Nanoporous smartPearls for dermal application – Identification of optimal silica types and a scalable production process as prerequisites for marketed products

• David Hespeler,
• Sanaa El Nomeiri,
• Jonas Kaltenbach and
• Rainer H. Müller

Beilstein J. Nanotechnol. 2019, 10, 1666–1678, doi:10.3762/bjnano.10.162

• Berlin, Germany Institute of Functional Interfaces, Karlsruher Institute of Technology, Hermann-von-Helmholtz-Platz 1, 76344 Eggenstein-Leopoldshafen, Germany 10.3762/bjnano.10.162 Abstract smartPearls are a dermal delivery system for poorly soluble active agents, consisting of nanoporous silica

• . 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. Keywords: amorphous dispersion; bioavailability enhancement; dermal delivery system; rutin; smartPearls; solubility enhancement; Introduction Many interesting active agents in pharma and cosmetics are poorly soluble