Mechanism Of Solubilization Research Articles

Transcriptomic and metabolomic analysis of recalcitrant phosphorus solubilization mechanisms in Trametes gibbosa

IntroductionPhosphorus (P) is a crucial growth-limiting nutrient in soil, much of which remains challenging for plants to absorb and use. Unlike chemical phosphate fertilizers, phosphate-solubilizing microorganisms (PSMs) offer a means to address available phosphorus deficiency without causing environmental harm. PSMs possess multiple mechanisms for phosphorus solubilization. Although the phosphorus-solubilizing mechanisms of phosphate-solubilizing bacteria (PSB) have been well characterized, the mechanisms utilized by phosphate-solubilizing fungi (PSF) remain largely unexplored.MethodsThis study isolated a PSF strain, Trametes gibbosa T-41, from soil and evaluated its phosphorus solubilizing capacity with organic (calcium phytin; Phytin-P) and inorganic (tricalcium phosphate; Ca-P) phosphorus sources. The phosphorus solubilization, enzyme activity, and organic acid production of T-41 were measured. And the P-solubilizing mechanism conducted by transcriptomic and metabolomic analyses.Results and discussionT-41 exhibited varying phosphorus solubilizing capacity when grown with organic (calcium phytin; Phytin-P) and inorganic (tricalcium phosphate; Ca-P) phosphorus sources (109.80 ± 8.9 mg/L vs. 57.5 ± 7.9 mg/L, p < 0.05). Compared with the Ca-P treatment, T-41 demonstrated a stronger alkaline phosphatase (ALP) production capacity under Phytin-P treatment (34.5 ± 1.2 μmol/L/h vs. 19.8 ± 0.8 μmol/L/h, p < 0.05). Meanwhile, the production of oxalic acid, maleic acid, and succinic acid was higher under Phytin-P treatment (p < 0.05). Transcriptomic and metabolomic analysis revealed that different phosphorus sources altered metabolic pathways such as galactose metabolism, glyoxylate and dicarboxylic acid metabolism, and ascorbate and aldolate metabolism. Key metabolites like myo-inositol, 2-oxoglutarate, and pyruvate were found to impact the performance of T. gibbosa T-41 differently under the two P sources. Notably, synthesis in Ca-P vs. Pytin-P, T-41 upregulated genes involved in myo-inositol synthesis, potentially enhancing its P-solubilizing ability. These results provide new insights into the molecular mechanisms of PSF at the transcriptomic and metabolomic levels, laying a theoretical foundation for the broader application of PSF as bio-phosphorus fertilizers in the future.

Formation and snake-eating like solubilization mechanisms of rhamnolipid vesicles for oil components and amino acids

Rhamnolipid vesicles hold significant potential across a wide range of applications, yet their formation mechanisms and selective solubilization of organic molecules remain elusive. Employing dissipative particle dynamics (DPD) simulations, this study delves deeply into these aspects, uncovering a stepwise formation pathway from dispersed monomers to complex multi-layer vesicle structures. The fusion and growth of three-layer structures were identified as crucial steps in the development of stacked vesicles. Notably, double-chain rhamnolipids (Rh-C10-C10) exhibited enhanced stability in self-assembled structures compared to their single-chain counterparts (Rh-C10). Through a detailed analysis of parameters such as relative concentration distribution, radial distribution function, and density fields, the solubilization process of rhamnolipid vesicles was found to resemble a “snake-eating” mechanism. We also analyzed the solubilization sites, amounts, and vesicle sizes, elucidating the selective solubilization mechanisms of rhamnolipids for representative polar and non-polar compounds in crude oil, anisole and 1-hexene. The selectivity of rhamnolipid vesicles in solubilizing organic molecules was primarily influenced by polar attraction and steric hindrance, which together determined their solubilization sites within the vesicles. Additionally, the solubilization behavior and properties of five types of amino acids within rhamnolipid vesicles were explored, demonstrating analogous solubilization patterns that correlated with amino acid polarity. These results provide a foundation for optimizing the application of rhamnolipid vesicles, paving the way for potential advancements in drug delivery, environmental remediation, and oil recovery processes.

Isolation and characterization of phosphate solubilizing bacteria from the rhizosphere of lentil (Lens culinaris M.) collected from Hagere Mariam district, Central Ethiopia.

Phosphorus plays a crucial role in regulating many of the plant's metabolic activities by enhancing physiological functions and stimulating biological activities such as nodulation, nitrogen fixation, and nutrient uptake in the soil rhizosphere environment. Inoculants of phosphorus solubilizing bacteria serve as an eco-friendly alternative technology that positively influences both soil sustainability and plant growth. The majority of North Shewa highland areas are characterized by low available phosphorus, primarily acidic, and exhibit strong phosphorus absorption. The objective of this study was to isolate and identify phosphorus solubilizing bacteria from the rhizosphere of lentils and characterize their phosphate solubilizing activity. The cultural, biochemical, physiological microbial analysis was conducted in the microbiology laboratory, department of biology. Pikovskaya's medium was utilized for the isolation, screening, and maintenance of phosphate solubilizing bacteria. Phosphate Solubilizing Bacteria were isolated using tri-calcium phosphate as the sole source of phosphorus in indicator plates. Fifteen phosphate solubilizing bacteria were isolated from lentil rhizosphere soil samples, among which six were the most efficient phosphate solubilizers designated as PSBYE, PSBYR, PSBYM, PSBYL, PSBW, and PSBSW. All isolates notably solubilized tri-calcium phosphate compared to the uninoculated control. The highest phosphorous solubilization was observed from the isolate PSBYL, with a value of 10.61mg/50ml, followed by PSBW with a value of 9.08 mg/50ml. The decrease in pH value correlated with the levels of tri-phosphate solubilization in the PVK broth by the PSB isolates. The pH dropped to 4.64 from the initial pH of 7.2 when grown in the broth, which suggests that the production of organic acids is likely the primary mechanism for phosphate solubilization.

Management of soil phosphorous using phosphate solubilizing microorganisms: A sustainable approach

Phosphorus is crucial for plant growth and productivity, and its scarcity in soil negatively affects crop yields. A major portion of chemical phosphate fertilizer precipitates with soil minerals, making it unavailable for plant growth. Phosphate-solubilizing microorganisms play a pivotal role in enhancing phosphorus availability, facilitating better nutrient absorption, and ultimately boosting plant growth. This article presents a brief overview of the phosphorus status in Indian soil, discusses the various forms of phosphorus and its dynamics across different soil types, and analyses the factors involved, highlighting the importance of phosphorus management for sustainable agriculture. Physiological and molecular mechanisms of microbial phosphate solubilization provide deep insights into exploring PSMs for managing phosphorous in different soil types. It also provides a path for the necessity to explore the multifarious plant growth-promoting traits of PSMs underscoring its applicability for sustainable agricultural practices with viable economy. The mechanism of solubilization of phosphorus has been discussed to understand the role of microorganisms in different soils. The study highlights the role of significant microorganisms in developing tailored consortia of PSMs and other plant growth-promoting rhizobacteria (PGPR) based on the chemical composition of the soil, along with an integrated nutrient approach incorporating PSMs. This review offers valuable insights into harnessing PSMs and their practical applications, facilitating their broader adoption in agricultural systems to maintain soil health.

Study on several novel crystalline complexes of sorafenib with dicarboxylic acid: Nature identification and solubilization mechanism

