Mechanistic investigation of biopharmaceutic and pharmacokinetic characteristics of surface engineering of satranidazole nanocrystals

Dhat, Shalaka; Pund, Swati; Kokare, Chandrakant; Sharma, Pankaj Kumar; Shrivastava, Birendra

doi:10.1016/j.ejpb.2015.12.007

Cited by 8 publications

(5 citation statements)

References 35 publications

(46 reference statements)

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“…According to Figure , the same major intense characteristic peaks were observed at 15.4, 16.8, 18.5, 21.1, 22.2, 25.7, 27.3, 28.7, and 30.6° between the pure drug (SAT-1) and solid phases in equilibrium with saturation solutions (SAT-2) in monosolvents. These observed characteristic intense peaks were close to accessible literature data at 2-θ values of 16.84, 18.59, and 21.20° for SAT . These patterns also revealed that both the forms of SAT-1 and SAT-2 remained stable without showing any sign of solvate, polymorph, or amorphous formations during the entire experiment, and thus the reliability of solubility measurements could be guaranteed.…”

Section: Resultssupporting

confidence: 86%

“…These observed characteristic intense peaks were close to accessible literature data at 2-θ values of 16.84, 18.59, and 21.20°for SAT. 10 These patterns also revealed that both the forms of SAT-1 and SAT-2 remained stable without showing any sign of solvate, polymorph, or amorphous formations during the entire experiment, and thus the reliability of solubility measurements could be guaranteed.…”

Section: ■ Results and Discussionmentioning

confidence: 82%

“…As per the literature survey, SAT had not been official in any Indian (IP), British (BP), U.S. (USP), and Japanese pharmacopeias (JP) until now . It has low aqueous solubility and high permeability and could be classified as a class-II drug according to the biopharmaceutics classification system, because it does not meet the current Food and Drug Administration criteria for high solubility to be classified as a class-I drug. − It is highly recommended in the treatment of amoebic liver abscess, giardiasis, and trichomoniasis at relatively low doses, because it possesses potent broad-spectrum antiprotozoal activity against Entamoebia histolytica, Trepenoma vaginalis, and Giardia intestinalis. − Though the molecule is found to be effective against these microorganisms, its therapeutic efficacy is hindered because of its poor aqueous solubility. According to the literature, SAT is sparingly soluble in water because it could not effectively break the lattice structure of water .…”

Section: Introductionmentioning

confidence: 99%

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Thermodynamic Modeling and Solubility Study of Satranidazole in Different Monosolvents at Different Temperatures

Rathi¹,

Kale

Jouyban

2021

J. Chem. Eng. Data

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The solubility study of drugs in aqueous and organic solvents has practical importance in pharmaceutical industries. In this research work, the solubilities of satranidazole (SAT) were determined in 18 monosolvents, namely, methanol (MeOH), ethanol (EtOH), 1-propanol (1-PrOH), 2-propanol (2-PrOH), formamide, 1,4-dioxane, N,N-dimethyl formamide (DMF), N,N-dimethyl acetamide (DMA), dimethyl sulfoxide (DMSO), N-methyl-2-pyrrolidone (NMP), ethylene glycol (EG), propylene glycol (PG), 1,4-butanediol (BDOH), glycerin, polyethylene glycol-200 (PEG-200), PEG-400, PEG-600, and water, at five different temperatures (T = 293.2–313.2 K) and atmospheric pressure (p = 0.1 MPa). Experimental solubilities expressed in the molar fraction of SAT were correlated well with thermodynamic models including van’t Hoff model, Apelblat model, Buchowski–Ksiazczak model, and polynomial empirical model. The molar fraction solubility of SAT was recorded highest in NMP (7.963 × 10–2 at T = 293.2 K) followed by DMSO, formamide, DMF, DMA, PEG-600, PEG-400, PEG-200, 1,4-dioxane, PG, EG, BDOH, glycerin, MeOH, EtOH, 1-PrOH, 2-PrOH, and water as expected over the entire temperature range investigated.

