Search

(1) Background: Many drugs possess poor bioavailability, and many strategies are available to overcome this issue. In this study, smartFilm technology, i.e., a porous cellulose matrix (paper), in which the active compound can be loaded onto in an amorphous state was utilised for oral administration to improve the solubility and bioactivity of a poorly soluble BSC class IV antibiotic. (2) Methods: Norfloxacin was used as the model drug and loaded into commercially available paper. The resulting norfloxacin-loaded smartFilms were transformed into smartFilm granules via wet granulation and the resulting norfloxacin-loaded smartFilm granules were transformed into norfloxacin-loaded tablets made from paper, i.e., smartFilm tablets. The crystalline state of norfloxacin was investigated, as well as the pharmaceutical properties of the granules and the tablets. The bioactivity of the smartFilm tablets was assessed in vitro and ex vivo to determine the antibacterial activity of norfloxacin. The results were compared to a physical mixture tablet that contained non-loaded paper granules and equal amounts of norfloxacin as a crystalline powder. (3) Results: Norfloxacin-loaded smartFilm granules and norfloxacin-loaded smartFilm tablets contained norfloxacin in an amorphous state, which resulted in an improved and faster release of norfloxacin when compared to the physical mixture tablet. The bioactivity was up to three times higher when compared to the physical mixture tablet. The ex vivo model was demonstrated to be a useful tool that allows for a fast and cost-effective discrimination between "good" and "bad" formulations. It provides realistic physiological conditions and can therefore yield meaningful, additional biopharmaceutical information that cannot be assessed in classical in vitro experiments. (4) Conclusions: smartFilm tablets are a promising, universal, industrially feasible and cost-effective formulation strategy for improved solubility and enhanced bioactivity of poorly soluble drugs. [ABSTRACT FROM AUTHOR]

[Display omitted] • An amphiphobic paper was fabricated via internal sizing technology. • The modified paper exhibited high resistance to moisture and water vapor. • The modified paper maintained high fracture stress in high humidity environment. • The modified paper exhibited notable self-cleaning and antibacterial activity. Paper-based materials have been used in every aspect of social life. However, the current paper-based materials face unprecedented challenges, such as limited lifespan and poor mechanical strength, owing to the deformation after absorbing a large amount of water and bacterial erosion. Herein, superhydrophobic and lyophobic paper was fabricated using internal sizing technology. Hydrophobically modified starch and Ag@SiO 2 particles were added as two functional additives to paper pulp to promote a hierarchical structure formation with low surface energy. Consequently, the water and linseed oil contact angles of the obtained paper reached 154.8° and 138.4°, respectively. The resistance to moisture and water vapor also improved under high-humidity condition, the relative moisture content decreased from 511% to 278% and water vapor transmission rate also decreased from 97.44 to 21.23 g/m2·h. Furthermore, its mechanical properties could also be well maintained with a high fracture stress of 4.91 MPa. Besides, some liquid food, such as honey, easily rolled off the surface without leaving behind any residue, which demonstrated its self-cleaning ability. Furthermore, the modified paper exhibited notable bacterial repellency and antibacterial activity. This study provides an innovative method for endowing conventional paper with superhydrophobic and antibacterial properties, which can effectively expand their application scope. [ABSTRACT FROM AUTHOR]