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Paclitaxel/erlotinib-loaded mesoporous silica-hyaluronic acid hybrid targeted nano-particles

A technology of mesoporous silica and nanoparticles, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of less drug dosage, reduce toxic side effects, expand The effect of preparation and material availability

Active Publication Date: 2018-05-01
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The combination of two or more anti-tumor active ingredients has a good prognosis and fewer adverse reactions, which can reduce the occurrence of drug resistance, but the combined drug is easily affected by the metabolic properties of different drugs, resulting in a relatively small amount of drug reaching the tumor site. few

Method used

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  • Paclitaxel/erlotinib-loaded mesoporous silica-hyaluronic acid hybrid targeted nano-particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of Mesoporous Silica Nanoparticles (MSN)

[0032] After thoroughly mixing 0.1 g of TEA (triethanolamine) and 20 mL of deionized water, transfer to a 50 mL flask containing 2 g of CTAC (cetyltrimethylammonium chloride), and magnetically stir at 95 °C for 1 h. Then 1.5 mL of TEOS (tetraethyl silicate) was added dropwise to the flask via a syringe, during which the color of the solution gradually changed to milky white. After the addition was complete, stirring was continued for 1 hour under the same conditions, and then the solution was centrifuged at 12000 rpm for 15 minutes. The resulting crude product was washed twice with 20 mL of deionized water and 20 mL of ethanol, then dissolved in 20 mL of methanol, added with 2 g of NaCl, and stirred magnetically at room temperature for 4 hours to remove unreacted CTAC, then the mixture was centrifuged for 15 minutes, and the residue was washed with 20 mL of After washing with ethanol three times, dry in a...

Embodiment 2

[0034] Example 2 MSN-NH 2 Synthesis of nanoparticles

[0035] Add 100 mg of MSN into a 50 mL flask containing 20 mL of ethanol, followed by 400 μL of APTES (3-aminopropyltriethoxysilane) and magnetically stir for 12 h. After the reaction was completed, the mixture was centrifuged at 12,000 rpm for 15 minutes to remove the main solvent, and the residue was washed twice with 20 mL of deionized water and 20 mL of ethanol to remove unreacted substances, and then dried in a vacuum desiccator at -50 °C for 24 h to obtain approximately 100mg MSN-NH 2 Nanoparticles.

Embodiment 3

[0036] Example 3 Synthesis of MSN-HA nanoparticles

[0037] 30mg HA, 100mg EDC and 100mg NHS were dissolved in 40mL 0.1mol / L MES buffer, and stirred at room temperature for 24 hours to obtain HA-NHS. 40mg MSN-NH 2 Disperse in 20mL ethanol and stir for 1 hour, then add 12mg HA-NHS and stir for 4 hours to synthesize MSN-HA.

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Abstract

The invention discloses paclitaxel / erlotinib-loaded mesoporous silica-hyaluronic acid hybrid targeted nano-particles and application thereof to preparation of an anti-cancer drug. The targeted nano-particles are obtained by carrying out covalent coupling on hyaluronic acid to outer surfaces of mesoporous silica nano-particles after modifying the mesoporous silica nano-particles through surface amino functionlization and then mixing two types of mesoporous silica nano-particles in proportion after respectively loading paclitaxel and erlotinib into inner pore passages of the mesoporous silica nano-particles. According to the invention, not only can stability of the paclitaxel be improved, but also targeted drug delivery of paclitaxel / erlotinib can be implemented, and by combined use of the paclitaxel and the erlotinib, an effect of synergistically resisting to cancer metastasis is played.

Description

technical field [0001] The invention belongs to the technical field of preparation of antitumor drugs, and in particular relates to a mesoporous silicon dioxide-hyaluronic acid mixed targeting nanoparticle loaded with paclitaxel / erlotinib and an application thereof. Background technique [0002] In recent years, novel drug delivery systems have always been a research hotspot in the field of medicine. The nano-drug delivery system can transport two or more drugs at the same time, and can improve the in vivo distribution and pharmacokinetic properties of anti-tumor drugs, improve the selectivity of drugs to specific targets, and achieve the therapeutic purpose of high efficiency and low toxicity. The combination of two or more anti-tumor active ingredients has a good prognosis and fewer adverse reactions, which can reduce the occurrence of drug resistance, but the combined drug is easily affected by the metabolic properties of different drugs, resulting in a relatively small a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61K31/337A61K9/50A61K47/04A61K47/36A61P35/00
CPCA61K9/501A61K9/5036A61K31/337A61K31/517A61K2300/00
Inventor 邵敬伟王贠莞彬郑桂容
Owner FUZHOU UNIV
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