Solubility Enhancement of Nitazoxanide Using Solid Dispersion

Ahirrao, Sapana; Rathi, Kishor S; Koli, Diksha B; Kshirsagar, Sanjay J.; Pawar, Sarita S.

doi:10.21276/irjps.2018.5.4.6

Cited by 6 publications

(3 citation statements)

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“…The FTIR spectrum of NTZ (figure 4 a ) indicated a characteristic peak of N-H stretching at 3356.14 cm −1 and aromatic C-H stretching at 3090.12 cm −1 . The other characteristic bands at 1770.65 cm −1 and 1523.76 cm −1 are indicative of the C = O and N = O stretching, respectively [75]. On the other hand in the FTIR spectrum of PL90G shown in figure 4 b , the absorbance band at 2924.09 cm −1 indicated the O-H stretching, while the characteristic peak at 1172.72–1247.94, 968.27 cm −1 and 1090.71 showed the P=O, N(CH 3 ) 3 and P-O-C stretching, respectively [76].…”

Section: Resultsmentioning

confidence: 99%

Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis

et al. 2022

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Topical delivery is preferable over systemic delivery for cutaneous leishmaniasis, because of its easy administration, reduced systemic adverse effects and low cost. Nitazoxanide (NTZ) has broad-spectrum activity against various parasites and has the potential to avoid drug resistance developed by enzymatic mutations. NTZ oral formulation is associated with severe dyspepsia and stomach pain. Herein, NTZ-transethosomes (NTZ-TES) were prepared and loaded into chitosan gel (NTZ-TEG) for topical delivery. NTZ-TES were prepared by the thin-film hydration method and optimized statistically via the Box-Behnken method. The optimized formulation indicated excellent particle size (176 nm), polydispersity index (0.093), zeta potential (−26.4 mV) and entrapment efficiency (86%). The transmission electron microscopy analysis showed spherical-sized particles and Fourier-transform infrared spectroscopy analysis indicated no interaction among the excipients. Similarly, NTZ-TEG showed optimal pH, desirable viscosity and good spreadability. NTZ-TES and NTZ-TEG showed prolonged release behaviour and higher skin penetration and deposition in the epidermal/dermal layer of skin in comparison with the NTZ-dispersion. Moreover, NTZ-TES showed higher percentage inhibition, lower half-maximal inhibitory concentration (IC 50 ) against promastigotes and higher macrophage uptake. Additionally, skin irritation and histopathology studies indicated the safe and non-irritant behaviour of the NTZ-TEG. The obtained findings suggested the enhanced skin permeation and improved anti-leishmanial effect of NTZ when administered as NTZ-TEG.

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Section: Resultsmentioning

confidence: 99%

Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis

et al. 2022

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“…11 Besides, Ahirrao and coworkers improved the solubility of NTZ using a solid dispersion. 12 With the development of the chemical pharmaceutical industry, various other methods were also used to increase the solubility of drugs, such as particle size reduction, salt preparation, and cosolvent. However, studying the solubility of drugs is helpful to optimize the synthesis and purification process and also has important value in the preparation of derivatives.…”

Section: Introductionmentioning

confidence: 99%

“…Professor Patnala and co-workers found that the solubility of the crystal form II of NTZ in water is higher than that of the crystal form I . Besides, Ahirrao and co-workers improved the solubility of NTZ using a solid dispersion . With the development of the chemical pharmaceutical industry, various other methods were also used to increase the solubility of drugs, such as particle size reduction, salt preparation, and cosolvent.…”

Section: Introductionmentioning

confidence: 99%

Solubility Determination of Nitazoxanide in Twelve Organic Solvents from T = 273.15 to 313.15 K

2020

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The objective of the present study was to study the solubility of nitazoxanide (NTZ) in 12 organic solvents such as methanol, ethanol, isopropanol, n-propanol, 1-butanol, ethyl acetate, toluene, acetonitrile, 1,4-dioxane, N-methyl-2-pyrrolidone (NMP), N,N-dimethylformamide (DMF), and 2-butanone by using the isothermal saturation method over a temperature range of 273.15–313.15 K under 101.3 kPa. Experimental solubility data of NTZ was fitted with the modified Apelblat and λh equations. The maximum mole fraction solubility of NTZ was found in NMP (1.127 × 10–1 at 313.15 K) followed by DMF (1.043 × 10–1 at 313.15 K), 1,4-dioxane (3.107 × 10–2 at 313.15 K), 2-butanone (2.286 × 10–2 at 313.15 K), ethyl acetate (3.99 × 10–3 at 313.15 K), acetonitrile (2.011 × 10–3 at 313.15 K), 1-butanol (6.17 × 10–4 at 313.15 K), isopropanol (5.80 × 10–4 at 313.15 K), n-propanol (5.25 × 10–4 at 313.15 K), ethanol (4.50 × 10–4 at 313.15 K), methanol (3.34 × 10–4 at 313.15 K), and toluene (2.91 × 10–4 at 313.15 K). The maximum values of relative average deviation (RAD) and root-mean-square deviation (RMSD) were 4.62% and 9.478 × 10–4, respectively, and were obtained in 2-butanone with the λh equation. Through the analysis of RAD and RMSD values, it was found that the calculated value of the modified Apelblat equation was closer to the experimental value. The solubility data obtained in the present study could be useful for optimizing the purification process of NTZ.

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Nitazoxanide and quercetin co-loaded nanotransfersomal gel for topical treatment of cutaneous leishmaniasis with macrophage targeting and enhanced anti-leishmanial effect

Bashir,

Shabbir,

Din

et al. 2023

Heliyon

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Solubility Enhancement of Nitazoxanide Using Solid Dispersion

Cited by 6 publications

References 0 publications

Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis

Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis

Solubility Determination of Nitazoxanide in Twelve Organic Solvents from T = 273.15 to 313.15 K

Nitazoxanide and quercetin co-loaded nanotransfersomal gel for topical treatment of cutaneous leishmaniasis with macrophage targeting and enhanced anti-leishmanial effect

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