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Article

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

Department of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan
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Authors to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(11), 383; https://doi.org/10.3390/ph13110383
Received: 16 September 2020 / Revised: 5 November 2020 / Accepted: 6 November 2020 / Published: 12 November 2020
(This article belongs to the Section Pharmaceutical Technology)
Solubility is an important physicochemical property affecting drug bioavailability. One approach to improve drug solubility is using amorphous formulations, which can improve solubility by up to a 1000-fold. Herein, amorphous curcumin (CUR) and amorphous solid dispersions (SDs) consisting of CUR, hydroxypropyl cellulose (HPC) and/or sodium dodecyl sulfate (SDS) were developed using vibrational ball milling. The resulting ground mixtures (GMs) were characterized using powder X-ray diffractometry, Fourier transform infrared spectroscopy, differential scanning calorimetry and a dissolution test. The 60-min GM containing 90% HPC significantly increased the drug solubility. Presence of SDS in the GMs containing 90% HPC reduced the grinding duration from 60 min to 30 min in forming a ground SD that significantly increased the CUR dissolution rate. This amorphous state was stable for 30 days when stored at 40 °C/RH 75%. View Full-Text
Keywords: amorphous solid dispersion; solubility; stability; poorly water-soluble drug; vibrational ball milling; Fourier transform infrared spectroscopy; X-ray powder diffraction; differential scanning calorimetry; dissolution amorphous solid dispersion; solubility; stability; poorly water-soluble drug; vibrational ball milling; Fourier transform infrared spectroscopy; X-ray powder diffraction; differential scanning calorimetry; dissolution
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    Doi: 10.5281/zenodo.4032414
    Link: http://<a href="https://doi.org/10.5281/zenodo.4032414"><img src="https://zenodo.org/badge/DOI/10.5281/zenodo.4032414.svg" alt="DOI"></a>
    Description: Figure S1. PXRD patterns of (A) ground curcumin (CUR) crystals; (B) ground mixtures (GMs) containing CUR and 10% hydroxypropyl cellulose (HPC); (C) GMs containing CUR and 25% HPC, and SDS; (D) GMs containing CUR and 50% HPC; (E) GMs containing CUR and 75% HPC; (F) GMs containing CUR and 90% HPC; (G) GMs containing CUR and sodium dodecyl sulfate (SDS), (H) GMs containing CUR, 10% HPC, and SDS; (I) GMs containing CUR, 25% HPC, and SDS; (J) GMs containing CUR, 50% HPC, and SDS; (K) GMs containing CUR, 75% HPC, and SDs; (L) GMs containing CUR, 90% HPC, and SDS Figure S2. FTIR spectra of (A) ground curcumin (CUR) crystals; (B) ground mixtures (GMs) containing CUR and 10% hydroxypropyl cellulose (HPC); (C) GMs containing CUR and 25% HPC, and SDS; (D) GMs containing CUR and 50% HPC; (E) GMs containing CUR and 75% HPC; (F) GMs containing CUR and 90% HPC; (G) GMs containing CUR and sodium dodecyl sulfate (SDS), (H) GMs containing CUR, 10% HPC, and SDS; (I) GMs containing CUR, 25% HPC, and SDS; (J) GMs containing CUR, 50% HPC, and SDS; (K) GMs containing CUR, 75% HPC, and SDs; (L) GMs containing CUR, 90% HPC, and SDS Figure S3. DSC curves of (A) ground curcumin (CUR) crystals; (B) ground mixtures (GMs) containing CUR and 10% hydroxypropyl cellulose (HPC); (C) GMs containing CUR and 25% HPC, and SDS; (D) GMs containing CUR and 50% HPC; (E) GMs containing CUR and 75% HPC; (F) GMs containing CUR and 90% HPC; (G) GMs containing CUR and sodium dodecyl sulfate (SDS), (H) GMs containing CUR, 10% HPC, and SDS; (I) GMs containing CUR, 25% HPC, and SDS; (J) GMs containing CUR, 50% HPC, and SDS; (K) GMs containing CUR, 75% HPC, and SDs; (L) GMs containing CUR, 90% HPC, and SDS Figure S4. Dissolution profiles of (A) ground curcumin (CUR) crystals; (B) ground mixtures (GMs) containing CUR and 10% hydroxypropyl cellulose (HPC); (C) GMs containing CUR and 25% HPC, and SDS; (D) GMs containing CUR and 50% HPC; (E) GMs containing CUR and 75% HPC; (F) GMs containing CUR and 90% HPC; (G) GMs containing CUR and sodium dodecyl sulfate (SDS), (H) GMs containing CUR, 10% HPC, and SDS; (I) GMs containing CUR, 25% HPC, and SDS; (J) GMs containing CUR, 50% HPC, and SDS; (K) GMs containing CUR, 75% HPC, and SDs; (L) GMs containing CUR, 90% HPC, and SDS
MDPI and ACS Style

Mai, N.N.S.; Otsuka, Y.; Kawano, Y.; Hanawa, T. Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling. Pharmaceuticals 2020, 13, 383. https://doi.org/10.3390/ph13110383

AMA Style

Mai NNS, Otsuka Y, Kawano Y, Hanawa T. Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling. Pharmaceuticals. 2020; 13(11):383. https://doi.org/10.3390/ph13110383

Chicago/Turabian Style

Mai, Nguyen N.S., Yuta Otsuka, Yayoi Kawano, and Takehisa Hanawa. 2020. "Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling" Pharmaceuticals 13, no. 11: 383. https://doi.org/10.3390/ph13110383

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