The development of solid-state forms of drugs is an effective approach to increase solubility. This study developed three crystalline complexes of sorafenib (SF) with oxalic acid (OA) and malonic acid (MA) using a solvent method, named SF+·OA-·THF, SF+·OA-, and SF-MA. The formation of these complexes was influenced by the crystalline method, solvent polarity, and the carbon chain length of the dicarboxylic acids. Single-crystal X-ray diffraction revealed proton transfer in SF+·OA-·THF, classifying it as a channel-type salt solvate and conformational polymorph due to hydrogen bond formation. 13C solid-state nuclear magnetic resonance and X-ray photoelectron spectroscopy confirmed proton transfer in SF+·OA-·THF and SF+·OA-, but not in SF-MA, indicating that SF+·OA- is a salt while SF-MA is a co-crystal. Fourier Transform Infrared Spectroscopy further supported these findings. Compared with Form Ⅰ, SF+·OA-, SF+·OA-·THF, and SF-MA increased the apparent solubility of SF by 8.3, 7.9, and 6.4 times in pH 1.2 HCl buffer, and by 4.0, 3.1, and 4.5 times in pH 6.8 PBS buffer, respectively. All crystalline complexes exhibited a “spring and parachute” phenomenon due to the solubility difference between the drug and the dicarboxylic acids. Notably, the intermolecular forces between SF and THF in SF+·OA-·THF prolonged the “spring and parachute” process. Additionally, these crystalline complexes demonstrated good stability. This study provides valuable insights into the development and identification of crystalline complexes and their dissolution mechanisms.

Distinct Solubilization Mechanisms of Medroxyprogesterone in Gemini Surfactant Micelles: A Comparative Study with Progesterone

The solubilization behavior of medroxyprogesterone (MP) within gemini surfactant micelles (14-6-14,2Br−) was investigated and compared with that of progesterone to uncover distinct solubilization mechanisms. We employed 1H-NMR and 2D ROESY spectroscopy to elucidate the spatial positioning of MP within the micelle, revealing that MP integrates more deeply into the micellar core. This behavior is linked to the unique structural features of MP, particularly its 17β-acetyl group, which promotes enhanced interactions with the hydrophobic regions of the micelle, while the 6α-methyl group interacts with the hydrophilic regions of the micelle. The 2D ROESY correlations specifically highlighted interactions between the hydrophobic chains of the surfactant and two protons of MP, H22 and H19. Complementary machine learning and electron density analyses supported these spectroscopic findings, underscoring the pivotal role of the molecular characteristics of MP in its solubilization behavior. These insights into the solubilization dynamics of MP not only advance our understanding of hydrophobic compound incorporation in gemini surfactant micelles but also indicate the potential of 14-6-14,2Br− micelles for diverse drug delivery applications.

The role of proton excreted by Advenella kashmirensis DF12 during ammonium assimilation in phosphate solubilization.

Phosphate-solubilizing bacteria (PSB) can solubilize soil fixed phosphorus (P) to plant available forms. In previous studies, the mechanisms of inorganic phosphate solubilization by PSB mostly focused on the acidolysis of organic acids. Here we screened a highly efficient PSB, Advenella kashmirensis DF12, with the maximum P solubilization of 590 mg L- 1 at 6 days. In addition to its P solubilizing ability, DF12 also showed a tolerance to pH from 5 to 10 and a nitrogen fixation potential. The multiple functions of DF12 and its wide adaptability to various environmental conditions make it a promising biofertilizer candidate. The combined analysis of extracellular metabolites and intracellular metabolome data revealed that the production of organic acid (mainly gluconic acid) is not the only mechanism of P solubilized by DF12, the solubilized P content was not correlated with the gluconic acid concentration but was in a highly significant positive correlation with proton concentration, extrusion of proton during NH4+ assimilation plays a key role in phosphate solubilization. Moreover, the contribution of NH4+ assimilation to phosphorus solubilization is generally present in PSB. Therefore, we proposed that applying ammonium fertilizer in P-deficient soil is more appropriate, it can not only supplement nitrogen fertilizer, but also enhance P use efficiency, which contributes to worldwide fertilizer use reduction and efficiency improvement.

White rot fungi as a multifaceted biocontrol agent: Metabolic disruption and algal inhibition in Microcystis aeruginosa

Microcystis aeruginosa is a prevalent cyanobacterium linked to water eutrophication and harmful algal blooms. While bacterial control strategies are well-studied, the effects of white rot fungi on Microcystis aeruginosa are less understood. This study examines the impact of whole fungal liquid, its centrifuged supernatant, and sterilized solutions on the algae’s physiological and biochemical traits. Metabolomics and multivariate analysis identified significant changes in 47 metabolic markers, including carbohydrates, amino acids, and fatty acids, across treatments. The complete fungal liquid exhibited the strongest algicidal effect, likely due to synergistic solubilization mechanisms mediated by extracellular enzymes such as manganese peroxidase, catalase, and laccase. Notably, algicidal activity persisted even after sterilization, suggesting the presence of non-proteinaceous compounds like polysaccharides or lipids. The metabolic disturbances included downregulation of the TCA cycle and reduced fatty acid synthesis, leading to inhibited photosynthesis and compromised nucleic acid integrity in the algal cells. This research enhances our understanding of how white rot fungi disrupt Microcystis aeruginosa metabolism, providing a theoretical basis for their potential use in bioremediation of eutrophic aquatic environments.

