Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet

Cho, Jung-Hyun; Kim, Yong‐Il; Kim, Dong-Wuk; Yousaf, Abid Mehmood; Kim, Jong Oh; Woo, Jong Soo; Yong, Chul Soon; Choi, Han‐Gon

doi:10.1016/j.ejps.2013.12.016

Cited by 39 publications

(15 citation statements)

References 30 publications

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“…Recently, much attention has been focused on the development of solid dispersion oral tablets for the solubility enhancement of poorly water soluble drugs (Cho, et al, 2014;Tran, et al, 2014). Solid dispersions are defined as the dispersion of one or more active ingredients in a matrix at solid state (Chaudhari, 2006).…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Ramadhani

Shabir

McConville

2014

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Ramadhani

Shabir

McConville

2014

International Journal of Pharmaceutics

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“…Solid dispersion − the dispersal of a hydrophobic drug in a hydrophilic polymer with or without the addition of a surfactant − is an excellent strategy to enhance the solubility and dissolution of water-insoluble drugs. [9][10][11][12][13][14][15][16][17][18][19] A solid dispersion prepared with the addition of a surfactant (a ternary solid dispersion) results in greater improvement of the solubility and dissolution of BCS class 2 drugs as compared to solid dispersions prepared without a surfactant (binary solid dispersions). 20 Solid dispersions can be prepared conventionally by the melting method, 21 the kneading method, 22 the solvent evaporation method, 9 or the lyophilization technique.…”

Section: Introductionmentioning

confidence: 99%

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

Yousaf

Zulfiqar²,

Shahzad

et al. 2019

Polim. Med.

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Background. Eprosartan mesylate is a poorly water-soluble drug. It does not dissolve well in the aqueous gastrointestinal fluid, which means it is not absorbed well via the oral route, because a drug can cross cell membranes when it is dissolved in the gastrointestinal fluid. Objectives. The purpose of this research was to enhance the aqueous solubility and dissolution rate of eprosartan mesylate using the solid dispersion technique. Enhancing the solubility and dissolution leads to better absorption via the oral route. Material and methods. A number of eprosartan mesylate-laden polymeric solid dispersions were prepared with hydroxypropyl methylcellulose (HPMC) and polysorbate 80 by means of the solvent evaporation technique. The impact of the weight ratios of the constituents on the solubility and dissolution rate was studied in comparison with the plain drug. The formulation presenting the optimal solubility and dissolution underwent the solid-state characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR). Results. Both polysorbate 80 and HPMC positively affected the solubility and dissolution of eprosartan mesylate. Conclusions. In particular, a ternary solid dispersion consisting of eprosartan mesylate, HPMC and polysorbate 80 at a weight ratio of 1:4.2:0.3 showed the highest solubility (36.39 ± 3.95 mg/mL) and dissolution (86.19 ±4.09% in 10 min). Moreover, the drug was present in the amorphous form in the solid dispersion with no covalent drug-excipient interactions.

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“…There was no shift of the chief distinguishing spikes; therefore, the drug had no covalent interaction with the excipients in the nanospherule formulation. [11][12][13] The SEM outcomes of the study of fenofibrate powder and electrosprayed nanospherule are presented in Figure 5. The free drug showed crystals of irregular shape and surface ( Figure 5A).…”

Section: 12mentioning

confidence: 99%

“…6,7 A pharmaceutical nanoparticle is a particle having a correspondence: han-gon choi college of Pharmacy and Institute of Pharmaceutical science and Technology, hanyang University, 55 hanyangdaehak-ro, sangnok-gu, ansan, gyeonggi 426-791, south Korea Tel +82 31 400 5802 Fax +82 31 400 5958 email hangon@hanyang.ac.kr [10][11][12][13] Electrospraying is a promising technique for the preparation of pharmaceutical nanoparticles. 14,15 In the preparation of a nanospherule via this technique, all of the constituents are comprehensively dissolved and the final transparent solution is subjected to electrospraying.…”

Section: Introductionmentioning

confidence: 99%

“…14,15 Generally, improvement in aqueous solubility and bioavailability of poorly water-soluble drugs by conventional solid dispersion systems is due to wetting enhancement, particle size reduction, and/or a change of the crystalline drug to the amorphous form. [11][12][13]32 Thus, in this study, the electrosprayed nanospherule may have improved the aqueous solubility and bioavailability of poorly water-soluble fenofibrate by the same mechanisms, except through wetting enhancement. On the other hand, unlike other microcapsules and solid dispersions, the electrosprayed nanospherule could be manufactured without heat, leading to production of more stable formulations compared to the former two.…”

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confidence: 99%

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Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

Yousaf

Mustapha

Kim

et al. 2016

IJN

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Purpose The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. Methods Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil ® M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed. The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion. Results All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug. Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the electrosprayed nanospherule. Increases were observed as the PVP/drug ratio increased to 4:1, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of 1:4:0.5 resulted in a particle size of <200 nm with the drug present in the amorphous state. It demonstrated the highest solubility (32.51±2.41 μg/mL), an excellent dissolution (~85% in 10 minutes), and an oral bioavailability ~2.5-fold better than that of the free drug. It showed similar oral bioavailability compared to the conventional solid dispersion. Conclusion Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate.

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Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet

Cited by 39 publications

References 30 publications

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

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