Quantitation of polymeric-microneedle-delivered HA15 in tissues using liquid chromatography-tandem mass spectrometry

J Pharm Biomed Anal. 2020 Jun 5:185:113230. doi: 10.1016/j.jpba.2020.113230. Epub 2020 Mar 4.

Abstract

A rapid and sensitive liquid chromatography-tandem mass spectrometric method was developed and validated for the determination of HA15, an emerging anticancer compound targeting GSPA5/BIP delivered by dissolvable polymeric microneedles. The linear range of quantification for HA15 was 2.5-1000 ng/ml in plasma and tissue homogenate and the limit of detection and lower limit of quantification are 1 and 2.5 ng/ml, respectively. The inter- and intra-day accuracy and precision were within the acceptable range. HA15 was extracted from mouse plasma and organs using protein precipitation and using dabrafenib as an internal standard and the drug was stable under relevant analytical conditions. The method was used to analyze drug loading, dissolution in vitro, and release ex vivo from dissolvable polymeric microneedles and used to compare these materials to subcutaneous injection for the tissue distribution in tumor bearing nude mice.

Keywords: Drug distribution; HA15; Liquid chromatography-tandem mass spectrometry; Microneedle.

Publication types

  • Validation Study

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / analysis*
  • Antineoplastic Agents / pharmacokinetics
  • Cell Line, Tumor / transplantation
  • Chemistry, Pharmaceutical / methods*
  • Chromatography, High Pressure Liquid / methods
  • Drug Liberation
  • Female
  • Limit of Detection
  • Melanoma, Experimental / drug therapy*
  • Melanoma, Experimental / pathology
  • Mice
  • Mice, Nude
  • Needles
  • Reproducibility of Results
  • Sulfonamides / administration & dosage
  • Sulfonamides / analysis*
  • Sulfonamides / pharmacokinetics
  • Tandem Mass Spectrometry / methods
  • Thiazoles / administration & dosage
  • Thiazoles / analysis*
  • Thiazoles / pharmacokinetics
  • Tissue Distribution
  • Transdermal Patch*

Substances

  • Antineoplastic Agents
  • HA15 compound
  • Sulfonamides
  • Thiazoles