Development and validation of an HPLC method for pentazocine quantification: Insights into pharmacokinetics using...

Area of Science:

• Pharmacology
• Nanotechnology
• Analytical Chemistry

Background:

• High-Performance Liquid Chromatography (HPLC) is crucial for accurate drug quantification in pharmaceutical and biological samples.
• Biodegradable polymeric nanoparticles offer enhanced drug stability, controlled release, and improved bioavailability.
• Accurate analytical methods are essential for pharmacokinetic studies, especially with novel drug delivery systems.

Purpose of the Study:

• To develop and validate a High-Performance Liquid Chromatography (HPLC) method for pharmacokinetic analysis.
• To apply the validated method for profiling the behavior of biodegradable polymeric nanoparticles.
• To assess the pharmacokinetic profile of pentazocine delivered via developed nanoparticle formulations.

Main Methods:

• Pentazocine-loaded biodegradable nanoparticles (chitosan-STPP and PLGA) were prepared using ionic gelation and emulsion solvent evaporation.
• An HPLC method was optimized and validated per ICH Q2(R1) guidelines, assessing linearity, precision, accuracy, LOD, and LOQ.
• In vivo pharmacokinetic studies were conducted in rabbits, comparing nanoparticle formulations against a pentazocine solution.

Main Results:

• The HPLC method exhibited excellent linearity (R²=0.9983), precision (<2% RSD), accuracy (98-102%), with LOD of 3.3 ng/mL and LOQ of 10 ng/mL.
• Nanoparticle formulations resulted in higher Cmax (185.26-193.71 ng/mL) and prolonged half-life (8.58-9.50 h) compared to the control (101.49 ng/mL; 1.69 h).
• Area Under the Curve (AUC) values were significantly increased, indicating enhanced bioavailability of pentazocine delivered by nanoparticles.

Conclusions:

• The validated HPLC method is suitable for pharmacokinetic profiling of drug delivery systems.
• Biodegradable nanoparticles demonstrate significant potential for improving pentazocine delivery and therapeutic efficacy.
• The study confirms the utility of developed nanoparticle formulations for enhanced drug bioavailability.