Lapdesf GL-FT 5 nanocrystals for the treatment of diabetic macular edema: the preparation and physico-chemical characterization

• Grant number: 18/24529-4
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: March 01, 2019
• End date: February 29, 2020
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Nádia Araci Bou-Chacra
• Grantee: Isabela Fernandes de Oliveira
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

The main complications related to the increase of glycemia, within the Diabetes Mellitus (DM), are microangiopathies, which cause changes in the permeability of the retinal vessels, due to the excess production of the growth of vascular endothelium factor (GVEF). These modifications may induce a disease called Diabetic Macular Edema (DME). Current therapies for DME may include laser photocoagulation, intravitreal administration of glucocorticoids and GVEF inhibitors. However, adverse effects related to these therapies, its high cost and invasive techniques, makes necessary the development of therapies that are potentially safer and more effective. The hybrid compound Lapdesf GL-FT 5, formed from budesonide (glucocorticoid) and phthalimide, a steroid with active anti-inflammatory, drug presents potential application in the treatment of DME. However, this compound presents low solubility in water, what make the tests impossible for this therapy. Nanocrystals are structures from 100 nm to 1000nm which have the ability to increase the saturation solubility and the dissolution rate of the drugs, in addition to increasing the contact of the particle's surface with the biological membrane of the eye, the development of Lapdesf GL-FT 5 nanocrystals by wet milling is shown as an alternative to the treatment of Diabetic Macular Edema.

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

DE OLIVEIRA, ISABELA FERNANDES; BARBOSA, EDUARDO JOSE; CAMASMIE PETERS, MARIA CHRISTINA; BAZAN HENOSTROZA, MIRLA ANALI; YUKUYAMA, MEGUMI NISHITANI; NETO, EDSON DOS SANTOS; LOBENBERG, RAIMAR; BOU-CHACRA, NADIA. Cutting-edge advances in therapy for the posterior segment of the eye: Solid lipid nanoparticles and nanostructured lipid carriers. International Journal of Pharmaceutics, v. 589, NOV 15 2020. (18/24529-4)