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Drug delivery system targeting posterior segment of eye, formulation and preparation method thereof

A drug delivery system and the technology of the posterior segment of the eye, which are applied in the field of dendritic polymer compositions with targeting integrin receptors and cell penetration functions and their preparation, can solve the problem of dipeptides that are difficult to function at the same time and lose dipeptide modification And other issues

Active Publication Date: 2019-11-22
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still problems in the form of connecting the RGD peptide and the cell-penetrating peptide in series. When the targeted liposome or nanoparticle travels to the tumor or disease site, it is difficult for the double peptide to function simultaneously due to steric hindrance, thus losing The significance of dipeptide modification

Method used

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  • Drug delivery system targeting posterior segment of eye, formulation and preparation method thereof
  • Drug delivery system targeting posterior segment of eye, formulation and preparation method thereof
  • Drug delivery system targeting posterior segment of eye, formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Embodiment 1: Preparation of PAMAM-PEG-c (RGDyC) (TAT)

[0079] 1) Synthesis of PAMAM-PEG-c (RGDyC)

[0080] Weigh 4.0 generations of PAMAM (M.W.14214.17, 11.0 mg) and dissolve in 2 mL of borax-NaOH buffer (pH 8.6). Dissolve c(RGDyC) (11.0 mg) in 2 mL of PBS buffer (pH=6.0), add heterobifunctional PEG (M.W.3500, 67.0 mg) to react for 1 min, and immediately add to the borax-NaOH buffer of PAMAM solution, heated in a water bath at 28°C, protected from light, filled with nitrogen, and stirred for 12 hours. After the reaction solution was purified by dialysis in deionized water with a 14000MWCO dialysis bag, the inner solution of the dialysis was collected and lyophilized to obtain PAMAM-PEG-c (RGDyC).

[0081] 2) Synthesis of PAMAM-PEG-c(RGDyC)(TAT)

[0082] TAT (sequence RKKRRQRRRC, 5.0mg) and heterobifunctional group PEG (M.W.3500, 13.0mg) were dissolved in 2mL borax-borate buffer (pH8.0) and vortexed for 1min, then added dropwise to 4mL PAMAM-PEG - c(RGDyC) (62.0 mg...

Embodiment 2

[0084] Embodiment 2: Preparation of PAMAM-PEG-iRGD (TAT)

[0085] 1) Synthesis of PAMAM-PEG-iRGD

[0086] Weigh 4.0 generation PAMAM (M.W.14214.17, 15.0mg) and dissolve in 4mL borax-NaOH buffer (pH8.0). Dissolve iRGD (sequence c(CRGDKGPDC), 15.0mg) in 4mL PBS buffer (pH=7.2), add heterobifunctional PEG (M.W.5000, 71.0mg) to react for 1min, and immediately add to the above PAMAM In borax-NaOH buffer solution, heated in a water bath at 28°C, protected from light, filled with nitrogen, and stirred for 12 hours. After the reaction solution was purified by dialysis in deionized water with a 14000MWCO dialysis bag, the inner solution of the dialysis was collected and lyophilized to obtain PAMAM-PEG-iRGD.

[0087] 2) Synthesis of PAMAM-PEG-iRGD (TAT)

[0088] TAT (sequence RKKRRQRRRC, 7.0mg) and heterobifunctional group PEG (M.W.5000, 39.0mg) were dissolved in 2mL borax-borate buffer (pH8.5) and vortexed for 1min, then added dropwise to 8mL PAMAM-PEG - iRGD (101.0 mg) in borax-bo...

Embodiment 3

[0090] Embodiment 3: Preparation of PAMAM-PEG-c (RGDf-N (Me) (Penetratin)

[0091] 1) Synthesis of PAMAM-PEG-c(RGDf-N(Me)-V)

[0092] Weigh 5.0 generations of PAMAM (M.W.28824.81, 15.0 mg) and dissolve in 2 mL of borax-NaOH buffer (pH 8.6). First thiolate c(RGDf-N(Me)-V), then dissolve the thiolated c(RGDf-N(Me)-V) (12.0mg) in 3mL PBS buffer (pH=6.8), add iso PEG (M.W.3500, 56.0 mg) with bifunctional groups was reacted for 1 min, then immediately added to the borax-NaOH buffer solution of PAMAM, heated in a water bath at 28°C, protected from light and filled with nitrogen, and stirred for 12 h. After the reaction solution was purified by dialysis in deionized water with a 14000MWCO dialysis bag, the inner solution of the dialysis was collected and lyophilized to obtain PAMAM-PEG-cRGDf-N(Me)-V).

[0093] 2) Synthesis of PAMAM-PEG-c(RGDf-N(Me)-V)(Penetratin)

[0094] First thiolate Penetratin (sequence: RQIKIWFQNRRMKWKKK), then dissolve thiolated Penetratin (10.0mg) and heter...

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Abstract

The invention relates to the field of medicinal preparations, and concretely provides a targeting posterior segment eye drug delivery system, a preparation thereof and a preparation method of the preparation. The system comprises a drug and a polymer prepared from a dendritic polymer, polyethylene glycol, an RGD peptide and a CPP peptide, wherein the dendritic polymer is a 3.0-10.0 generation polyamide-amine dendritic macromolecule, the polyethylene glycol is polyethylene glycol with the molecular weight range of 2000-5000 Da, and the RGD peptide is cyclopeptide. The drug delivery system and the preparation thereof effectively conveys the drug to the pathologic position of a posterior segment eye, reduce damages of the drug to normal tissues, reduce the medication pains of patients, and increase the medication compliance of the patients.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a drug delivery system targeting the posterior segment of the eye and a preparation method thereof, in particular to a dendrite polymer composition with targeting integrin receptor and cell penetration functions and a preparation method thereof . Background technique [0002] Anatomically, the eyeball can be divided into two parts: the anterior segment and the posterior segment. The anterior segment mainly includes the cornea, anterior chamber, iris, lens, and ciliary body; the posterior segment includes the retina, choroid, and vitreous. Many ophthalmic diseases that cause visual impairment or even blindness occur in the retina and choroid at the back of the eye, such as age-related macular degeneration (age-related macular degeneration, AMD), diabetic retinopathy (diabetic retinopathy, DR) and choridal neovascularization (choridal neovascularization) , CNV) etc. [1] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K9/08A61K9/19A61K47/42A61K47/34A61K47/10A61K47/18A61P27/02
Inventor 孙考祥张雪梅李静静
Owner YANTAI UNIV
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