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Nanoporous smartPearls for dermal application – Identification of optimal silica types and a scalable production process as prerequisites for marketed products
- Source :
- Beilstein journal of nanotechnology, 10, 1666–1678, Beilstein Journal of Nanotechnology, Vol 10, Iss 1, Pp 1666-1678 (2019), Beilstein Journal of Nanotechnology
- Publication Year :
- 2019
- Publisher :
- Beilstein-Institut, 2019.
-
Abstract
- smartPearls are a dermal delivery system for poorly soluble active agents, consisting of nanoporous silica particles loaded with a long-term stable, amorphous active agent in its mesopores (2–50 nm). The amorphous state of the active agent is known to increase dermal bioavailability. For use in marketed products, optimal silica types were identified from commercially available, regulatory accepted silica. In addition, a scalable production process was demonstrated. The loading of the particles was performed by applying the immersion–evaporation method. The antioxidant rutin was used as a model active agent and ethanol was applied as the solvent. Various silica particles (Syloid®, Davisil®) differing in particle size (7–50 µm), pore diameter (3–25 nm) and pore volume (0.4–1.75 mL/g) were investigated regarding their ease of processing. The evaporation from the silica–ethanol suspensions was performed in a rotary evaporator. The finest powders were obtained with larger-sized silica. The maximum loading staying amorphous was achieved between 10% and 25% (w/w), depending on the silica type. A loading mechanism was also proposed. The most suitable processing occurred with the large-sized Syloid® XDP 3050 silica with a 50 µm particle size and a pore diameter of 25 nm, resulting in 18% (w/w) maximum loading. Based on a 10% (w/w) loading and the amorphous solubility of the active agent, for a 100 kg dermal formulation, about 500 g of loaded particles were required. This corresponds to production of 5 kg of loaded smartPearls for a formulation batch size of a ton. The production of 5 kg (i.e., about 25 L of solvent removal) can be industrially realized in a commercial 50 L rotary evaporator.
- Subjects :
- Life sciences
biology
Materials science
bioavailability enhancement
General Physics and Astronomy
02 engineering and technology
lcsh:Chemical technology
lcsh:Technology
030226 pharmacology & pharmacy
Full Research Paper
03 medical and health sciences
0302 clinical medicine
smartPearls
ddc:570
dermal delivery system
Nanotechnology
lcsh:TP1-1185
General Materials Science
Electrical and Electronic Engineering
Solubility
lcsh:Science
lcsh:T
Nanoporous
rutin
021001 nanoscience & nanotechnology
Rotary evaporator
Evaporation (deposition)
lcsh:QC1-999
Amorphous solid
Solvent
Nanoscience
Chemical engineering
solubility enhancement
lcsh:Q
Particle size
amorphous dispersion
600 Technik, Medizin, angewandte Wissenschaften::610 Medizin und Gesundheit::615 Pharmakologie, Therapeutik
0210 nano-technology
Mesoporous material
lcsh:Physics
Subjects
Details
- Language :
- English
- ISSN :
- 21904286
- Database :
- OpenAIRE
- Journal :
- Beilstein journal of nanotechnology, 10, 1666–1678, Beilstein Journal of Nanotechnology, Vol 10, Iss 1, Pp 1666-1678 (2019), Beilstein Journal of Nanotechnology
- Accession number :
- edsair.doi.dedup.....6edab55a8c921e98179c5399782e803d