HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Enhanced oral bioavailability of a cancer preventive agent (SR13668) by employing polymeric nanoparticles with high drug loading.

Abstract
SR13668 [2,10-Dicarbethoxy-6-methoxy-5,7-dihydro-indolo-(2,3-b)carbazole] has been proven effective in cancer prevention, but the limited bioavailability has hindered its clinical translation. In this study, we have developed a continuous, scalable process to form stable poly(lactic-co-glycolic acid) nanoparticles encapsulating SR13668, based on understanding of the competitive kinetics of nanoprecipitation and spray drying. The optimized formulation achieved high drug loading (33.3 wt %) and small particles (150 nm) with narrow size distribution. The prepared nanoparticle suspensions through flash nanoprecipitation were spray dried to achieve long-term stability and to conveniently adjust the nanoparticle concentration before use. In vitro release of SR13668 from the nanosuspensions was measured in a solution with separated organic and aqueous phases to overcome the limit of SR13668 low water solubility. Higher oral bioavailability of SR13668 by employing polymeric nanoparticles compared with the Labrasol® formulation was demonstrated in a mouse model.
AuthorsHao Shen, Aryamitra A Banerjee, Paulina Mlynarska, Mathew Hautman, Seungpyo Hong, Izet M Kapetanovic, Alexander V Lyubimov, Ying Liu
JournalJournal of pharmaceutical sciences (J Pharm Sci) Vol. 101 Issue 10 Pg. 3877-85 (Oct 2012) ISSN: 1520-6017 [Electronic] United States
PMID22821759 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
CopyrightCopyright © 2012 Wiley-Liss, Inc.
Chemical References
  • Carbazoles
  • Polymers
  • SR 13668
  • Suspensions
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
Topics
  • Administration, Oral
  • Animals
  • Biological Availability
  • Carbazoles (administration & dosage, chemistry, pharmacology)
  • Chemistry, Pharmaceutical (methods)
  • Drug Stability
  • Kinetics
  • Lactic Acid (administration & dosage, chemistry)
  • Mice
  • Nanoparticles (administration & dosage, chemistry)
  • Particle Size
  • Polyglycolic Acid (administration & dosage, chemistry)
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers (administration & dosage, chemistry)
  • Solubility
  • Suspensions (administration & dosage, chemistry, pharmacology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: