Nanocrystalline of hydrophobic drug, as well as preparation and application methods of nanocrystalline

A technology of hydrophobic drugs and nanocrystals, which is applied in the field of insoluble hydrophobic drug nanocrystals and insoluble hydrophobic drug nanocrystals, can solve the problems of decomposition loss of effective components of drugs, drug pollution, and hydrophobic and insoluble drugs, and achieves good general applicability. high drug loading, narrow particle size distribution

Inactive Publication Date: 2015-04-29
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the "top-down" technology requires mechanical grinding and high-pressure homogenization, the preparation conditions are severe, and the drug loss is serious during the process. Especially for heat-sensitive drugs, it will also lead to the decomposition and loss of active ingredients of the drug; secondly, the long-term contact between the grinding medium and the drug is still May cause drug contamination; in addition, most mechanical grinding is an intermittent batch process, the quality of each batch of drugs is not suitable for precise control, and it is difficult to meet the clinical approval requirements
Although the "bottom-up" technology does not have the above problems, because this technology does not change the surface properties of the drug

Method used

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  • Nanocrystalline of hydrophobic drug, as well as preparation and application methods of nanocrystalline
  • Nanocrystalline of hydrophobic drug, as well as preparation and application methods of nanocrystalline
  • Nanocrystalline of hydrophobic drug, as well as preparation and application methods of nanocrystalline

Examples

Experimental program
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[0059] Example 1

[0060] A paclitaxel nanocrystal preparation is prepared by the following method:

[0061] (1) Dissolve 20 mg of paclitaxel in 100 μL of dichloromethane and mix with 10 mL of 0.1 wt% poloxamer The aqueous solution of F127 was mixed; the emulsification treatment was carried out by ultrasonic with a power of 20W to obtain an O / W emulsion with paclitaxel dissolved in the oil phase;

[0062] (2) soak the O / W emulsion obtained in step (1) in liquid nitrogen to solidify, then immediately transfer it to a freeze dryer for drying for 48 hours, remove the solvent molecules therein, and obtain a crude paclitaxel nanocrystal, which is then subjected to repeated Resuspension-centrifugation-resuspension for purification to obtain paclitaxel nanocrystal products, which are recorded as NPs;

[0063] figure 1 It is a transmission electron microscope (TEM) photograph of the paclitaxel nanocrystals (NPs) in Example 1; the prepared paclitaxel nanocrystals have an average pa...

Example Embodiment

[0064] Example 2

[0065] A nanocrystal of iRGD functionalized paclitaxel, the difference between its preparation method and Example 1 is only: Full or partial replacement of F127 with iRGD-modified poloxamers F127, the obtained iRGD functionalized paclitaxel nanocrystals were denoted as iNPs.

[0066] figure 2 This is the TEM image of the iRGD functionalized paclitaxel nanocrystals (iNPs) in Example 2; the prepared iRGD functionalized paclitaxel nanocrystals have an average particle size of 71.3 nm and a drug loading of 94.33 wt% respectively.

Example Embodiment

[0067] Example 3

[0068] A paclitaxel nanocrystal preparation is prepared by the following method:

[0069] (1) 1 mg of paclitaxel was dissolved in 1 mL of dichloromethane, and mixed with 1 mL of 2.0 wt% poloxamer The aqueous solution of F127 was mixed and emulsified by ultrasonic with a power of 100W to obtain an O / W emulsion with paclitaxel dissolved in the oil phase;

[0070] (2) soak the O / W emulsion obtained in step (1) in liquid nitrogen to solidify, then immediately transfer it to a freeze dryer for drying for 48 hours, remove the solvent molecules therein, and obtain a crude paclitaxel nanocrystal, which is then subjected to repeated Resuspension-centrifugation-resuspension for purification to obtain paclitaxel nanocrystal products, which are recorded as NDs;

[0071] image 3 It is the TEM image of the paclitaxel nanocrystals (NDs) in Example 3; the prepared paclitaxel nanocrystals have an average particle size of 8.6 nm and a drug loading of 80.57 wt% respective...

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Abstract

The invention relates to nanocrystalline of a hydrophobic drug. The nanocrystalline of the hydrophobic drug is characterized by comprising the hydrophobic drug and amphipathic molecule of wrapping the outside of the hydrophobic drug, wherein the nanocrystalline is obtained by removing solvent molecules of an O/W type emulsion containing the hydrophobic drug. The nanocrystalline of the hydrophobic drug provided by the invention is uniform in particle size and good in dispersity in water and has universality; the effective components of the drug are kept well; the surface-wrapped amphipathic molecule can be doped with a targeting molecule; after the amphipathic molecule is doped with the targeting molecule, the targeting functionalization of a nanocrystalline preparation can be achieved; distribution of the drug in a tumor tissue is increased; and the toxic and side effects of chemotherapy drugs are reduced. The preparation method of the nanocrystalline of the hydrophobic drug provided by the invention is simple to operate and good in repeatability; the controllability of the particle size of the hydrophobic drug can be achieved; the product quality is easy to control; and the batch reproducibility of the drug is good.

Description

technical field [0001] The invention relates to a nanocrystal of a hydrophobic drug, a preparation method and a use method, in particular to a nanocrystal of an insoluble hydrophobic drug, a preparation method and a use method. Specifically, the present invention relates to an insoluble hydrophobic drug nanocrystal prepared by emulsion crystallization method, preparation and use method, the prepared hydrophobic drug nanocrystal can treat malignant tumors, such as breast cancer, ovarian cancer, leukemia, lymphoma And pancreatic cancer, etc., produce the ideal effect of treatment and prevention of tumor metastasis and recurrence. Background technique [0002] Administration of cytotoxic chemical drugs through the blood system is one of the important means of clinical tumor treatment. Compared with surgical treatment and radiotherapy, chemotherapy is a systemic treatment plan, which can exert a therapeutic effect on advanced tumors, metastatic and diffuse tumors, etc. Because...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/107A61K31/337A61K47/10A61K47/42A61K31/4745A61K47/32A61K31/12A61K47/34A61K31/436A61P35/00
Inventor 马光辉魏炜倪德志岳华周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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