CN102697664B - Tanshinone lipidosome and preparation method thereof - Google Patents

Abstract

The invention discloses tanshinone lipidosome which takes tanshinone as the carrier and has the effects of resisting bacteria, resisting resistance, removing acne and eliminating acne marks. The tanshinone lipidosome is characterized in that the preparation method of the lipidosome is a propylene glycol injection method and the carrier comprises the following components according to weight percent: 0.01 to 5% of tanshinone, 8 to 25% of emulsifier, 2 to 18% of lecithin, and 0.1 to 1% of antioxidant, and the rest is deionized water, wherein the material of emulsifier is a compound taken from atleast two of the following materials: Tween 20, Tween 60, Tween 80, PEG-200, alcohol, propylene glycol and 1,3-butanediol; the material of lecithin is taken from the following compounds: egg yolk lecithin and soya lecithin; and the antioxidant is vitamin E acetate. The lipidosome preparation agent has good stability and can carry high-content tanshinone; and the preparation method is simple and controllable, has good repeatability and can be applied to cosmetic for removing acne and eliminating acne marks.

Description

Tanshinone liposome and preparation method thereof

Technical field

The invention belongs to the carrier system technical field in the cosmetics technology of preparing, relate to a kind of nano carrier and preparation method thereof, particularly a kind of is the preparation method of the liposome of active component with the TANSHINONES.

Background technology

Radix Salviae Miltiorrhizae cold nature bitter in the mouth has the effect of blood circulation promoting and blood stasis dispelling, nourishing blood to tranquillize the mind, menstruction regulating and pain relieving, removing heat from blood eliminating carbuncle, is the blood-activating stasis-removing kind Chinese medicine of using always.The content of TANSHINONES (tanshinone) in salviamiltiorrhizabung (SalviamiltiorrhizaBge) is higher, and stronger physiologically active is arranged, and is one of main effective ingredient of Radix Salviae Miltiorrhizae.Studies show that tanshinone all contains o-quinone or para-quinoid structure, has natural anti-oxidation effect, cardiovascular pharmacological effect and antibacterial and anti-inflammation functions.

TANSHINONES is supercritical (carbon dioxide) extract or the extract of organic solvents such as ether, alcohol of salviamiltiorrhizabung root, wherein contains multiple composition, the general name TANSHINONES.The various preparations of tanshinone medicine have been widely used in diseases such as treatment cardiovascular and cerebrovascular vessel, hepatitis, dermatosis and ulcer.TANSHINONES also has the effect of eliminating cutaneous pigmentation, speckle and treatment acne, has been applied in some functional cosmetics, but because of its poorly water-soluble, half-life weak point, has limited the application on market.

Liposome (liposome) is that Britain scholar Bangham and Standish found in nineteen sixty-five; 1971, people such as Lai Men began liposome is used for pharmaceutical carrier.Liposome is made up of phospholipid and additives, and phospholipid is amphiprotic substance, has hydrophilic and lipophilic group on its structure, and commonly used have lecithin, a fabaceous lecithin etc.The hydrophilic stem that constitutes the lipoid of bilayer forms the surfaces externally and internally of film, and lipophilic end section is in the centre of film, and wall thickness is about 5～7nm, and the diameter of capsule is generally between 25～50nm.This structure of liposome can enough be carried various hydrophilic or lyophobic dusts.Can be divided into according to structure and particle diameter: unilamelar liposome, multilamelar liposome, contain surface-active liposome etc.

Liposome is similar to biofilm structure, can stronger affinity be arranged with cell membrane, and penetrating ability that can the enhanced activity thing improves curative effect; Drug encapsulation becomes liposome, can prolong action time, reduces elimination factor; Active matter can be controlled the release of active matter after wrapping up, can control it in in-house distribution by the size that changes liposome.

Summary of the invention

The object of the invention is to provide the cosmetics-stage Liposomal formulation of the character gentleness that a kind of stability is high, TANSHINONES load content is high, solved poorly water-soluble in the prior art, TANSHINONES content low, can not directly apply to problem such as cosmetics.

In order to solve these problems of the prior art, technical scheme provided by the invention is:

A kind of tanshinone liposome, described carrier loaded active ingredient is TANSHINONES, it is characterized in that composition is counted by its percentage by weight in the described liposome:

All the other are deionized water;

Wherein phospholipid is selected from a kind of of following chemical compound: Ovum Gallus domesticus Flavus lecithin, soybean lecithin; Antioxidant is Vitamin E acetate.

