Delivery of loperamide across the blood-brain barrier with polysorbate 80-coated polybutylcyanoacrylate nanoparticles

被引:291
作者
Alyautdin, RN
Petrov, VE
Langer, K
Berthold, A
Kharkevich, DA
Kreuter, J
机构
[1] UNIV FRANKFURT,INST PHARMACEUT TECHNOL,D-60439 FRANKFURT,GERMANY
[2] IM SECHENOV MED ACAD,DEPT PHARMACOL,MOSCOW 119881,RUSSIA
关键词
loperamide; nanoparticles; polysorbate; 80; drug delivery; brain; PHYSICOCHEMICAL CHARACTERIZATION; CARRIERS; SURFACE;
D O I
10.1023/A:1012098005098
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Purpose, The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid agonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used to indicate drug transport through this barrier. Methods. Loperamide was incorporated into PBCA nanoparticles. Drug-containing nanoparticles were coated with polysorbate 80 and injected intravenously into mice. Analgesia was then measured by the tail-flick test. Results. Intravenous injection of the particulate formulation resulted in a long and significant analgesic effect. A polysorbate 80 loperamide solution induced a much less pronounced and very short analgesia. Uncoated nanoparticles loaded with loperamide were unable to produce analgesia. Conclusions. Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain.
引用
收藏
页码:325 / 328
页数:4
相关论文
共 16 条
[1]  
ALYAUTDIN R, 1995, EUR J PHARM BIOPHARM, V41, P44
[2]   EFFECTS OF POLYSORBATE 80 ON THE ABSORPTION AND DISTRIBUTION OF ORAL METHOTREXATE (MTX) IN MICE [J].
AZMIN, MN ;
STUART, JFB ;
CALMAN, KC ;
FLORENCE, AT .
CANCER CHEMOTHERAPY AND PHARMACOLOGY, 1982, 9 (03) :161-164
[3]  
AZMIN MN, 1985, CANCER CHEMOTH PHARM, V14, P238
[4]  
BECK PH, 1994, EUR J PHARM BIOPHARM, V40, P134
[5]   COLLOIDAL CARRIERS FOR INTRAVENOUS DRUG TARGETING - PLASMA-PROTEIN ADSORPTION PATTERNS ON SURFACE-MODIFIED LATEX-PARTICLES EVALUATED BY 2-DIMENSIONAL POLYACRYLAMIDE-GEL ELECTROPHORESIS [J].
BLUNK, T ;
HOCHSTRASSER, DF ;
SANCHEZ, JC ;
MULLER, BW ;
MULLER, RH .
ELECTROPHORESIS, 1993, 14 (12) :1382-1387
[6]   UPTAKE OF SURFACTANT-COATED POLY(METHYL METHACRYLATE)-NANOPARTICLES BY BOVINE BRAIN MICROVESSEL ENDOTHELIAL-CELL MONOLAYERS [J].
BORCHARD, G ;
AUDUS, KL ;
SHI, FL ;
KREUTER, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1994, 110 (01) :29-35
[7]   PARTICLE SIZING BY PHOTON-CORRELATION SPECTROSCOPY .1. MONODISPERSE LATTICES - INFLUENCE OF SCATTERING ANGLE AND CONCENTRATION OF DISPERSED MATERIAL [J].
DEJAEGER, N ;
DEMEYERE, H ;
FINSY, R ;
SNEYERS, R ;
VANDERDEELEN, J ;
VANDERMEEREN, P ;
VANLAETHEM, M .
PARTICLE & PARTICLE SYSTEMS CHARACTERIZATION, 1991, 8 (03) :179-186
[8]   LOPERAMIDE - EVIDENCE OF INTERACTION WITH MU-OPIOID AND DELTA-OPIOID RECEPTORS [J].
GIAGNONI, G ;
CASIRAGHI, L ;
SENINI, R ;
REVEL, L ;
PAROLARO, D ;
SALA, M ;
GORI, E .
LIFE SCIENCES, 1983, 33 :315-318
[9]   PASSAGE OF PEPTIDES THROUGH THE BLOOD-BRAIN-BARRIER WITH COLLOIDAL POLYMER PARTICLES (NANOPARTICLES) [J].
KREUTER, J ;
ALYAUTDIN, RN ;
KHARKEVICH, DA ;
IVANOV, AA .
BRAIN RESEARCH, 1995, 674 (01) :171-174
[10]   PHYSICOCHEMICAL CHARACTERIZATION OF POLYACRYLIC NANOPARTICLES [J].
KREUTER, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1983, 14 (01) :43-58