@article {19061, title = {Novel delivery system combining therapeutic deep eutectic solvents and supercritical technology}, booktitle = {16 th European meeting on supercritical Technology (EMSF)}, year = {2017}, month = {2017-04-28 00:00:00}, abstract = {

In pharmaceutical sciences, one of the major challenges which still remain unanswered is the enhancement of the bioavailability of active pharmaceutical ingredients (API). Over the past years was the development of a new class of solvents, namely deep eutectic solvents (DES) have been described as a way to overcome the need to develop innovative, more effective and specialized release dosage forms. Thus, scientists are actively seeking for more efficient and patient-compliant drug delivery devices, especially for drugs with poor solubility and permeability. ]Herein, we explore the preparation of a new THEDES based on choline chloride-ascorbic acid. We further investigated the possibility to dissolve dexamethasone in this system and proposed it as a new class of API, with enhanced properties. The system was analyzed by polarized optical microscopy (POM) and the thermal behaviour and stability of the THEDES was measured. The solubility and permeability profile of both ascorbic acid and dexamethasone was performed in phosphate buffer solution (pH 7.4) and compared with those of the pure API. As expected, the solubility and permeability of the dexamethasone was greatly improved when in the THEDES system. Afterwards, this system was transposed and a controlled drug delivery systems were developed by supercritical fluid sintering, doping a blend of starch:poly-ɛ-caprolactone (SPCL) with choline chloride-ascorbic acid with or without dexamethasone. The morphological characterization of the impregnated matrices was evaluated by scanning electron microscopy (SEM) and by micro-computed tomography (micro-CT). Drug delivery studies were carried out in these impregnated matrices in physiologically like conditions and the results obtained demonstrate the potential of the developed THEDES to overcome the poor solubility of dexamethasone, while increasing its bioavailability. Biological tests were performed using different THEDES formulations and SPCL before and after doping with THEDES. The results indicate no cytotoxicity profile for the eutectic mixture. The present study highlights the potential future use of these THEDES to promote osteogenesis.\ 

}, keywords = {Deep Eutectic Solvents, green chemistry, supercritical technology}, author = {Silva, J. M. and Reis, R. L. and Paiva, A. and Duarte, A. R. C.} }