Study on co-amorphous emerging solubilization behavior after gelation during dissolution: The importance of complexation and anti-crystallization

Co-amorphous (CM) is a promising technology for enhancing the aqueous solubility of insoluble drugs, but the gelation phenomenon has often occurred during the dissolution process and seriously threatened their solubility/dissolution performance. Therefore, it’s quite important to design favorable CM systems to alleviate or even avoid the adverse effects of gelation phenomenon. In this study, CM systems of taxifolin (TAX) and oxymatrine (OMT) (TAX-OMT CMs) were constructed to improve the solubility and dissolution properties of TAX. Interestingly, TAX-OMT CMs gradually aggregated and obviously gelled during dissolution, but the solubility and dissolution of TAX in TAX-OMT CMs were significantly enhanced compared to crystalline TAX. Consequently, the underlying solubilization mechanisms of TAX-OMT CMs after gelation were systematically explored. For one thing, the complexation between the two components in TAX-OMT CMs was verified by phase solubility, fluorescence spectroscopy and isothermal titration calorimetry. For another, the residual solids of TAX-OMT CMs after dissolution evaluation were thoroughly characterized by means of powder X-ray diffraction, fourier transform infrared spectroscopy, scanning electron microscopy, which showed the anti-crystallization property of TAX-OMT CMs. Furthermore, molecular simulation demonstrated the intermolecular interactions of TAX-OMT CMs alone and TAX-OMT complexes in aqueous solution. Finally, pharmacokinetics study in rats suggested that the bioavailability of TAX in TAX-OMT CM (1:2) was approximately 5.5-fold higher than that of crystalline TAX after oral administration. Collectively, this study reveals the importance of complexation and anti-crystallization effects of CM systems on maintaining solubilization behavior after gelation, providing an effective strategy to improve the absorption performance of pharmaceutical CM systems.

Unveiling Solubilization Mechanisms of Natural Deep Eutectic Solvents in Triazole Fungicides: COSMO-RS Calculations and Screening for Eco-Friendly, High-Efficiency Pesticide Systems

Unveiling Solubilization Mechanisms of Natural Deep Eutectic Solvents in Triazole Fungicides: COSMO-RS Calculations and Screening for Eco-Friendly, High-Efficiency Pesticide Systems

Microbial phosphate solubilization mechanisms in P solubilizing in andisol

Phosphate (P) nutrient plays a significant role in plant growth and yield. P is an essential element that plays an important role in photosynthesis and root development. Phosphate nutrient availability is deficient in some soil types due to retention, such as in Andisol soil types. High phosphate retention in Andisol soil types causes P nutrients to be unavailable to plants and can reduce crop yields. The availability of P in Andisol soils can be done, among others, by applying phosphate solubilizing microbes. Phosphate solubilizing microorganisms are soil microorganisms consisting of bacteria and fungi that can mineralize organic P, dissolve inorganic P minerals, and store large amounts of P to make it available to plants. This literature review aims to determine the mechanism of phosphate-solubilizing microbes in P dissolution in Andisol soil. The methods used in this systematic review are collecting data through the internet and utilizing recognized sources such as Science Direct, Research Gate, Google Scholar, and Web of Science. Content analysis was performed on the collected data, and the results were organized into thematic categories. Furthermore, the findings are presented descriptively with the help of tables to facilitate understanding. Since phosphate-solubilizing microorganisms can dissolve P in the soil through chemical and biological mechanisms, it can be concluded that phosphate-solubilizing microorganisms also have an important role in the soil P cycle. The implications of this literature review are to understand the retention of P nutrients in Andisols and how the dissolution mechanism works, as well as the use of microbes as a solution to increase phosphate dissolution so that it is available to plants.

