A new approach to the determination of pKa and pKb of Brønsted–Lowry weak acid and weak base in aprotic solvent

Teng, Jiaojuan; Pang, Junjie; Sun, Yonghong; Wang, Jianguo

doi:10.1016/j.jelechem.2022.116172

Cited by 5 publications

(2 citation statements)

References 32 publications

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“…The pK a value is a fundamental measure of acid strength that evaluates the proton affinity of an acid in the context of Bronsted acid-base theory. 29 A lower pK a value signifies a stronger acid with a greater tendency to donate protons. On the other hand, for a base, the strength can be ascertained by the pK a value of its conjugate acid.…”

Section: Resultsmentioning

confidence: 99%

Pure Nano Genesis: Pioneering Universal Aqueous Nanostrategies from Pure Molecules to Revolutionise Diverse Applications

Zhao,

Li,

et al. 2024

Preprint

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In this paper, we propose a novel universal approach for the construction of stable and aqueous nanoparticles, Pure Nano systems, comprising solely small conjugated molecules without any excipients. Our experiments confirm that the generation of surface charges plays an essential role during the spontaneous aggregation of conjugated molecules in the process of Pure Nano system fabrication, as it governs growth and confers physiochemical stability to particles at the nano scale. This approach overcomes solubility challenges in highly hydrophobic conjugated molecules by obviating excipients and enabling up to 100% drug loading capacity. Confirmation of this capability stems from the successful preparation of approximately 100 Pure Nano systems, incorporating different combinations of 27 conjugated molecules distinguished by their diverse dissociation types and degrees. The proposed preparation method is robust, simple, fast, and reliable, making it well-suited for large-scale manufacturing due to its array of unique features. This strategy affords a singular, molecular-focused approach, showcasing the intrinsic bioactivity of its constituent molecules while enabling aqueous dispersion for diverse applications. And in vivo experiments confirm the exceptional efficacy of various Pure Nano systems in reinstating dextran sodium sulfate induced acute ulcerative colitis to a healthy state, restoring myocardial ischemia/reperfusion injury to normal levels, and effectively treating cancer in mice with significantly improved median survival rates. This innovative nano drug delivery system represents a groundbreaking advancement with the potential to revolutionise translational nanomedicine. Positioned at the forefront of therapeutic possibilities, it is anticipated to substantially improve the efficacy and safety of nano therapies. This advancement heralds a new era, offering a highly targeted and efficient approach in the treatment of diverse medical conditions.

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Section: Resultsmentioning

confidence: 99%

Pure Nano Genesis: Pioneering Universal Aqueous Nanostrategies from Pure Molecules to Revolutionise Diverse Applications

Zhao,

Li,

et al. 2024

Preprint

View full text Add to dashboard Cite

show abstract

“…Subsequently, the NOB crystallized in solitary form. Unlike other coformers, URE is a neutral compound, 41) and the NOB-URE cocrystals have a channel-like structure, which is easily penetrated by the solvent. It is believed that the NOB-URE cocrystals continued to dissolve because the solution remained neutral pH even after the cocrystals dissolved in the initial stages of this study.…”

Section: Resultsmentioning

confidence: 99%

Novel Pharmaceutical Cocrystals and Solvate Crystals of Nobiletin, a Citrus Flavonoid with Potent Pharmacological Activity

Tokunaga,

Uchikoshi,

Hayashi

et al. 2023

CHEMICAL & PHARMACEUTICAL BULLETIN

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Nobiletin (NOB) is a flavonoid with attractive pharmaceutical characteristics, including anti-Alzheimer's, anti-inflammation, and anti-cancer properties, but it has low solubility in water, resulting in reduced bioavailability. Its solubility must be improved to develop NOB as a drug. Cocrystal engineering can change the physicochemical properties of an active pharmaceutical ingredient and generate remarkable drug candidates that are superior in drug formulation. In this report, extensive co-crystal screening of NOBs with 31 cocrystal formers (coformers) with various functional groups was carried out by the liquid-assisted grinding method. As a result, four cocrystals (NOB with urea (URE), oxalic acid, gallic acid and salicylic acid) and one solvate crystal (NOB with formic acid (FOR)) were found. Powder X-ray diffraction and thermal analysis revealed the unique crystal morphology of all the obtained samples. In addition, the crystal structures of two of them (NOB-URE and NOB-FOR) were determined by single crystal X-ray diffraction. The results revealed that NOB-URE and NOB-FOR are new cocrystals or solvate crystals consisting of molar ratios of 1 : 2 and 1 : 0.73, respectively. In NOB-URE, we could observe a transient increase in solubility due to supersaturation, suggesting that URE is one of the better coformers of NOB.

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Charge balanced aggregation: A universal approach to aqueous organic nanocrystals

Zhao,

Li,

et al. 2024

Journal of Controlled Release

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A new approach to the determination of pKa and pKb of Brønsted–Lowry weak acid and weak base in aprotic solvent

Cited by 5 publications

References 32 publications

Pure Nano Genesis: Pioneering Universal Aqueous Nanostrategies from Pure Molecules to Revolutionise Diverse Applications

Pure Nano Genesis: Pioneering Universal Aqueous Nanostrategies from Pure Molecules to Revolutionise Diverse Applications

Novel Pharmaceutical Cocrystals and Solvate Crystals of Nobiletin, a Citrus Flavonoid with Potent Pharmacological Activity

Charge balanced aggregation: A universal approach to aqueous organic nanocrystals

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