Application of F5-peptide and/or P-gp inhibitor in preparation of cross-blood-testis barrier drug, oral targeting nanoparticle and drug

Abstract

The invention discloses application of F5-peptide and / or a P-gp inhibitor in preparation of a cross-blood-testis barrier drug, and oral targeting nanoparticles and a drug, and proposes that the physical barrier of BTB is destroyed by using F5-peptide and the biochemical barrier of BTB is destroyed by using Tariquilar to inhibit P-gp, so that BTB is instantaneously'open 'and'closed', and a basic ES protein and a tight junction protein are not tightly connected with BTB near a basement membrane any more, so that the BTB is not tightly connected with the BTB near the basement membrane. According to the present invention, the FAF5T-LAN oral targeting nano-preparation carrying the active Adjudin molecule is provided, the FAF5T-LAN oral targeting nano-preparation carrying the active Adjudin molecule is expected to become the high-compliance male contraceptive, and the important social significance and the important economic value are provided, such that the exogenous drug Adjudin cannot be pumped out of the BTB by the P-gp transport protein so as to smoothly transport the Adjudin to the spermatogenic epithelium;

Description

technical field [0001] The invention relates to the technical field of biopharmaceuticals, in particular to the application of F5-peptide and / or P-gp inhibitors in the preparation of drugs across the blood-testis barrier and the oral targeting of nanoparticles and drugs. Background technique [0002] The testicular seminiferous epithelium is the starting point of the spermatogenesis process, mainly composed of supporting cells connected to the basement membrane and a variety of germ cells, and a variety of intercellular connections between supporting cells constitute the blood-testis barrier (BTB). The presence of BTB prevents the transfer of harmful substances from the blood into the testicular seminiferous epithelium, but also prevents the transfer of most small and large molecule drugs (such as peptides, proteins and gene-based drugs). Studies have shown that BTB not only hinders the transport of drugs (such as contraceptives, antiviral drugs) in the seminiferous tubules,...

AI Technical Summary

Problems solved by technology

[0004] BTB has a physical and biochemical barrier function that significantly limits drug delivery to the testis

First of all, although BTB provides a good microenvironment for spermatogenesis, it also restricts the diffusion and transport of water, electrolytes, ions, hormones, paracrine factors and other cell bypass and transcellular pathways, and also greatly limits the drug delivery. Transport across barriers, e.g., small hydrophilic drugs and macromolecular drugs that cannot easily diffuse across lipid bilayers (such as antibodies and antibody-drug conjugates), etc.

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