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A kind of simvastatin-loaded bone targeting composite lipid nanoparticle and its application

A technology of simvastatin and compound lipids, which is applied in drug combinations, bone diseases, medical preparations of non-active ingredients, etc., can solve the problems of low water stability and achieve the effect of improving compliance and strong transport capacity

Active Publication Date: 2022-03-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a special member of the calcium carbonate family, amorphous calcium carbonate also has the above advantages, but its water stability is relatively low

Method used

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  • A kind of simvastatin-loaded bone targeting composite lipid nanoparticle and its application
  • A kind of simvastatin-loaded bone targeting composite lipid nanoparticle and its application
  • A kind of simvastatin-loaded bone targeting composite lipid nanoparticle and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] (1) Preparation of simvastatin-loaded bone-targeting composite lipid nanoparticles

[0019] Take 200mg CaCl 2 , accurately weighed, dissolved in 300 μL of ultrapure water, and the solution was added dropwise to 100 mL of absolute ethanol, placed in a round-bottomed flask, and sealed with a parafilm. After leaving a little air hole on the parafilm, put the round bottom flask and 3g of (NH 4 ) 2 CO 3 The glass bottles were placed together in a desiccator, and the gas diffusion reaction was carried out in a constant temperature and humidity chamber at 30°C. After reacting for 2-3 days, the absolute ethanol in the round bottom flask was centrifuged (15000 rpm for 10 min) to obtain white precipitated amorphous calcium carbonate nanoparticles. The resulting amorphous calcium carbonate nanoparticles were dispersed with an appropriate amount of absolute ethanol and then dispersed using a probe ultrasonic instrument (400W, working for 2s, stopping for 3s, ultrasonicating for...

Embodiment 2

[0036] Example 2 Bone Targeting Composite Lipid Nanoparticles (TC / GMS / ACC) Transport Amount Across MDCK Cell Monolayer Membrane

[0037] The ratio of simvastatin to soybean phospholipid 1:3, glyceryl monostearate to bone-targeting complex lipid nanoparticles 0.5:1-2:1 was used for monolayer membrane transport test. MDCK cells were seeded on Transwell polyester membrane and cultured for 7 days to form a cell monolayer. After washing the cell monolayer three times with HBSS, add 0.5mL 1mg / mL fluorescently-labeled oral composite lipid nanoparticles to the upper chamber of the Transwell for transmembrane transport for 4h, then remove all the liquid in the lower chamber, and measure the concentration of the lower chamber with a fluorescence spectrophotometer. Transport capacity of orally administered complex lipid nanoparticles. see results figure 1 , when the mass ratio of glyceryl monostearate (GMS) and composite lipid nanoparticles (PL / ACC) was 1:1, 138.68 μg of nanoparticles ...

Embodiment 3

[0038] Example 3 Transduodenal transport of bone-targeted complex lipid nanoparticles (TC / GMS / ACC) available for oral administration

[0039] The ratio of simvastatin to soybean phospholipid 1:3, and glycerol monostearate to bone-targeted complex lipid nanometer 0.5:1-2:1 was used to study the duodenal transport capacity. Female SD rats (180-200g) were randomly divided into 3 groups, with 3 rats in each group, fasting for 12h (without water) before the experiment. The rats were anesthetized with ether, killed by neck dislocation, the abdominal cavity was opened, and the duodenum about 10 cm long was quickly removed, immediately placed in Krebs-Ringer (K-R) intestinal nutrient solution at 4°C, and the small intestine was turned over after a brief flush. Use surgical thread to ligate each intestinal segment after valgus into a sac about 10 cm long (one end is tied tightly, and the other end is fixed on a thin plastic tube to facilitate sampling and fresh intestinal nutrient solu...

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Abstract

The invention provides a simvastatin-loaded bone-targeting composite lipid nanometer and application thereof. With amorphous calcium carbonate nanoparticles as the core, the surface is coated with simvastatin / soybean lecithin complex, glyceryl monostearate, and tetracycline stearic acid grafts in sequence. Glycerol monostearate, which is relatively stable in the gastrointestinal tract, is used for coating, and tetracycline stearic acid graft is used for bone-targeted modification, and at the same time, it carries soybean phospholipid / simvastatin complex, which can realize calcium supplementation and simvastatin synergistic therapeutic effect. The nanoparticles can be used orally to improve patient compliance. The bone-targeting effect can transport more calcium supplements and simvastatin to the bone tissue site to achieve their synergistic effect in the treatment of osteoporosis.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a bone-targeting complex lipid nanoparticle loaded with simvastatin and its application in the preparation of osteoporosis treatment medicine. Background technique [0002] Osteoporosis is a disease of the skeletal system characterized by microarchitectural degeneration of bone tissue, increased bone fragility, decreased bone mass, and increased risk of secondary fractures. The most serious symptom of osteoporosis is fracture. Unlike ordinary fractures, osteoporotic fractures are low-energy brittle fractures. The probability of comminuted fractures is greatly increased, and short-term treatment is difficult to work, which seriously affects the lives of patients. quality. The elderly and postmenopausal women are high-incidence groups of osteoporosis. With the increasing population aging, the incidence of osteoporosis has become higher and higher. The situation in the prevention and treatmen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/24A61K47/14A61K33/10A61P19/10A61K31/366
CPCA61K9/107A61K9/0053A61K47/24A61K47/14A61K33/10A61K31/366A61P19/10A61K2300/00
Inventor 袁弘陶珊胡富强孟廷廷王建卫
Owner ZHEJIANG UNIV
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