摘要:
A cyclotriphosphazene represented by Formula 1 prepared by introducing a dendritic tetrapeptide and a hydrophilic polyethylene glycol into a cyclotriphosphazene ring, a method of preparing the same, and a drug carrier including the cyclotriphosphazene of Formula 1.The compound according to the present invention may form a strong molecular hydrogel in a very low concentration of 2 w/w % or less. Furthermore, the hydrogel prepared using the compound of Formula 1 exhibits biodegradability, thermosensitivity at around body temperature, biocompatibility with protein drugs, and an easy way to prepare along with a sustained release property without any burst effect in the early stage of release. Therefore, the present cyclotriphosphazene molecular hydrogel may be efficiently used as a drug carrier for a sustained release of a drug, particularly, a protein drug.
摘要:
A cyclotriphosphazene represented by Formula 1 prepared by introducing a dendritic tetrapeptide and a hydrophilic polyethylene glycol into a cyclotriphosphazene ring, a method of preparing the same, and a drug carrier including the cyclotriphosphazene of Formula 1.The compound according to the present invention may form a strong molecular hydrogel in a very low concentration of 2 w/w % or less. Furthermore, the hydrogel prepared using the compound of Formula 1 exhibits biodegradability, thermosensitivity at around body temperature, biocompatibility with protein drugs, and an easy way to prepare along with a sustained release property without any burst effect in the early stage of release. Therefore, the present cyclotriphosphazene molecular hydrogel may be efficiently used as a drug carrier for a sustained release of a drug, particularly, a protein drug.
摘要:
The present invention relates to an amphiphilic cyclic phosphazene trimer which is biocompatible and a method for preparing the same. The present invention also relates to pharmaceutical formulations of hydrophobic drugs that are micelle-encapsulated by the amphiphilic cyclic phosphazene trimer and a method for preparing the same.
摘要:
Disclosed are a new class of a polyphosphazene-platinum(II) conjugate antitumor agent having high tumor tissue selectivity due to its enhanced permeability and retention effect to tumor tissues, and a preparation method thereof: wherein x represents the number of the ethylene oxide repeating unit and is 7, 12 or 16; y is 0, 1 or 2; z represents molar content of polyethylene glycol in the range of 0.5-1.5; n represents degree of polymerization of polyphosphazene in the range of 30-100; and A-A represents a diamine.
摘要:
The present invention relates to a thermosensitive and biocompatible poly(organophosphazenes) represented by Formula 1, and a preparation method thereof: wherein R is a methyl or ethyl group; R′ is selected from the group consisting of COOR, CH2COOR, CH2CH2COOR, CH2CH(CH3)2, CH2C6H5, CH(CH3)CH2CH3 and CH3; R″ is selected from the group consisting of CH2COOR, CH2CH2COOR, CH2CH(CH3)2, CH2C6H5, CH(CH3)CH2CH3 and CH3; R′″ is a group selected from the group consisting of CH2COOR, CH2CH2COOR and H, wherein R is the same as defined above; n is a number between from 30 to 100; x is a number selected from the integers of 3, 4, 7, 12 and 16; y is a number between from 0.5 to 1.5; a equals to 1; and b and c equal to 0 or 1.
摘要:
Disclosed are a platinum (II) complex of N-substituted amino dicarboxylate showing antitumor activity represented by the following formula (1) and a preparation method thereof: wherein n is 1 or 2; A—A is a diamine selected from the group consisting of trans-(±)-1,2-diaminocyclohexane, ethylenediamine and 2,2-dimethyl-1,3-propanediamine; and R1 is hydrogen and R2 is RCO or RSO2, wherein R is an alkyl selected from the group consisting of methyl, ethyl, n-propyl, n-butyl and t-butyl or an aryl selected from the group consisting of phenyl and substituted phenyl group, or R1R2 is phthaloyl.
摘要:
The present invention relates to novel cyclotriphosphazene derivatives represented by Formula (1) and a preparation method thereof wherein HNA is an amino acid group selected from glycine group(—NHCH2COO−), aminomalonic acid group(—NHCH(COO−)2), aspartic acid group (—NHCH(CH2COO−)COO−) and glutamic acid group (—NHCH(CH2CH2COO−)COO−), m is a repeating unit of poly(alkoxyethyleneglycol) selected from 2, 7, 12 and 16, and n is an integer representing number of alkyl carbons and selected from 0, 1, and 3.
摘要:
The present invention relates to novel biodegradable polyphosphazenes represented by Formula 1 and a preparation method thereof. Polyphosphazenes of the present invention not only have thermosensitivity and biodegradability simultaneously, but also their phase transition temperature and degradation rate can be controlled.
摘要:
Platinum (IV) complexes for oral administration represented by the structural formula ##STR1## where A--A is a symmetrical diamine that can chelate to platinum and is selected from the group consisting of ethylene diamine, t(.+-.)-1,2-diaminocyclohexane, 2,2-dimethyl-1,3-propanediamine, cyclohexane-1,1-dimethaneamine and tetrahydro-4H-pyran-4,4-dimethaneamine; and R is propionyl, butyryl or valeryl. These complexes are useful in the treatment of cancer.
摘要:
The present invention relates to a new class of cationic linear polyphosphazenes bearing as side groups a hydrophilic poly(ethylene glycol) and a spacer group selected from the group consisting of lysine, oligopeptides containing lysine, amino-ethanol, amino-propanol, amino-butanol, amino-pentanol and amino-hexanol, and the polyphosphazene-drug conjugates comprising hydrophobic anticancer drugs by covalent bonding and the preparation methods thereof. The present polyphosphazene-drug conjugates exhibit outstanding tumor selectivity and low toxicity.