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N-trimethyl chitosan modified baicalein ophthalmic lipid nanoparticle preparation and preparation method thereof

A technology of trimethyl chitosan and lipid nanoparticles, applied in the field of medicine, can solve problems such as low bioavailability, and achieve the effects of simple preparation process, improved compliance and strong drug-carrying capacity

Inactive Publication Date: 2019-07-26
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the bioavailability of traditional eye drops is extremely low (less than 5%)

Method used

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  • N-trimethyl chitosan modified baicalein ophthalmic lipid nanoparticle preparation and preparation method thereof
  • N-trimethyl chitosan modified baicalein ophthalmic lipid nanoparticle preparation and preparation method thereof
  • N-trimethyl chitosan modified baicalein ophthalmic lipid nanoparticle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation method of the baicalein ophthalmic lipid nanoparticle preparation of N-trimethyl chitosan modification comprises the steps:

[0040] (1) Take 310mg glycerol monooleate, 34.1mg poloxamer 407, 10mg baicalein, add appropriate amount of absolute ethanol, melt in a water bath at 55°C, and ultrasonicate for 5 minutes under the condition of power 400W to make them all Dissolved; rotary steaming under reduced pressure at 55°C to remove ethanol to obtain a homogeneous oil phase;

[0041] (2) Add 0.03mg of Gelucire 44 / 14 and 60mg of N-trimethyl chitosan with a viscosity-average molecular weight of 400,000 and a degree of quaternization ≥ 60% into 30mL of 20mM Tris-Hcl solution with a pH of 6.0, and heat to 55 °C and stirred until completely dissolved to obtain an aqueous phase;

[0042] (3) Add the water phase to the oil phase, shear and disperse at 10000rpm for 2min; cool to room temperature, and under the condition of power 400W, ultrasonicate for 5min to obtai...

Embodiment 2

[0045] The preparation method of the baicalein ophthalmic lipid nanoparticle preparation of N-trimethyl chitosan modification comprises the steps:

[0046] (1) Take 210mg glycerol monolinoleate, 16.8mg poloxamer 188, 5mg baicalein, add appropriate amount of absolute ethanol, put it in a water bath to melt at 35°C, and under the condition of power 300W, ultrasonic for 3min to make it All dissolved; rotary steaming under reduced pressure at 35°C to remove ethanol to obtain a homogeneous oil phase;

[0047] (2) Add 0.01mg of Labrasol and 60mg of N-trimethyl chitosan with a viscosity average molecular weight of 400,000 and a degree of quaternization ≥ 60% into 30mL of 20mM Tris-Hcl solution with a pH of 6.0, heat to 35°C and stir until completely dissolved to obtain an aqueous phase;

[0048] (3) Add the water phase to the oil phase, shear and disperse at 10,000rpm for 0.5min; cool to room temperature, and ultrasonicate for 3min under the condition of power 300W to obtain N-trime...

Embodiment 3

[0050] The preparation method of the baicalein ophthalmic lipid nanoparticle preparation of N-trimethyl chitosan modification comprises the steps:

[0051] (1) Take 510mg of diglycerin oleate, 91.8mg of polyvinyl alcohol, 30mg of baicalein, add appropriate amount of absolute ethanol, put it in a water bath to melt at 75°C, and under the condition of power of 500W, ultrasonic for 7min to dissolve them all; Rotary evaporation under reduced pressure at 75°C to remove ethanol to obtain a homogeneous oil phase;

[0052](2) Add 0.05 mg Transcutol P and 60 mg of N-trimethyl chitosan with a viscosity average molecular weight of 400,000 and a degree of quaternization ≥ 60% into 30 mL of 20 mM Tris-Hcl solution with a pH of 6.0, heat to 75 ° C and Stir until completely dissolved to obtain an aqueous phase;

[0053] (3) Add the water phase to the oil phase, shear and disperse at 10,000rpm for 3min; cool to room temperature, and under the condition of power 500W, sonicate for 7min to obt...

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Abstract

The invention discloses an N-trimethyl chitosan modified baicalein ophthalmic lipid nanoparticle preparation and a preparation method thereof. The preparation method includes (1) taking a lipid material, a stabilizer and baicalein, adding anhydrous ethanol, placing the mixture in a water bath for melting and conducting ultrasonic treatment to make all dissolved; conducting decompression spinning steaming to remove ethanol to obtain an oil phase; (2) adding a permeation enhancer and N-trimethyl chitosan to 20mM of Tris-Hcl solution with the pH of 6.0, stirring till complete dissolution, heatingto obtain an aqueous phase; (3) adding the aqueous phase to the oil phase and conducting shearing dispersion; cooling to the room temperature and conducting ultrasonic dispersing to obtain the N-trimethyl chitosan modified baicalein ophthalmic lipid nanoparticle preparation. The preparation has large membrane surface area, strong drug-loading capacity, good biocompatibility, high bioadhesion andlow eye irritation.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an N-trimethyl chitosan-modified baicalein ophthalmic lipid nanoparticle preparation and a preparation method thereof. Background technique [0002] Modern pharmacological studies have shown that baicalein has anti-inflammatory, anti-oxidation, free radical scavenging, anti-allergic, diuretic, choleretic, cholesterol-lowering, anti-thrombotic, and asthma-relieving effects. It has shown broad prospects in inhibiting ocular inflammatory response, resisting oxidative stress damage, and preventing eye diseases such as keratitis, glaucoma and retinopathy. However, baicalein is poorly soluble in water and has poor bioavailability, making it difficult for common preparations to exert biological activity through traditional ocular administration routes. [0003] Eye drops are easy to be accepted by patients because of their advantages of convenient administration, non-invasiveness, and low price...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/36A61K31/352A61P27/02A61P27/06
CPCA61K9/0048A61K9/5161A61K31/352A61P27/02A61P27/06
Inventor 刘睿李金景金鑫杨洋
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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