METHOD OF PREPARATION AND CHEMICAL PHYSICAL CHARACTERIZATION OF NP-HSA LOADED WITH MELATONIN WITH POSSIBLE APPLICATION IN NEURODEGENERATIVE EYE DISEASES

SOFÍA M. MARTINEZ; VICTORIA MANASSERO; DANIELA A. QUINTEROS; DANIEL A. ALLEMANDI

Mar del Plata

Congreso; Reunion anual de SOCIEDADES DE BIOCIENCIA 2019 SAIC. SAFE. SAB. SAP. AACYTAL. NANOMED-AR. HCS; 2019

The development of ophthalmic formulations for the treatment of ocular pathologies, such as glaucoma, presents a challenge due to the low absorption and bioavailability of drugs in the ocular pathway. Transport systems based on human serum albumin nanoparticles (NP-HSA) represent an important strategy, since in addition to being an endogenous molecule, significant amounts of active ingredients can be incorporated into the particle. NP-HSA are of our interest to transport melatonin, an insoluble drug that has been described as an effective antioxidant in the retina with direct and indirect free radical scavenging activity.The objective of this work was design, formulate and characterize NP-HSA loaded with melatonin with possible application in eye diseases, such as glaucoma.The obtaining of NP-HSA was carried out by desolvation process. Different crosslinking agents (CA) such as Gantrez, Polyethylene Glycol 400, Eudragit S100 and Hydroxypropylmethylcellulose-Phtalate were tested, based on the existence of functional groups capable of interacting with NP-HSA, all of them non-toxic compounds and approved as excipients for pharmaceutical formulations. In addition, it was evaluated if the change in the sequence of CA addition in the formulation, produces changes in obtaining NP-HSA, in order to achieve greater stability, yield and encapsulation efficiency.Colloidal dispersions with a pH close to neutrality were obtained. Regardless of the CA used and the order in which it was added to the system, all NP-HSA presented a unique and uniform population with a particle size between 150-230 nm. The percentages of yield (75,9%) and encapsulation efficiency (16,8%), showed that the method of obtaining NP-HSA whose CA is Eudragit S100, was the most efficient, obtaining optimal and stable systems in time. These results will allow us to advance in a greater physicochemical characterization, as well as in in vitro release tests of Melatonin to evaluate its release over time.