Preferably, described first emulsifying agent is selected from following chemical compound: polysorbas20, polysorbate60, Tween 80; Second emulsifying agent is propylene glycol.

Another object of the present invention is to provide a kind of method for preparing described tanshinone liposome, it is characterized in that said method comprising the steps of:

(1) presses formula proportion weighing emulsifying agent, lecithin, TANSHINONES and antioxidant, with raw material mixing post-heating and stir the homogeneous system of the oil phase that obtains being in a liquid state;

(2) press formula proportion weighing deionized water, heating obtains water;

(3) in 30-60 ℃ homogeneous system, add 30-60 ℃ water, in stir speed (S.S.) is the constant speed stirrer of 200r/min ~ 800r/min, stir 3 ~ 30min and obtain liposome solutions;

(4) the liposome solutions cool to room temperature is namely got described tanshinone liposome.

Preferably, the particle mean size of the liposome particles that obtains of described method is at 0.1 ~ 20um.

Preferably, the emulsifying agent of described method use is that first emulsifying agent and second emulsifying agent combine according to formula proportion.

Another purpose of the present invention is to provide the application of a kind of described tanshinone liposome aspect the preparation skin protection cosmetics.

Composition is counted by its percentage by weight in the preferred tanshinone liposome:

All the other are deionized water.

The application of the liposome that another purpose of the present invention is to provide a kind of load that TANSHINONES is arranged aspect the preparation skin protection cosmetics.

The present invention is applied to nanotechnology in the cosmetic field.Defective to traditional handicraft has been carried out good improvement.Liposome is that the bilayer that constitutes with lipoids (as lecithin, cholesterol) is that the film material comprises the microgranule that forms.Liposome is as pharmaceutical carrier, because its phospholipid is biodegradable, nontoxic, non-immunogenicity, biocompatibility is very good, and self-isolation on the structure, have protection medicine biological activity, effectively control drug release, thereby reach prolong half-life, improve effects such as curative effect; And liposome has the class cellularity, thereby improves the toxicity of the therapeutic index of medicine, the dosage that reduces medicine and reduction medicine.Liposome has advantages such as bioavailability height, Thermodynamically stable, viscosity be low, thereby can adopt liposomal systems to improve the bioavailability of TANSHINONES.

Utilize liposome technology that TANSHINONES is wrapped up, increase its load content, and improving its water solublity, can effectively to solve TANSHINONES not high at cosmetics product formula content, the problem of poorly water-soluble.

With respect to scheme of the prior art, advantage of the present invention is:

A kind of tanshinone liposome of the present invention is controlled.Can to prepare TANSHINONES content be 0.01 ~ 5% liposome by regulating conditions such as temperature, mixing speed.

Liposome preparation technology among the present invention improves its activity substance content, is conducive to give full play to the effect of the flat trace of anti-pox of active substance.The liposome stability of the present invention preparation is better, has good water solublity, makes that the preparation of the cosmetics that contain tanshinone liposome is convenient, simple.

The raw material of the tanshinone liposome that the present invention prepares and skin have the good compatibility, are easy to give full play to the effect of TANSHINONES.

Preparation method of the present invention is simple, good reproducibility.It can be added in the cosmetic formulations, or directly use.

Description of drawings

Below in conjunction with drawings and Examples the present invention is further described:

Fig. 1 is the preparation method flow chart of the present composition.

The specific embodiment

Below in conjunction with specific embodiment such scheme is described further.These embodiment are not limited to limit the scope of the invention for explanation the present invention.The implementation condition that adopts among the embodiment can be done further adjustment according to the condition of concrete producer, and not marked implementation condition is generally the condition in the normal experiment.

The preparation of embodiment 1 tanshinone liposome

Composite formula

As shown in Figure 1, the preparation process of this embodiment is as follows:

1. take by weighing 2.5 gram soybean lecithins, 0.4 gram polysorbate60,8.0 gram propylene glycol, 0.2 gram Vitamin E acetate, 0.1 gram TANSHINONES is put into beaker, carries out 50 ℃ heating in water bath.

2. take by weighing 88.8 gram deionized waters and put into beaker, carry out 50 ℃ heating in water bath.

3. water is joined in the above-mentioned system, stir;

4. the high temperature liposomal systems that stirs is placed cooling and namely get liposome, it is 10.38um that this liposome records its particle diameter by photon correlation spectroscopy (PCS).

The preparation of embodiment 2 tanshinone liposomes

Composite formula

As shown in Figure 1, the preparation process of this embodiment is as follows:

1. take by weighing 5.0 gram egg yolk lecithin, 1.4 gram polysorbas20s, 2.8 gram propylene glycol, 0.6 gram Vitamin E acetate, 1.2 gram TANSHINONES are put into beaker, carry out 50 ℃ heating in water bath.

