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Preparation method of all-trans tretinoin solid lipid nanoparticles

A technology of solid lipid nano and all-trans retinoic acid, which is applied in the direction of microcapsules, nanocapsules, metabolic diseases, etc., can solve problems such as the difficulty of finding organic solvents and the inability to use lipid nanoparticles, so as to reduce energy consumption, The effect of enhanced optical stability and simplified production process

Inactive Publication Date: 2013-10-23
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dong's method cannot be used for the preparation of lipid nanoparticles with glyceryl behenate or glyceryl monostearate as the lipid wall material, because it is difficult to find a method that can dissolve both and all-trans retinoic acid in it. And organic solvents that are harmless to the body, for example, although all-trans retinoic acid can be dissolved in ethanol, glyceryl behenate is almost insoluble

Method used

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  • Preparation method of all-trans tretinoin solid lipid nanoparticles
  • Preparation method of all-trans tretinoin solid lipid nanoparticles
  • Preparation method of all-trans tretinoin solid lipid nanoparticles

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Embodiment 1

[0024] Embodiment 1: The preparation method of all-trans retinoic acid solid lipid nanoparticles described in this embodiment comprises the following steps:

[0025] Step 1: Preparation of the oil phase

[0026] 25 mg of all-trans retinoic acid and 500 mg of glyceryl behenate were added to 50 mL of absolute ethanol solution to obtain a lipid concentration of 10 mg / mL and a drug concentration of 0.5 mg / mL. The solution is yellow and turbid at room temperature. The obtained solution was heated in a water bath at 75° C. for 30 s to obtain a clear and transparent oil phase solution.

[0027] Step 2: Preparation of the aqueous phase

[0028] Add 10 g of Poloxamer 188 to 500 mL of distilled water to prepare an aqueous solution of Poloxamer 188 with a concentration of 20 mg / mL, cool it down to 5 °C in an ice-water bath, and store it in a refrigerator at 4 °C for preparation of solid lipid nanoparticles .

[0029] Step 3: Continuous production of solid lipid nanoparticles in a sta...

Embodiment 2

[0036] Embodiment 2: The preparation method of all-trans retinoic acid-loaded solid lipid nanoparticles described in this embodiment comprises the following steps:

[0037] Step 1: Preparation of the oil phase

[0038] Add 25mg of all-trans retinoic acid and 500mg of glyceryl behenate into 50mL of absolute ethanol solution, and the solution is yellow and turbid at room temperature. The resulting lipid concentration was 10 mg / mL and the drug concentration was 0.5 mg / mL. The obtained solution was heated in a water bath at 75° C. for 30 s to obtain a clear and transparent yellow oil phase solution.

[0039] Step 2: Preparation of the aqueous phase

[0040] Add 10 g of Tween-80 to 500 mL of distilled water to prepare a Tween-80 aqueous solution with a concentration of 20 mg / mL, cool to 5°C in an ice-water bath, and store in a refrigerator at 4°C for preparation of solid lipid nanoparticles.

[0041] Step 3: Continuous production of solid lipid nanoparticles in a static mixer

...

Embodiment 3

[0048] Embodiment 3: The preparation method of all-trans retinoic acid-loaded solid lipid nanoparticles described in this embodiment comprises the following steps:

[0049] Step 1: Preparation of the oil phase

[0050] Add 50 mg of all-trans retinoic acid and 500 mg of glyceryl behenate into 50 mL of absolute ethanol solution, and the solution is yellow and turbid at room temperature. The resulting lipid concentration was 10 mg / mL, and the drug concentration was 1 mg / mL. The obtained solution was heated in a water bath at 75° C. for 30 s to obtain a clear and transparent yellow oil phase solution.

[0051] Step 2: Preparation of the aqueous phase

[0052] Add 10 g of Tween-80 to 500 mL of distilled water to prepare a Tween-80 aqueous solution with a concentration of 20 mg / mL, cool to 5°C in an ice-water bath, and store in a refrigerator at 4°C for preparation of solid lipid nanoparticles.

[0053] Step 3: Continuous production of solid lipid nanoparticles in a static mixer ...

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Abstract

A preparation method of all-trans tretinoin solid lipid nanoparticles relates to solid lipid nanoparticles. The preparation method comprises following steps: (1) adding lipid wall materials and target drugs in an organic solvent, heating in water bath to fully dissolve the lipid wall materials thus obtaining a clarified oil phase; (2) adding surfactant into water to obtain a surfactant water solution, cooling the surfactant water solution until the temperature of the solution arrives at 4 DEG C through the ice-water bath method, storing the cooled surfactant water solution in a refrigerator; (3) transporting the oil phase prepared in the step (1) and the water phase prepared in the step (2) by a peristaltic pump to a static mixer at the same time for a reaction, collecting the solid lipid nanoparticle fluid suspension; (4) adjusting the pH value of the solid lipid nanoparticle fluid suspension to a range of 6.2 to 6.7, then adding hydrochloric acid to adjust the pH to a range of 1.2 to 1.3, then subjecting the fluid suspension to a centrifugation treatment, freeze-drying the deposition obtained by centrifugation, thus obtaining the all-trans tretinoin solid lipid nanoparticles. The obtained all-trans tretinoin solid lipid nanoparticles have relatively good encapsulation efficiency and uniform particle size distribution.

Description

technical field [0001] The invention relates to solid lipid nanoparticles, in particular to a preparation method of all-trans retinoic acid solid lipid nanoparticles. Background technique [0002] All-trans retinoic acid, also known as retinoic acid and retinoic acid, is an intermediate product of vitamin A metabolism and is widely used in modern medicine. First of all, in terms of skin disease treatment, it can be used to treat acne, lichen planus, leukoplakia, multiple warts and other keratotic skin diseases; secondly, it has a strong effect of inducing differentiation of tumor cells, and can be used to treat cancer, acute Promyelocytic leukemia, bone marrow dysplasia (preleukemia); finally, it activates genes necessary for regeneration and is essential for the regeneration of limbs in animals. However, the application of all-trans retinoic acid is limited by its own physical and chemical properties: poor hydrophilicity and poor photostability. When it is exposed to air,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/203A61P3/02
Inventor 肖宗源吴爽邵文尧陈森元冯艳玲
Owner XIAMEN UNIV