Application of celastrol to preparing eye drop preparation for inhibiting alkali burn corneal neovascularization and promoting corneal alkali burn healing
A corneal neovascularization and triptolide technology, which is applied in the field of biomedical materials and medicine, can solve the problems of undiscovered ophthalmic diseases, limited clinical application and curative effect, poor water solubility, etc., and achieves inhibition of alkali-burned corneal neovascularization, The effect of promoting corneal alkali burn healing and high encapsulation efficiency
Active Publication Date: 2017-01-04
河南省眼科研究所
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Problems solved by technology
Although Celastrol has strong biological activity and is a potential drug for anti-inflammation and anti-corneal neovascularization, its poor water solubility limits its further clinical application and curative effect. Reports on Eye Diseases
Method used
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Effect test
Embodiment 1
[0016] Weigh 10.0 g of ternary block copolymer PEG-PCL-PEI and 3.0 g of tripterine, and dissolve them together in 20 mL of a mixed solvent consisting of methanol and acetonitrile at a volume ratio of 1:1; then, under ultrasonic stirring, Add the mixture dropwise to 50mL of water for injection, vacuum distill to remove the organic solvent, and then pass through an ultrafiltration device (molecular weight cut-off: 100,000 Da) for 3 times to remove free tripterine to obtain drug-loaded polymer micelles , adding water for injection to make the volume to 100mL, to obtain tripterine eye drops.
Embodiment 2
[0018] The difference from Example 1 is: 10.0 g of PEG-PCL-PEI, 1.5 g of tripterine, and the others are the same as in Example 1.
Embodiment 3
[0020] The difference from Example 1 is: 10.0 g of PEG-PCL-PEI, 0.75 g of tripterine, and the others are the same as in Example 1.
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Abstract
The invention belongs to the field of biomedical-material-and-medical crossover, and particularly discloses an application of celastrol to preparing an eye drop preparation for inhibiting alkali burn corneal neovascularization and promoting corneal alkali burn healing. 7.04 g-67.55 g of triblock copolymer PEG-PCL-PEi and 0.68 g-2.11 g of the celastrol are weighed and jointly dissolved into a mixed solvent prepared from methyl alcohol and acetonitrile in the volume ratio of 1:(1-3); under ultrasonic stirring, mixed liquid is dropwise added into dissolving equivalent amount of injection water, an organic solvent is removed in a vacuum-distillation mode, dissociative celastrol is removed in an ultra-filtration mode, a medicine loading polymeric micelle is obtained, injection water is additionally added till the volume is fixed to be 100 mL, and eye drop is obtained. According to the celastrol, the PEG-PCL-PEi firstly serves as a carrier, and loads the celastrol, the eye drop is prepared, the medicine feeding mode of eye-surface dropping is achieved, and the celastrol has the milepost-type significance.
Description
technical field [0001] The invention belongs to the interdisciplinary field of biomedical materials and medicine, and specifically relates to the application of tripterine in the preparation of eye drops for inhibiting alkali-burned corneal neovascularization and promoting corneal alkali-burn healing. Background technique [0002] Corneal alkali burn is a common blinding eye disease in ophthalmology. Once it occurs, the treatment is quite difficult and the prognosis is extremely poor. Many studies have shown that after corneal alkali burn, various effector cells and inflammatory cells participate in the pathological injury process, and the subsequent immune inflammatory response can cause corneal ulcers, perforations, corneal neovascularization, secondary glaucoma and concurrent cataracts, etc. , its prognosis is closely related to the extent, time, and treatment of corneal damage. Inhibiting the formation of corneal neovascularization and promoting corneal wound healing are...
Claims
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IPC IPC(8): A61K31/56A61K9/107A61K47/34A61P27/02
CPCA61K9/0048A61K9/1075A61K31/56A61K47/34
Inventor 栗占荣李景果张颖祝磊张俊杰王丽娅
Owner 河南省眼科研究所
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