Co-grinding with surfactants as a new approach to enhance in vitro dissolution of praziquantel

Gaggero, Alessio; Dukovski, Bisera Jurišić; Radić, Irena; Šagud, Ivana; Škorić, Irena; Cinčić, Dominik; Jug, Mario

doi:10.1016/j.jpba.2020.113494

Cited by 8 publications

(6 citation statements)

References 27 publications

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“…This is due to the ability of cationic Gemini surfactants to solubility enhancement 53 . Our results went in agreement with Gaggero et al 54 who use surfactants to enhance in vitro dissolution of poorly soluble drugs like praziquantel which use for the treatment of schistosomiasis. Also shown with Kolenyak-Santos et al 55 .…”

Section: Parasitological Examinationsupporting

confidence: 92%

In vivo evaluation the efficiency of nitazoxanide with cationic Gemini surfactant on Cryptosporidiosis

et al. 2023

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Infection with cryptosporidiosis endangers the lives of many people with immunodeficiency, especially HIV patients. Nitazoxanide is one of the main therapeutic drugs used to treat cryptosporidiosis. However, it is poorly soluble in water, which restricts its usefulness and efficacy in immunocompromised patients. Surfactants have an amphiphilic character which indicates their ability to improve the water solubility of the hydrophobic drugs. Our research concerns the synthesis of new cationic Gemini surfactants that have the ability to improve the solubility of the drug Nanazoxide. So, we synthesized cationic Gemini surfactants. N1,N1,N3,N3-tetramethyl-N1,N3-bis(2-octadecanamidoethyl)propane-1,3-diaminium bromide (CGSPS18) and 2,2‘-(ethane-1,2-diylbis(oxy))bis(N-(2-octadecanamidoethyl)-N,N-dimethyl-2-oxoethane-1-aminium) dichloride (CGSES18) and the detection of their chemical composition by spectroscopic methods, as well as studying the properties of their surfaces and their toxicity. Furthermore, the efficacy of nitazoxanide in infected mice was studied in conjunction with three different doses of surfactants. To assess the effect of nitazoxanide and surfactants, the infection was parasitologically counted before and after treatment, and the intestinal, liver, and lung tissues were also examined histopathologically. In this study, it was found that the combination of the drug nitazoxanide with surfactants, especially the compound (CGSPS18) at a concentration of 25% increased the efficacy and resulted in a percentage reduction of 90.8%. Histopathological examination revealed that the group treated with the drug nitazoxanide in combination with CGSPS18 showed the best results exhibiting an almost normal villous pattern. This study demonstrated an increase in the effectiveness of nitazoxanide when combined with surfactants, and this suggests a promising future for the use of surfactants as an adjunct to enhance the effectiveness of nitazoxanide for the treatment of cryptosporidiosis in immunocompromised patients, particularly HIV patients.

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Section: Parasitological Examinationsupporting

confidence: 92%

In vivo evaluation the efficiency of nitazoxanide with cationic Gemini surfactant on Cryptosporidiosis

et al. 2023

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“…In the case of the binary mixture (IB/βCD), the frequency shift of the carbonyl group of IB (Table 4) [29], could be attributed to the breaking of certain intermolecular bonds (hydrogen bonds) associated with IB dimmers, largely described in the literature [33]. The shift of the CO (primary alcohol) band and the OH (associated) band of βCD compared to physical mixtures, as well as the disappearance of the NMR proton of the carboxylic group of IB and the hydroxyls peaks of βCD (2,3,6) suggested the presence of hydrogen bonds between the carboxylic group of IB and hydroxyl groups of βCD [29]. DSC results ( Table 5) have shown that the ternary mixture (IB/βCD/PVP) exhibited higher glass transition temperature (Tg˃250°C).…”

Section: Resultsmentioning

confidence: 86%

“…The presence of these two carriers has increased the glass transition temperature of Indomethacin, the Tg of ternary system was higher than that of binary ground mixtures (IM-SiO 2 , Table 1. Some examples of drug molecules exhibiting solubility enhancement by binary solid dispersion using co-milling technique [1][2][3][4][5][6][7][8][9]. IM-Mg(OH) 2 ).…”

Section: Ternary Solid Dispersion: a New Alternative To Promote Drug mentioning

confidence: 99%

“…In recent years, solid dispersion technology by milling technique was largely utilized by researchers in order to enhance dissolution rate, bioavailability and thus therapeutic efficiency of several poorly water-soluble drugs ( Table 1), as it represents a simple, economic and environmental process without using solvents [1][2][3][4][5][6][7][8][9]. In fact, millings enable particle size reduction and promote the formation of drug nanoparticles, which enhance solubility, flow properties and content uniformities of pharmaceutical dosage forms [10].…”

Section: Introductionmentioning

confidence: 99%

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Ternary Solid Dispersion Strategy for Solubility Enhancement of Poorly Soluble Drugs by Co-Milling Technique

Béjaoui¹,

Oueslati²,

Galai³

2021

Chitin and Chitosan - Physicochemical Properties and Industrial Applications [Working Title]

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Amorphous ternary solid dispersion has become one of the strategies commonly used for improving the solubility and bioavailability of poorly water soluble drugs. Such multicomponent solid dispersion can be obtained by different techniques, this chapter provides an overview of ternary solid dispersion by co-milling method from the perspectives of physico-chemical characteristics in vitro and in vivo performance. A considerable improvement of solubility was obtained for many active pharmaceutical ingredients (e.g., Ibuprofen, Probucol, Gliclazid, Fenofibrate, Ibrutinib and Naproxen) and this was correlated to the synergy of multiple factors (hydrophilicity enhancement, particle size reduction, drug-carrier interactions, anti-plasticizing effect and complexation efficiency). This enhanced pharmacokinetic properties and bioavailability of these drug molecules (1.49 to 15-folds increase in plasma drug concentration). A particular focus was accorded to compare the ternary and binary system including Ibuprofen and highlighting the contribution of thermal and spectral characterization techniques. The addition of polyvinylpyrrolidone (PVP K30), a low molecular weight molecule, into the binary solid dispersion (Ibuprofen/β-cyclodextrin), leads to a 1.5–2 folds increase in the drug intrinsic dissolution rate only after 10 min. This resulted from physical stabilization of amorphous Ibuprofen by reducing its molecular mobility and inhibiting its recristallization even under stress conditions (75% RH and T = 40°C for six months).

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“…Pluronic F127 and sucrose stearate to improve physicochemical and biopharmaceutical properties of poorly soluble drug Praziquantel. The obtained formulations with co-grinding approach embarked the improved in vitro dissolution properties as well as in vitro permeability tested in Caco-2 cells [265].…”

Section: Pluronics As Stabilizer For the Formation Of Different Nano-...mentioning

confidence: 99%

Advances in the therapeutic delivery and applications of functionalized Pluronics: A critical review

Singla

Garg²,

McClements³

et al. 2022

Advances in Colloid and Interface Science

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Co-grinding with surfactants as a new approach to enhance in vitro dissolution of praziquantel

Cited by 8 publications

References 27 publications

In vivo evaluation the efficiency of nitazoxanide with cationic Gemini surfactant on Cryptosporidiosis

In vivo evaluation the efficiency of nitazoxanide with cationic Gemini surfactant on Cryptosporidiosis

Ternary Solid Dispersion Strategy for Solubility Enhancement of Poorly Soluble Drugs by Co-Milling Technique

Advances in the therapeutic delivery and applications of functionalized Pluronics: A critical review

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