pH-sensitive nanoparticles for oral insulin delivery

一种纳米粒子、敏感性的技术，应用在纳米粒子和其制备领域，达到避免包封率、避免低、好胰岛素释放的效果

Active Publication Date: 2013-02-06
NANO & ADVANCED MATERIALS INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

HP55 can withstand prolonged contact with the acidic gastric environment, but dissolves readily in the slightly acidic to neutral fluid of the small intestine

Method used

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  • pH-sensitive nanoparticles for oral insulin delivery
  • pH-sensitive nanoparticles for oral insulin delivery
  • pH-sensitive nanoparticles for oral insulin delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of Insulin-loaded PLGA / HP55 Nanoparticles

[0030] PLGA / HP55 nanoparticles were prepared by two different methods using HP55 as the pH sensitive substance / polymer. Method A: HP55 was dissolved in an organic phase of acetone and ethanol to form a mixture, which was used as a coating for PLGA nanoparticles to form PLGA / HP55 nanoparticles. Method B: Both PLGA and HP55 were dissolved in the organic phase dichloromethane and acetone to form a mixture which was directly used to form PLGA / HP55 nanoparticles.

[0031] Table 1

[0032]

[0033]As shown in Table 1, the encapsulation efficiency of nanoparticles in method B is higher than that in method A. The reasons for the lower encapsulation efficiency in method A are: (i) during prolonged magnetic stirring, insulin easily diffuses into the outer aqueous phase, and (ii) part of the HP55 dissolves during water washing, resulting in the protection of insulin The layer becomes thinner. In addition, the nanoparti...

Embodiment 2

[0036] Characterization of insulin-loaded PLGA / HP55 nanoparticles

[0037] figure 1 The SEM images shown indicate that the insulin-loaded PLGA / HP55 nanoparticles have a white fine powder morphology. The PLGA / HP55 nanoparticles prepared from Method B in Example 1 had an average particle size of 181.9±19.0 nm with a PDI of 0.093±0.031. The insulin encapsulation efficiency was 90.85±1.09%. The insulin-loaded PLGA / HP55 nanoparticles prepared by the double emulsion solvent evaporation method used in the method of the present invention have high encapsulation efficiency and smaller nanometer size.

Embodiment 3

[0039] Insulin release study in vitro

[0040] The amount of HP55 coated on PLGA / HP55 nanoparticles will affect the pH sensitivity of PLGA / HP55 nanoparticles. Therefore, an in vitro insulin release study was performed to determine the effect of different amounts of HP55 on the pH sensitivity of PLGA / HP55 nanoparticles. The effect of different amounts of HP55 on insulin release properties was evaluated in simulated gastrointestinal fluid. figure 2 In vitro release rates of insulin from nanoparticles with different amounts of HP55 are shown in solutions with pH=7.4 PBS (a) and pH=1.2 HCl (b), respectively.

[0041] PLGA / HP55 nanoparticles with different amounts of HP55 released more than 75% of insulin at pH = 7.4 PBS. When both PLGA and HP55 were dissolved in an organic solvent to capture insulin, the interaction between HP55 and insulin was stronger than that between PLGA and insulin; most insulin molecules tended to disperse in HP55 rather than PLGA. In the case of pH=7.4...

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Abstract

The present invention discloses the pH-sensitive nanoparticles composed of pH-sensitive polymer, hydrophobic material, internal stabilizer, external stabilizer content and insulin drug. The present invention also includes a method for preparation of pH-sensitive nanoparticles, in particular, a multiple emulsions solvent evaporation method. The pH-sensitive nanoparticles of the present invention show good pH-sensitive property with 100-300 nanometer particle size. Significant decrease in blood glucose level is observed in streptozotocin (STZ)-induced diabetic rats and the bioavailability of insulin is more than 10% after oral administration of the insulin-loaded pH-sensitive nanoparticles.

Description

[0001] Cross References to Related Applications [0002] This patent application claims priority to US Provisional Patent Application Serial No. 61 / 573,009, filed August 4, 2011, the disclosure of which is incorporated herein by reference. technical field [0003] The invention relates to a nano particle which can be used in the technical field of biomedicine and a preparation method thereof, in particular to a pH sensitive nano particle and a preparation method thereof. Background technique [0004] Diabetes is characterized by persistently high blood glucose levels. As of 2007, there are approximately 250,000,000 diabetics worldwide, especially in underdeveloped and developing countries. It is estimated that by 2025 there will be 380,000,000 patients. Diabetes is therefore a serious global problem. [0005] Because insulin has a short half-life and degrades in the gastrointestinal tract, insulin is delivered in liquid injection form for the treatment of diabetes. It ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K47/34A61K38/28A61P3/10
CPCA61K38/28Y10S977/906A61K9/5161A61K47/38A61K9/5153A61K9/5192A61K47/34A61P3/10
Inventor 章莉娟凌莉周丽英吴志民郭新东蒋薇罗茜钱宇
Owner NANO & ADVANCED MATERIALS INST
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