Light effect on the stability of β-lapachone in solution: pathways and kinetics of degradation

Abstract

This study provides useful information for the development of βLAP dosage forms, their storage, manipulation and quality control.

Effect of storage conditions on the stability of β-lapachone in solid state and in solution

“…HPLC chromatograms of the βLAP samples stored in the dark did not show modifications after 1 month and 3 months (profiles not shown). However, after storage for 6 months, the significant reduction of the βLAP peak combined with the appearance of an extra small peak, characteristic of hydroxylapachol, indicated that hydrolytic degradation of the drug had occurred, as previously described for degradation of βLAP in solution . Chromatograms of samples exposed to the light showed changes after a 3‐month period that can be related to the main photodegradation products, phthalic acid and the 6‐hydroxy‐3methylene‐3H‐isobenzofuran‐1‐one, which is in agreement with our previous results …”

“…An additional problem for βLAP formulation development is its instability. We have previously investigated the degradation mechanisms of βLAP in aqueous solution under both light conditions and in darkness, and identified the main degradation products . Light greatly accelerated drug degradation in aqueous medium, giving different degradation products depending on storage conditions .…”

Temperature-Sensitive Gels for Intratumoral Delivery ofβ-Lapachone: Effect of Cyclodextrins and Ethanol

“…No crystalline growth was observed under optical microscopy. Samples show that the same UV-visible spectra and β LAP amount before and after autoclaving are not significantly different [32]. Therefore, autoclaving could be recommended as a sterilization method for these intratumoral formulations.…”

Fast dissolving β-lapachone particles and tablets: an approach using surface adsorption technique

“…Chromatographic detection was set at 253 nm with a photodiode array detector. The mobile phase and samples were filtered using a 0.45 μm nylon membrane (Waters, Milford, MA) 14 .…”