Enteric nano-microparticles loaded with insulin as well as preparation method and applications of enteric nano-microparticles

An insulin and enteric technology, which is applied in the field of insulin-loaded enteric nanoparticles and their preparation, can solve problems such as low oral bioavailability, and achieve high oral bioavailability, simple and convenient administration, and relief of diabetes symptoms. Effect

Active Publication Date: 2018-08-10
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to overcome the defects and deficiencies of the above-mentioned prior art, and provide a new method for fast, efficient, and in-situ preparation of enteric nanoparticle, and the prepared nanoparticle solves the problem of existing insulin nano preparations. Problematic with low oral bioavailability

Method used

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  • Enteric nano-microparticles loaded with insulin as well as preparation method and applications of enteric nano-microparticles
  • Enteric nano-microparticles loaded with insulin as well as preparation method and applications of enteric nano-microparticles
  • Enteric nano-microparticles loaded with insulin as well as preparation method and applications of enteric nano-microparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Synthesis of quaternized chitosan (HTCC)

[0057] Chitosan (2g) was dissolved in 100mL aqueous solution containing 2wt% acetic acid, then heated to 80 o After C, 5 mL glycidyltrimethylammonium chloride (GTMAC) aqueous solution was slowly added dropwise to the solution for further reaction for 24 hours. After cooling, the resulting solution was precipitated in 10 times the volume of acetone for 3 times, then dialyzed against water for 3 days, and freeze-dried. , to obtain the final product HTCC. The degree of quaternization of HTCC is 43%.

Embodiment 2

[0058] Example 2 Preparation of Enteric Nanoparticles Loaded with Insulin

[0059] Fast nanocomposite (FNC) technology is a method for rapidly mixing polyelectrolyte aqueous solution with a multi-channel vortex mixer to prepare drug-loaded particles in an efficient, continuous and controllable way (recorded in the inventor's previous patent application number PCT / US2017 / 014080 middle). The nanoparticles prepared by this method have the advantages of small particle size, uniform size distribution, and high batch reproducibility, and the preparation process does not involve the use of organic solvents, which is very suitable for the nano-formulation of biological agents such as proteins, polypeptides, and nucleic acids. The multi-channel vortex mixer device diagram is shown in figure 1 A and 1B, figure 1 A is the overall structural diagram of the device, which is composed of three identical cylindrical metal bodies; figure 1 B is the top view of the structure of three identic...

Embodiment 3

[0078] Example 3 Particle size, potential and morphology characterization

[0079] The particle size, polydispersity index and surface potential of the particle samples in Example 2 were measured by a Malvern particle sizer, and the structure and morphology of various particles were characterized by a transmission electron microscope.

[0080] Figure 11 TEM images of composite nanoparticles (particle-a), enteric particles (particle-b1, particle-b2, particle-b3) are shown. From the electron microscope images, it can be seen that the sizes of particles-a, particles-b1, particles-b2, and particles-b3 are consistent with the particle size results measured by the Malvern particle sizer.

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Abstract

The invention discloses enteric nano-microparticles loaded with insulin as well as a preparation method and applications of the enteric nano-microparticles. The nano-microparticles are composed of nanoparticles obtained by compounding quaternization chitosan, insulin and sodium tripolyphosphate through the electrostatic interaction, and eudragit coating the surfaces of the nanoparticles. The compound nanoparticles loaded with insulin and having positive charges on the surface are prepared first by utilizing the FNC technology, and then eudragit coats the surfaces of the compound nanoparticles;the preparation method has the advantages that the continuous preparation is realized, the controllability is high, the batch repeatability is high, etc., and the obtained medicine-carrying particleshave high medicine loading capacity and high encapsulation efficiency. The enteric material coats the surfaces of the particles, after oral medication of the medicine-carrying particles, the loaded protein medicine can be effectively protected against the degradation of gastric acid and gastrointestinal tract protease, and thus the oral medication absorption efficiency of insulin at the small intestine part is improved. Compared with the subcutaneous injection, the enteric nano-microparticles loaded with insulin have the advantages that after oral medication, the good and stable effect of reducing blood glucose is shown, the high oral medication bioavailability is also obtained, and thus the application prospect is great.

Description

technical field [0001] The present invention relates to the technical field of biomedicine, and more specifically, relates to an insulin-loaded enteric nanoparticle and a preparation method and application thereof. Background technique [0002] Diabetes is a chronic metabolic disorder that can be divided into two categories: type 1 and type 2. Insulin has always been an important therapeutic drug for diabetic patients, but its traditional subcutaneous injection method has brought great physical pain or poor compliance to patients, so people have been devoting themselves to the development of non-injectable insulin preparations. Among them, oral administration of insulin is more popular among the public. Compared with other routes of administration, oral insulin has the following advantages: 1. It is convenient and non-invasive, which improves patient compliance; 2. Prevents the symptoms of hyperinsulinemia in peripheral blood and reduces the adverse reactions caused by trad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K47/69A61K47/61A61K9/50A61K9/51A61K47/34A61P3/10
CPCA61K9/5031A61K9/5153A61K38/28A61K47/6939A61P3/10A61K9/0053A61K9/5138A61K9/5192A61K47/02A61K47/36
Inventor 刘志佳孙立泷陈永明刘利新毛海泉梁锦荣孙成新
Owner SUN YAT SEN UNIV
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