Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling

Sao, Nguyen Ngoc; Otsuka, Yuta; Kawano, Yoshiro; Hanawa, Takehisa

doi:10.3390/ph13110383

Cited by 14 publications

(18 citation statements)

References 47 publications

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“…The amorphous state of polyphenols is most often stabilized by hydrogen bonds. Recent work shows the amorphous solid dispersion of such polyphenols as quercetin [11,16,17], resveratrol [18], curcumin [18][19][20], naringenin [21], daidzein [22], and genistein [23]. The amorphous form of pterostilbene was obtained, for example, by Tzeng et al via nanoprecipitation with Eudragit ® e100 and polyvinyl alcohol (PVA) [24].…”

Section: Introductionmentioning

confidence: 99%

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

2023

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The aim of our research was to improve the solubility and antioxidant activity of pterostilbene (PTR) by developing a novel amorphous solid dispersion (ASD) with Soluplus® (SOL). DSC analysis and mathematical models were used to select the three appropriate PTR and SOL weight ratios. The amorphization process was carried out by a low-cost and green approach involving dry milling. An XRPD analysis confirmed the full amorphization of systems in 1:2 and 1:5 weight ratios. One glass transition (Tg) observed in DSC thermograms confirmed the complete miscibility of the systems. The mathematical models indicated strong heteronuclear interactions. SEM micrographs suggest dispersed PTR within the SOL matrix and a lack of PTR crystallinity, and showed that after the amorphization process, PTR-SOL systems had a smaller particle size and larger surface area compared with PTR and SOL. An FT-IR analysis confirmed that hydrogen bonds were responsible for stabilizing the amorphous dispersion. HPLC studies showed no decomposition of PTR after the milling process. PTR’s apparent solubility and antioxidant activity after introduction into ASD increased compared to the pure compound. The amorphization process improved the apparent solubility by ~37-fold and ~28-fold for PTR-SOL, 1:2 and 1:5 w/w, respectively. The PTR-SOL 1:2 w/w system was preferred due to it having the best solubility and antioxidant activity (ABTS: IC50 of 56.389 ± 0.151 µg·mL−1 and CUPRAC: IC0.5 of 82.52 ± 0.88 µg·mL−1).

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Section: Introductionmentioning

confidence: 99%

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

2023

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“…The use of the ball milling method was also reported by Mai et al [47], using Hydroxypropyl Cellulose (HPC) and Sodium Dodecyl Sulfate (SDS) as carriers. The results showed that with an increase in HPC, the solubility of curcumin also increased.…”

Section: Co-milling Methodsmentioning

confidence: 95%

Solid Dispersion as a Potential Approach to Improve Dissolution and Bioavailability of Curcumin From Turmeric (Curcuma Longa L.)

AGUSTINA,

SETYANINGSIH

2023

Int J App Pharm

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This review article attempts to outline techniques and solid dispersion carriers that have been applied to improve curcumin's solubility and bioavailability in turmeric extract. This paper also examines the variables that impact the efficacy of curcumin solid dispersion. Turmeric (Curcuma longa L.) contains curcuminoids as bioactive compounds consisting of curcumin, dimethoxy-curcumin, and bis-dimethoxy-curcumin. Curcumin, as the main component, is proven to have several pharmacological effects. However, it has limitations in modern drug development, such as poor stability, solubility, and bioavailability. Many studies have been conducted to overcome these limitations, including the application of solid dispersion. The preparation methods of curcumin solid dispersions are carried out by solvent evaporation, fusion/melting, and co-milling, using various types of carriers. However, the formation of a solid dispersion system only sometimes provides a considerable improvement in solubility, dissolution, and bioavailability. Differences in the selection of preparation methods, carriers, and solvents result in various arrangements of particles in the solid dispersion that may affect the performance of the system. In addition, the type of carrier also has a role in increasing curcumin permeability and bioavailability. Hydrophilic surfactant carriers have inhibitory activity against body transporters, such as P-gp and MRP, that can help to increase curcumin’s bioavailability. Natural Deep Eutectic Solvent (NADES) as a novel alternative solvent also has promising opportunities for the development of curcumin solid dispersion. Therefore, selecting appropriate preparation methods, carriers, and solvents should be considered to achieve optimum solubility, dissolution, and bioavailability of curcumin.

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“…The mechanism underlying increased solubility involves the hydrophilic carrier enhancing the drug dissolution rate by reducing crystal size and particle porosity. Solid dispersions are categorized into eutectic systems, glass solutions, suspensions, and solid solutions based on molecular arrangement ( Malkawi et al, 2022 ; van Hoogevest, 2017 ; Mai et al, 2020 ). Various technologies, including the hot-melt extrusion method, solvent method, electro-spinning, and spray drying, have been employed for solid dispersion preparation ( Williams et al, 2013 ).…”

Section: Introductionmentioning

confidence: 99%

Enabling a novel solvent method on Albendazole solid dispersion to improve the in vivo bioavailability

Han,

Zou

2024

European Journal of Pharmaceutical Sciences

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Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling

Cited by 14 publications

References 47 publications

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

Solid Dispersion as a Potential Approach to Improve Dissolution and Bioavailability of Curcumin From Turmeric (Curcuma Longa L.)

Enabling a novel solvent method on Albendazole solid dispersion to improve the in vivo bioavailability

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