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Rapamycin nano-micelle eye drops and preparation method thereof

A technology of rapamycin and nano-micelle, which is applied in the field of rapamycin nano-micelle eye drops and its preparation, can solve the problems that it is difficult to reach the drug concentration in the eye and restrict the application of rapamycin

Active Publication Date: 2017-09-01
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the unique anatomical structure of the eyeball, that is, the existence of "blood-ocular barrier" and "corneal barrier", it is difficult to achieve effective intraocular drug concentration with systemic medication and current ophthalmic preparations, which restricts the application of rapamycin in ophthalmic clinical treatment. application

Method used

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  • Rapamycin nano-micelle eye drops and preparation method thereof
  • Rapamycin nano-micelle eye drops and preparation method thereof
  • Rapamycin nano-micelle eye drops and preparation method thereof

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preparation example Construction

[0028] The invention provides a preparation method of rapamycin nano micellar eye drops, comprising the following steps:

[0029] 1) mixing polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, rapamycin, absolute ethanol and glucose to obtain a mixed solution containing rapamycin;

[0030] 2) Evaporate the mixture containing rapamycin obtained in the step 1) at a temperature of 38-42°C and a pressure of 0.085-0.095MPa for 55-65min, and then evaporate it at a temperature of 58-62°C and a pressure of 0.085 Evaporate for 12-18 minutes at ~0.095MPa to form a film;

[0031] 3) After mixing the membrane obtained in step 2) with phosphate buffer, hydrate at a temperature of 38-42°C for 10-20 minutes, and then at a temperature of 23-27°C for 170-190 minutes to obtain the hydrated the mixture;

[0032] 4) The hydrated mixed solution in step 3) is ice-bathed until transparent to obtain rapamycin nano-micelle eye drops.

[0033] In the present invention, the...

Embodiment 1

[0049] Dissolve 900.0mg of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and 50.0mg of rapamycin in 10.0ml of absolute ethanol, add 425.0mg of glucose after fully dissolving and mix; place in rotary evaporation On the instrument, evaporate at a temperature of 40.0°C and a pressure of 0.09MPa for 60.0min, then evaporate at a temperature of 60.0°C and a pressure of 0.09MPa for 15.0min to form a film; then add 10.0ml of phosphate buffer, and then Hydrate at 40.0°C for 15.0min, then hydrate at 25°C for 180.0min; then ice-bath until the solution is transparent to obtain nanomicelle eye drops with a mass percentage of rapamycin of 0.5%; the eye drops use 0.22 After sterile filtration with a μm microporous filter membrane, dilute with sterile phosphate buffer to obtain nanomicelle eye drops with a mass percentage of 0.1% rapamycin, and adjust the pH value of the eye drops to 6.8.

[0050] Phosphate buffered saline includes: Na 2 HPO 4 12H 2 O6.301m...

Embodiment 2

[0052] Dissolve 920.0mg of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and 55.0mg of rapamycin in 12.0ml of absolute ethanol, add 425.0mg of glucose after fully dissolving and mix; place in rotary evaporation On the instrument, evaporate at a temperature of 42.0°C and a pressure of 0.09MPa for 65.0min, then evaporate at a temperature of 62.0°C and a pressure of 0.09MPa for 20.0min to form a film; then add 10.0ml of phosphate buffer, and then Hydrate at 42.0°C for 20.0min, then hydrate at 25°C for 190.0min; then ice-bath until the solution is transparent to obtain nanomicelle eye drops with a mass percentage of rapamycin of 0.55%; the eye drops use 0.22 After aseptic filtration with a μm microporous membrane, it is diluted with sterile phosphate buffer to obtain nanomicelle eye drops with a mass percentage of rapamycin of 0.1%, and the pH value of the eye drops is adjusted to 7.0.

[0053] Phosphate buffered saline includes: Na 2 HPO 4 12H ...

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Abstract

The invention provides a preparation method of rapamycin nano-micelle eye drops. The preparation method comprises the following steps: mixing a polyethylene caprolactam-polyvinyl acetate-polyethylene glycol grafting polymer, rapamycin, absolute ethyl alcohol and glucose to obtain a mixed solution containing the rapamycin; carrying out evaporation and hydration steps on the mixed solution containing the rapamycin and putting the mixed solution on ice; treating in an ice bath until the mixed solution is transparent, so as to obtain the rapamycin nano-micelle eye drops. A result of the embodiment of the invention shows that after the rapamycin nano-micelle eye drops are used for treating, corneal grafts of mice and rabbits continuously keep transparent; the rapamycin nano-micelle eye drops can be used for effectively prolonging the survival time of the corneal grafts; the rapamycin nano-micelle eye drops can be used for effectively reducing inflammatory cell infiltration, inhibiting corneal edema and maintaining normal structures of the corneal grafts; CD11b+macrophage, Ly6G+neutrophil, CD11c+dendritic cells and CD4+T cells, which are infiltrated in the corneal grafts, are remarkably reduced.

Description

technical field [0001] The invention belongs to the technical field of ophthalmic disease treatment, and in particular relates to a rapamycin nano-micelle eye drop and a preparation method thereof. Background technique [0002] According to statistics, there are currently about 4 million patients who are blinded by corneal diseases in my country, and corneal transplantation is the main means for them to recover their eyesight. Corneal transplantation is to replace the cloudy or diseased part of the cornea with a transparent corneal piece, so as to increase vision, treat some corneal diseases and improve the appearance. However, the occurrence of postoperative immune rejection may lead to edema and even cloudiness of the corneal graft, which eventually leads to the failure of the operation. Research data show that the 2-year survival rate of corneal grafts in non-high-risk patients undergoing corneal transplantation for the first time is as high as 90%, while high-risk patie...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/436A61P37/06A61P27/02
CPCA61K9/0048A61K9/1075A61K31/436A61K47/34
Inventor 韦超高华刘廷王月新吴祥根向德猛张婷
Owner SHANDONG EYE INST
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