Development and single dose clinical pharmacokinetics investigation of novel zein assisted- alpha lipoic acid nanoencapsulation of vardenafil

Abstract

The aim of this study was to utilize the biocompatibility of the natural ingredients zein and alpha lipoic acid (ALA) as a novel nanosphere matrix formulation that encapsulates vardenafil (VRD) for improved drug delivery and bioavailability. Three formulations were prepared using zein: ALA ratio of 1:1, 2:1 and 3:1 by liquid–liquid phase separation method. Physicochemical characterization and in vitro diffusion evaluation were carried out for the prepared formulations. A single dose clinical pharmacokinetic study was carried out for the selected formulation. Results revealed VRD formulations showed particle size of 836.7 ± 191.3, 179.8 ± 18.4 and 147.3 ± 18.1 nm and encapsulation efficiency of 55.72 ± 4.36, 65.33 ± 7.82 and 69.38 ± 6.83% for F1, F2 and F3, respectively. Single dose clinical pharmacokinetic results, in healthy human volunteers, showed improved VRD bioavailability by 2.5 folds from nanosphere formula (F3) compared with the marketed tablets. The formulation of novel zein-ALA nanospheres offers the possibility for application of a biocompatible nano-carrier system in drug delivery for improved drug delivery and efficacy.

Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies

“…Preparation of VNP-TPgs-ala micelles VNP-loaded TPGS-ALA micelles were prepared by dissolving VNP, TPGS, and ALA in ethanol using a magnetic stirrer for 5 minutes. 27 Distilled water was then added to the prepared solution. After dispersion of the components, ethanol was removed using a rotary evaporator (BÜCHI Labortechnik AG, Flawil, Switzerland).…”

<p>Pumpkin Oil–Based Nanostructured Lipid Carrier System for Antiulcer Effect in NSAID-Induced Gastric Ulcer Model in Rats</p>

“…The optimized PSO-NLCs formula and formula components were assessed using Fourier-transform infrared (FTIR) analysis as previously described. 39 Briefly, FTIR spectra of PSO, precirol, TPGS, Tween 80, soybean lecithin and the prepared optimized PSO-NLCs formula were recorded over the wavelength range from 400 to 4000 cm-1 using FTIR spectrophotometer (Nicolet IZ 10, Thermo Fisher Scientific, Waltham, MA, USA). Samples were directly applied to the FTIR spectrophotometer without treatment.…”

Formulation and Optimization of Avanafil Biodegradable Polymeric Nanoparticles: A Single-Dose Clinical Pharmacokinetic Evaluation

“…A single 50 mg AVA dose was administered orally with 250 mL of water by healthy male subjects (25 to 45 years of age). The design and method followed were previously reported [ 24 ]. The design was briefly open label, with one period that was carried out at the Egyptian Research and Development Company (ERDC), Cairo, Egypt.…”