Key result
The addition of diethyl tartrate to poly(lactic acid) film markedly enhanced the release of argatroban by increasing water uptake and forming open pores at the surface.
The addition of specific tartrates like DET and DMT to PLA films significantly enhances the controlled release of argatroban, which may inform the development of drug-eluting stents for vein restenosis.
Answers are grounded in this paper and cite their sources.
May guide argatroban-eluting coating design; leaves open in vivo validation before clinical stent use.
The aim of this study was to develop a drug eluting stent that prevents vein restenosis. For this, we selected argatroban as the study drug and poly(lactic acid) (PLA) as the matrix. To enhance the release of argatroban from PLA film, the addition of hydroxylesters (additives) was investigated. The additives investigated were diethyl tartrate (DET), diethyl malate (DEM), and triethyl citrate (TEC). Marked enhancement of drug release was observed in DET‐added film, while TEC‐ or DEM‐added film showed little enhancement. To clarify the effect of DET, the release profile based on the contents of the drug and DET in the film and the effect of alkyl chain length of tartrate were studied. Tartrates used were dimethyl, di‐i‐propyl, and di‐n‐butyl esters (DMT, DiPT, and DnBT, respectively), and the enhancement order was DMT ≅ DET ≫ DiPT ≅ DBT ≅ PLA alone. The reasons for enhancement were discussed from the viewpoint of drug release behavior, degradation of PLA, water uptake within the film, and SEM observations. It was concluded that enhancement of drug release was due to large amounts of water uptake within the film which resulted in the formation of open pores at its surface.
No takes yet. Share an insight, caveat, or question.
Mochizuki et al. (2008) studied Vein restenosis. Argatroban in PLA film with hydroxylesters (e.g., diethyl tartrate) vs. PLA alone was evaluated on Drug release enhancement. The addition of diethyl tartrate to poly(lactic acid) film markedly enhanced the release of argatroban by increasing water uptake and forming open pores at the surface.
Synapse has enriched 10 related papers. Consider them for comparative context: