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Tacrolimus loaded micelle and preparation method and applications thereof

A technology of tacrolimus and micelles, applied in the field of tacrolimus-loaded micelles and its preparation, can solve the problems of poor corneal penetration, poor hydrophilicity, unstable bioavailability of aqueous solution, etc., and achieve dispersion coefficient The effect of small and uniform particle size

Inactive Publication Date: 2018-11-06
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to improve the problems of poor corneal penetration, poor hydrophilicity, unstable aqueous solution and low bioavailability of tacrolimus, the present invention designs two-block biodegradable polymer block copolymers with different molecular weights. The diblock copolymer has both a hydrophilic segment and a hydrophobic segment. After loading tacrolimus, it can significantly increase the solubility and stability of tacrolimus in aqueous solution, and can carry tacrolimus to penetrate the cornea. Accumulated and released at a higher concentration in the eye, and then can fully exert the drug effect of tacrolimus to prevent and / or treat rejection after corneal transplantation

Method used

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  • Tacrolimus loaded micelle and preparation method and applications thereof
  • Tacrolimus loaded micelle and preparation method and applications thereof
  • Tacrolimus loaded micelle and preparation method and applications thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0070] A micellar-loaded tacrolimus eye drop for treating corneal transplant rejection and its preparation method, weighing 25gmPEG (2000) - b -P(LA- co -GA) (8000) (n=35, x=30, y=90) and 5g of tacrolimus powder were dissolved in 1mL of acetone, and were added dropwise into 10mL of pure water under ultrasonic stirring. After dialyzing the aqueous solution for 8 hours, add 0.5% (wt%) hydroxypropylmethylcellulose, mix well, and filter with a 0.22 μm microporous membrane. Spherical micelles with a diameter of about 91 nm and a drug loading of about 8.8% were obtained and stored at 4°C.

[0071] The drug loading means the ratio of the mass of tacrolimus in the micellar eye drops to the mass of the micelles (diblock copolymer loaded with tacrolimus).

[0072] Prepared mPEG (2000) - b -P(LA- co -GA) (8000) The NMR spectrum of figure 1 shown. The transmission electron microscope image of the prepared tacrolimus-loaded micelles is shown in figure 2 shown, from figure 2...

Embodiment 2

[0075] A micellar-loaded tacrolimus eye drop for treating corneal transplant rejection and its preparation method, weighing 25gmPEG (2000) - b -P(LA- co -GA) (12000) (n=35, x=45, y=135) and 5g of tacrolimus powder were dissolved in 1mL of acetone, and were added dropwise into 10mL of pure water under ultrasonic stirring, and the obtained mixture was rotary evaporated for 1 hour to remove acetone, and the gel After dialyzing the aqueous solution for 8 hours, add 0.5% (wt%) hydroxypropylmethylcellulose, mix well, and filter with a 0.22 μm microporous membrane. Spherical micelles with a particle size of about 103 nm and a drug loading of 9.3% were obtained and stored at 4°C.

Embodiment 3

[0077] A micellar-loaded tacrolimus eye drop for treating corneal transplant rejection and its preparation method, weighing 25gmPEG (2000) -b-P(LA-co-GA) (15000) (n=35, x=55, y=165) and 5g of tacrolimus powder were dissolved in 1mL of acetone, and were added dropwise into 10mL of pure water under ultrasonic stirring, and the obtained mixture was rotary evaporated for 1 hour to remove the acetone, and the gel After dialyzing the aqueous solution for 8 hours, add 0.5% (wt%) hydroxypropylmethylcellulose, mix well, and filter with a 0.22 μm microporous membrane. Spherical micelles with a particle size of about 113 nm and a drug loading of 9.5% were obtained and stored at 4°C.

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Abstract

The invention discloses a tacrolimus loaded micelle and a preparation method and applications thereof. The micelle comprises tacrolimus and a di-block copolymer. The di-block copolymer is mPEG-b-P(LA-co-GA) or mPEG-b-PLA, the structure of the di-block polymer is represented by the formula (I) or the formula (II), n is a positive integer (10-100), x is a positive integer (10-300), and y is a positive integer (30-300). Di-block biodegradable high molecular segmented copolymers with different molecular weights are designed and taken as a carrier to load tacrolimus so as to prepare the tacrolimusloaded micelle, which has the advantages of uniform particle size, low polydispersity index (PDI=0.1), and good stability. Eye drops prepared from the micelle can well relieve the rejection reactionsafter corneal transplantation, and compared with tacrolimus eye drops (0.05%) used in clinic, the bioavailability is much better.

Description

technical field [0001] The invention belongs to the field of macromolecule biomedicine, and more specifically relates to a tacrolimus-loaded micelle and a preparation method and application thereof. Background technique [0002] A variety of corneal diseases, such as keratoconus, corneal chemical injury, congenital corneal degeneration and corneal dystrophy, will eventually require corneal transplantation to save visual function. Among many factors affecting the success rate of corneal transplantation, rejection after keratoplasty is the primary reason for corneal transplantation failure. [0003] Local application of immunosuppressants is a routine method for the prevention and treatment of corneal immune rejection at this stage. In recent years, tacrolimus (FK506) immunosuppressant is often used in the clinical treatment of corneal immune rejection. Although some clinical effects have been achieved, there are still many problems. 1) Due to the low corneal penetration of ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/436A61P27/02
CPCA61K9/1075A61K31/436A61K47/34A61P27/02
Inventor 祝方明刘冬吴倩妮刘奕均梁华晴
Owner SUN YAT SEN UNIV
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