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L-palmitoyl ascorbate/paclitaxel composition lipidosome

A technology of ascorbate and ascorbyl palmitate, which is applied in the field of liposome preparation of compound palmitoyl ascorbate and paclitaxel, can solve difficult drug encapsulation, large liposome particle size, inability to achieve sustained release, targeted Dosing and other issues

Inactive Publication Date: 2016-11-30
陈西敬
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The research of the present invention shows that when the ratio of palmitoyl ascorbate is greater than 16%, it is difficult to encapsulate the drug into liposomes, and the prepared liposomes have a larger particle size, and palmitoyl ascorbate is easy to separate out during placement, which cannot To achieve the purpose of sustained release and targeted drug delivery

Method used

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  • L-palmitoyl ascorbate/paclitaxel composition lipidosome
  • L-palmitoyl ascorbate/paclitaxel composition lipidosome
  • L-palmitoyl ascorbate/paclitaxel composition lipidosome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Embodiment 1: a kind of composition liposome formulation of compound palmitoyl ascorbate / paclitaxel and its preparation are as follows:

[0108] Experimental method: The liposome preparation process of the compound palmitoyl ascorbate / paclitaxel is as follows: paclitaxel, palmitoyl ascorbate, dimyristate phosphatidylcholine, and cholesterol are dissolved in chloroform, vortexed to complete After dissolving, add it to a 500mL eggplant-shaped flask, remove the organic solvent by rotary decompression evaporation at 70°C, and obtain a uniform lipid film on the wall of the bottle, dry it in a vacuum oven at 75°C overnight, add distilled water, and ultrasonically disperse the lipid film. After the plasma film was washed off, the probe was ultrasonicated for 2 cycles (30%, 20s, ultrasonic 1s off for 1s) in an ice-water bath, and the product was obtained.

[0109] Liposome evaluation method:

[0110] The measurement of the particle diameter of liposome: adopt laser particle si...

Embodiment 2

[0118] Embodiment 2: a kind of composition liposome formulation of compound palmitoyl ascorbate / paclitaxel and its preparation are as follows:

[0119] Experimental method: The liposome preparation process of the compound palmitoyl ascorbate / paclitaxel is as follows: paclitaxel, palmitoyl ascorbate, soybean lecithin, and sitosterol are dissolved in chloroform, vortexed until completely dissolved, and then 500 mL of solanum is added. In a shaped flask, the organic solvent was removed by rotary decompression evaporation at 60°C, and a uniform lipid film was prepared on the wall of the bottle. After drying overnight at 35°C in a vacuum oven, distilled water was added, and the lipid film was washed off by ultrasonic waves. , Probe ultrasound 4 cycles (80%, 50s, ultrasound 1s stop 1s) under ice-water bath, namely.

[0120] Experimental results:

[0121] Table 2. The experimental result of embodiment 2

[0122]

[0123] Paclitaxel: PTX, Palmitoyl Ascorbate: PA

[0124] Prepara...

Embodiment 3

[0125] Embodiment 3: a kind of composition liposome formulation of compound palmitoyl ascorbate / paclitaxel and its preparation are as follows:

[0126] Experimental method: the liposome preparation technology of described compound palmitoyl ascorbate / paclitaxel is: paclitaxel, palmitoyl ascorbate, dipalmitoyl phosphatidylcholine, cholesterol hemisuccinate are dissolved in chloroform, vortexed Rotate until completely dissolved, add to a 500mL eggplant-shaped flask, and evaporate under reduced pressure at 70°C to remove the organic solvent, and obtain a uniform lipid film on the wall of the bottle, place it in a vacuum drying oven at 75°C to dry overnight, then add distilled water, After the lipid film was washed off by ultrasound, the probe was ultrasonicated for 6 cycles in an ice-water bath (30%, 60s, ultrasonic 1s off for 1s), and the product was obtained.

[0127] Experimental results:

[0128] Table 3. The experimental result of embodiment 3

[0129]

[0130] Paclitax...

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Abstract

The invention discloses a composition lipidosome preparation used for parenteral administration tumor treatment. The composition lipidosome preparation comprises following ingredients: paclitaxel, L-palmitoyl ascorbate, a phospholipid substance, and a cholesterol analogue. According to a preparation method, L-palmitoyl ascorbate and paclitaxel are combined, the particle size of the obtained lipidosome is uniform, encapsulation efficiency is high, and drug releasing properties are excellent. It is found via in vivo and in vitro experiments that anti-tumor effect of paclitaxel is improved obviously; drug effect of paclitaxel can be achieved at a relatively low dosage; drug administration is realized via intravenous administration, artery administration, intramuscular administration, subcutaneous administration, intraperitoneal administration, and the like; and especially, clinical application availability and safety of paclitaxel are improved via interventional administration methods such as intravenous injection or intratumor injection.

Description

technical field [0001] The invention relates to a composition liposome preparation for injecting drugs for treating tumors, in particular to a method for preparing a composition liposome of compound palmitoyl ascorbate and paclitaxel. Background technique [0002] Paclitaxel (Paclitaxel, PTX, chemical structure see Figure 8 ) is a diterpenoid compound originally isolated from the bark of the plant Yew brevifolia, and is one of the most effective natural anticancer drugs found so far. Paclitaxel has a significant effect on advanced ovarian cancer, breast cancer, melanoma, lung cancer, head and neck squamous cell carcinoma, cervical cancer, esophageal cancer, lymphoma, and brain tumor, and has a high cure rate for refractory ovarian cancer and metastatic breast cancer. It has good prospects for the treatment of prostate cancer, gastrointestinal cancer, small cell and non-small cell lung cancer. Paclitaxel is a white crystalline powder, and its chemical properties are relativ...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K31/375A61K9/127A61P35/00
CPCA61K9/127A61K31/337A61K31/375A61K2300/00
Inventor 卢杨王子厚封帆陈西敬赵娣李宁陈琪马恩龙张玲
Owner 陈西敬
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