Use of Phosphorus-Solubilizing Microorganisms as a Biotechnological Alternative: A Review.

Microorganisms with the ability to dissolve phosphorus have the potential to release this essential nutrient into the soil through natural solubilization processes, which allows for boosting plant growth and development. While literature reviews acknowledge their potential, unexplored territories concerning accessibility, application, and effective integration into sustainable agriculture necessitate further research. This manuscript employed distinct methodologies to execute a bibliometric analysis and a literature review. The combined application of both methodologies enables a holistic understanding of the domain landscape and its innovative facets. For the bibliometric analysis, the propositions of Donthu and Jia were utilized, supplemented by tools, such as Bibliometrix. The literature review adhered to a systematic methodology predicated on Petersen's guidelines to represent the domain accurately, pinpointing trends and gaps that could steer future, more detailed research. This investigation uncovers an escalating interest in studying these microorganisms since the 2000s, emphasizing their significance in sustainable agriculture and the context of phosphorus scarcity. It was also discerned that India and China, nations with notable agricultural sectors and a high demand for phosphorus fertilizers, spearheaded research output on this subject. This signifies their substantial contribution to the progression of this scientific field. Furthermore, according to the research consulted, phosphorus-solubilizing microorganisms play a pivotal role in the symbiotic interaction of soil with plant roots and represent an efficacious strategy to counteract the low availability of phosphorus in the soil and sustainably enhance agricultural systems. Finally, this review contributes to the relevant domain by examining existing empirical evidence with special emphasis on sustainable agriculture, improved understanding of phosphorus solubilization mechanisms, and recognition of various microbial entities.

True-solution-scale utilization of natural chlorophyll a in aqueous media through cooperative aggregation with phycocyanin

The challenge of applying chlorophyll(Chl) in aqueous media has been a significant obstacle to the diversified development of Chl a-related industries. This study presents the first report on the true-solution-scale utilization of Chl in aqueous media through the construction of chlorophyll a-phycocyanin (Chls-PC) composite nanoparticles. This study determined the optimal conditions for Chls-PC preparation: a composite ratio of 1:25, a solvent ratio of 1:4, and a stirring time of 1 h. Fluorescence spectroscopy, transmission electron microscope, and confocal microscopy confirmed Chl a and PC aggregation. Surface hydrophobicity and contact angle measurements showed that Chls-PC water solubility was similar to PC and much higher than Chl. Infrared spectroscopy, quantum chemical calculations, X-ray photoelectron spectroscopy, and molecular dynamics simulations elucidated the water solubilization mechanism of Chls-PC both experimentally and theoretically. This research provides theoretical guidance for the development and production of water-based products using Chl as a raw material.

Isolation and Characterization of Potassium-Solubilizing Rhizobacteria (KSR) Promoting Cotton Growth in Saline-Sodic Regions.

Cotton is highly sensitive to potassium, and Xinjiang, China's leading cotton-producing region, faces a severe challenge due to reduced soil potassium availability. Biofertilizers, particularly potassium-solubilizing rhizobacteria (KSR), convert insoluble potassium into plant-usable forms, offering a sustainable solution for evergreen agriculture. This study isolated and characterized KSR from cotton, elucidated their potassium solubilization mechanisms, and evaluated the effects of inoculating KSR strains on cotton seedlings. Twenty-three KSR strains were isolated from cotton rhizosphere soil using modified Aleksandrov medium. Their solubilizing capacities were assessed in a liquid medium. Strain A10 exhibited the highest potassium solubilization capacity (21.8 ppm) by secreting organic acids such as lactic, citric, acetic, and succinic acid, lowering the pH and facilitating potassium release. A growth curve analysis and potassium solubilization tests of A10 under alkali stress showed its vigorous growth and maintained solubilization ability at pH 8-9, with significant inhibition at pH 10. Furthermore, 16S rRNA sequencing identified strain A10 as Pseudomonas aeruginosa. Greenhouse pot experiments showed that inoculating cotton plants with strain A10 significantly increased plant height and promoted root growth. This inoculation also enhanced dry biomass accumulation in both the aerial parts and root systems of the plants, while reducing the root-shoot ratio. These results suggest that Pseudomonas aeruginosa A10 has potential as a biofertilizer, offering a new strategy for sustainable agriculture.

