Simultaneously Improving the Physicochemical Properties, Dissolution Performance, and Bioavailability of Apigenin and Daidzein by Co-Crystallization With Theophylline

Huang, Shan; Xue, Qunji; Xu, Jia; Ruan, Sida; Cai, Ting

doi:10.1016/j.xphs.2019.04.017

Cited by 46 publications

(47 citation statements)

References 65 publications

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“…An interesting example is that Cai and co-workers used theophylline (Thp) to cocrystallize with two flavonoid compounds apigenin (Agn) and daidzein (Dai), and their results indicated that the solubilities, intrinsic dissolution rates, and permeabilities of the Agn-Thp cocrystal and the Dai-Thp cocrystal are improved compared to those of parent flavonoids. This work supports the fact that the synergistic effect of multibioactive components improves the performance of the herb aggregates and provides a new viewpoint for understanding the therapeutic effect of Chinese herbal medicines . The idea of aggregate science thus could potentially be used to study the pharmacological action of Chinese herbal medicines. Organic electronic materials and devices constitute an important branch of aggregate science.…”

Section: Conclusion and Perspectivessupporting

confidence: 72%

Aggregate Materials beyond AIEgens

Zhao

Tang

2021

Acc. Mater. Res.

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Metrics & MoreArticle RecommendationsCONSPECTUS: Aggregate materials focus on the materials that are constituted by more than a single entity. It could be dimers, trimers, or multimers formed by the group of same molecules or mixtures formed by different molecules. Although materials have different forms such as liquid, hydrogel, colloidal suspension, and powder, aggregates undisputedly are among the most commonly existing forms, which involve many aspects of human daily life such as the clothes we wear, the drugs we take, the food we eat, and the tools and devices we use. Sciences related to aggregate materials are also rich. From molecules to aggregates, different aspects of science such as crystallography, interfacial science, supramolecular science, and engineering science may be involved. Therefore, research on aggregate materials and related mechanisms that dominate the properties of aggregate materials is significant. However, it is noteworthy that reductionism is the dominant research philosophy for the design of traditional materials, and it claims that a molecule is the smallest particle of a substance that retains all of the properties of the substance. Consequently, scientists have expended a lot of effort to develop new molecules and to study the relationships between molecular structure and properties without paying attention to aggregate tuning. Actually, more and more research supports the fact that aggregate control such as the tuning of the packing mode, self-assembly, and morphology could work as a more versatile and effective strategy to endow materials with rich properties and functions. A prototype of the aggregate research is the aggregation-induced emission (AIE) phenomenon and materials. AIE research mainly focuses on the luminescence change accompanied by the aggregation process. After more than 20 years of flourishing development, AIE research has made great advances in new material development, mechanism studies, and hightechnology applications. More importantly, AIE research opens the window to aggregate science and demonstrates that new behaviors and functions that are absent in single molecular species can be generated in molecular aggregates.In this Account, we highlight our efforts toward aggregate materials beyond AIE luminogens (AIEgens), with a special focus on new properties in addition to luminesce endowed by aggregation. We first summarize the chirality that is induced by the aggregation process of prochiral molecules. Then we present the aggregation resulting from the transformation between hydrophilicity and hydrophobicity. After that, the aggregation-induced generation of reactive oxygen species (ROS) is described and the regulation of the aggregation state for tuning the ROS generation efficiency is discussed. We also discuss how to achieve the switch between radiative decay and nonradiative decay through the regulation of the aggregation extent to afford luminescence and photothermy (photothermal effect), respectively. Additionally, different strategies to accelerate th...

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Section: Conclusion and Perspectivessupporting

confidence: 72%

Aggregate Materials beyond AIEgens

Zhao

Tang

2021

Acc. Mater. Res.

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“…Drug-delivery systems, such as nanoparticles [ 6 , 7 ], inclusion complexes [ 8 ], microemulsions [ 9 ], solid dispersion [ 10 ], and cocrystallization [ 11 ], are commonly used to resolve the poor water solubility of active ingredients for increasing their absorption and bioavailability. Nontoxic nanocarriers with good manufacturing processes are the first choice for producing safe nanoparticle formulations.…”

Section: Introductionmentioning

confidence: 99%

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

et al. 2021

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Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility of raw ACM has limited its applications in medicine and cosmetics. Topical antioxidant nanoparticles are one of the drug-delivery systems for overcoming the poor water solubility of antioxidants for increasing their skin penetration. The present study demonstrated that ACM-loaded hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone K30 nanoparticles (AHP) were successfully prepared and could effectively increase the skin penetration of ACM through changing the physicochemical characteristics of raw ACM, including reducing the particle size, increasing the surface area, and inducing amorphous transformation. Our results also revealed that AHP had significantly better antioxidant activity than raw ACM for preventing photocytotoxicity because the AHP formulation increased the cellular uptake of the ACM in UVB-irradiated HaCaT keratinocytes. In conclusion, our results suggest that AHP may be used as a good topical antioxidant nanoparticle for delivering ACM into deep layers of the skin for preventing UVB-induced skin problems.

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“…Several strategies have been applied to tackle this challenge, including adding appropriate excipients in the formulation, applying proper packing for reducing moisture uptake or coating the drug product by enteric polymers 86 . Indeed, some studies have demonstrated that cocrystal formation could improve the hygroscopic stability of drugs 86 , 92 , 93 , 94 It is suspected that the hydrogen bonds formed between API and coformer in the cocrystal could occupy the hydrogen bonding donor and acceptor sites of API to block the water molecules 95 . Huang et al.…”

Section: Physicochemical Properties and Applications Of Cocrystalsmentioning

confidence: 99%

“…Huang et al. 93 demonstrated that flavonoid‒theophylline cocrystals exhibited greater resistance to hydration than theophylline alone.…”

Section: Physicochemical Properties and Applications Of Cocrystalsmentioning

confidence: 99%

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

Guo

Sun

Chen

et al. 2021

Acta Pharmaceutica Sinica B

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164

106

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Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.

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Simultaneously Improving the Physicochemical Properties, Dissolution Performance, and Bioavailability of Apigenin and Daidzein by Co-Crystallization With Theophylline

Cited by 46 publications

References 65 publications

Aggregate Materials beyond AIEgens

Aggregate Materials beyond AIEgens

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

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