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A kind of high drug-loaded photo-chemotherapy bifunctional nanoparticle and preparation method thereof

A high drug loading, nanoparticle technology, applied in the field of medicine, can solve the problems of easy removal of molecular state, limited practical application, lack of targeting, etc., to improve bioavailability, achieve synergistic anti-tumor, and simple preparation method easy effect

Active Publication Date: 2022-07-29
深圳乐土沃森精准医疗有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although photodynamic therapy is widely used and develops rapidly, photosensitizers, such as the second-generation photosensitizer chlorin e6 (Ce6), are mostly hydrophobic, generally have poor water solubility, easy removal of molecular states, and lack of targeting. However, there are disadvantages such as sexiness, which limit its practical application in tumor therapy, so photodynamic therapy has not been accepted as a first-line treatment option.

Method used

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  • A kind of high drug-loaded photo-chemotherapy bifunctional nanoparticle and preparation method thereof
  • A kind of high drug-loaded photo-chemotherapy bifunctional nanoparticle and preparation method thereof
  • A kind of high drug-loaded photo-chemotherapy bifunctional nanoparticle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045]Example 1 Preparation of 7-ethyl-10-hydroxycamptothecin (SN38) / chlorin e6 (Ce6) high drug-loading bifunctional nanoparticles (SN38 / Ce6 NPs): accurately weigh 7.6 mg of SN38 powder and 3.8mg Ce6 were dissolved in 0.5mL DMF, dissolved by ultrasonic to form an organic phase; the above organic phase was added dropwise to 15mL deionized water under 250W ultrasonic conditions, and the temperature was controlled below 20°C, and the ultrasonic wave was continued for 10min; accurately weighed. Take 11.4mg DSPE-PEG 2000 The powder was dissolved in 0.5mL DMF, dissolved by ultrasonic to form an organic phase, and added dropwise to the above aqueous phase under 250W ultrasonic conditions, the temperature was controlled below 20°C, and the ultrasonic wave was continued for 10min; the organic solvent was removed by dialysis; 3 times for 1.5 min each time to obtain SN38 / Ce6 NPs. The particle size was measured by dynamic light scattering (DLS). After being placed at 4°C for 21 days, th...

Embodiment 2

[0047] Embodiment 2 adopts scanning electron microscope (Scanning electron microscopy, SEM) to observe the morphology of SN38 / Ce6 NPs: after the SN38 / Ce6 NPs obtained in Example 1 is freeze-dried without adding a freeze-drying protective agent, the freeze-dried powder is fixed on copper with conductive glue The column was sprayed with gold for 240s under the condition of vacuum and 30mA current. observed under a scanning electron microscope.

[0048] The SN38 / Ce6 NPs observed in Example 2 showed a regular rod-like structure ( figure 2 ), the length and diameter of the nanorods are relatively consistent, with an average length of 300 nm and a diameter of about 20 nm. Since the particles in the solution are assumed to be spherical during DLS measurement, the measured particle size is the equivalent volume particle size. So SEM and DLS results will be slightly biased.

Embodiment 3

[0049] Example 3 Determination of the in vitro release curve of double drug-loaded and carrier-free nanoparticles by dynamic membrane dialysis: three batches of SN38 / Ce6 NPs were prepared according to Example 1, and diluted with deionized water to a concentration of SN38 of 25 μg / mL and a concentration of Ce6 of 12.5 μg / mL, in vitro drug release test. Precisely draw 2 mL of the drug-containing solution, put it into a dialysis bag (MWCO=8000~14000) soaked in distilled water, tie the bag tightly, add 100 mL of 0.01M PBS (containing 1% SDS), and shake at a constant temperature in a water bath at 37°C released in the device (100 rpm). 5mL was sampled at preset time points (0.0833, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120h), and an isothermal and equal volume of release medium was added at the same time. According to the measured drug concentration, the cumulative drug release percentage was calculated, and the drug release curve was drawn.

[0050] The in vitro rel...

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Abstract

The invention provides a photo-chemotherapy bifunctional nanoparticle with high drug loading and a preparation method thereof. The nanoparticle is composed of a photosensitizer, a chemotherapeutic drug and a stabilizer carrier, and the photosensitizer and the chemotherapeutic drug constitute a drug part, The mass ratio of the drug part to the stabilizer carrier is 1:1-1:2, which is prepared by an anti-solvent precipitation method combined with a high-pressure homogenization method, the particle size is about 200 nm, and the placement stability is good; ‑Chemotherapy bifunctional nanoparticles realize the synergistic effect of phototherapy-chemotherapy, with strong singlet oxygen generation ability, remarkable anti-tumor effect in vitro and in vivo, and potential clinical application value.

Description

【Technical field】 [0001] The invention relates to the technical field of medicine, in particular to a photo-chemotherapy bifunctional nanoparticle with high drug loading and a preparation method thereof. 【Background technique】 [0002] According to reports, cancer remains one of the leading life-threatening and fatal diseases worldwide. In addition to surgery and radiotherapy, systemic chemotherapy remains the method of choice for cancer treatment. Thus, over the past century, tremendous efforts have been devoted to discovering potential chemotherapeutic agents that act through specific targeting pathways. The natural alkaloid camptothecin (CPT) and its derivatives have attracted extensive attention as broad-spectrum chemotherapeutic drugs, and exert anti-tumor effects by inhibiting the activity of topoisomerase I and blocking the DNA production pathway. However, like most chemotherapeutic drugs, the application of CPT is limited by many limitations, such as its poor water...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00A61K31/4745A61K9/107A61K47/24A61K47/34A61K47/28A61K47/42A61P35/00
CPCA61K41/0071A61K31/4745A61K9/1075A61K47/24A61K47/34A61K47/28A61K47/42A61P35/00A61K2300/00
Inventor 赵燕娜蒋欣欣刘敏丁壮韩军
Owner 深圳乐土沃森精准医疗有限公司
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