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A kind of insulin liposome penetration enhancer and preparation method thereof

A technology of transdermal enhancer and liposome, which is applied in liposome delivery, pharmaceutical formulations, peptide/protein components, etc., can solve problems such as the complexity of the triggering mechanism, increase the transdermal rate, and promote liposome penetration. skin, no toxic side effects

Inactive Publication Date: 2018-01-19
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The current research on macromolecular transdermal, the current high popularity is microwave, current channel, ultrasound, etc., but because of its complicated trigger mechanism, how to improve the transdermal amount and transdermal efficiency of insulin liposomes is an important issue. current hot spots

Method used

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  • A kind of insulin liposome penetration enhancer and preparation method thereof
  • A kind of insulin liposome penetration enhancer and preparation method thereof
  • A kind of insulin liposome penetration enhancer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Insulin liposome transdermal enhancer and synthesis of insulin liposome.

[0028] (1) Accurately weigh 1 g of kojic acid, dissolve it in 100 g of Phosphate Buffered Saline-Tween-20 (PBS-T), shake it for 5 minutes to obtain the accelerator, and then put it in a 4-degree refrigerator Save it for later use and take it out when in use.

[0029] (2) Preparation of insulin liposome: the rotary evaporation method prepares soybean lecithin film (lecithin 25mg, cholesterol 5mg), controls temperature during rotary evaporation to be 45 ℃, then will contain the triethanolamine hydrochloride buffer solution (1mg) of insulin ( 15mL) was poured into the film; the probe-type ultrasonic instrument was used for 10 minutes, and then placed on a rotary evaporator to rotate for 1 hour to obtain the corresponding liposome gel solution. Wherein, step (2) is embodiment 1a.

[0030] (3) Preparation of insulin flexible liposomes: prepare soybean lecithin film (lecithin 25mg, cholesterol 5mg) b...

Embodiment 2

[0034] Rat skin collection and in vitro transdermal experiment.

[0035] (1) Randomly select 10 SD rats with a body weight of 130-150g. The rats were bought and fed adaptively for 2 days before they were killed. The rat skin was peeled off, and after the abdominal skin was specially collected, the superficial adipose tissue was removed. As for storage at -80°C refrigerator.

[0036] (2) Get the skin of the rat and put it on the transdermal instrument, give different groups of corresponding kojic acid solutions (mass fraction is 0.5%, 1.0%, 1.5% and 2.0%) to process, give insulin liposome 500ug (embodiment 1a Insulin liposome) in Example 1a) was applied, and the ordinary liposome in Example 1a was applied to rat skin without kojic acid treatment, and the flexible liposome in Example 1b was applied to rat skin without kojic acid treatment. Rat skin, test rat skin transdermal amount, and compare with ordinary liposome and flexible liposome, as shown in Figure 2. Wherein, the pe...

Embodiment 3

[0038] In vivo hypoglycemic observation of insulin liposomes.

[0039] (1) Establishment of type 2 diabetes rat animal model, give high-fat feed to feed for 6 months to establish type 2 diabetes rat model, high-fat feed consists of 10% lard, 18.9% protein powder, 70% common feed , 1% cholesterol and 0.1% sodium cholate.

[0040] (2) At the beginning of the experiment, the hair on the surface of the rat was pushed away, and after kojic acid treatment of different concentrations (mass fraction was 0.5%, 1.0%, 1.5% and 2.0%), the insulin liposome (in Example 1a) was coated. Insulin liposome), in addition, choose the common liposome in Example 1a and apply it to the rat skin without kojic acid treatment, and get the flexible liposome in Example 1b and apply it to the rat skin without kojic acid treatment At 0h, 1h, 2h, 3h, 4h, 5h, and 6h, blood was taken from the tail vein, and blood glucose was measured with a Sinocare blood glucose meter to observe the hypoglycemic characterist...

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Abstract

The invention relates to a penetration enhancer for insulin liposomes as well as a preparation method of the penetration enhancer. The penetration enhancer comprises components, namely, kojic acid and PBS-T (Phosphate Buffered Saline-Tween20). The preparation method comprises steps as follows: the kojic acid is dissolved in the PBS-T, and the enhancer is obtained through vibration. The kojic acid is used as the penetration enhancer for the insulin liposomes, the penetration enhancer is wide in source and low in price and has the practical value, and the preparation method is simple. The kojic acid is used as the penetration enhancer, the penetration enhancer has the obvious effect on enhancing penetration of the insulin liposomes, the penetration rate of insulin is increased, and the enhancer has the good hypoglycemic effect.

Description

technical field [0001] The invention belongs to the field of insulin transdermal accelerator and its preparation, in particular to an insulin liposome transdermal accelerator and its preparation method. Background technique [0002] Kojic acid, also known as kojic acid and kojic acid, is a melanin-specific inhibitor. After entering skin cells, it can complex with copper ions in cells, change the three-dimensional structure of tyrosinase, and prevent the activation of tyrosinase , thereby inhibiting the formation of melanin. Kojic acid whitening active agents have better tyrosinase inhibitory effect than other whitening active agents. It does not act on other biological enzymes in the cells, and has no toxic effect on the cells. At the same time, it can also enter the intercellular matrix to form intercellular glial, which can retain water and increase skin elasticity. [0003] In human skin, under the catalysis of tyrosinase, tyrosine undergoes complex oxidation and polyme...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/22A61K9/127A61K38/28A61P3/10
Inventor 朱利民武俊紫权静吴焕岭孙晓竹李赫宇
Owner DONGHUA UNIV
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