Taxane medicines albumin nanoparticle preparation for injection and preparation method thereof

A technology of albumin nanoparticles and taxanes, which is applied in the field of taxane drug albumin nanoparticle preparations for injection and its preparation. Sex and other issues, to achieve good clinical application prospects, improve anti-tumor effect, reduce the effect of dosage

Active Publication Date: 2012-11-21
FUDAN UNIV
18 Cites 13 Cited by

AI-Extracted Technical Summary

Problems solved by technology

[0004] At present, although taxanes have good anti-tumor effects, the treatment practice shows that they still have the following defects: (1) Because the drug is poorly soluble in water (paclitaxel has a solubility of 0.0005 mg/mL in water at room temperature, docetaxel Almost insoluble in water)), clinically used injections all need to add a large amount of surfactants, such as paclitaxel using Cremophor EL to help dissolve, docetaxel using Tween 80 to help dissolve, etc., resulting in relatively large toxic side effects of the injection in clinical application, It is easy to cause complications, such as allergic reaction, bone marrow suppressi...
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Abstract

The invention belongs to the field of medicinal preparation, and relates to taxane medicines albumin nanoparticle preparation for injection and a preparation method of the preparation. According to the invention, the albumin nanoparticle preparation is prepared by combining the albumin with the taxane medicines to form the albumin nanoparticles by dispersing and stabilizing with the phospholipid. According to the invention, the strengthened osmosis and retention effect on the tumors by the nanoparticles are utilized, and more medicines are passively targeted and concentrated on the tumor tissues so as to improve the antitumor effect; simultaneously, due to the fact that the bioavailability in the injection way is high and the soluble albumin nanoparticle preparation for injection exists passive targeting, the administration dose can be greatly reduced, so that the medicinal concentration on the non-target parts can be effectively reduced, the toxic and side effects of the medicines can be reduced, and the good clinical application prospect can be implemented. The preparation is convenient in preparation method and is suitable for industrial mass production.

Application Domain

Powder deliveryOrganic active ingredients +2

Technology Topic

Albumin nanoparticlesTumor tissue +9

Image

  • Taxane medicines albumin nanoparticle preparation for injection and preparation method thereof
  • Taxane medicines albumin nanoparticle preparation for injection and preparation method thereof
  • Taxane medicines albumin nanoparticle preparation for injection and preparation method thereof

Examples

  • Experimental program(7)

Example Embodiment

[0040] Example 1. Prescription process of paclitaxel albumin nanoparticles
[0041] Table 1 The proportion of each component in the formulation of paclitaxel-containing albumin nanoparticles (mg)
[0042]
[0043]
[0044] Dissolve paclitaxel in prescriptions 1-30 in Table 1 in an appropriate amount of ethanol or other suitable solvents, dissolve the phospholipids in an appropriate amount of dichloromethane, and mix the two as the oil phase; dissolve albumin and antioxidants in an appropriate amount to remove Ionized water (water phase), drop the oil phase into the magnetically stirred water phase at room temperature or in an ice water bath, and continue to stir for a certain period of time, and then rotate and evaporate the ethanol and dichloromethane in a 40°C water bath to obtain paclitaxel-containing Albumin nanoparticles.

Example Embodiment

[0045] Example 2. Prescription process of docetaxel albumin nanoparticles
[0046] Table 2 The proportion of each component in the formulation of docetaxel-containing albumin nanoparticles (mg)
[0047]
[0048]
[0049] Dissolve docetaxel in prescriptions 1-30 in Table 2 in an appropriate amount of ethanol or other suitable solvents, dissolve the phospholipids in an appropriate amount of dichloromethane, and mix the two as the oil phase; dissolve albumin and antioxidants in an appropriate amount In deionized water (water phase), drop the oil phase into the magnetically stirred water phase at room temperature or in an ice water bath, and continue to stir for a certain period of time, and then rotate and evaporate in a water bath at 40°C to remove ethanol and dichloromethane. Albumin nanoparticles of paclitaxel.

Example Embodiment

[0050] Example 3 Pharmacodynamic test of paclitaxel-coated albumin nanoparticles on subcutaneous non-small cell lung cancer
[0051] Tumor cells: human non-small cell lung cancer A549 cells (purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences), cultured in DMEM medium containing 10% fetal bovine serum.
[0052] Animals: Balb/c nude mice, 4 weeks old, male. The test group and the negative control group had 6 nude mice in each group.
[0053] Tumor cell inoculation: use the right axillary subcutaneous inoculation model, take the vigorously growing A549 cells under aseptic conditions, digest the cells and resuspend them to about 2.0E7/ml cell suspension, and inoculate 0.1 subcutaneously in the right axillary of each mouse ml cancer cell suspension.
[0054] The tumor volume and tumor inhibition rate were calculated with the same method as before.
[0055] Each group was administered according to the dosing schedule in Table 3 for two weeks.
[0056] Table 3 The dosing schedule of each experimental group
[0057] Group
[0058] Table 4 Tumor suppression effect of different treatment groups
[0059] Group
[0060] * P<0.05, compared with the normal saline group; ※ P<0.05, compared with the paclitaxel injection group.
[0061] The experimental results of tumor volume and tumor inhibition rate are shown in Table 4, and the tumor volume changes are shown in figure 1 As shown; the results showed that the tumor volume of each drug treatment group was significantly smaller than the normal saline group on day 20 (p <0.05), indicating that each preparation has a certain therapeutic effect on subcutaneous tumors inoculated with A549 cells. But paclitaxel prescription 11 albumin nanoparticles at a dose of 5mg/kg have better tumor suppressing effects than paclitaxel injection at 10mg/kg, but there is no significant difference. At this time, the dose of albumin nanoparticles is only oral 50%; and paclitaxel prescription 11 albumin nanoparticles at a dose of 10mg/kg, its anti-tumor effect is significantly better than paclitaxel injection 10mg/kg group; albumin nanoparticles prepared by the present invention are better than the existing clinical paclitaxel The injection has a better therapeutic effect.
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