Highly water-soluble dapsone nanocrystals: Towards innovative preparations for an undermined drug

Rocha, Nataly Paredes da; Souza, Aline de; Yukuyama, Megumi Nishitani; Barreto, Thayná Lopes; Macedo, Luiza de O.; Löbenberg, Raimar; Araújo, Gabriel Lima Barros de; Ishida, Kelly; Bou‐Chacra, Nádia Araci

doi:10.1016/j.ijpharm.2022.122428

Cited by 12 publications

(5 citation statements)

References 60 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“… 388 In addition, the preparation of antibiotics as nanocrystals is also a means of overcoming poor bioavailability: dapsone nanocrystal suspensions produced by Nataly et al are smaller, more soluble and more stable compared to the original drug. 389 SLNs loaded with antimicrobials were found to improve the effectiveness of fluconazole (FLZ) in treating phytolacca vulgaris. Clinical studies demonstrated that FLZ-SLNs exhibited high encapsulation rate, good stability, prolonged release time, and higher cure rate compared to Candistan 1% cream.…”

Section: Nanotechnology’s Application In Infectious Diseasesmentioning

confidence: 99%

Nanotechnology’s frontier in combatting infectious and inflammatory diseases: prevention and treatment

Huang,

Guo,

et al. 2024

Sig Transduct Target Ther

View full text Add to dashboard Cite

Inflammation-associated diseases encompass a range of infectious diseases and non-infectious inflammatory diseases, which continuously pose one of the most serious threats to human health, attributed to factors such as the emergence of new pathogens, increasing drug resistance, changes in living environments and lifestyles, and the aging population. Despite rapid advancements in mechanistic research and drug development for these diseases, current treatments often have limited efficacy and notable side effects, necessitating the development of more effective and targeted anti-inflammatory therapies. In recent years, the rapid development of nanotechnology has provided crucial technological support for the prevention, treatment, and detection of inflammation-associated diseases. Various types of nanoparticles (NPs) play significant roles, serving as vaccine vehicles to enhance immunogenicity and as drug carriers to improve targeting and bioavailability. NPs can also directly combat pathogens and inflammation. In addition, nanotechnology has facilitated the development of biosensors for pathogen detection and imaging techniques for inflammatory diseases. This review categorizes and characterizes different types of NPs, summarizes their applications in the prevention, treatment, and detection of infectious and inflammatory diseases. It also discusses the challenges associated with clinical translation in this field and explores the latest developments and prospects. In conclusion, nanotechnology opens up new possibilities for the comprehensive management of infectious and inflammatory diseases.

show abstract

Section: Nanotechnology’s Application In Infectious Diseasesmentioning

confidence: 99%

Nanotechnology’s frontier in combatting infectious and inflammatory diseases: prevention and treatment

Huang,

Guo,

et al. 2024

Sig Transduct Target Ther

View full text Add to dashboard Cite

show abstract

“…Furthermore, transdermal delivery makes it possible to limit the adverse effects of dapsone, such as hemolyticanemia or nausea, which are the result of the production of metabolites in the liver [24]. These mentioned solubility limitations were the inspiration for various strategies aimed at resolving the poor aqueous solubility and low bioavailability of dapsone [25,26]. Additionally, the number of studies on the solubility of dapsone in various solvent systems [27][28][29][30] including neat solvents [28], as well as co-solvency systems [27].…”

Section: Introductionmentioning

confidence: 99%

Experimental and Theoretical Insights into the Intermolecular Interactions in Saturated Systems of Dapsone in Conventional and Deep Eutectic Solvents

