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Taxol-loaded nano lipid carrier and preparation method thereof

A nano-lipid carrier and paclitaxel technology, which is applied in liposome delivery, pharmaceutical formulations, non-active ingredients of oil/fat/wax, etc., can solve the problems of complex process and difficult control, and achieve simple process, controllable quality, Good biocompatibility effect

Inactive Publication Date: 2013-01-02
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods require material synthesis, or chemical bond modification, and the process is complex and difficult to control.

Method used

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  • Taxol-loaded nano lipid carrier and preparation method thereof
  • Taxol-loaded nano lipid carrier and preparation method thereof
  • Taxol-loaded nano lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: 1 mg of paclitaxel, 20 mg of glyceryl monostearate, 15 mg of soybean oil and 25 mg of lecithin were accurately weighed and dissolved in 2 mL of ethanol to form an oil phase. A certain amount of CTAB was accurately weighed and dissolved in water to form a CTAB solution with a concentration of 0.1% (w / v) to form an aqueous phase. Take 40mL of CTAB solution and heat it to 70°C under temperature-controlled stirring and stir at a speed of 600r / min. Add the oil phase dropwise to the stirred water phase at a rate of 30mL / h, and continue to stir and emulsify for 30min after the dropwise addition. Then go to the ice bath and carry out the ice bath, and continue to stir at 600r / min for 2h, and prepare the cationic paclitaxel-loaded nano-lipid carrier, and its transmission electron micrograph is as follows figure 1 As shown, it can be seen from the figure that the particle size of the nano-lipid carrier is 50-300nm, and the particle size distribution is as follows: i...

Embodiment 2

[0035] Example 2: Accurately weigh 5 mg of paclitaxel, 40 mg of glyceryl monostearate, 30 mg of soybean oil and 50 mg of lecithin, and dissolve them in 2 mL of acetone to form an oil phase. A certain amount of CTAB was accurately weighed and dissolved in water to form a CTAB solution with a concentration of 0.5% (w / v) to form an aqueous phase. Take 40mL of CTAB solution and heat it to 70°C under temperature-controlled stirring and stir at a speed of 600r / min. Add the oil phase dropwise to the stirred water phase at a rate of 20mL / h, and continue to stir and emulsify for 30min after the dropwise addition. Then switch to an ice bath for ice bathing, and continue stirring at 600r / min for 2h to prepare a cationic paclitaxel-loaded nanolipid carrier.

Embodiment 3

[0036] Example 3: 8 mg of paclitaxel, 60 mg of glyceryl monostearate, 45 mg of soybean oil and 75 mg of lecithin were accurately weighed and dissolved in 2 mL of ethanol to form an oil phase. A certain amount of CTAB was accurately weighed and dissolved in water to form a CTAB solution with a concentration of 1.0% (w / v) to constitute the water phase. Take 40mL of CTAB solution and heat it to 70°C under temperature-controlled stirring and stir at a speed of 600r / min. Add the oil phase dropwise to the stirred water phase at a rate of 10 mL / h, and continue to stir and emulsify for 30 min after the dropwise addition. Then switch to an ice bath for ice bathing, and continue stirring at 600r / min for 2h to prepare a cationic paclitaxel-loaded nanolipid carrier.

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Abstract

The invention discloses a taxol-loaded nano lipid carrier and preparation thereof. The taxol-loaded nano lipid carrier comprises the following ingredients: taxol with the concentration of 0.5 to 10 mg / mL, solid lipid with the concentration of 5 to 100 mg / mL, liquid lipid with the concentration of 5 to 100 mg / mL, emulsifying agent with the concentration of 0.1 to 5 mg / mL and hyaluronic acid with the concentration of 0.1 to 3 mg / mL. The taxol-loaded nano lipid carrier prepared by the method has round appearance, uniform mass, entrapment rate of over 80 percent and uniform appearance and mass after being modified by the hyaluronic acid. The taxol is coated and loaded by the lipid carrier with biocompatibility and biodegradability, so the solubility of the taxol is improved; and the hyaluronic acid, serving as a targeted factor of tumor, is used for performing surface modification on the nano lipid carriers, so the taxol-loaded nano lipid carrier has long circulation in blood, achieves tumor active targeted property and reduces toxic or side effect.

Description

technical field [0001] The invention relates to a paclitaxel-loaded nano-lipid carrier and a preparation method thereof, in particular to a paclitaxel-loaded nano-lipid carrier modified by hyaluronic acid and a preparation method thereof. Background technique [0002] Paclitaxel is a tetracyclic diterpenoid compound extracted from the bark of Taxus chinensis, which can combine with cell microtubules during cell division, form stable vascular bundles in cells, inhibit cell division and proliferation, and make cancer cells Stop in G2 phase and M phase, thereby inhibiting the growth of tumor cells. Paclitaxel has a broad anti-tumor spectrum and high therapeutic index. In recent years, it has been widely used in the treatment of breast cancer, ovarian cancer, uterine cancer, non-small cell lung cancer, gastric cancer, etc., and has achieved good clinical effects. [0003] However, paclitaxel is almost insoluble in water and has poor oral bioavailability. There are two clinical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/44A61K47/36A61K47/28A61K47/14A61P35/00A61K47/12A61K47/24
Inventor 张娜杨晓燕刘永军
Owner SHANDONG UNIV
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