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Core-shell structured bioadhesive polymer nanoparticle, and preparation method and application thereof

A nanoparticle, core-shell structure technology, used in drug combinations, sexual diseases, pharmaceutical formulations, etc., can solve the problems of difficult to reach mucous membranes, difficult to effectively penetrate mucus, small particle size, etc., and achieve good hydrophilicity and biological viscosity. Additive effect

Active Publication Date: 2015-05-13
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, related reports on boronic acid group-functionalized materials / drug delivery systems targeting mucin on the mucus layer and mucous membranes include a contact lens with mucin affinity (CN101312754); a cyclosporine A-loaded ophthalmic nanoparticle (Shengyan Liu, Lyndon Jones, Frank X Gu, Macromol Biosci.2012 Dec;12(12):1622-6); but the boronic acid functionalized bioadhesive nanoparticles described therein exist as follows: the particle size is small ( <50nm), there are difficulties in effectively penetrating mucus, it is difficult to reach the mucous membrane, and the preparation involves the synthesis of boric acid functionalized polymers, and the process is cumbersome and other defects.

Method used

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  • Core-shell structured bioadhesive polymer nanoparticle, and preparation method and application thereof
  • Core-shell structured bioadhesive polymer nanoparticle, and preparation method and application thereof
  • Core-shell structured bioadhesive polymer nanoparticle, and preparation method and application thereof

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Embodiment 1

[0029] 1. Preparation of core-shell polymer nanoparticles

[0030] 1) Formation of silver nuclei: add 2.5mL of sodium borohydride aqueous solution (10mM) dropwise to 200mL of silver nitrate (0.1mM) and sodium citrate (0.1mM) mixed aqueous solution under stirring conditions, and react at room temperature to obtain silver nuclei ;

[0031] 2) Polymerized encapsulation: Add sodium lauryl sulfate as a stabilizer to the obtained silver core at a concentration of 0.5% (w / w). Add 4-vinylphenylboronic acid (1.00 g), N,N'-methylenebisacrylamide crosslinker (2 mg) and ethylene glycol dimethacrylate (40 μL) to 100 mL of silver core solution, and pass through N2 removes O that may be dissolved in solution 2 , add 1 mL of 0.1M 2,2'-azobisisobutylamidine dihydrochloride to initiate the polymerization reaction, and react at 70°C for 5 hours;

[0032] 3) Separation and purification: The reaction solution obtained in 2) was dialyzed with pure water for 72 hours to remove unreacted monomers ...

Embodiment 2

[0042] Drug loading of embodiment 2 core-shell structure polymer nanoparticles

[0043] In this example, recombinant human α-interferon was used as a model drug, which was dissolved in 10mM citric acid / sodium citrate with pHs of 4, 5, and 6 and Tris-HCl buffer solutions with pHs of 7, 8, and 9, respectively. , so that the concentration is 0.8mg / mL. Mix the above 6 kinds of interferon solutions and nanoparticle dispersion (10mg nanoparticle per ml) at a volume ratio of 1:1, place at room temperature overnight, after centrifugation, measure the interferon concentration in the supernatant with a BCA kit, according to the following formula Calculate drug loading.

[0044] Drugloading ( mg / mg ) = ( C Drug , origin ...

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Abstract

The invention belongs to the field of medicinal preparations, and relates to a core-shell structured bioadhesive polymer nanoparticle for vaginal administration, and a preparation method and an application thereof. The polymer nanoparticle adopts a silver nanoparticle as a core, and is prepared through copolymerizing an acrylamide cross-linking agent and a mono-olefin phenyl boric acid function monomer on the surface of the silver nanoparticle to form a shell. The polymer nanoparticle has good affinity to mucoproteins, has a long in-vivo retention time after mucosal administration, and has good practical values and application prospect in the vaginal administration field.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a bioadhesive polymer nanoparticle with a core-shell structure, a preparation method thereof and an application in vaginal administration. Background technique [0002] The prior art discloses that when the drug is administered to the mucous membrane of the vagina and other parts, the bioadhesive drug delivery system can realize the continuous and tight contact between the preparation and the mucous membrane, and the drug released continuously from the drug delivery system may be maintained locally. High concentration, long-term onset, or continuous absorption into the body circulation, play a role in the whole body. Studies have shown that for vaginal administration, bioadhesive nanoparticles with a particle size of 100-500nm have no foreign body sensation, are easy to distribute, and have strong mucus penetration ability, which is one of the most ideal for...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F230/06C08F222/38C08F222/14C08K3/08A61K47/32A61K38/21A61P15/02
Inventor 刘瑜李春燕许书源陆伟跃
Owner FUDAN UNIV
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