Cysewski,

Jeliński,

Przybyłek

2024

Molecules

View full text Add to dashboard Cite

Solubility is not only a crucial physicochemical property for laboratory practice but also provides valuable insight into the mechanism of saturated system organization, as a measure of the interplay between various intermolecular interactions. The importance of these data cannot be overstated, particularly when dealing with active pharmaceutical ingredients (APIs), such as dapsone. It is a commonly used anti-inflammatory and antimicrobial agent. However, its low solubility hampers its efficient applications. In this project, deep eutectic solvents (DESs) were used as solubilizing agents for dapsone as an alternative to traditional solvents. DESs were composed of choline chloride and one of six polyols. Additionally, water–DES mixtures were studied as a type of ternary solvents. The solubility of dapsone in these systems was determined spectrophotometrically. This study also analyzed the intermolecular interactions, not only in the studied eutectic systems, but also in a wide range of systems found in the literature, determined using the COSMO-RS framework. The intermolecular interactions were quantified as affinity values, which correspond to the Gibbs free energy of pair formation of dapsone molecules with constituents of regular solvents and choline chloride-based deep eutectic solvents. The patterns of solute–solute, solute–solvent, and solvent–solvent interactions that affect solubility were recognized using Orange data mining software (version 3.36.2). Finally, the computed affinity values were used to provide useful descriptors for machine learning purposes. The impact of intermolecular interactions on dapsone solubility in neat solvents, binary organic solvent mixtures, and deep eutectic solvents was analyzed and highlighted, underscoring the crucial role of dapsone self-association and providing valuable insights into complex solubility phenomena. Also the importance of solvent–solvent diversity was highlighted as a factor determining dapsone solubility. The Non-Linear Support Vector Regression (NuSVR) model, in conjunction with unique molecular descriptors, revealed exceptional predictive accuracy. Overall, this study underscores the potency of computed molecular characteristics and machine learning models in unraveling complex molecular interactions, thereby advancing our understanding of solubility phenomena within the scientific community.

show abstract

“…14 These limitations were the inspiration for various strategies aimed at resolving the poor aqueous solubility and low bioavailability of DAP. 15,16 Solubility, as a fundamental characteristic, holds significant importance in the pharmaceutical realm and plays a crucial role in drug design and formulation. 17,18 The reactivity, stability and bioavailability of a chemical compound are significantly influenced by its capacity for dissolution in a specific solvent.…”

Section: Introductionmentioning

confidence: 99%

Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions

Jeliński,

Przybyłek,

Różalski

et al. 2024

Polim. Med.

View full text Add to dashboard Cite

Background. Dapsone (DAP) is an anti-inflammatory and antimicrobial active pharmaceutical ingredient used to treat, e.g., AIDS-related diseases. However, low solubility is a feature hampering its efficient use.Objectives. First, deep eutectic solvents (DES) were used as solubilizing agents for DAP as an alternative to traditional solvents. Second, intermolecular interactions in the systems were described and quantified. Finally, the solubility prediction model, previously created using the machine learning protocol, was extended and improved using new data obtained for eutectic systems.Material and methods. New DES were created by blending choline chloride (ChCl) with 6 selected polyols. The solubility of DAP in these solvents was measured spectrophotometrically. The impact of water dilution on the solubility curve was investigated. Experimental research was enriched with theoretical interpretations of intermolecular interactions, identifying the most probable pairs in the systems. Dapsone self-association and its ability to interact with components of the analyzed systems were considered. Thermodynamic characteristics of pairs were utilized as molecular descriptors in the machine learning process, predicting solubility in both traditional organic solvents and the newly designed DES. Results.The newly formulated solvents demonstrated significantly higher efficiency compared to traditional organic solvents, and a small addition of water increased solubility, indicating its role as a co-solvent. The interpretation of the mechanism of DAP solubility highlighted the competitive nature of self-association and pair formation. Thermodynamic parameters characterizing affinity were instrumental in developing an efficient model for theoretical screening across diverse solvent classes. The study emphasized the necessity of retraining models when introducing new experimental data, as exemplified by enriching the model with data from DES.Conclusions. The research showcased the efficacy of developing new DES for enhancing solubility and creating environmentally and pharmaceutically viable systems, using DAP as an example. Molecular interactions proved valuable in understanding solubility mechanisms and formulating predictive models through machine learning processes.

show abstract

Highly water-soluble dapsone nanocrystals: Towards innovative preparations for an undermined drug

Cited by 12 publications

References 60 publications

Nanotechnology’s frontier in combatting infectious and inflammatory diseases: prevention and treatment

Nanotechnology’s frontier in combatting infectious and inflammatory diseases: prevention and treatment

Experimental and Theoretical Insights into the Intermolecular Interactions in Saturated Systems of Dapsone in Conventional and Deep Eutectic Solvents

Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions

Contact Info

Product

Resources

About