Exploring the Organic Acid Secretion Pathway and Potassium Solubilization Ability of Pantoea vagans ZHS-1 for Enhanced Rice Growth.

Soil potassium deficiency is a common issue limiting agricultural productivity. Potassium-solubilizing bacteria (KSB) show significant potential in mitigating soil potassium deficiency, improving soil quality, and enhancing plant growth. However, different KSB strains exhibit diverse solubilization mechanisms, environmental adaptability, and growth-promoting abilities. In this study, we isolated a multifunctional KSB strain ZHS-1, which also has phosphate-solubilizing and IAA-producing capabilities. 16S rDNA sequencing identified it as Pantoea vagans. Scanning electron microscopy (SEM) showed that strain ZHS-1 severely corroded the smooth, compact surface of potassium feldspar into a rough and loose state. The potassium solubilization reached 20.3 mg/L under conditions where maltose was the carbon source, sodium nitrate was the nitrogen source, and the pH was 7. Organic acid metabolism profiling revealed that strain ZHS-1 primarily utilized the EMP-TCA cycle, supplemented by pathways involving pantothenic acid, glyoxylic acid, and dicarboxylic acids, to produce large amounts of organic acids and energy. This solubilization was achieved through direct solubilization mechanisms. The strain also secreted IAA through a tryptophan-dependent metabolic pathway. When strain ZHS-1 was inoculated into the rhizosphere of rice, it demonstrated significant growth-promoting effects. The rice plants exhibited improved growth and root development, with increased accumulation of potassium and phosphorus. The levels of available phosphorus and potassium in the rhizosphere soil also increased significantly. Additionally, we observed a decrease in the relative abundance of Actinobacteria and Proteobacteria in the rice rhizosphere soil, while the relative abundance of genera associated with acid production and potassium solubilization, such as Gemmatimonadota, Acidobacteria, and Chloroflexi, as well as Cyanobacteria, which are beneficial to plant growth, increased. These findings contribute to a deeper understanding of the potassium solubilization mechanisms of strain ZHS-1 and highlight its potential as a plant growth-promoting rhizobacteria.

Improving the solubilization, stability, dialysis performance and antioxidant properties of quercetin in surfactant-free microemulsion

The flavonol compound quercetin with poor water solubility, was solubilized in a novel green solvent constructed in this work. The solvent is composed of tributyl citrate, ethanol and water, recognized as surfactant-free microemulsion (SFME). The solubilization behavior and mechanism of quercetin were investigated, the light, thermal, storage stability and antioxidant properties were examined, as well as the dialysis properties and release kinetics. The results reveal that there are interactions existing between quercetin and tributyl citrate. Ethanol and tributyl citrate in SFME also have a synergistic solubilization effect on quercetin. Therefore, the content of quercetin increases with tributyl citrate, and the solubility of quercetin in oil in water SFME (RE/W = 7:3, ƒO = 0.1) is 9.88 mg/ml, much higher than that in water or ethanol. The light, heat, storage stability and antioxidant properties of quercetin are greatly improved by SFME. In the dialysis process, the release of quercetin in SFME follows a non-Fickian diffusion mechanism with a slow-release action. The SFME established has green and non-toxic advantages in the application of the solubilization field, and it is expected to provide important guidance for the extraction and separation of natural foods.

