Clear Search sequence regions


  • behavior (3)
  • drug carriers (2)
  • erlotinib (2)
  • erlotinib (8)
  • glycols (2)
  • polymers (2)
  • rats (1)
  • wistar rats (2)
  • Sizes of these terms reflect their relevance to your search.

    The present study was undertaken to synthesize PEGylated monomethoxy poly (ethylene glycol)-poly (ε-Caprolactone) (mPEG-PCL) block copolymer and formulate Erlotinib HCl-loaded mPEG-PCL nanoparticles for enhancing the bioavailability of the drug. Using the ring-opening polymerization technique, PEGylated mPEG-PCL block copolymer was synthesized, and the structure of the copolymer was characterized using FTIR, 1H-NMR, and DSC techniques. The solvent evaporation approach was used to effectively encapsulate Erlotinib HCl within block copolymeric nanoparticles. Erlotinib HCl-loaded mPEG-PCL nanoparticles had a mean particle size of 146.5 ± 2.37 nm and a zeta potential of -27.8 ± 2.77 mV. The nanoparticles had a percent entrapment efficiency of 80.78 ± 0.09%. The in vitro drug release of Erlotinib HCl-loaded copolymeric nanoparticles showed a slow and sustained release behavior which could be maintained for up to 72 h. The Korsmeyer-Peppas fitting findings indicated that the drug release process followed a non-Fickian diffusion mechanism. The pharmacokinetic (PK) behavior of the developed nanoformulation was studied in albino Wistar rats, and the relative bioavailability of the optimized NP formulation given by intravenous route was found to be 187.33%. The PK data suggested that Erlotinib HCl-loaded mPEG-PCL copolymeric nanoparticles can dramatically alter the PK behavior of Erlotinib HCl and greatly improve the drug's bioavailability by as much as three times when compared to the oral formulation. As a result, it was established that the block copolymeric nanoparticles have promise for the effective encapsulation of Erlotinib HCL for an injectable formulation with increased bioavailability. © 2023. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.

    Citation

    Hardik Bhargave, Harsh Nijhawan, Khushwant S Yadav. PEGylated Erlotinib HCl Injectable Nanoformulation for Improved Bioavailability. AAPS PharmSciTech. 2023 Apr 10;24(4):101

    Expand section icon Mesh Tags

    Expand section icon Substances


    PMID: 37038015

    View Full Text