Drug silica nanocomposite: preparation, characterization and skin permeation studies

Abstract

The aim of this work was to evaluate silica nanocomposites as topical drug delivery systems for the model drug, caffeine. Preparation, characterization, and skin permeation properties of caffeine-silica nanocomposites are described. Caffeine was loaded into the nanocomposites by grinding the drug with mesoporous silica in a ball mill up to 10 h and the efficiency of the process was studied by XRPD. Formulations were characterized by several methods that include FTIR, XRPD, SEM and TEM. The successful loading of caffeine was demonstrated by XRPD and FTIR. Morphology was studied by SEM that showed particle size reduction while TEM demonstrated formation of both core-shell and multilayered caffeine-silica structures. Solid-state NMR spectra excluded chemical interactions between caffeine and silica matrix, thus confirming that no solid state reactions occurred during the grinding process. Influence of drug inclusion in silica nanocomposite on the in vitro caffeine diffusion into and through the skin was investigated in comparison with a caffeine gel formulation (reference), using newborn pig skin and vertical Franz diffusion cells. Results from the in vitro skin permeation experiments showed that inclusion into the nanocomposite reduced and delayed caffeine permeation from the silica nanocomposite in comparison with the reference, independently from the amount of the tested formulation.

Centella asiaticaextract‐SiO2 nanocomposite: More than a drug‐delivery system for skin protection from oxidative damage

“…According to this purpose, the prepared novel silica‐based biomaterials containing C. asiatica glycolic extract, totally accomplish the extract protection, and controlled release as previously found in our studies 18 . Ball milling is revealed a feasible technique for the preparation of C. asiatica extract‐SiO 2 nanocomposites.…”

“…[32][33][34][35][36] According to this purpose, the prepared novel silica-based biomaterials containing C. asiatica glycolic extract, totally accomplish the extract protection, and controlled release as previously found in our studies. 18 Ball milling is revealed a feasible technique for the preparation of C. asiatica extract-SiO 2 nanocomposites. The milling process promotes the inclusion of the C. asiatica glycolic extract within the silica pores without affecting the extract properties.…”

“…15 We recently developed a one-pot-production method loading silica matrix with active substances using ball milling, which allows the retention of the properties of the bioactive after the milling process along with their metabolic composition. [16][17][18] In a previous study, Vitis Vinifera ethanolic extract was delivered in the silica matrix and the obtained nanocomposite was able to improve its antioxidant activity. 17 According to these promising results, in this paper, we present a novel nanocomposite based on C. asiatica glycolic extract and fumed SiO 2 , which was prepared as new strategy to treat skin damages linked to oxidative stress.…”

Advanced Inorganic Nanosystems for Skin Drug Delivery

“…Besides, it was proved that MSNs act not only as efficient topical nanocarriers but also show interesting properties to increase the stability of delicate antioxidant molecules such as derivatives of flavonoids like quercetin and of the vitamin E, trolox. Caffeine‐MSNs hybrid system obtained via ball milling was subjected to in‐vitro permeation tests using newborn pig skin and vertical Franz diffusion cells. Furthermore, the in‐vitro penetration and in vivo anti‐inflammatory and analgesic effects of curcumin‐loaded MSNs were determined.…”

Impact of mesoporous silica on the chemical degradation of Praziquantel upon grinding

“…The applied solvent-free loading methods include simple dry blending [5], classical melt-quenching of the drug in the presence of the carrier [6], microwaveassisted heating [7], hot-melt extrusion [8] supercritical carbon dioxide impregnation [9], milling [6] and cryomilling [10]. Among these, several published works and patents [6,[11][12][13][14][15] endorse the importance of this processing method for obtaining physically stable amorphous dispersions capable of enhancing drug dissolution. However, the investigation of drug chemical stability upon milling in the presence of mesoporous silica has received only very poor attention, and, even when there was interest, differences in chemical stability were attributed to the higher molecular mobility and reactivity inherent in the amorphous state rather than being evaluated in the relation to the excipient and technology.…”