NANOEMULSION BREAKTHROUGH: A NEW MILESTONE IN ORAL DACLATASVIR DELIVERY – SCREENING, FORMULATION, IN-VITRO EVALUATION, AND IN-VIVO PHARMACOKINETIC ASSESSMENT.

Document Type : Original Article

Authors

1 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, Egypt

2 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt

3 New Products Development, Eva Pharma, Giza, Egypt

Abstract

The current study aimed to evaluate the efficacy of orally delivered Daclatasvir-loaded nanoemulsion (DAC-NE) for enhanced bioavailability. Solubility studies and phase diagram studies were performed to select the best formulation parameters. The formulation of DAC-NEs systems was achieved utilizing oleic acid and Tween 80/propylene glycol mix representing surfactant/cosurfactant. The key aspects of DAC-NE such as droplet size, zeta potential, pH, and transmittance were assessed. Stability was confirmed by centrifugation studies and heating-cooling cycles. The best DAC-NE system (NE-3) was selected with a droplet size of 54. 30±1.63 nm, drug content of 98.49±1.17 % and a zeta potential of -49.7±0.07 mV. Further studies were conducted for NE-3 such as morphological visualization using Transmission electron microscopy, in-vitro dissolution in addition to Fourier transform infrared analysis (FTIR), viscosity and refractive index. Results revealed complete DAC dissolution within the first 60 min from the prepared DAC-NE (NE-3), outperforming the DAC suspension and FTIR revealed compatibility between the drug and excipient components. Morphological outcomes suggest the presence of spherical globules within the nano-scale range. Furthermore, an in-vivo study using rats was conducted and revealed improved pharmacokinetic parameters of DAC from the prepared NE-3 system, where the AUC (0–∞) for NE-3 was 1.53-fold higher than DAC suspension verifying that the former recorded a notable enhancement in the level of DAC absorption and bioavailability.

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