Abstract Nanocrystals refer to materials with at least one dimension smaller than 100 nm, composing of atoms arranged in single crystals or polycrystals. Nanocrystals have significant research value as they offer unique advantages over conventional pharmaceutical formulations, such as high bioavailability, enhanced targeting selectivity and controlled release ability and are therefore suitable for the delivery of a wide range of drugs such as insoluble drugs, antitumor drugs and genetic drugs with broad application prospects. In recent years, research on nanocrystals has been progressively refined and new products have been launched or entered the clinical phase of studies. However, issues such as safety and stability still stand that need to be addressed for further development of nanocrystal formulations, and significant gaps do exist in research in various fields in this pharmaceutical arena. This paper presents a systematic overview of the advanced development of nanocrystals, ranging from the preparation approaches of nanocrystals with which the bioavailability of poorly water‐soluble drugs is improved, critical properties of nanocrystals and associated characterization techniques, the recent development of nanocrystals with different administration routes, the advantages and associated limitations of nanocrystal formulations, the mechanisms of physical instability, and the enhanced dissolution performance, to the future perspectives, with a final view to shed more light on the future development of nanocrystals as a means of optimizing the bioavailability of drug candidates. This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies Nanotechnology Approaches to Biology > Nanoscale Systems in Biology
Driven by the clinical demand on improving the oral bioavailability and reducing the side effects of insoluble drug, aminoated mesoporous silica xerogel (named L/d-BPEIN-MSX) with chiral surface topology was constructed through a facile, economical, and biomimetic strategy within 2 min, and served as the carrier of indomethacin (IMC). In the synthetic process, L/d-tartaric acid (L/d-TA) self-assembled with branched polyethyleneimine (BPEI) to endow chirality and synergistic promoted silica deposition, while 3-aminopropyl triethoxysilane (APTES) polycondensated with the silica source to form aminoated mesostructure. By premixed strategy, IMC can be in situ loaded into L/d-BPEIN-MSX with high efficiency, which then became active in circular dichroism (CD) spectra owing to induced chirality. Noteworthy, IMC-L/d-BPEIN-MSX significantly improved the release rate of IMC with multiple controlled release manners. That is, d-BPEIN-MSX had favorable drug release behavior which could respond to the chiral stimuli, whereas l-BPEIN-MSX exhibited advantageous chiral surface topology that was beneficial for bio-processes related to oral adsorption. Undoubtedly, they increased the bioavailability of IMC to 8–9 times, displayed good anti-inflammatory effect, and reduced the gastrointestinal irritation of IMC. In addition, L/d-BPEIN-MSX had low toxicity and irritation, and was proven to be biodegradable and biocompatible, which could meet the requirement for biomedical applications.
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