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Elastic nano vesicle carrier and preparation and application thereof

A technology of nanovesicles and elasticity, applied in the field of medicine, can solve the problems of inconspicuous hydration gradient and difficulty for transfer bodies to penetrate the skin, and achieve the effect of improving transdermal permeability

Inactive Publication Date: 2008-07-02
TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In a closed system, the hydration gradient is not obvious, so it is difficult for the transfer body to penetrate the skin

Method used

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  • Elastic nano vesicle carrier and preparation and application thereof
  • Elastic nano vesicle carrier and preparation and application thereof
  • Elastic nano vesicle carrier and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 Elastic nanovesicle carrier

[0042] Dissolve soybean lecithin and vitamin E with an appropriate amount of ethanol, mix well, blow nitrogen to volatilize the ethanol, then add sodium cholate and a certain amount of 5mM phosphate buffer pH 6.5, and add hexylene glycol, stir at room temperature for 1 hour, then water bath Sonicate for 30 minutes to obtain elastic nanovesicles. The elastic nanovesicles are suspended in a mixed solution of various components remaining after the above components are mixed to form vesicles. Wherein, the content of soybean lecithin is 5.6%, the content of sodium cholate is 1%, the content of vitamin E is 0.1%, and the content of hexanediol is 15%. The particle size was measured with a laser particle size light scattering instrument to be 61 nm.

Embodiment 2

[0043] Embodiment 2 Elastic nanovesicle carrier

[0044] Dissolve soybean lecithin and phenol with an appropriate amount of ethanol, mix well, pass nitrogen gas to volatilize the ethanol, then add dipotassium glycyrrhizinate and a certain amount of 5mM phosphate buffer pH 6.5, and add a mixture of isopropanol and ethanol, of which isopropanol The weight ratio of alcohol to ethanol is 6:4, stirred at room temperature for 1 hour, and homogenized to obtain elastic nanovesicles. The elastic nanovesicles are suspended in a mixed solution of various components remaining after the above components are mixed to form vesicles. Wherein, the content of soybean lecithin is 10%, the content of phenol is 0.1%, the content of dipotassium glycyrrhizinate is 2%, and the total content of isopropanol and ethanol is 15%. The particle size was measured with a laser particle size light scattering instrument to be 230 nm.

Embodiment 3～4

[0046] Dissolve soybean lecithin, paclitaxel and vitamin E with appropriate amount of ethanol, mix well, remove ethanol by rotary evaporation, then add sodium cholate and a certain amount of 5mM phosphate buffer pH 6.5, and add a certain amount of ethanol, stir at room temperature for 1 hour, then Sonicate in a water bath for 30 minutes to obtain elastic nanovesicles. The elastic nanovesicles are suspended in a mixed solution of various components remaining after the above components are mixed to form vesicles. Wherein, the content of soybean lecithin is 5%, the content of sodium cholate is shown in Table 1, the content of paclitaxel is 1%, the content of vitamin E is 0.2%, and the content of ethanol is 10%.

[0047] Separate free drug and vesicles with Sephadex G-50 gel, use HPLC to detect encapsulation efficiency (detection wavelength 230nm, flow rate 1ml / min, mobile phase is acetonitrile: ultrapure water=65:35 [V:V]), The particle size was measured with a laser particle si...

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Abstract

The invention pertains to the field of pharmaceutical technology, which more particularly relates to an elastic nano-vesicle carrier which can transport the active ingredients of the drug to penetrate the natural permeability barrier or pores (such as skin, mucosa, and organs, etc.) and the preparation method, as well as the usage. The vesicle has lipid double molecular layers for transporting one or more active ingredients to penetrate the natural barrier. The vesicle at least contains three dressing components of phospholipid, membrane softener and alcohol, and the three have different physical and chemical properties. The diameter of the typical nano-vesicle is less than 200nm. The vesicle carrier containing the active ingredients of the drug can be applied in the injection, spray and the transdermal preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an elastic nanovesicle carrier capable of transporting active pharmaceutical ingredients through natural permeable barriers or pores (such as skin, mucous membranes, organs, etc.) and its preparation method and application. Background technique [0002] Intact skin has always been considered to be a very effective barrier to protect the body, but it is also the largest barrier for drugs to enter the body through the skin. Conventional pharmaceutical formulations such as hydrogels, ointments or creams, as well as modern formulations such as liposomes are pharmaceutically safe but cannot effectively overcome the skin barrier. The research on liposomes has a long history. The basic composition of liposomes is phospholipid / cholesterol / water. Cholesterol has the effect of stabilizing liposomes, but it makes liposomes show rigid characteristics. Liposomes are applied to th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/24A61K9/00A61K45/00A61P35/00A61P29/00A61P15/00A61P11/06A61P9/00A61P9/02A61P9/12A61P7/02A61P3/10A61P1/08A61N1/30A61N7/02A61H39/00A61M37/00
Inventor 高云华徐百
Owner TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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