Abstract
The advances in pharmaceutical technology allow for the development of various
region-selective delivery systems for oral administration to optimize local and
systemic therapy. In this paper, micronization associated with a polymorph
modification approach was proposed for improving the solubility of hydrophobic
drugs for developing a Zein-based colon-targeted delivery system. A microcarrier based on self-assembled structures of Zein was fabricated via a built-in ultrasonic dialysis process, which displayed high payload of a model drug, indomethacin (Indo), with its optimal crystal form. The possible self-assembly mechanism of Zein/Indo forming porous structure in the ultrasonic dialysis process was attributed to the results of intra- and/or inter-molecular interactions between Zein and Indo. The designed microspheres, Zein-Indo@PDA, with a surface coating of polydopamine (PDA) not only rendered them enhanced stability and mechanical resistance, but also hindered the premature drug release at undesired sites. This innovative formulation design may offer better chances of colon-targeted release.
region-selective delivery systems for oral administration to optimize local and
systemic therapy. In this paper, micronization associated with a polymorph
modification approach was proposed for improving the solubility of hydrophobic
drugs for developing a Zein-based colon-targeted delivery system. A microcarrier based on self-assembled structures of Zein was fabricated via a built-in ultrasonic dialysis process, which displayed high payload of a model drug, indomethacin (Indo), with its optimal crystal form. The possible self-assembly mechanism of Zein/Indo forming porous structure in the ultrasonic dialysis process was attributed to the results of intra- and/or inter-molecular interactions between Zein and Indo. The designed microspheres, Zein-Indo@PDA, with a surface coating of polydopamine (PDA) not only rendered them enhanced stability and mechanical resistance, but also hindered the premature drug release at undesired sites. This innovative formulation design may offer better chances of colon-targeted release.
| Original language | English |
|---|---|
| Pages (from-to) | 12689-12699 |
| Journal | Industrial & Engineering Chemistry Research |
| Volume | 57 |
| Issue number | 38 |
| Early online date | 5 Sept 2018 |
| DOIs | |
| Publication status | Published - 26 Sept 2018 |
Keywords
- Zein
- self-assembly
- colon-targeted
- polydopamine
- micronization
- polymorph modification