Camptothecin type medicine loaded on high molecular nano-microsphere, and its prepn. method

A technology of nano-microspheres and camptothecin, which is applied in the direction of medical preparations of non-active ingredients, drug combinations, anti-tumor drugs, etc., can solve the problems of low affinity and self-aggregation tendency, and achieve enhanced anti-tumor effects in vivo, The method is simple and easy, and the effect of low preparation cost

Inactive Publication Date: 2006-11-15
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In summary, although some exciting results have been obtained in the research on the loading and delivery system of non-water-soluble camptothecin drugs, due to the unique solubility of camptothecin drugs and the affinity of various carrier materials Too low and strong self-aggregation tendency, it is still impossible to use conventional carrier materials and processes to prepare camptothecin-carrying materials that are very satisfactory in terms of carrier size, drug loading, preparation cost, stability and biocompatibility. medicine system

Method used

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  • Camptothecin type medicine loaded on high molecular nano-microsphere, and its prepn. method
  • Camptothecin type medicine loaded on high molecular nano-microsphere, and its prepn. method
  • Camptothecin type medicine loaded on high molecular nano-microsphere, and its prepn. method

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preparation example 1

[0031] Preparation Example 1: Preparation of poly(lactide-caprolactone)-polyethylene glycol-poly(lactide-caprolactone) amphiphilic block copolymer (PCLLA-PEG-PCLLA)

[0032] Add calculated amounts of caprolactone (CL, Aldrich, USA) and lactide (LA, Aldrich, USA) and 0.1% (w / w) octanoic acid to a polymerization tube filled with an appropriate amount of polyethylene glycol (PEG). Stannous, wherein the number average molecular weight of PEG varies from 6000 to 10000 depending on the requirements of the product, but it is not limited to the above molecular weights. The tube was sealed under vacuum and placed at 130°C for 48 hours. The crude product obtained by the reaction was dissolved in chloroform and precipitated in a large amount of cold methanol to remove unreacted monomers and other low-molecular weight substances, and then the precipitate was collected and washed with water for several times and then dried under reduced pressure to obtain PCLLA-PEG-PCLLA 3 block polymers....

preparation example 2

[0033] Preparation example 2: Preparation of polycaprolactone-polyethylene glycol-polycaprolactone amphiphilic block copolymer (PCL-PEG-PCL)

[0034] Add a calculated amount of caprolactone (CL, Aldrich, USA) and 0.1% (w / w) stannous octoate into a polymerization tube filled with an appropriate amount of polyethylene glycol (PEG), wherein the number average molecular weight of PEG is based on the The requirements of the products are different, ranging from 2000, 6000 and 10000 respectively, but it is not limited to the above molecular weights. The tube was sealed under vacuum and placed at 130°C for 48 hours. The crude product obtained by the reaction was dissolved in chloroform and precipitated in a large amount of cold methanol to remove unreacted monomers and other low molecular weight substances, and then the precipitate was collected and washed with water several times and dried under reduced pressure to obtain PCL-PEG-PCL three block polymers. Corresponding to PEG molec...

preparation example 3

[0035] Preparation example 3: Preparation of diethylenetriaminepentaacetic acid-polycaprolactone-diethylenetriaminepentaacetic acid (DTPA-PCL-DTPA)

[0036] Diethylenetriaminepentaacetic acid (DTPA) dianhydride was prepared according to literature (CH Paik et al., Journal of Nuclear Medicine, Vol 24, Issue 12 1158-1163). The prepared DTPA bis-acid anhydride is stored in a desiccator after being purified and dried. A calculated amount of ethylene glycol (Aldrich, USA) was added into a sealed glass tube, and α, ω-dihydroxypolycaprolactone with a molecular weight of 2000 was prepared by ring-opening polymerization under the catalysis of stannous octoate. Add a certain amount of α, the anhydrous DMF solution (30%) of ω-dihydroxy polycaprolactone in the dropping funnel on the 100mL three-necked bottle, add excessive DTPA bis-acid anhydride and catalytic amount in the three-necked bottle The 4-dimethylaminopyridine (DMAP) was stirred and dissolved with an appropriate amount of anhy...

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Abstract

A camptothecine kind of medicines carried by high-molecular nanospheres for intravenous injection is composed of the biodegradable high-molecular nanospheres prepared from polyester or polyester-polyethanediol block copolymer and at least one camptothecine medicine (30 mass%). Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to camptothecin drugs, more specifically, to camptothecin drugs loaded on polymer nanospheres and a preparation method thereof. Background of the invention [0002] Camptothecin (CPT) is a cytotoxic alkaloid extracted from Campylodon chinensis, which acts on the cell's topoisomerase I (Top I), by preventing the cut DNA chain The recombination of camptothecin can effectively kill tumor cells. Although camptothecin and many of its derivatives have shown obvious antitumor effects in in vitro tumor model experiments, the solubility of these drugs in water or various biocompatible organic solvents is extremely low, so the dissolution rate is unsatisfactory. characteristics greatly restrict their practical application. In order to solve the solubility problem of camptothecin drugs, people have to use hydroxycamptothecin (HCPT) or CPT carboxylate aqueous solution with low drug efficacy and large toxic and side effects, or camptothecin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/16A61K31/47A61K47/34A61P35/00
Inventor 蒋锡群张乐洋杨昌正
Owner NANJING UNIV
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