2. take by weighing 89.0 gram deionized waters and put into beaker, carry out 50 ℃ heating in water bath.

3. water is joined in the above-mentioned system, stir;

4. the high temperature liposomal systems that stirs is placed cooling and namely get liposome, it is 6.36um that this liposome records its particle diameter by photon correlation spectroscopy (PCS).

The preparation of embodiment 3 tanshinone liposomes

Composite formula

As shown in Figure 1, the preparation process of this embodiment is as follows:

1. take by weighing 10.0 gram egg yolk lecithin, 3.6 gram Tween 80s, 12.6 gram propylene glycol, 0.6 gram Vitamin E acetate, 0.8 gram TANSHINONES is put into beaker, carries out 50 ℃ heating in water bath.

2. take by weighing 72.4 gram deionized waters and put into beaker, carry out 50 ℃ heating in water bath.

3. water is joined in the above-mentioned system, stir;

4. the high temperature liposomal systems that stirs is placed cooling and namely get liposome, it is 0.86um that this liposome records its particle diameter by photon correlation spectroscopy (PCS).

The preparation of embodiment 4 tanshinone liposomes

Composite formula

As shown in Figure 1, the preparation process of this embodiment is as follows:

1. take by weighing 16.0 gram soybean lecithins, 4.5 gram polysorbate60s, 15.0 gram propylene glycol, 0.8 gram Vitamin E acetate, 2.0 gram TANSHINONES are put into beaker, carry out 50 ℃ heating in water bath.

2. take by weighing 61.7 gram deionized waters and put into beaker, carry out 50 ℃ heating in water bath.

3. water is joined in the above-mentioned system, stir;

4. the high temperature liposomal systems that stirs is placed cooling and namely get liposome, it is 7.38um that this liposome records its particle diameter by photon correlation spectroscopy (PCS).

Above-mentioned example only is explanation technical conceive of the present invention and characteristics, and its purpose is to allow the people who is familiar with this technology can understand content of the present invention and enforcement according to this, can not limit protection scope of the present invention with this.All equivalent transformations that spirit is done according to the present invention or modification all should be encompassed within protection scope of the present invention.

Claims (3)

1. tanshinone liposome, described carrier loaded active ingredient is TANSHINONES, it is characterized in that composition is counted by its percentage by weight in the described liposome:

TANSHINONES 0.01～5%;

First emulsifying agent 0.1～5%;

Second emulsifying agent 2～15%;

Lecithin 2～18%;

Antioxidant 0.1～1%;

All the other are deionized water;

Wherein phospholipid is selected from a kind of of following chemical compound: Ovum Gallus domesticus Flavus lecithin, soybean lecithin; Antioxidant is Vitamin E acetate; Described first emulsifying agent is selected from following chemical compound: polysorbas20, polysorbate60, Tween 80; Second emulsifying agent is propylene glycol; Be prepared as follows:

(1) presses formula proportion weighing emulsifying agent, lecithin, TANSHINONES and antioxidant, with raw material mixing post-heating and stir the homogeneous system of the oil phase that obtains being in a liquid state; The emulsifying agent that uses is that first emulsifying agent and second emulsifying agent combine according to formula proportion;

(2) press formula proportion weighing deionized water, heating obtains water;

(3) in 30-60 ℃ homogeneous system, add 30-60 ℃ water, in stir speed (S.S.) is the constant speed stirrer of 200r/min～800r/min, stir 3～30min and obtain liposome solutions;

(4) the liposome solutions cool to room temperature is namely got described tanshinone liposome.

2. method for preparing the described tanshinone liposome of claim 1 is characterized in that said method comprising the steps of:

(1) presses formula proportion weighing emulsifying agent, lecithin, TANSHINONES and antioxidant, with raw material mixing post-heating and stir the homogeneous system of the oil phase that obtains being in a liquid state; The emulsifying agent that uses is that first emulsifying agent and second emulsifying agent combine according to formula proportion;

(2) press formula proportion weighing deionized water, heating obtains water;

(3) in 30-60 ℃ homogeneous system, add 30-60 ℃ water, in stir speed (S.S.) is the constant speed stirrer of 200r/min～800r/min, stir 3～30min and obtain liposome solutions;

(4) the liposome solutions cool to room temperature is namely got described tanshinone liposome.

3. according to the method for claim 2, it is characterized in that the particle mean size of the liposome particles that described method obtains is at 0.1～20um.