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Section: Resultssupporting

confidence: 86%

Section: ■ Results and Discussionmentioning

confidence: 82%

Section: Introductionmentioning

confidence: 99%

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Thermodynamic Modeling and Solubility Study of Satranidazole in Different Monosolvents at Different Temperatures

Rathi¹,

Kale

Jouyban

2021

J. Chem. Eng. Data

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“…However, the developed formulation did not show the same high energy peaks ( Figure 8 b). A significant reduction in peak intensities indicates the loss of crystallinity of fluvastatin in SLNPs [ 25 ]. This may be due to the presence of excipients and also due to solubilization of the active in the lipidic carrier.…”

Section: Resultsmentioning

confidence: 99%

Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 32 Factorial Design Approach

et al. 2022

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The purpose of the present research work was to design, optimize, and evaluate fluvastatin-loaded solid lipid nanoparticles (FLV-SLNPs) using 32 factorial design for enhancing the bioavailability. Fluvastatin has several disadvantages, including the low solubility and substantial first-pass metabolism resulting in a low (30%) bioavailability and a short elimination half-life. FLV-SLNPs were prepared using the nano-emulsion technique. For the optimization of the FLV-SLNPs, a total of nine formulations were prepared by varying two independent factors at three levels, using full factorial design. In this design, lipid (A) and surfactant (B) concentrations were chosen as independent factors, whereas entrapment efficiency (Y1) and in-vitro drug release (Y2) were selected as the dependent variables. Additionally, the prepared SLNPs were characterized for X-ray diffraction, Fourier transform-infrared spectroscopy, and differential scanning calorimetry. These studies revealed that there were no interactions between the drug and the selected excipients and the selected formulation components are compatible with the drug. Pharmacokinetic studies in rats confirmed significant improvement in AUC and MRT of SLNPs in comparison with the pure drug indicating the enhanced bioavailability of SLNPs. This study provides a proof-of-concept for the fact that SLNPs can be effectively developed via experimental factorial design, which requires relatively minimal experimentation.

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“…At the same time, adding particular type of alcohol to the emulsion mix can enhance the activity of emulsifiers and produce even smaller nanoemulsions via HPH [22] . Nevertheless, HPH's setting and optimized stabilizer conditions are key to reducing drying frequencies for increasing the stability of the nanoemulsions produced [23] .…”

Section: Introductionmentioning

confidence: 99%

Continuous manufacturing of carboxyamidotriazoleencapsulated nanoemulsions using adaptive focused acoustics: Potential green technology for the pharmaceutical industry

Choi

Kakumanu

Schmitz

et al. 2016

JBEI

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Nanoemulsions containing hydrophobic drugs have a great potential in the pharmaceutical industries to improve the bioavailability of the drug. However, currently there is no cost-effective way of producing nanoemulsions in large scale. The need of subjecting emulsions to an extreme pressure of 50 MPa demands a large excess of energy for the manufacturing process, while low-energy method requires large amount of solvents. Here, nanoemulsions containing a well-characterized hydrophobic drug, carboxyamidotriazole (CAI), are produced in both batch and continuous modes to demonstrate the scalability of nanoemulsion production using Covaris' Adaptive Focused Acoustics™ (AFA) technology. To move from batch scale to continuous flow, the acoustic and thermal energy inputs can be manipulated to adjust particle size, while the composition and temperature of starting materials can be altered to achieve complete dissolution of hydrophobic drugs, thus providing 100% encapsulation efficiency. Furthermore, using two AFA systems in series can drastically enhance the production flow rates, making AFA a competitive means for producing nanoemulsions in the pharmaceutical industry.

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Mechanistic investigation of biopharmaceutic and pharmacokinetic characteristics of surface engineering of satranidazole nanocrystals

Cited by 8 publications

References 35 publications

Thermodynamic Modeling and Solubility Study of Satranidazole in Different Monosolvents at Different Temperatures

Thermodynamic Modeling and Solubility Study of Satranidazole in Different Monosolvents at Different Temperatures

Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 32 Factorial Design Approach

Continuous manufacturing of carboxyamidotriazoleencapsulated nanoemulsions using adaptive focused acoustics: Potential green technology for the pharmaceutical industry

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