Hyaluronic acid modified ethosome, acupoint drug delivery system containing hyaluronic acid modified ethosome and application of system

A technology of hyaluronic acid modification and hyaluronic acid, which is applied in the field of medicine, can solve the problems of drug loss and slow diffusion, and achieve the effect of enhancing absorption, increasing delivery, and improving the effect of treatment

Pending Publication Date: 2021-12-03
SHANGHAI UNIV OF T C M
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The purpose of the present invention is to overcome the defect that the existing acupoint drug delivery system is easily trapped in the epidermis of the lipid environment after percutaneous administration when the volatile oil of Dingguisan is coated, and the deep layer of the acupoint area diffuses slowly and easily causes drug loss. , to provide an acupoint drug delivery system that can effectively contain the effective parts of Dingguisan volatile oil, and at the same time deliver the drug to the deep layer of the acupoint area, thereby strengthening the special effect of the acupoint area after administration of the umbilicus

Method used

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  • Hyaluronic acid modified ethosome, acupoint drug delivery system containing hyaluronic acid modified ethosome and application of system
  • Hyaluronic acid modified ethosome, acupoint drug delivery system containing hyaluronic acid modified ethosome and application of system
  • Hyaluronic acid modified ethosome, acupoint drug delivery system containing hyaluronic acid modified ethosome and application of system

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Experimental program
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Effect test

Embodiment 1

[0058] Construction of a novel acupoint drug delivery system with hyaluronic acid-modified ethosomes (HA-ES) loaded with Dingguisan volatile oil

[0059] 1.1 Extraction of Dingguisan volatile oil

[0060] Referring to the clove and cinnamon medicinal materials stipulated in the 2015 edition of "Chinese Pharmacopoeia", weigh 200.3g clove and 200.6g cinnamon medicinal materials, crush them into a 20-mesh coarse powder, add 8 times the amount of water, soak for 1h, and extract by steam distillation at 200°C for 6h , to collect the volatile oil. Get 3mL cinnamon volatile oil and 15mL clove volatile oil. After it is mixed evenly, it is used as Ding Gui scattered volatile oil. Using HPLC detection, the contents of eugenol and cinnamon aldehyde in clove volatile oil and cinnamon volatile oil were 85.8±0.43% and 93.1±4.45%, respectively, which met the quality standards for “clove” and “cinnamon” medicinal materials in the 2015 edition of the Chinese Pharmacopoeia.

[0061] 1.2 Synt...

Embodiment 2

[0066] Evaluation and characterization of hyaluronic acid-modified ethosomes (HA-ES) loaded with Dingguisan volatile oil:

[0067] 2.1 Determination of particle size and potential

[0068] The particle size distribution of each nano-preparation was measured by a dynamic light scattering method with a Malvern particle size potentiometer. Three samples were prepared in parallel, and the particle size and Zeta potential were measured. The results showed that the average particle size of HA-ES loaded with Dingguisan volatile oil was 299.5±54.3nm, and the Zeta potential was -31.7±0.47mV.

[0069] 2.2 Transmission electron microscope observation

[0070] Each preparation was diluted with deionized water to a certain multiple, dropped on the copper grid, and after natural drying, it was negatively stained with uranyl acetate for 2 minutes, and then the excess negative staining solution was absorbed with filter paper, dried, and observed under a transmission electron microscope Pre...

Embodiment 3

[0084] In vitro transdermal behavior:

[0085] 3.1 In vitro transdermal behavior

[0086] Take SD rats, anesthetized with 10% chloral hydrate, depilate the abdomen with a razor, scrub with normal saline, peel off the abdominal skin with a scalpel, remove subcutaneous tissue and fat, wash with normal saline, store in a -4°C refrigerator, and use within one week , Check the integrity of the mouse skin carefully before use. The modified Franze diffusion cell was used, and the isolated mouse skin was taken, with the cuticle facing the supply pool and the subcutaneous tissue facing the receiving pool. The receiving tank was filled with receiving solution (12.5 mL of 10% PEG-200 / PBS [w / v] solution), the air bubbles were exhausted, and the mixture was equilibrated for 30 min. Add 1mL of the preparation to the supply pool, so that the stratum corneum layer is in good contact with the preparation. The supply cell was sealed with a parafilm, and the receiving solution was magneticall...

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Abstract

The invention discloses hyaluronic acid modified ethosome, an acupoint drug delivery system containing the hyaluronic acid modified ethosome and application of the system. The hyaluronic acid modified ethosome is formed by inserting a phospholipid material into a phospholipid membrane of ethosome, wherein the phospholipid material is formed by grafting hyaluronic acid to dioleoyl phosphatidyl ethanolamine molecules through covalent bonds. The acupoint drug delivery system containing the hyaluronic acid modified ethosome comprises the hyaluronic acid modified ethosome and more than one traditional Chinese medicine for warming middle and dispelling cold or extract of the traditional Chinese medicine, wherein the traditional Chinese medicine or extract is coated in the hyaluronic acid modified ethosome. The acupoint drug delivery system can be applied to treatment of ulcerative colitis and symptoms such as stomachache, diarrhea and dysmenorrhea caused by cold symptoms. HA is used for modifying the ethosome, leakage of entrapped medicine can be reduced, the stability of the preparation is effectively improved, and therefore delivery of the medicine to the skin along with a carrier is increased; and HA-ES is selected as a transdermal delivery carrier of the traditional Chinese medicine for warming the middle and dispelling cold or the extract thereof, and the HA-ES can strengthen the special effect of an acupoint area after administration, so that the HA-ES can be used for treating symptoms such as stomachache, diarrhea and dysmenorrhea caused by cold symptoms.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a hyaluronic acid-modified ethosome, an acupoint drug delivery system containing it and the application of the system. Background technique [0002] Acupoint transdermal drug delivery is a drug delivery method based on the theory of "external treatment of traditional Chinese medicine". The international medical community has also conducted in-depth research on this science, and this unique drug delivery method is called the transdermal drug delivery system ( trandermal therapeutic systems, TTS), it is administered on the surface of the skin, through the dilation of pores, so that the drug passes through each layer of the skin at a constant speed (or close to a constant speed), and enters the systemic circulation to produce systemic or local therapeutic effects. [0003] Umbilicus administration is one of the most distinctive traditional Chinese medicine meridian and acupoint admin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K9/127A61K36/61A61K9/00A61P29/00A61P1/12A61P15/00A61P1/04A61P1/00
CPCA61K47/36A61K9/127A61K36/61A61K36/54A61K9/0014A61P29/00A61P1/12A61P15/00A61P1/04A61P1/00A61K2300/00
Inventor 张永太冯年平张洪宇王志郭腾侯晓琳何泽慧
Owner SHANGHAI UNIV OF T C M
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