Engineering of Long-Term Stable Transparent Nanoemulsion Using High-Gravity Rotating Packed Bed for Oral Drug Delivery.
Administration, Oral
Biological Availability
Caco-2 Cells
Drug Delivery Systems
/ methods
Drug Liberation
Drug Stability
Emulsions
/ administration & dosage
Humans
Hydrophobic and Hydrophilic Interactions
Nanostructures
/ administration & dosage
Particle Size
Rosuvastatin Calcium
/ administration & dosage
Silybin
/ administration & dosage
Surface-Active Agents
/ chemistry
Caco-2 permeability
Rosuvastatin calcium
Silybinin
high-gravity rotating packed bed
in vitro dissolution
nanoemulsion
stability
Journal
International journal of nanomedicine
ISSN: 1178-2013
Titre abrégé: Int J Nanomedicine
Pays: New Zealand
ID NLM: 101263847
Informations de publication
Date de publication:
2020
2020
Historique:
received:
15
11
2019
accepted:
11
03
2020
entrez:
21
4
2020
pubmed:
21
4
2020
medline:
11
8
2020
Statut:
epublish
Résumé
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. 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. 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. These results demonstrate that RPB can be a potential device to facilitate the industrial production of drug nanoemulsion.
Sections du résumé
BACKGROUND
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
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
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
CONCLUSIONS
These results demonstrate that RPB can be a potential device to facilitate the industrial production of drug nanoemulsion.
Identifiants
pubmed: 32308390
doi: 10.2147/IJN.S238788
pii: 238788
pmc: PMC7154039
doi:
Substances chimiques
Emulsions
0
Surface-Active Agents
0
Silybin
4RKY41TBTF
Rosuvastatin Calcium
83MVU38M7Q
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2391-2402Informations de copyright
© 2020 Wu et al.
Déclaration de conflit d'intérêts
The authors report no conflicts of interest in this work.
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