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Comparison of Pharmacokinetic Profiles of PM02734 Loaded Lipid Nanoparticles and Cyclodextrins: In Vitro and In Vivo Characterization

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Abstract:

PM02734 is a chemically synthesized depsipeptide derived from the marine kahalalides family with a broad spectrum of activity against solid tumors in vitro and in vivo, but presenting low bioavailability. In this work, solid lipid nanoparticles made of Precirol® ATO 5 have been developed using a hot homogenization method followed by high shear homogenization and ultrasonication. These solid lipid nanoparticles show suitable size (around 150 nm) and encapsulation efficiency (nearly 70%) for the oral administration of the compound PM02734. A physical-chemical stability study was performed after 6 months of storage at different thermical conditions, concluding that solid lipid nanoparticles stored at 4 °C were more stable than solid lipid nanoparticles stored at 25 °C. The pharmacokinetic profile of drug-loaded solid lipid nanoparticles was also evaluated in Beagle dogs and compared with that of a cyclodextrin-based delivery system by means of AUC, C max and T max parameter estimation. Solid lipid nanoparticle based formulation provided a sustained release of the drug for a longer period of time than the cyclodextrins.

Keywords: CANCER TREATMENT; IN VITRO; IN VIVO; LIPID NANOPARTICLES; PHARMACOKINETICS; PM02734

Document Type: Research Article

DOI: http://dx.doi.org/10.1166/jbn.2012.1420

Publication date: August 1, 2012

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  • Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
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