共 150 条
Transporter targeted drug delivery
被引:6
作者:
Mandava, N.
[1
]
Oberoi, R. K.
[1
]
Minocha, M.
[1
]
Mitra, A. K.
[1
]
机构:
[1] Univ Missouri, Sch Pharm, Div Pharmaceut Sci, Kansas City, MO 64108 USA
基金:
美国国家卫生研究院;
关键词:
Efflux proteins;
Multi-drug resistance;
ATP-binding cassette;
Substrate;
Transporter;
Transporter targeted drug delivery;
Pro-drug;
Bioavailability;
AMINO-ACID TRANSPORTER;
MULTIDRUG-RESISTANCE PROTEIN;
DEPENDENT MULTIVITAMIN TRANSPORTER;
ORGANIC ANION TRANSPORTER;
BLOOD-BRAIN-BARRIER;
MONOESTER GANCICLOVIR PRODRUGS;
DIPEPTIDE ESTER PRODRUGS;
ABC HALF-TRANSPORTER;
P-GLYCOPROTEIN;
PEPTIDE TRANSPORTERS;
D O I:
10.1016/S1773-2247(10)50012-1
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
The pharmacological behavior of various drugs is severely affected by biological barrier,. such as epithelial tight junctions, efflux proteins and metabolizing enzymes. Apart from the biological barriers, physicochemical properties of drug molecules such as molecular weight, lipophilicity, surface charge and solubility also play MIC ill absorption characteristics of drug candidates. Pharmacological properties affected by efflux pumps such as P-gp and MRPs include bioavailability, hepatobiliary and urinary excretion of drugs as well as drug metabolites. This leads to sub-therapeutic concentrations of various potential drugs at the target site. One of the strategies to overcome these biological barriers is transporter targeted prodrug design. Prodrag derivatization targeting membrane transporters and receptors improves drug absorption. Various prodrugs which have been synthesized solar demonstrated enhanced bioavailability and tissue specilicity. This review mainly focuses on the efflux pumps which play an important role in drag absorption and a few strategies to overcome these efflux pumps.
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页码:89 / 99
页数:11
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