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 so

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

Example Embodiment

[0062] Example 1

[0063] Preparation of novel Bodipy amphiphilic compounds (see the synthetic route figure 1 )

[0064] 1) Preparation of compound 3:

[0065] Dissolve pentaerythritol (68.0 g, 0.5 mol) in NaOH solution (9.6 g, 200 mL), add allyl bromide (24.2 g, 0.2 mol) dropwise and stir 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×5). The combined organic layer was dried with anhydrous sodium sulfate, concentrated in vacuo and purified with a 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 are performed under argon protection. The DMF solution of compound 3 (7.0 g, 40.0 mmol) was added dropwise to the DMF suspension of NaH (5.8 g, 240.0 mmol) under ice bath conditions. After stirring...

Example Embodiment

[0090] Example 2

[0091] Preparation of nanoemulsion

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

[0093] 2) The preparation method of the nanoemulsion 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 and particle size distribution are as follows image 3 Shown.

[0095] image 3 Middle (a) represents the roadmap for preparing nanoemulsions loaded with perfluorocarbons (PFC@Bodipy), where Bodipy stands for fluoroboron and PFC stands for perfluorocarbons; (b) and (c) stand for nanoemulsions (PFC@Bodipy),...

Example Embodiment

[0096] Example 3

[0097] Evaluation of the performance of nanoemulsion in vitro photodynamic therapy

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

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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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