the biological tolerance of the drug are improved, and the effect of hydrogen sulfide for treating pulmonary arterial hypertensionis greatly enhanced.

Description

technical field [0001] The invention relates to the field of polymer materials, in particular to a slow-release hydrogen sulfide donor microsphere and its preparation method and application. Background technique [0002] Pulmonary hypertension is a complex disease of the cardiopulmonary vascular system, which is mainly manifested by elevated vascular pressure and pulmonary vascular remodeling, severely restricting the function of the right ventricle, and leading to right heart failure and even death. Currently commonly used therapeutic drugs include endothelin receptor antagonists, prostacyclin and its analogs, and phosphatase inhibitors. The main problem with these drugs is that they usually need to be used in combination and have low targeting, and the side effects of the drugs are large. Endogenous hydrogen sulfide gas is a gas medium that participates in various physiological activities of the human body, and plays a role in relaxing blood vessels and lowering blood pre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/34A61K9/72A61K31/616A61K33/04A61P11/00A61P9/12
CPCA61K9/007A61K9/5031A61K31/616A61K33/04A61P9/12A61P11/00
Inventor 张绘莉陈爱政高祺张卉郝浏智
Owner SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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