L-ascorbyl palmitate modified small molecule peptide liposome as well as preparation and application thereof

A technology of ascorbyl palmitate and small molecular peptides, applied in the nano field, can solve the problems of poor absorption of small molecular peptides, and achieve the effects of good biocompatibility, simple preparation method and avoiding degradation

Active Publication Date: 2022-02-08
UNIV OF SHANGHAI FOR SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method can not only solve the problem of poor absorption of small molecule peptides, but also improve the stability of small molecule peptides in the gastrointestinal environment

Method used

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  • L-ascorbyl palmitate modified small molecule peptide liposome as well as preparation and application thereof
  • L-ascorbyl palmitate modified small molecule peptide liposome as well as preparation and application thereof
  • L-ascorbyl palmitate modified small molecule peptide liposome as well as preparation and application thereof

Examples

Experimental program
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preparation example Construction

[0037] The present invention provides a kind of preparation method of the above-mentioned L-ascorbyl palmitate modified small molecule peptide liposome, comprising the following steps:

[0038] (1) mix soybean lecithin and L-ascorbyl palmitate in absolute ethanol, get supernatant after centrifugation;

[0039] (2) The supernatant obtained in step (1) is rotary-evaporated under gradient decompression conditions to remove absolute ethanol to form a thin film;

[0040] (3) centrifuging after dissolving the small molecular peptide, taking the supernatant and hydrating the film obtained in step (2) to obtain a mixture;

[0041] (4) The mixture obtained in step (3) is broken and centrifuged, and the supernatant is retained; the precipitate is repeatedly broken and centrifuged to obtain a suspension of small molecule peptide liposomes modified with L-ascorbyl palmitate.

[0042] In one embodiment of the present invention, in step (2), the gradient decompression process is first to q...

Embodiment 1

[0050] This example provides a small molecule peptide liposome modified with L-ascorbyl palmitate.

[0051] Dissolve 120 mg of soybean lecithin and 30 mg of L-ascorbyl palmitate in 40 mL of absolute ethanol, stir at room temperature for 1 hour, then centrifuge at 5000 g for 10 minutes, and take the supernatant. Transfer the supernatant into a rotary evaporating flask, first evaporate ethanol rapidly under the condition of a vacuum of 0.095MPa, then reduce the vacuum to 0.07MPa when the remaining solvent is about 10mL, and continue to slowly evaporate the remaining ethanol. The rotary evaporation temperature is At 41°C, the film was formed by rotary evaporation, and the solvent was removed. In addition, 10 mg of the small molecule peptide AFGIN was added to 15 mL of deionized water, and then the solution in which the small molecule peptide was dissolved was added to a rotary film-forming flask, and hydrated by rotating and shaking at 37°C for 1 hour at a frequency of 90 rpm. T...

Embodiment 2

[0053] This example provides a small molecule peptide liposome modified with L-ascorbyl palmitate.

[0054] Dissolve 100 mg of soybean lecithin and 20 mg of L-ascorbyl palmitate in 60 mL of absolute ethanol, stir at room temperature for 1 hour, then centrifuge at 5000 g for 10 minutes, and take the supernatant. Transfer the supernatant to a rotary evaporating flask, first evaporate ethanol rapidly under the condition of a vacuum of 0.09MPa, then reduce the vacuum to 0.06MPa when the remaining solvent is about 15mL, and continue to slowly evaporate the remaining ethanol. The rotary evaporation temperature is At 45°C, the film was formed by rotary evaporation, and the solvent was removed. In addition, 10 mg of the small molecular peptide QDGNPL was added to 10 mL of deionized water, and then the solution in which the small molecular peptide was dissolved was added to a rotating film-forming flask, and hydrated by rotating and shaking at 45°C for 1 hour at a frequency of 160 rpm....

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Abstract

The invention relates to the technical field of nanotechnology, in particular to an L-ascorbyl palmitate modified small molecule peptide liposome as well as preparation and application thereof, and solves the problem of poor absorptivity of small molecule peptide at the present stage. The L-ascorbyl palmitate modified small molecule peptide liposome comprises small molecule peptide, L-ascorbyl palmitate and soya bean lecithin, and does not contain cholesterol. During preparation, the L-ascorbyl palmitate modified small molecule peptide liposome is obtained through gradient reduced-pressure rotary evaporation film forming and circulating low-temperature ultrasonic-high-speed centrifugation. The method is simple to operate, and the particle size of the prepared liposome is small (less than 120nm). Soybean lecithin can wrap hydrophilic small molecule peptide in a hydrophilic core, so that the degradation of the small molecule peptide by intestinal environment and digestive enzyme is reduced. Meanwhile, the hydrophobic tail is embedded on the surface of the soybean lecithin by the L-ascorbyl palmitate, so that a sodium-dependent vitamin C transporter 1 can be targeted, and the absorption of small molecule peptides by small intestine cells is remarkably improved.

Description

technical field [0001] The invention relates to the field of nanotechnology, in particular to a small molecule peptide liposome modified by L-ascorbyl palmitate and its preparation and application. Background technique [0002] In recent years, food-derived small molecule peptides have attracted widespread attention due to their unique physiologically active functions, and are currently a research hotspot in the field of functional foods. Including anti-oxidation, immune regulation, antibacterial, lowering blood pressure, lowering cholesterol, etc. However, small molecular peptides have the problem of low bioavailability after oral intake. The reasons for the low oral bioavailability of small molecule peptides mainly include: (1) Poor stability, most small molecule peptides are hydrophilic, have poor stability in the complex environment of the gastrointestinal tract, and are easily digested by gastric acid, pepsin, trypsin, etc. , a variety of peptidases, etc.; (2) poor ab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K38/08A61K38/07A61P39/06A61P37/04A61P31/04A61P9/12A61P3/06B82Y5/00B82Y40/00
CPCA61K47/6911A61K47/545A61K9/0053A61K38/07A61K38/08A61P39/06A61P37/04A61P31/04A61P9/12A61P3/06B82Y5/00B82Y40/00
Inventor 宋洪东管骁彭诗雨
Owner UNIV OF SHANGHAI FOR SCI & TECH
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