Dra. Andrea Araya

 

 

NANOSTRUCTURED MULTICOMPONENT ORGANIC MATERIAL OF

POORLY WATER SOLUBLE DRUGS AND NUTRACEUTICS

Andrea Mariela ARAYA-SIBAJA1,2*, Krissia WILHELM3, José Roberto VEGA- BAUDRIT1,4, Teodolito GUILLÉN-GIRÓN5, Mirtha NAVARRO-HOYOS3

1Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, 1174-1200, San José, Costa Rica; Universidad Técnica Nacional, Alajuela 1902-4050, Costa Rica; Escuela de Química, Universidad de Costa Rica, San José 11501-2060, Costa Rica; 4Laboratorio de Investigación y Tecnología de Polímeros POLIUNA, Escuela de Química, Universidad Nacional de Costa Rica, Heredia 86-3000, Costa Rica; Escuela de Ciencia e Ingeniería de los Materiales, Tecnológico de Costa Rica, Cartago 159-7050, Costa Rica

*aarayas@cenat.ac.cr

Multicomponent organic materials (MOM) are solids formed by incorporating one or more coformer molecule into the matrix of a parent molecule via non-covalent interactions. They have arisen as a strategy to improve the physicochemical properties of drugs and nutraceuticals possessing well-known therapeutic effects [1]. In these molecules the solubility, dissolution rate and metabolic degradation have a profound impact in the oral bioavalaibility. Organic eutectic mixtures (OEM) are MOM which have been used to improve solubility and dissolution rate of bioactive molecules. Nanoparticles, on the other hand haven useful to protect molecules against metabolism [2]. Therefore, a combination of nanostructured MOM is a novel and relatively unexplored strategy to improve oral bioavailability of poorly water-soluble molecules and protect them against metabolism. Hence, in this work lovastatin (LOV) an antihypertensive drug and curcumin (CUR) an antioxidant both exhibiting low aqueous solubility have been studied as candidate molecules to produce nanostructured MOM. EM of LOV with carboxylic acids have been developed in our laboratory with improvements in solubility of LOV [3]. In addition, piperine (PIP) has been reported as preventing CUR metabolism; therefore, PIP has been selected as coformer molecule to prepare OEM with CUR. Hence, in this work, OEM of LOV and CUR have been prepared. Then, three different types of nanomaterials: a polymeric, a solid-lipid and a lipid-polymer hybrid nanoparticles loaded with these MOMs based on LOV and CUR were prepared. Nanoparticles characterization through PXRD, TEM, IR, DLS and antioxidant potential using ORAC method are in progress.

Key Words: Multicomponent organic materials, solubility enhancement, drug delivery, nanoparticles, lovastatin, curcumin.

References

[1] A. M. Araya-Sibaja, C. Fandaruff, K. Wilhelm, J. R. Vega-Baudrit, T. Guillén-Girón, and M. Navarro- Hoyos. Mini. Rev. Org. Chem 16, (2019).

[2] S. A. A. Rizvi and A. M. Saleh. Saudi Pharm 26, (1) 64–70, (2018).
[3] A. Araya-Sibaja, J. Vega-Baudrit, T. Guillén-Girón, M. Navarro-Hoyos, and S. Cuffini,

Pharmaceutics 11, (3) 112, (2019).