PEGylated Erlotinib HCl Injectable Nanoformulation for Improved Bioavailability
Hardik Bhargave1, Harsh Nijhawan1, Khushwant S Yadav2
1Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS Deemed to be University, Mumbai, 400056, India.
AAPS Pharmscitech
|April 10, 2023
Summary
This study synthesized PEGylated monomethoxy poly (ethylene glycol)-poly (ε-Caprolactone) (mPEG-PCL) nanoparticles to enhance Erlotinib HCl bioavailability. The nanoformulation significantly increased drug bioavailability by 187.33% in rats, showing promise for injectable drug delivery.
Area of Science:
- Polymer Chemistry
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Erlotinib HCl, a cancer therapeutic, suffers from poor oral bioavailability.
- Developing effective drug delivery systems is crucial for improving therapeutic outcomes.
Purpose of the Study:
- To synthesize mPEG-PCL block copolymer and formulate Erlotinib HCl-loaded nanoparticles.
- To evaluate the physicochemical properties, in vitro release, and pharmacokinetic behavior of the nanoformulation.
Main Methods:
- mPEG-PCL block copolymer synthesized via ring-opening polymerization.
- Erlotinib HCl encapsulated using solvent evaporation technique.
- Characterization included FTIR, 1H-NMR, DSC, particle size, zeta potential, and entrapment efficiency analysis.
Main Results:
- Synthesized mPEG-PCL copolymer characterized successfully.
- Erlotinib HCl-loaded nanoparticles exhibited a mean size of 146.5 nm and 80.78% entrapment efficiency.
- In vitro release was sustained for 72h, following a non-Fickian diffusion mechanism.
- Pharmacokinetic studies in rats showed a 187.33% increase in relative bioavailability via intravenous route.
Conclusions:
- mPEG-PCL nanoparticles effectively encapsulate Erlotinib HCl.
- The nanoformulation demonstrates sustained drug release and significantly enhances bioavailability.
- These block copolymeric nanoparticles hold promise for developing injectable Erlotinib HCl formulations with improved efficacy.
