PMID: 8953502Oct 1, 1996Paper

Blood-brain-barrier transport of lipid microspheres containing clinprost, a prostaglandin I2 analogue

The Journal of Pharmacy and Pharmacology
T MinagawaA Tsuji

Abstract

Because the permeability of the blood-brain barrier to lipid microspheres (LMs) has not hitherto been demonstrated, blood-brain-barrier permeability to LM containing the prostaglandin I2 analogue clinprost has been evaluated for an in-vitro system of primary cultured monolayers of bovine brain capillary endothelial cells (BCECs), by a capillary depletion study in rats and by an in-situ brain perfusion study in normal and 4-vessel-occluded fore brain ischaemic rats. Although energy-dependency was not observed in [3H]clinprost uptake by BCECs, in accordance with results for simple diffusional transport, uptake of [3H]clinprost contained in lipid microspheres (denoted [3H]clinprost(LM)) was significantly inhibited by the endocytosis inhibitor, dansylcadaverine. The transport of LM into BCECs by endocytosis was also confirmed by fluorescence microscopy and flow-cytometric analysis using LM labelled with a fluorescent probe, 1,1'-dioctadecyl-3,3,3',3'-tetramethylindocarbocyanine perchlorate (Dil). The absolute uptake of Dil(LM) by BCECs, measured by HPLC, was, however, almost 1/10 that of [3H]clinprost(LM), results which suggest the superiority of simple diffusion of clinprost over endocytosis of its LM form in the uptake of clinpro...Continue Reading

References

May 1, 1979·Stroke; a Journal of Cerebral Circulation·W A Pulsinelli, J B Brierley
Jan 1, 1994·Biological & Pharmaceutical Bulletin·T TakinoM Hashida

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Citations

Aug 7, 2002·European Journal of Pharmacology·Yasuko KarasawaHiroaki Araki
May 20, 1999·Journal of Controlled Release : Official Journal of the Controlled Release Society·S C YangC Z Yang
Apr 5, 2013·Expert Opinion on Drug Delivery·Medha PatelKamalinder K Singh
Mar 4, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Indu Pal KaurVandita Kakkar
Sep 1, 2015·Neurochemistry International·Rajat SandhirNitin Singhal
Oct 25, 2000·The Journal of Pharmacy and Pharmacology·V PodioM R Gasco
Nov 7, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mona QushawyAli Nasr
Nov 25, 2020·Organic Letters·Nariyoshi Umekubo, Yujiro Hayashi

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