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Oil-in-water composite nanometer emulsion loaded with hydrophobic medicine and nutrients and preparation method thereof

A hydrophobic drug and nanoemulsion technology, applied in the field of medicine, can solve the problems of poor water solubility of hydrophobic drugs and nutrients, reduced drug efficacy, limited effective utilization of drugs and nutrients, etc., to improve oral bioavailability, promote absorption, Easily absorbed effect

Active Publication Date: 2018-06-01
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Many hydrophobic drugs and nutrients cannot be well absorbed by the human body due to poor water solubility, which reduces their efficacy in the body, thus limiting the effective utilization of these drugs and nutrients [Nature Reviews Drug Discovery6 (2007) 231-248 】

Method used

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  • Oil-in-water composite nanometer emulsion loaded with hydrophobic medicine and nutrients and preparation method thereof
  • Oil-in-water composite nanometer emulsion loaded with hydrophobic medicine and nutrients and preparation method thereof
  • Oil-in-water composite nanometer emulsion loaded with hydrophobic medicine and nutrients and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1. Bovine serum albumin (BSA, isoelectric point 4.7) and dextran (DEX, molecular weight 10 kDa) were dissolved in deionized water, the concentration of bovine serum albumin was 15 mg / mL, bovine serum albumin The molar ratio of protein to dextran is 1:6 (mass ratio is 1:0.9). The solution was stirred overnight to fully dissolve it, the pH of the solution was adjusted to 8.0 with 1 mol / L NaOH, and then the solution was freeze-dried. Put the lyophilized solid into a beaker, place it in a closed container filled with a saturated KBr solution (the relative humidity is 79%), and carry out Maillard reaction at 60°C for 48 hours to obtain bovine serum albumin-dextran Grafted complex (BD), in which approximately 73% of dextran was grafted onto bovine serum albumin. The obtained Maillard reaction product was directly used to prepare nanoemulsion without isolation. For the sake of simplicity, in the following description, the globulin concentration is used to represent t...

Embodiment 2

[0035] Example 2. Prepare @BD / PRO emulsion according to the method in Example 1, wherein the bovine serum albumin concentration is 7.5 mg / mL, the protamine concentration is 0.5 mg / mL, and the emulsification pH value is 6.0. The hydrated diameter (D h ). It can be seen from the data in Table 3 that @BD / PRO can still be successfully prepared by changing the concentration of bovine serum albumin to 7.5 mg / mL, and the particle size of the milk droplet is 398 nm; the pH value of the emulsion is adjusted to 2, 5 and 7 After that, the emulsion did not appear unstable phenomena such as flocculation and delamination, and the particle size of emulsion droplets did not change significantly.

[0036] Table 3. Emulsion particle size of freshly prepared @BD / PRO emulsion adjusted to different pH

[0037] .

Embodiment 3

[0038] Example 3. The @BD / PRO emulsion was prepared according to the method in Example 1, wherein the bovine serum albumin concentration was 10 mg / mL, the protamine concentration was 0.5 mg / mL, and the emulsification pH value was 7.0. The prepared emulsion was adjusted to pH 2, 5, and 7 with 1 mol / L HCl or NaOH, and then stored at 4°C. The properties of the emulsion were regularly observed and the hydrated diameter of the emulsion droplet (D h ). From the data in Table 4, it can be seen that the @BD / PRO emulsion can still be successfully prepared by changing the emulsification pH value to 7.0, and the particle size of the emulsion droplet is 296nm. After 40 days of storage under the same conditions, the emulsion did not appear flocculation, stratification, etc., and the particle size of emulsion droplets did not change significantly.

[0039] Table 4. Droplet size of @BD / PRO emulsion before and after storage at different pH values ​​and 4°C

[0040] .

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Abstract

The invention belongs to the technical field of medicine, particularly relates to oil-in-water composite nanometer emulsion loaded with hydrophobic medicine and nutrients and a preparation method thereof. The oil-in-water composite nanometer emulsion is characterized by being obtained by introducing protamine into a protein-polysaccharide covalence grafting emulsion. An emulsion drop is structurally characterized in that an oil drop containing hydrophobic medicine and nutrients is used as an inner core; globulin / protamine is used as an oil-water interface film; polysaccharide / protamine is positioned outside the oil drop so as to maintain the dispersion stability of the oil drop in the water phase and to promote the absorption characteristics. The prepared oil-in-water composite nanometer emulsion can be used as an oral preparation of hydrophobic medicine and nutrients. Compared with the injection preparation of the corresponding medicine, the prepared emulsion has the advantages that the oral administration efficacy can reach 30 to 40 percent of the injection preparation; under the administration condition of reaching the same treatment effect, the prepared oral emulsion has lowertoxicity than the injection preparation; in addition, the administration is more convenient.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oil-in-water composite emulsion loaded with hydrophobic drugs and nutrients. Background technique [0002] Many hydrophobic drugs and nutrients cannot be well absorbed by the human body due to poor water solubility, which reduces their efficacy in the body, thus limiting the effective utilization of these drugs and nutrients [Nature Reviews Drug Discovery6 (2007) 231-248 】. It is of great significance to design and prepare a universal oral delivery system for hydrophobic drugs and nutrients, to achieve efficient embedding, transportation and protection of hydrophobic drugs and nutrients, and to improve their absorption, oral bioavailability and therapeutic effect at home and abroad. [European journal of pharmaceutical sciences 29 (2006) 278-287; Drug discovery today 16 (2011) 354-360]. [0003] Oil-in-water nanoemulsions can efficiently load hydrophobic drugs an...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/42A61K47/36A61K31/337A61K31/12A61P35/00A23L2/52A23L33/12A23L33/125A23L33/17
CPCA23L2/52A23L33/12A23L33/125A23L33/17A23V2002/00A61K9/1075A61K31/12A61K31/337A61K47/36A61K47/42A61K2300/00A23V2200/32
Inventor 姚萍徐广锐
Owner FUDAN UNIV
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