All-trans-retinoic acid nanodisks.
Nanodisks are nanoscale, disk-shaped phospholipid bilayers whose edge is stabilized by association of apolipoprotein molecules. Self-assembled ND particles enriched with all-trans-retinoic acid (ATRA) (phospholipid:ATRA molar ratio = 5.5:1) were generated wherein all reaction components were solubilized. ATRA-ND migrated as a single band (Stokes' diameter approximately 20 nm) on native gradient polyacrylamide gel electrophoresis. ATRA, phospholipid and apolipoprotein co-eluted from a Sepharose 6B gel filtration column, consistent with stable integration of ATRA into the ND particle milieu. Spectroscopic analysis of ATRA-ND in buffer yielded an absorbance spectrum characteristic of ATRA. ATRA-ND mediated time-dependent inhibition of cultured HepG2 cell growth more effectively than free ATRA. The nanoscale size of the formulation particles and the stable integration of biologically active ATRA suggest ND represent a potentially useful vehicle for solubilization and in vivo delivery of ATRA.
Redmond
Katherine A
KA
Center for Prevention of Obesity, Cardiovascular Disease and Diabetes, Children's Hospital Oakland Research Institute, 5700 Martin Luther King Jr. Way, Oakland, CA 94609, USA.
Nguyen
Thanh-Son
TS
Ryan
Robert O
RO
D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D006801:Humans; D008051:Lipid Bilayers / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D014212:Tretinoin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology
D008051:Lipid Bilayers; D014212:Tretinoin