Microsphere drug carrier, preparation method, composition and use thereof
AssigneeXi'an Libang Medical Technology Co., Ltd.
InventorsRenle Hu, Jiucheng Wang, Tao Chen, Hua Liang, Duohao Ding, Yaqi Jiao
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Abstract
A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).
Claims12
A methoxy end-capped polyethylene glycol-polylactic acid block copolymer represented by the following formula (I):
- wherein:
- m=4˜454, preferably 20˜454, more preferably 120˜230 or 20˜45, and most preferably 45;
- n=4˜2778, preferably 60˜1400, more preferably 300˜1400 or 60˜150, and most preferably 400˜555;
- substituent group R is selected from:
- a. a neutral terminal group
- —H, —CH3, —CH2CH3, —CH2(CH2)xCH3, wherein x=1-8;
- b. a negatively charged terminal group
- one negative charge:
- —COCH2CH2CO2H
- two negative charges:
- —COCH2CH2CONHCH(CO2H)(CH2)2CO2H
- four negative charges:
- —COCH2CH2CONHCH[CONHCH(CO2)(CH2)2CO2H](CH2)2[CONHCH(CO2)(CH2)2CO2H];
- and
- c. a positively charged terminal group
- one positive charge:
- —COCH2CH2NH2
- two positive charges:
- —COCH2CH2NHCOCH(NH2)(CH2)4NH2
- four positive charges:
- —COCH2CH2NHCOCH[NHCOCH(NH2)(CH2)4NH2](CH2)4NH[COCH(NH2)(CH2)4NH2].
Use of a biodegradable methoxy end-capped polyethylene glycol-polylactic acid block copolymer or a derivative thereof represented by the following formula (I) in the preparation of a drug carrier,
- wherein:
- m=4˜454, preferably 20˜454, more preferably 120˜230 or 20˜45, and most preferably 45;
- n=4˜2778, preferably 60˜1400, more preferably 300˜1400 or 60˜150, and most preferably 400˜555;
- substituent group R is selected from:
- a. a neutral terminal group
- —H, —CH3, —CH2CH3, —CH2(CH2)xCH3 wherein x=1-8;
- b. a negatively charged terminal group
- one negative charge:
- —COCH2CH2CO2H
- two negative charges:
- —COCH2CH2CONHCH(CO2H)(CH2)2CO2H
- four negative charges:
- —COCH2CH2CONHCH[CONHCH(CO2)(CH2)2CO2H](CH2)2[CONHCH(CO2)(CH2)2CO2H];
- and
- c. a positively charged terminal group
- one positive charge:
- —COCH2CH2NH2
- two positive charges:
- —COCH2CH2NHCOCH(NH2)(CH2)4NH2
- four positive charges:
- —COCH2CH2NHCOCH[NHCOCH(NH2)(CH2)4NH2](CH2)4NH[COCH(NH2)(CH2)4NH2].
A methoxy end-capped polyethylene glycol-polylactic acid block copolymer derivative represented by the following formula (I):
- wherein:
- m=4˜454, preferably 20˜454, more preferably 120˜230 or 20˜45, and most preferably 45;
- n=4˜2778, preferably 60˜1400, more preferably 300˜1400 or 60˜150, and most preferably 400˜555;
- substituent group R is selected from:
- a. a negatively charged terminal group
- one negative charge:
- —COCH2CH2CO2H
- two negative charges:
- —COCH2CH2CONHCH(CO2H)(CH2)2CO2H
- four negative charges:
- —COCH2CH2CONHCH[CONHCH(CO2)(CH2)2CO2H](CH2)2[CONHCH(CO2)(CH2)2CO2H];
- and
- b. a positively charged terminal group
- one positive charge:
- —COCH2CH2NH2
- two positive charges:
- —COCH2CH2NHCOCH(NH2)(CH2)4NH2
- four positive charges:
- —COCH2CH2NHCOCH[NHCOCH(NH2)(CH2)4NH2](CH2)4NH[COCH(NH)(CH2)4NH2].
Dependencies are inferred from the claim text.