Solubilization and formulation of chrysosplenol C in solid dispersion with hydrophilic carriers

Ng, Choon Lian; Lee, Sang-Eun; Lee, Joon-Kyung; Kim, Tae-Hyeon; Jang, Won Il; Choi, Jin‐Seok; Kim, Young‐Ho; Kim, Jin‐Ki; Park, Jeong Sook

doi:10.1016/j.ijpharm.2016.08.062

Cited by 36 publications

(7 citation statements)

References 29 publications

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“…A significant endothermic sharp peak appeared at 188 °C in the DSC graph of curcumin, resulting from melting of curcumin crystals (Figure a). PVP exhibited a wide DSC thermal absorption peak around 100 °C due to desorption of crystalline water . The physical mixture of curcumin/PVP had a small peak close to the peak of curcumin, suggesting the presence of curcumin crystals.…”

Section: Resultsmentioning

confidence: 99%

Curcumin solid dispersion-loaded in situ hydrogels for local treatment of injured vaginal bacterial infection and improvement of vaginal wound healing

Zhang

Zhuang²,

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives Injured vaginal infection is detrimental to women. A curcumin hydrogel was studied for local treatment of injured vaginal infection. Methods Curcumin solid dispersions (CSDs) were prepared from polyvinyl pyrrolidone and characterized by differential scanning calorimetry and an X-ray diffraction method. An in situ hydrogel CSD hydrogel (CSDG) was prepared with CSD/poloxamers and characterized. In vitro curcumin release and antibacterial effects of CSDs, CSDGs and curcumin were compared. The therapeutic effect of the CSDGs and Lincomycin/Lidocaine Gel was explored after intravaginal administration on the injured rat vaginal infection models. Key findings Curcumin was amorphous in CSDs where curcumin rapidly released in simulated vaginal fluids. However, CSDGs showed sustained release. CSDGs quickly formed gels in the vagina. CSDGs showed high in vivo anti-Escherichia coli or Staphylococcus aureus effect though weak in vitro effect. The recovery of vaginal microenvironment and improvement of intravaginal Lactobacillus growth may be the major reason. Furthermore, CSDGs remarkably improved vaginal wound healing by alleviating inflammation and restoring vaginal epidermal tissues compared with the Lincomycin/Lidocaine Gel. Conclusion CSDGs are a promising topical formulation for local treatment of vaginal bacterial infection and improvement of vaginal wound healing.

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Section: Resultsmentioning

confidence: 99%

Curcumin solid dispersion-loaded in situ hydrogels for local treatment of injured vaginal bacterial infection and improvement of vaginal wound healing

Zhang

Zhuang²,

et al. 2019

Journal of Pharmacy and Pharmacology

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“…In this study, contact angle analysis showed that Iso–Zn (17.4°) had better hydrophilicity than Iso (37.8°) (Figure B). Biological activity of flavonoids was improved because of increased hydrophilicity . Iso–Zn synthesis maybe could provide the basis for enhancing the water solubility and increasing the biological activity of Iso, and it is expected to be used for food preservation.…”

Section: Discussionmentioning

confidence: 99%

Synthesis, Structure Characterization, and Antioxidant and Antibacterial Activity Study of Iso-orientin–Zinc Complex

Wang

et al. 2021

J. Agric. Food Chem.

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Flavonoid−metal complexes possess more effective functional properties than flavonoids. However, the research of iso-orientin (Iso)−metal complex has rarely been reported. In this study, Iso−zinc complex (Iso−Zn, [Zn 3 (C 21 H 14 O 11 ) 2 ]•4H 2 O) had been synthesized and characterized. From the UV−vis spectra and IR spectra, the 4-carbonyl group in the C-ring of Iso was involved in the metal chelation besides A-ring and B-ring hydroxyl group. Thermal gravimetric analysis and the water contact angle test showed that Iso−Zn had higher thermal stability and better hydrophilicity than Iso, respectively. The radical scavenger and antibacterial potencies of Iso−Zn were significantly stronger than those of Iso. Furthermore, Iso−Zn showed lower erythrocytes hemolysis ratio and cytotoxicity. The present study demonstrated that Iso−Zn exhibited better water solubility, antioxidative and antibacterial activities, and lower cytotoxicity and provided a theoretical basis for expanding the utilization scope of Iso through enhancing its hydrophilicity.

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“…The DSC thermogram of the physical mixture showed a shallow endothermic peak at 171.5 °C, indicating the presence of Cur crystals. The melting peaks of Cur were broadened and shifted more to a lower temperature, which could be attributable to the mixing effect [ 37 ]. By contrast, the SD of the Cur-EPO samples presented no endothermic peak around the melting point of the crystals.…”

Section: Resultsmentioning

confidence: 99%

Preparation of Curcumin-Eudragit® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion

Zhang

Zhu

et al. 2021

Molecules

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Hot-melt extrusion (HME) has great advantages for the preparation of solid dispersion (SD), for instance, it does not require any organic solvents. Nevertheless, its application to high-melting-point and thermosensitive drugs has been rarely reported. In this study, thermally unstable curcumin (Cur) was used as a drug model. The HME process was systematically studied by adjusting the gradient temperature mode and residence time, with the content, crystallinity and dissolution of Cur as the investigated factors. The effects of barrel temperature, screw speed and cooling rate on HME were also examined. Solubility parameters and the Flory–Huggins method were used to evaluate the miscibility between Cur and carriers. Differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, equilibrium solubility and in vitro and in vivo experiments were used to characterize and evaluate the results. An amorphous Cur SD was successfully obtained, increasing the solubility and release of Cur. In the optimal process, the mass ratio of Cur to Eudragit® E PO (EPO) was 1:4 and the barrel temperature was set at a gradient heating mode (130 °C–135 °C–140 °C–145 °C–150 °C–155 °C–160 °C) at 100 rpm. Related pharmacokinetic test results also showed the improved bioavailability of the drug in rats. In a pharmacodynamic analysis of Sprague–Dawley rats, the Cmax and the bioavailability of the Cur-EPO SD were 2.6 and 1.5 times higher than those of Cur, respectively. The preparation of the amorphous SD not only provided more solubility but also improved the bioavailability of Cur, which provides an effective way to improve the bioavailability of BCS II drugs.

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Solubilization and formulation of chrysosplenol C in solid dispersion with hydrophilic carriers

Cited by 36 publications

References 29 publications

Curcumin solid dispersion-loaded in situ hydrogels for local treatment of injured vaginal bacterial infection and improvement of vaginal wound healing

Curcumin solid dispersion-loaded in situ hydrogels for local treatment of injured vaginal bacterial infection and improvement of vaginal wound healing

Synthesis, Structure Characterization, and Antioxidant and Antibacterial Activity Study of Iso-orientin–Zinc Complex

Preparation of Curcumin-Eudragit® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion

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