An antineoplastic dendritic polymer drug delivery system

A dendritic and polymer technology, applied in antineoplastic drugs, drug combinations, pharmaceutical formulations, etc.

Inactive Publication Date: 2004-12-29
DENDRITIC NANO TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, U.S. Patent No. 5,338,532 does not specifically teach or mention the application of polymer complexes as carriers for releasing cisplatin, carboplatin, titanium dichlorocyclopentadienyl and dihalogenated diorganotin or other antineoplastic agents

Method used

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  • An antineoplastic dendritic polymer drug delivery system
  • An antineoplastic dendritic polymer drug delivery system
  • An antineoplastic dendritic polymer drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0052] The preparation method of the antitumor dendritic polymer complex is to dissolve the dendritic polymer in a suitable solvent, such as water, and the dendritic polymer and the dissolved antitumor agent are sufficient to make the two combine to form the dendritic polymer-anti-tumor agent. exposure to tumor agent complexes under conditions. The molar ratio of cisplatin to dendrimer (PAMAM with a degree of polymerization of 3.5, EDA core, and dendrimer dendrimer) is 35:1, which is the ratio used in the experiments in the examples of the present invention. The ratio of cisplatin to polymer molecules is important. Platinum esters of dendrimers having a molar ratio of cisplatin to polymer of 100:1 to 1:1 may have good practical advantages. Antineoplastic agents are encapsulated in polymers using shunt technology, and the anions (such as carboxylate groups) on the surface of the polymers have weak forces to enable antineoplastic agents to be taken up by dendrimers (primary act...

Embodiment 1

[0094] Example 1 Effects of PAMAM dendrimers on the stability of mouse erythrocytes cultured in vitro

[0095] method

[0096] Poly(amidoamine) dendrimers (cationic and anionic) of increasing degrees of polymerization were incubated with erythrocytes from adult Wistar rats. Interaction of dendrimer with erythrocytes was assessed spectrophotometrically by cytolysis-induced release of hemoglobin, detection at 550 nm. Different concentrations of dendrimer, control (methanol (BOH)), poly-L-lysine (hydrobromide-56.5KD Mw (Sigma)) and dextran (74KD Mw (Sigma)) (solution in physiological buffered saline) and mouse erythrocytes were co-cultured for 1 hour at 37°C and 10 rpm (in a shaking water bath). Afterwards, the erythrocytes were centrifuged at 1500×g for 10 minutes to pellet the cells, 100 μl of floating matter on the surface were removed, and PBS was used as a blank for spectrophotometric analysis. see attached results figure 1 and 2 As indicated, the percent hemoglob...

Embodiment 2

[0099] Example 2 Cytotoxicity of unmodified dendrimers on B16F10 cells

[0100] method

[0101] B16F10 cells are an adherent murine melanoma cell line. B16F10 cells at 1 x 10 per ml 5 pcs (1×10 per hole 4 cells) in 96-well microtiter plates (Costar) in RPMI 1640 tissue culture medium (Gibco) supplemented with 10% FCS (Gibco). All cell growth and cytotoxic incubations were performed at 37°C, 5% CO 2 under conditions.

[0102] Evaluation of cell density was performed with a modified neurenbrow cell counter (Sigma). Cells were washed twice with PBS and fresh RPMI medium (and supplemented with FCS) was added, and cells were then cultured on microtiter plates. Cells were left for 24 hours and recovered and reattached.

[0103] All polymers and controls were dissolved in RPMI medium (supplemented with FCS) and sterilized through a 0.2 [mu]m sterile filter with initial minimal loss of solution due to filter adhesion. Cells were then added at increasing concentrations of...

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Abstract

Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared. The antineoplastic agent is encapsulated within the dendritic polymer using an ionic charge shunt mechanism, whereby, the antineoplastic agent interacts with the anionic functional groups on the surface of the dendritic polymer allowing the antineoplastic agent to be uptaken by the dendritic polymer through an association with the functional groups of the interior of the dendritic polymer. The antineoplastic dendritic polymer conjugates may be administered intravenously, orally, parentally, subcutaneously, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, and reduced toxicity.

Description

technical field [0001] The present invention relates to the application of dendritic polymer complexes loaded with antineoplastic drugs to treat animal, especially human cancer. Background technique [0002] Polymers as drug carriers, especially for those drugs that have low solubility at physiological pH, are toxic to normal tissues, or cannot be administered in sufficient doses, have become the subject of interesting research in recent years[ For example, H. Ringsdorf, J. Polymer Sci.: Symp. 51 , 135-153 (1975)] Polymeric carriers of antineoplastic drugs can provide effective drug delivery systems because of their solubility, toxicity and high dose characteristics in terms of release properties. Some research results on the release of doxorubicin are cited here for explanation [such as: R.Duncan et al., "Preclinical Toxicology of a Novel Polymeric Antitumor Agent: I-copolymer-doxorubicin (PK1)", Hum.Exp.Toxiocol. 17 (2), 93-104 (1998); P.A. Vassey et al., "Phase I Clini...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K33/24A61K47/48A61P35/00A61P35/02C08G73/04
CPCA61K47/48207A61K47/595A61P35/00A61P35/02
Inventor N·马利克R·敦坎D·A·托马利亚R·爱斯芬德
Owner DENDRITIC NANO TECH INC
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