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Intraocular drug delivery composition and preparation method thereof

A composition and drug delivery technology, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of low eye bioavailability, short residence time, and failure to reach the posterior segment of the eye, etc., to achieve Improve the efficiency of membrane penetration and eye bioavailability, the preparation method is simple, and the effect of promoting rapid penetration

Inactive Publication Date: 2018-01-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The present invention is aimed at the poor compliance of intraocular implants and intraocular injections, which are likely to cause serious complications. Ordinary eye drops have a short retention time in the conjunctival sac and poor absorption effects, especially for biomacromolecules such as genes, polypeptides and proteins. The ocular bioavailability of the drug is extremely low, and it is almost impossible to reach the posterior segment of the eye. The membrane-penetrating peptide is used to construct a complex that can achieve intraocular drug delivery through a non-damaging route. The complex acts as a gene, polypeptide or protein The carrier of biomacromolecular drugs can efficiently penetrate the absorption barrier of the ocular surface, promote biomacromolecules to enter the eye and reach the posterior segment of the eye, thereby improving the ocular bioavailability of such drugs

Method used

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  • Intraocular drug delivery composition and preparation method thereof
  • Intraocular drug delivery composition and preparation method thereof
  • Intraocular drug delivery composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of the primary composition pRFP / BCP using branched cationic polymers (BCP) to encapsulate red fluorescent protein particles (pRFP): different concentrations of polyethyleneimine (PEI), polylysine (DGLs) Mix with polyamide-amine dendrimer (PAMAM) solution in equal volume with 0.05 mg / ml plasmid DNA solution according to a certain charge ratio (nitrogen / phosphorus ratio), vortex for 30 s, and place at room temperature for 30 min to obtain freshly prepared different Primary composition solution for charge ratio (nitrogen / phosphorus ratio);

[0036] Preparation of surface-modified penetrating peptide (CPP) composition pRFP / BCP / CPP: The pRFP / BCP primary composition prepared above was mixed with different concentrations of TAT, Penetratin, oligo-arginine short peptide Poly(arginine) n (where n=6-12), low molecular weight protamine (LMW Protamine), Transportan, VP-22, HCT (9-32) and Pvec solution are mixed in equal volumes according to a certain charge ratio, v...

Embodiment 2

[0038] Use agarose gel electrophoresis (AGE) to screen the ratio of the three components in the composition described in Example 1, which are respectively red fluorescent protein particles (pRFP), branched cationic polymers (PEI, DGLs and PAMAM ) and penetrating peptides (TAT, Penetratin, Poly(arginine) n where n=6-12, LMWProtamine, Transportan, VP-22, HCT(9-32) and Pvec). Observe DNA bands under UV light and take pictures;

[0039] The results showed that the ability of branched cationic polymer PEI to form complexes with pRFP and CPP was poor, while the complexes formed by DGLs and PAMAM were stable when the charge ratio of pRFP was 1:3-10:1. PAMAM with a molecular weight between 2,000-200,000 can form a primary complex with pRFP, and the preferred molecular weight range is 5,000-50,000. DGLs with a molecular weight between 5,000 and 200,000 can form primary complexes with pRFP, and the preferred molecular weight range is 8,000 to 80,000. A stable secondary complex can be...

Embodiment 3

[0041] According to the formulation screening results, the composition solution was prepared; the particle size and polydispersity index (PDI) of each sample were quantitatively measured with a dynamic light scattering particle size analyzer (Malvern Zetasizer Nano S). Taking the complex pRFP / BCP / Penetratin formed by red fluorescent protein particles, branched cationic polymers and Penetratin as an example, the measurement results are shown in Table 1 below:

[0042] Table 1. Particle size distribution table of pRFP / BCP / Penetratin composition

[0043]

[0044] Note: P20 means that the charge ratio of Penetratin to pRFP in the prescription is 20:1; DGLsG2 means the 2nd generation DGLs with a molecular weight of 8600; DGLsG3 means the 3rd generation DGLs with a molecular weight of 22000;

[0045] Adopt transmission electron microscope to carry out morphological detection to composition sample, the result is as attached figure 1 As shown, the shape of the complex is a solid s...

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Abstract

The invention belongs to the field of medicinal preparations, and in particular relates to an intraocular drug delivery composition and a preparation method of the intraocular drug delivery composition. The composition is a nano-composite prepared from cell-penetrating peptide, a ramous cationic polymer and a bio-macromolecular medicine, wherein in appearance, the composition is nanoparticles withthe particle size being 100-500 nm; the bio-macromolecular medicine is the medicine such as genes, polypeptides and protein with negative charges under the condition that the pH is 7.4; the electriccharge ratio of the ramous cationic polymer to the pharmaceutical molecules is (1:3) to (10:1), and the electric charge ratio of the cell-penetrating peptide to the medicine is (1:1) to (50:1). The composition is administrated by adopting the manner of dropping the medicine into the conjunctival sac, the absorption of the bio-macromolecular medicine in the eyes is promoted, and the bio-macromolecular medicine is delivered to the retina part at the posterior eye segment; with the composition, the compliance in treating eye diseases by adopting the bio-macromolecular medicines such as genes, polypeptides or protein of patients can be improved, and the bioavailability of the eyes for the medicine is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an intraocular drug delivery composition and a preparation method thereof. The drug composition realizes intraocular drug delivery through a non-damaging route, which helps to promote the absorption of drugs in the eye and improve biological The ocular bioavailability of molecular drugs can help clinically replace intraocular injections and other administration methods with low patient compliance. Background technique [0002] The prior art discloses that the eye is an important sensory organ of the human body, and its structure is mainly divided into eyeball, visual pathway (nerve tissue) and ocular appendages (including eyelids, conjunctiva, extraocular muscles, lacrimal apparatus); wherein, the cornea, The conjunctiva and sclera are the main barriers to protect the eyes from exogenous substances. Practice has proved that it is difficult for harmful foreig...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/56A61K47/59A61P27/02
Inventor 魏刚刘畅江宽陆伟跃
Owner FUDAN UNIV
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