Co-delivery of Dexamethasone-Melatonin-CoQ10 from a microparticulate drug delivery system. Potential usefulness in neuroprotective therapy.

Abstract

Purpose : Design and characterization of a novel microparticulate Drug Delivery System (DDS) loaded with three active substances (Dexamethasone, Melatonin and Coenzyme Q10) with potential use in neuroprotective therapy.

Methods : Poly(lactic-co-glycolic) (PLGA) acid microspheres (MPs) loaded with Dexamethasone (DX), Melatonin (MEL) and Coenzyme Q10 (CoQ10) were prepared according to the extraction-evaporation technique from an Oil/Water emulsion. Microspheres were characterized in terms of morphology, mean particle size, encapsulation efficiencies and in vitro release studies. The amount of drugs encapsulated and released from the microspheres were quantified by HPLC-MS. A retinal cell line (RC28) was used as in vitro model for toxicity and bioactivity studies.

Results : PLGA microspheres ranged from 20-30 µm in size and were spherical in shape with rough surfaces. The microencapsulation efficiencies resulted 78.20±0.42 % (115.85±0.62 µg DX/mg MPs), 61.83±2.51% (45.80±1.86µg MEL/mg MPs) and 96.42±4.12% (35.71±1.53µg CoQ10/mg MPs). The active agents were released in vitro in a controlled fashion up to 30 days. The DX/MEL/CoQ10-MPs significantly promoted survival (p<0.05) of retinal cells from glutamate excitoxicity (IC50: 10.00±0.94) compared with non-loaded-MPs (IC50: 6.35±1.91) and control (IC50: 6.89±0.82).

Conclusions : The novel multiloaded microparticulate Drug Delivery System showed potential usefulness in neuroprotective therapy.

This is an abstract that was submitted for the 2018 ARVO Annual Meeting, held in Honolulu, Hawaii, April 29 - May 3, 2018.