Thermally reactive N-(2-hydroxypropyl)methacrylamide (HPMA) amphiphiles for drug solubilisation

Thermally active polymers, can respond structurally to temperature changes, making them interesting as potential drug delivery vehicles. Polymers of N-(3-aminopropyl) methacrylamide hydrochloride (APMA) are cationic with primary amine groups in their structure, which have been explored biomedical applications via post-polymerisation modifications. In this work, we synthesised amphiphilic APMA monomers using hydrophobic pendant conjugation onto group. The chosen study were palmitoyl, dansyl and cholesteryl moieties. subsequently copolymerized N-(2-hydroxypropyl)methacrylamide (HPMA) varied monomer feed ratios resulting a thermo-responsive system. ability the resultant aggregates aqueous solution encapsulate liberate model drugs (e.g., propofol, griseofulvin prednisolone) was then determined. Our data showed that HPMA based formulations capable loading molecules inside lipophilic core; HPMA-co-(APMA-Dansyl 2%) exhibited largest encapsulation ability. Subsequently, poly(ethylene glycol) (PEG) incorporated into intrinsic polymer structure. This resulted more rapid release profile, whereby 100% prednisolone liberated after only 4 h, 5% 10% before PEG inclusion, respectively. Similarly, propofol 70% liberation from aggregate 24 compared 30% pre-PEGylation. These studies give an insight HMPA amphiphiles thermally responsive cargo carrier/release systems could be exploited poorly soluble drugs.