Cloud Point Extraction Coupled to Flame Atomic Absorbance Spectroscopy for Cobalt (II) determination with Azo-Azomethine Dye

The azo-azomethine dye 6,6'-((1E,1'E)-((4-methyl-1,2-phenylene)bis(azanylylidene))bismethanylylidene))bis(2-methoxy-3-(o-tolyldiazenyl) phenol) (L3) were synthesized and characterized by UV-visible, FT-IR, 1H-NMR and Mass spectroscopy. The effect of the several factors on the CPE pre-concentration of Cobalt (II) with L3 was optimized. Extensive thermodynamic study has been presented to understand the mechanism of extraction and solubilization of studied complex in Triton X-100 micelles. Under the optimized conditions, enrichment factor of 54 is achieved leading to limit of detection and limit of quantitation of 11.5 and 38.4 ngmL-1 respectively. Under the optimal conditions the calibration plot is linear in the range of 0.025-3 μg mL-1, the precision (RSD%; n=8) of the proposed method is of 0.823% at 0.05 μg mL-1 of Co (II). This method is applied to the determination of Co (II) in various environmental samples.

Complete genome sequence of Bacillus subtilis NA05 (=NBRC 116153), a phosphate-solubilizing bacterium isolated from crop field soil.

We report the complete genome sequence of the phosphate-solubilizing bacterium Bacillus subtilis NA05 (=NBRC 116153), consisting of a circular chromosome of ~3.8 M bp and two circular plasmids. The data presented here provide further insight into the genetic and functional potential of B. subtilis and the mechanism of phosphate solubilization.

Solubilization mechanism of α-glycosylated naringin based on self-assembled nanostructures and its application to skin formulation

We previously reported that α-glycosylated naringin (naringin-G), synthesized by enzyme-catalyzed transglycosylation, can enhance the solubility of poorly water-soluble compounds without surface-active property. However, the solubilization mechanism has not been fully elucidated. In this study, the solubilization mechanism of naringin-G was investigated using nuclear magnetic resonance (NMR) spectroscopy, and its application in skin formulations was further investigated. 1H NMR and dynamic light scattering measurements at various concentrations confirmed the self-assembled nanostructures of naringin-G above a critical aggregation concentration of approximately 2.2 mg/mL. Two-dimensional 1H–1H nuclear Overhauser effect spectroscopy and solubility tests revealed that flavone with poor water solubility, could be solubilized in its self-assembled structure with a stoichiometric relationship with naringin-G. When naringin-G was included in the skin formulation, the permeated amount and permeability coefficient (Papp) of flavones improved up to four times with increasing amounts of naringin-G. However, flavone solubilization by adding an excessive amount of naringin-G resulted in a decreased permeated amount and Papp of flavones, indicating the interplay between the apparent solubility and skin permeability of flavones. Naringin-G, which forms a nanoaggregate structure without exhibiting surface-active properties, has the potential to enhance the solubility and skin permeation of poorly water-soluble compounds.

Inclusion Complexes of Ethanamizuril with β- and Hydroxypropyl-β-Cyclodextrin in Aqueous Solution and in Solid State: A Comparison Study.

Ethanamizuril (EZL) is a new anticoccidial drug developed by our Shanghai Veterinary Research Institute. Since EZL is almost insoluble in water, we conducted a study to improve the solubility of EZL by forming inclusion complexes with β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD). In this study, we performed molecular docking and then systematically compared the interactions of EZL with β-CD and HP-β-CD in both aqueous solution and the solid state, aiming to elucidate the solubilization effect and mechanism of cyclodextrins (CDs). The interactions were also examined in the solid state using DSC, PXRD, and FT-IR. The interactions of EZL with CDs in an aqueous solution were investigated using PSA, UV-vis spectroscopy, MS, 1H NMR, and 2D ROESY. The results of phase solubility experiments revealed that both β-CD and HP-β-CD formed inclusion complexes with EZL in a 1:1 molar ratio. Among them, HP-β-CD exhibited higher Kf (stability constant) and CE (complexation efficiency) values as well as a stronger solubilization effect. Furthermore, the two cyclodextrins were found to interact with EZL in a similar manner. The results of our FT-IR and 2D ROESY experiments are in agreement with the theoretical results derived from molecular simulations. These results indicated that intermolecular hydrogen bonds existing between the C=O group on the triazine ring of EZL and the O-H group of CDs, as well as the hydrophobic interactions between the hydrogen on the benzene ring of EZL and the hydrogen of CDs, played crucial roles in the formation of EZL/CD inclusion complexes. The results of this study can lay the foundation for the future development of high-concentration drinking water delivery formulations for EZL.