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Liposome microemulsion containing nano cross-linked hyaluronic acid as well as preparation method and application thereof

A technology for cross-linking hyaluronic acid and hyaluronic acid, which is applied in the directions of liposome delivery, medical preparations of inactive ingredients, pharmaceutical formulations, etc., can solve the problem of poor use value and insufficient storage stability of liquid crystal drug delivery systems. Long, unable to form shelf life products and other problems, to prevent wrinkles, delay skin aging around the eyes, and smooth fine lines

Pending Publication Date: 2019-12-13
CHANGZHOU INST OF MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, according to the records of this patent document, the storage stability of this liquid crystal drug delivery system is not long enough, the maintenance time is only 3-6 months, and it cannot form a commodity with a long enough shelf life, and its components do not contain moisturizing factor hyaluronic acid Sodium acid, poor use value

Method used

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  • Liposome microemulsion containing nano cross-linked hyaluronic acid as well as preparation method and application thereof
  • Liposome microemulsion containing nano cross-linked hyaluronic acid as well as preparation method and application thereof
  • Liposome microemulsion containing nano cross-linked hyaluronic acid as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] (Example 1, liposome solution containing hyaluronic acid)

[0054] The liposome solution containing hyaluronic acid of the present embodiment, the liposome solution is a microemulsion, and the liposome solution is composed of the following components by weight percentage: phospholipid 1%, cholesterol 0.2%, nano-crosslinked hyaluronic acid Acid or its sodium salt 0.1%, Tween 800.20%, water balance.

[0055] The pharmaceutical surfactant used in this embodiment is Tween 80, and the pharmaceutical surfactant can also be selected from Span and Poloxamer.

[0056] The phospholipid is soybean lecithin.

[0057] The nano-crosslinked hyaluronic acid or its sodium salt raw material is prepared by the method of the Chinese patent document entitled "Nano-crosslinked sodium hyaluronate gel and its preparation method and application" filed by the applicant in 2016 Cross-linked sodium hyaluronate gel with an average particle size of 100nm to 250nm.

[0058] The preparation method ...

Embodiment 2 to Embodiment 8

[0065] (Example 2 to Example 8, liposome solution containing hyaluronic acid)

[0066] See Table 1 for the composition of the liposome solutions containing hyaluronic acid in Examples 2 to 8.

[0067] Table 1 Composition of liposome solution containing hyaluronic acid (wt%)

[0068]

[0069] See Table 2 for the average particle diameter, zeta potential, and osmotic pressure of the liposome solutions of Examples 1 to 8.

[0070] The measuring instruments of average particle diameter, zeta potential and osmotic pressure are the same as in Example 1.

[0071] Table 2

[0072]

[0073] From the detection results, the liposome solution of the present invention has high absolute value of zeta potential, high system stability, and the storage time can be as long as more than 24 months.

Embodiment 9

[0074] (Example 9, the preparation method of the liposome solution containing hyaluronic acid)

[0075] What the preparation method of the present embodiment prepared is the liposome solution containing hyaluronic acid of embodiment 1, comprises the following steps:

[0076] ① Dissolve the phospholipids, cholesterol and Tween 80 weighed according to weight percentage in ethanol, shake well to obtain lipid solution.

[0077] ②Mix the nano-crosslinked sodium hyaluronate gel with water as a dispersant evenly to obtain a hydration solution.

[0078] ③ Mix the lipid solution obtained in step ① with the hydration solution in step ②, and stir to obtain a microemulsion; the microemulsion is distilled under reduced pressure at 45°C to remove ethanol; the microemulsion after alcohol removal is passed through a high-pressure homogenizer, A liposome microemulsion solution containing hyaluronic acid is obtained.

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Abstract

The invention discloses a lipidosome microemulsion containing hyaluronic acid as well as a preparation method and an application thereof. The liposome microemulsion is prepared from the following components in percentage by weight: 0.5%-1.5% of phospholipid, 0.1%-0.6% of cholesterol, 0.05%-0.5% of nano cross-linked hyaluronic acid or sodium salt thereof, 0.1%-0.6% of a medicinal surfactant and thebalance of water. The liposome solution is used as a carrier of an ophthalmic preparation such as an eye spray, eye nutrient substances are conveyed to the surfaces of eyeballs, and lipid substancesare conveyed to the eyeballs at the same time, so that xerophthalmia caused by liposome disorder can be improved; in addition, moisturizing factor nano cross-linked sodium hyaluronate is added into the liposome solution, and cross-linked sodium hyaluronate nano particles can penetrate through eyelids to reach the surfaces of eyeballs, so that the effect of moistening the eyeballs is achieved.

Description

technical field [0001] The invention relates to a liposome microemulsion containing nano-crosslinked hyaluronic acid, a preparation method and application thereof. Background technique [0002] The main way currently used to treat dry eye is eye drops or artificial "tears", unfortunately these are not always effective. The reason is that not all of the "dry eye" is caused by too little tear fluid, but some are caused by the rapid loss of lipids caused by the disorder of liposomes on the surface of the eyeball. [0003] Dry eye is mainly divided into water-deficient dry eye, evaporative dry eye and mixed dry eye. Aqueous dry eye is caused by insufficient tear production. Evaporative dry eye is caused by excessive loss of tear fluid from the exposed eyeball surface under the condition of normal tear secretion function. Etiology (eg, meibomian gland dysfunction and eyelid closure disorders). [0004] For evaporative dry eye and mixed dry eye, eye drops or artificial "tears"...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K9/107A61K47/24A61K47/36A61P27/02
CPCA61K9/0048A61K9/12A61K9/1075A61K47/24A61K47/36A61P27/02A61K9/107A61P27/04A61K9/127
Inventor 何浩明杨一菲于一帆
Owner CHANGZHOU INST OF MATERIA MEDICA