<p>Engineering of Long-Term Stable Transparent Nanoemulsion Using High-Gravity Rotating Packed Bed for Oral Drug Delivery</p>

Abstract

Background: Oil-in-water drug nanoemulsion forms drug delivery systems with high oral bioavailability. The conventional fabrication methods of nanoemulsion are low energy emulsification methods and high energy emulsification methods. However, both two methods are not ideal for industrial production. The problem of low energy emulsification methods is the high dosage of surfactant and co-surfactant which has potential biosecurity issues. What is more, high energy emulsification methods have some disadvantages, like the destruction of drug components, the price of equipment and the difficulties of industrial production. Hence, there have been a few commercial drug nanoemulsions so far. Methods: In this work, we reported a novel method for the fabrication of stable and transparent drug nanoemulsion which contains hydrophilic drug rosuvastatin (ROS) calcium or hydrophobic drug silybinin (SYN) by using high-gravity rotating packed bed (RPB). The drug nanoemulsion was systematically characterized by droplet size, size distribution, stability and in vitro drug release as well as Caco-2 cells permeability. Results: Compared with the self-emulsification method (SE), high-gravity technology could reduce 75% amount of mixed surfactants. The as-prepared nanoemulsion exhibited a very narrow droplet size distribution with a size of 13.53 ± 0.53 nm and a polydispersity index of 0.073 ± 0.018. Meanwhile, the drug nanoemulsion was physicochemically stable at 25°C and 4°C for one-year storage. Furthermore, both ROS and SYN nanoemulsion displayed higher cell permeability and in vitro dissolution than that of commercial formulations. Conclusion: These results demonstrate that RPB can be a potential device to facilitate the industrial production of drug nanoemulsion.

A Novel Nanoemulsion Formula for an Improved Delivery of a Thalidomide Analogue to Triple-Negative Breast Cancer; Synthesis, Formulation, Characterization and Molecular Studies

“…Then, they were checked for phase separation and optical clarity by visual inspection as well as measuring their droplet size and zeta potential. As reported by Wu group, 43 they tested the long-term stability of NE after 1 year of preparation stored at room temperature by measuring their average droplet size and examining their physical characteristics. 43 Alliod et al 44 measured the droplet size and zeta potential for their NE after 9 months of storage at room temperature.…”

Dasatinib Nanoemulsion and Nanocrystal for Enhanced Oral Drug Delivery

“…The nanoformulation, with a smaller size and higher dissolution, makes it possible to improve cell permeability and finally realize a superior bioavailability. Compared with the nanocrystal, the nanoemulsion formulation had an enhanced permeability on Caco-2 cell monolayers due to the usage of surfactants and the formation of tiny oil-in-water droplets [32][33][34].…”

“…The nanoformulation, with a smaller size and higher dissolution, makes it possible to improve cell permeability and finally realize a superior bioavailability. Compared with the nanocrystal, the nanoemulsion formulation had an enhanced permeability on Caco-2 cell monolayers due to the usage of surfactants and the formation of tiny oil-in-water droplets [32][33][34]. The in vitro antiproliferative activities of the DAS nanoformulation and raw DAS on MDA-MB-231 triple negative breast cancer cells were measured using the MTT method (Figure 13).…”

“…The fluids going through the packing of RPB are spread or split into very fine droplets, threads, and thin films by strong shear force, resulting in a significant intensification of micro-mixing and mass transfer between the fluid elements and, hence, benefiting from the form of uniform concentration distribution. RPB, with an ultrashort residence time (<1 s) of reactants, has proved to be an ideal device for the preparation of nanoparticles and successfully applied in the pharmaceutical industry [31][32][33][34].…”

Nano Spray-Dried Drugs for Oral Administration: A Review

“…Nanoemulsions show several advantages in oral administration, such as increasing bioavailability, preventing the first-pass metabolism, and enhancing lymphatic absorption. 94 Nanosuspensions are submicron colloidal dispersions comprising drug nanocrystals, stabilizing agents (e.g., surfactants and/or polymeric stabilizers), and a liquid dispersion medium. 95 In recent years, oral nanosuspension systems have been successfully used to increase the solubility, dissolution rate, and bioavailability of water-insoluble drugs.…”