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A carbowax modified stealthy liposome nanosphere of hydroxycamtothecine and preparation method thereof

A technology of hydroxycamptothecin and stealth lipids, which is applied in the field of medicine, can solve the problems of increasing the toxicity of the reticuloendothelial system, affecting the stability of preparations, and leakage of hydroxycamptothecin, so as to improve long-term stability and improve passive targeting The effect of simple and easy preparation method

Active Publication Date: 2006-12-13
JIANKANGYUAN PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a drug delivery system, the emulsion has obvious targeting of the lymphatic system and the mononuclear phagocyte system (MPS), and has a better therapeutic effect on liver cancer. Toxicity of the reticuloendothelial system
In addition, due to the thin interfacial film of the emulsion, hydroxycamptothecin leakage is prone to occur during long-term storage, resulting in a decrease in encapsulation efficiency and drug precipitation, thereby affecting the stability of the formulation

Method used

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  • A carbowax modified stealthy liposome nanosphere of hydroxycamtothecine and preparation method thereof
  • A carbowax modified stealthy liposome nanosphere of hydroxycamtothecine and preparation method thereof
  • A carbowax modified stealthy liposome nanosphere of hydroxycamtothecine and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] prescription:

[0036] Hydroxycamptothecin 0.02%

[0037] Vitamin E 2%

[0038] MCT 8%

[0039] Macrogol 1000 Vitamin E Succinate 3%

[0040]Soy Lecithin 2%

[0041] water balance

[0042] Preparation:

[0043] Take the prescription amount of hydroxycamptothecin, vitamin E, MCT, polyethylene glycol 1000 vitamin E succinate, soybean lecithin and dissolve them in ethanol, evaporate the organic solvent with a rotary evaporator as the organic phase, and mix with the prescription amount of water Mix and homogenize under high pressure, and store in a sealed container at 4°C. After diluting with normal saline, measure the average particle size with Nicomp TM 380ZLS particle size analyzer, see figure 1 .

[0044] The average particle diameter of the obtained product is 130.9nm, and the polydispersity index (PI)=0.063.

Embodiment 2

[0046] prescription:

[0047] Hydroxycamptothecin 0.04%

[0048] Vitamin E 2%

[0049] MCT 8%

[0050] Macrogol 2000 Vitamin E Succinate 5%

[0051] Yolk Lecithin 3%

[0052] Oleic acid 0.02%

[0053] water balance

[0054] Preparation:

[0055] Dissolve hydroxycamptothecin, vitamin E, MCT, polyethylene glycol 2000 vitamin E succinate, egg yolk lecithin, and oleic acid in ethanol in the prescribed amount, and use a rotary evaporator to evaporate the organic solvent as the organic phase; Amount of water mixed, high-pressure homogenization, 4 ℃ sealed storage. After diluting with normal saline, measure the average particle size with Nicomp TM 380ZLS particle size analyzer, see image 3 .

[0056] The average particle diameter of the obtained product is 102.9 nm, and the polydispersity index (PI)=0.174.

Embodiment 3

[0058] prescription:

[0059] Hydroxycamptothecin 0.02%

[0060] MCT 15%

[0061] Macrogol 1000 Vitamin E Succinate 6%

[0062] Soy Lecithin 4%

[0063] Vitamin C 0.02%

[0064] water balance

[0065] Preparation:

[0066] Take the prescription amount of hydroxycamptothecin, MCT, polyethylene glycol 1000 vitamin E succinate, soybean lecithin and dissolve them in dichloromethane, evaporate the organic solvent with a rotary evaporator as the organic phase; take the prescription amount of vitamin C Soluble in water, mix the aqueous phase with the organic phase, homogenize under high pressure, and store in a sealed container at 4°C.

[0067] The freeze-drying process is as follows: get 10% (by weight) trehalose, dissolve it in the aqueous dispersion of hydroxycamptothecin stealth lipid nanospheres modified by polyethylene glycol, divide it into vials, and place it in a freeze-drying apparatus. Pre-freeze at -40°C for 3 hours, then raise the temperature to -10°C at 5°C / h, ma...

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Abstract

The invention relate to polyethylene glycol modified hydroxycamptothecin stealth greasy nano balls for intravenous injection and its preparing process, which comprises treatment effective amount of hydroxycamptothecin, polyethylene glycol esters, oil for injection, phosphatides and pharmaceutically acceptable auxiliary material by the weight ratio of 0.01-0.2%, 1-10%, 5-25%, 0-10%, 0-10%, and balancing water. The invention also discloses the preparing prcesss including dissolving liposoluble materials into organic solvents, dissolving water-soluble auxiliary materials and addition agents into water, mixing with organic phase, homogenizing or carrying out supersonic treatment.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a polyethylene glycol-modified stealth lipid nanosphere and a preparation method thereof, in particular to a polyethylene glycol-modified hydroxycamptothecin stealth lipid nanosphere and a preparation method thereof. Background technique [0002] Hydroxycamptothecin is a trace alkaloid with the strongest anti-cancer effect among similar anti-tumor monomers extracted from camptotheca in the 1960s and 1970s, and it was used clinically in the 1980s. Hydroxycamptothecin is a cell cycle-specific drug that mainly acts on the DNA synthesis phase (S phase). Pharmacological studies have shown that its anti-cancer mechanism is to inhibit DNA topoisomerase I (Topo I), and it has certain curative effects on ascites-type liver cancer, head and neck tumors, gastric cancer, bladder cancer and leukemia. Hydroxycamptothecin is a cytotoxic drug, which has obvious effects on normal cells while kill...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/19A61K31/4745A61K31/685A61K47/30A61P35/00
Inventor 甘勇张馨欣甘莉
Owner JIANKANGYUAN PHARMA GROUP
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