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Nano emulsion as well as preparation method and application thereof

A nano-emulsion, nano-emulsion technology, applied in general/multifunctional contrast agents, pharmaceutical formulations, photodynamic therapy and other directions, can solve problems such as limited efficacy, achieve good application prospects, and enhance the effect of photodynamic therapy.

Active Publication Date: 2018-08-14
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The effect of photodynamic therapy is limited by the oxygen content of tumor tissue, and the depth of solid tumors is usually lack of oxygen, which limits the efficacy of photodynamic therapy for solid tumors

Method used

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  • Nano emulsion as well as preparation method and application thereof
  • Nano emulsion as well as preparation method and application thereof
  • Nano emulsion as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] The preparation of novel Bodipy amphiphilic compound (synthetic route sees figure 1 )

[0064] 1) Preparation of compound 3:

[0065] Pentaerythritol (68.0 g, 0.5 mol) was dissolved in NaOH solution (9.6 g, 200 mL), and allyl bromide (24.2 g, 0.2 mol) was added dropwise and stirred for 2 hours. The reaction was heated to 70°C for 8 hours. The mixture was diluted with 100 mL of water and extracted with EA (150 mL x 5). The combined organic layers were dried over anhydrous sodium sulfate, concentrated in vacuo and purified by silica gel column (PE / EA=1 / 1) to obtain compound 3 as a clear oil. 1 H NMR (400MHz, CDCl 3 )δ5.82-5.92(m,1H),5.18-5.28(m,2H),3.97(d,J=8.0Hz,2H),3.76(s,3H),3.68(s,6H),3.44(s ,2H).

[0066] 2) Preparation of compound 4:

[0067] All the following operations were carried out under argon protection. A DMF solution of compound 3 (7.0 g, 40.0 mmol) was added dropwise to a DMF suspension of NaH (5.8 g, 240.0 mmol) under ice-cooling conditions. Afte...

Embodiment 2

[0091] Preparation of nanoemulsions

[0092] 1) Dissolve compound 1 in water (0.1 mg / mL), add PFH (0.5% v / v), stir for 10 minutes, and sonicate (100 W) in an ice bath to form a uniform nanoemulsion. Then, the compounds in the supernatant were removed by low-speed centrifugation to obtain a high-concentration nanoemulsion. Infuse oxygen with an oxygen pump for 5 minutes.

[0093] 2) The nanoemulsion preparation method for in vivo testing is the same as that described in step 1), the concentration of compound 1 is 1 mg / mL, and the concentration of perfluorohexane is 3% v / v.

[0094] The preparation method of nanoemulsion (PFC@Bodipy) and the corresponding TEM image, particle size distribution such as image 3 shown.

[0095] image 3 (a) represents the roadmap for the preparation of nanoemulsions loaded with perfluorocarbons (PFC@Bodipy), where Bodipy represents bodipyr, and PFC represents perfluorocarbons; (b) and (c) represent nanoemulsions (PFC @Bodipy) TEM images and pa...

Embodiment 3

[0097] Performance evaluation of nanoemulsion photodynamic therapy in vitro

[0098] A375 cells were cultured in DMEM (10% fetal calf serum), and 1 × 10 per well 4 cells at a density of 96 wells. After 24 hours of incubation in the incubator, the cells were washed once with PBS. Cells were incubated with PFH@Bodipy and free Bodipy (0, 0.1, 0.25, 0.5, 2.5, 5 and 10 μM Bodipy) at 37°C under the same conditions for 12 hours. To evaluate cytotoxicity, the cells of each group were washed twice with PBS. A standard CCK-8 assay was performed to assess cell viability. Cells in each group were rinsed twice with PBS. Then use a power density of 200mW / cm 2 Irradiate the cells with a 660nm laser for 5 min. After irradiation, cells were incubated for an additional 24 hours. The control group was protected from light, and the other conditions were the same. Subsequently, a standard CCK-8 assay was performed to assess cell viability.

[0099] Figure 4 Indicates the effect of diffe...

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Abstract

The invention discloses nano emulsion as well as a preparation method and application thereof. The nano emulsion comprises a Bodipy amphiphilic compound and perfluocarbon loaded inside the Bodipy amphiphilic compound, wherein the nano emulsion carries oxygen gas. The nano emulsion can realize activated fluorescent, opto-acoustic and 19F magnetic resonance imaging for a tumor site as well as photodynamic therapy of tumors. The preparation process is simple, is convenient to operate, does not need complex and dear equipment, easily realizes industrial production, and has a good application prospect in the field of tumor diagnosis and treatment.

Description

technical field [0001] The invention relates to the field of medical nanomaterials, in particular to a nanoemulsion and its preparation method and application. Background technique [0002] The nano-diagnosis and treatment platform is expected to provide a personalized and precise treatment method by integrating diagnostic agents and therapeutic agents into a nano-sized system, so that the treatment plan can be optimized and adjusted in real time and quickly according to the monitoring results. However, nanocarriers only serve as excipients for drug delivery, and the loaded multiple diagnostic agents reduce the drug-carrier ratio. A high content of carriers will increase the metabolic burden and toxicity, and the integration of multiple drugs will complicate the synthesis process of nano-therapeutic agents and increase the cost, which will affect the clinical approval of nano-medicines. In order to maximize the drug-carrier ratio and simplify the preparation process of nano...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K49/12A61K49/18A61K49/22A61K41/00A61K9/107A61P35/00
CPCA61K9/1075A61K41/0057A61K49/0002A61K49/0021A61K49/0054A61K49/0078A61K49/126A61K49/1806A61K49/226A61P35/00
Inventor 黄鹏张一帆薄少伟林静江中兴
Owner SHENZHEN UNIV
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