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Lactoferrin modified solid lipid nanoparticles, as well as preparation method and application thereof

A technology of solid lipid nano and lactoferrin, which is applied in the field of medicine, can solve the problems of less active targeting and difficulty in targeting functional molecules of connexins, and achieve good brain targeting effects

Inactive Publication Date: 2014-02-19
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since SLN is based on lipids, and most lipid compounds lack active groups, unlike polymers, which are not easy to carry out surface modification, it is difficult to target functional molecules of linker proteins, so they actively target There are few reports, and receptor-mediated brain targeting has not been reported yet

Method used

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  • Lactoferrin modified solid lipid nanoparticles, as well as preparation method and application thereof
  • Lactoferrin modified solid lipid nanoparticles, as well as preparation method and application thereof
  • Lactoferrin modified solid lipid nanoparticles, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1: Preparation of loperamide solid lipid nanoparticles modified by lactoferrin

[0049] Step 1 Synthesis of maleic anhydride-6-aminocaproic acid-polyethylene glycol monostearate (mal-sac-PEG-MS)

[0050] Mal-sac uses dichloromethane as a solvent, adds 1 / 3 mal-sac molar amount of PEG-MS, under ice bath conditions, adds DMAP (5% of PEG-MS), and then adds DCC dropwise (with mal-sac etc. mol), stirred at room temperature for 10 hours, using dichloromethane: methanol (8:2) as the developer, thin layer chromatography analysis to determine the end point of the reaction, ether precipitation, methanol recrystallization, mal-sac-PEG-MS was obtained under low temperature conditions, The melting point is 50-53°C, and the yield is 82%. .

[0051] Step 2 Preparation of loperamide solid lipid nanoparticles (L-SLN) by high-speed shear-melt ultrasonic method

[0052] Weigh the prescribed amount of loperamide and MTS into a test tube, heat and ultrasonically dissolve it as ...

Embodiment 2

[0068] Embodiment 2: Preparation of lactoferrin-modified coumarin 6 solid lipid nanoparticles

[0069] Step 1 Synthesis of maleic anhydride-6-aminocaproic acid-polyethylene glycol monostearate (mal-sac-PEG-MS) mal-sac uses dichloromethane as solvent, adding 1 / 3mal-sac molar amount PEG-MS, under ice bath conditions, add DMAP (5% of PEG-MS), then drop DCC (equimolar to mal-sac), stir at room temperature for 10h, dichloromethane: methanol (8:2 ) as developing agent, thin-layer chromatographic analysis to determine the reaction end point, ether precipitation, methanol recrystallization, mal-sac-PEG-MS was obtained under low temperature conditions, melting point 50-53 ℃, yield 82%. .

[0070] Step 2 Preparation of mal-sac-PEGylated coumarin 6 solid lipid nanoparticles (mal-sac-PEG-Co-SLN) by high-speed shear-melt ultrasonic method

[0071] Weigh 61 mg of coumarin, 50 mg of MTS, and 0.5 mg of mal-sac-PEG-MS into a test tube, heat and ultrasonically dissolve it as the oil phase; we...

Embodiment 3

[0076] Embodiment 3: Analgesic experiment of Lf-L-SLN

[0077]Step 1 Animal grouping and administration: 110 qualified ICR mice were divided into 11 groups: (1) control group: normal saline 0.15ml / 10g; (2) blank SLN group: 0.15ml / 10g blank solid lipid nanoparticles (not Protein-modified nanoparticles without adding loperamide); (3) blank Lf-SLN group: 0.15ml / 10g, i.e. protein-modified blank solid lipid nanoparticles; (4) positive drug group: morphine hydrochloride 15mg / kg, ( 0.15ml / 10g); (5) Loperamide (L) solution group: 3.6mg / kg (0.15ml / 10g); (6) L-SLN low-dose group: 1.8mg / kg, that is, loperamide solid lipid nanoparticles (0.075ml / 10g); ⑺L-SLN medium-dose group: 2.7mg / kg (0.1ml / mg); ⑻L-SLN high-dose group: 3.6mg / kg (0.15ml / mg); ⑼Lf-L-SLN low-dose Group: 1.8mg / kg, that is, lactoferrin modified loperamide solid lipid nanoparticles (0.075ml / 10g); ⑽Lf-L-SLN medium dose group: 2.7mg / kg (0.1ml / 10g); ⑾Lf- L-SLN high dose group: 3.6mg / kg (0.15ml / 10g). Except for the positive gro...

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to lactoferrin modified solid lipid nanoparticles, as well as a preparation method and application thereof. The lactoferrin modified solid lipid nanoparticles are characterized in that lactoferrin is modified on the surfaces of solid lipid nanoparticles. The lactoferrin modified solid lipid nanoparticles can wrap medicines therein and can be used as a medicine transfer carrier. The preparation method disclosed by the invention comprises the following steps: synthesising mal-sac-PEG-MS through DCC dehydration reaction, and preparing a nanosuspension by using mal-sac-PEG-MS; then, carrying out lactoferrin sulfhydrylation (Lf-SH) by virtue of a Traut's agent, adding Lf-SH into the nanosuspension, and stirring at a room temperature to carry out protein modification. The lactoferrin modified solid lipid nanoparticles disclosed by the invention have good particle size, Zeta potential and stability. Experimental results show that the lactoferrin modified solid lipid nanoparticles disclosed by the invention are capable of transferring model medicines, such as loperamide and coumarin 6, into brain.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a lactoferrin-modified solid lipid nanoparticle and a preparation method and application thereof. Background technique [0002] The blood-brain barrier (BBB) ​​can prevent harmful substances in the blood from entering the brain, and at the same time can expel harmful or excess substances in the brain, thereby maintaining the stability of the internal environment of the brain and ensuring the normal function of the brain , has a very good protective effect on the central nervous system (central nervous system, CNS). However, the existence of the BBB prevents 98% of small-molecule chemical drugs and almost all macromolecular drugs, including proteins, peptides, and gene drugs from entering the brain, or it is difficult to reach an effective concentration in the brain, making the treatment of brain diseases extremely difficult. difficulty. [0003] In past studies, sc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K9/51A61P29/00A61K31/451A61K31/37
Inventor 葛晓群郭荣高纬康赵宇蕾吕丹颜玉文鞠婧婧
Owner YANGZHOU UNIV
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