Polyactives: controlled and sustained bioactive release via hydrolytic degradation

Abstract

Significant and promising advances have been made in the polymer field for controlled and sustained bioactive delivery. Traditionally, small molecule bioactives have been physically incorporated into biodegradable polymers; however, chemical incorporation allows for higher drug loading, more controlled release, and enhanced processability. Moreover, the advent of bioactive-containing monomer polymerization and hydrolytic biodegradability allows for tunable bioactive loading without yielding a polymer residue. In this review, we highlight the chemical incorporation of different bioactive classes into novel biodegradable and biocompatible polymers. The polymer design, synthesis, and formulation are summarized in addition to the evaluation of bioactivity retention upon release via in vitro and in vivo studies.

Athero-inflammatory nanotherapeutics: Ferulic acid-based poly(anhydride-ester) nanoparticles attenuate foam cell formation by regulating macrophage lipogenesis and reactive oxygen species generation

“…To meet the challenge of harnessing the anti-atherogenic properties of antioxidant compounds, more targeted and robust delivery systems are needed to achieve an efficacious dose while limiting localized spikes in pro-oxidants. The emergence of controlled release mechanisms using polymer chemistry coupled with advances in nanotechnology could be one avenue for development of novel, bioactive antioxidant formulations for atherosclerosis applications [43-45]. In this study, we advanced the delivery and formulation of antioxidants through development of ferulic acid-based polymer nanoparticles, which are completely biodegradable and can achieve a sustained and tunable release of ferulic acid to obtain maximum bioactivity for limiting macrophage foam cell formation.…”

One‐Pot Polymerization Syntheses: Incorporating Bioactives into Poly(anhydride‐esters)

“…Bioactive‐based PAEs, are polymer systems in which bioactives are incorporated into the polymer backbone and thus posses high bioactive‐loading, offering a means to overcome low payload associated with traditional drug‐eluting polymers . Similar to polyanhydrides, PAEs are commonly synthesized via melt‐condensation polymerization and triphosgene‐mediated solution polymerization, and with the most recent development established by Qian and Mathiowitz in 2007 using (trimethylsilyl)ethoxyacetylene as a mild dehydrating agent . Thus, to enhance synthetic efficiency, minimize waste, and improve atom economy our group sought to apply the idea of multicomponent reactions, in which multiple sequential reactions are occurring in one‐pot in high convergence, to improve our bioactive‐based PAE syntheses.…”

Pinosylvin‐Based Polymers: Biodegradable Poly(Anhydride‐Esters) for Extended Release of Antibacterial Pinosylvin

“…PAEs are predominantly surface‐eroding polymers with minimal burst release, allowing for controlled and sustained release of bioactives in a near‐zero order manner . Additionally, PAEs can be prepared to achieve higher bioactive loadings (50%–100%), and formulated into different geometries, hence offering the potential to satisfy diverse applications …”