Abstract：
:The objective of the current study was to develop and evaluate VLDL-resembling phospholipid-submicron emulsion (PSME) as a carrier system for new cholesterol-based compounds for targeted delivery to cancer cells. BCH, a boronated cholesterol compound, was originally developed in our laboratory to mimic the cholesterol esters present in the LDL and to follow a similar pathway of cholesterol transport into the rapidly dividing cancer cells. The VLDL-resembling system was then designed to solubilize BCH, facilitate the interaction with LDL, and thus assist the BCH delivery to cancer cells. BCH-containing PSME was prepared by sonication. Chemical compositions and particle sizes of different PSME fractions were determined. The lipid structure of PSME and location of BCH in the formulation were assessed based on experimental results. Density gradient ultracentrifugation fractionated the emulsion into three particle-size populations with structures and compositions resembling native VLDL. In vitro interaction between PSME and LDL was evident by agarose electrophoresis, as both formed a single band with an intermediate mobility. The transfer of BCH from PSME to LDL was also observed in the presence of other serum components including serum proteins. Cell culture data showed sufficient uptake of BCH in rat 9L glioma cells (> 50 microg boron/g cells). In conclusion, this system has the capability to incorporate the cholesterol-based compound, interact with native LDL, and assist the delivery of this compound into cancer cells in vitro.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Shawer M,Greenspan P,ØIe S,Lu DRdoi
10.1002/jps.10117subject
Has Abstractpub_date
2002-06-01 00:00:00pages
1405-13issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(16)31022-Xjournal_volume
91pub_type
杂志文章abstract：:The thermodynamic relationship between FI and FII of ethyl 4-aminobenzoate (benzocaine) has been investigated. Slurry conversion experiments show that the transition temperature below which FI is stable is located between 302 K-303 K (29 °C-30 °C). The polymorphs FI and FII have been characterised by infrared spectros...
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600651036
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更新日期：1979-11-01 00:00:00
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更新日期：2019-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：1986-09-01 00:00:00
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abstract：:The intense blue color formed in the official assay of menadione injection by treatment of the sample with 2,4-dinitrophenylhydrazine and ammonia is shown by data from visible light spectra and mass spectra and by comparison of the pKa value with that of the corresponding reaction product of acetone to be due to proto...
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