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Characterization of thymoquinone/hydroxypropyl-ß-cyclodextrin inclusion complex: Application to anti-allergy properties.
Al-Qubaisi, Mothanna Sadiq; Rasedee, Abdullah; Flaifel, Moayad Husein; Eid, Eltayeb E M; Hussein-Al-Ali, Samer; Alhassan, Fatah H; Salih, Ashraf M; Hussein, Mohd Zobir; Zainal, Zulkarnain; Sani, Dahiru; Aljumaily, Abdulmajeed Hammadi; Saeed, Mohammed Ibrahim.
Afiliación
  • Al-Qubaisi MS; Institute of Bioscience, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.
  • Rasedee A; Institute of Bioscience, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia; Department of Veterinary Laboratory Diagnosis, Faculty of Veterinary Medicine, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia. Electronic address: rasedee@upm.edu.my.
  • Flaifel MH; Department of Physics, College of Science, Imam Abdulrahman Bin Faisal University, 32256 Dammam, Saudi Arabia.
  • Eid EEM; Department of Pharmaceutical Chemistry and Pharmacognosy Unaizah College of Pharmacy, Qassim University, Saudi Arabia.
  • Hussein-Al-Ali S; Faculty of Pharmacy, Isra University, Amman 11622, Jordan.
  • Alhassan FH; Department of Applied Chemistry and Technology, College of Science and Arts, Alkamel University of Jeddah, Jeddah 21589, Saudi Arabia.
  • Salih AM; Department of Radiation Processing, Sudan Atomic Energy Commission, Khartoum 1111, Sudan.
  • Hussein MZ; Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.
  • Zainal Z; Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.
  • Sani D; Institute of Bioscience, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia; Department of Veterinary Pharmacology and Toxicology, Faculty of Veterinary Medicine, Ahmadu Bello University Zaria, Kaduna State, Nigeria.
  • Aljumaily AH; Department of Computer and Communications System Engineering, Faculty of Engineering, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.
  • Saeed MI; Faculty of Medical Laboratory Sciences, National Ribat University, Khartoum 11111, Sudan.
Eur J Pharm Sci ; 133: 167-182, 2019 May 15.
Article en En | MEDLINE | ID: mdl-30902654
Thymoquinone is an effective phytochemical compound in the treatment of various diseases. However, its practical administration has been limited due to poor aqueous solubility and bioavailability. In this work, we developed a novel inclusion complex of thymoquinone and hydroxypropyl-ß-cyclodextrin that features improved solubility and bioactivity. The drug solubility was markedly accelerated in the increasing ratio of hydroxypropyl-ß-cyclodextrin to thymoquinone amount. The formation of the thymoquinone/hydroxypropyl-ß-cyclodextrin inclusion complex was evidenced using X-ray diffraction, differential scanning calorimetry, thermal gravimetric analysis, Fourier transform infrared, scanning electron microscopy and nuclear magnetic resonance. The release behavior of the complex, as well as of their mixtures, was examined in artificial gastric (pH 1.2) and intestinal (pH 6.8) dissolution media. The formulated complex released the drug rapidly at the initial stage, followed by a slow release. Thermodynamic parameters ΔH, ΔS and ΔG were calculated with temperatures ranging from 20 to 45 °C to evaluate the complexation process. The activity of the inclusion complex was evaluated on IgE-mediated allergic response in rat basophilic leukemia (RBL-2H3) cells by monitoring key allergic mediators. The results revealed that compared with free thymoquinone, the inclusion complex more strongly inhibited the release of histamine, tumor necrosis factor-α, and interleukin-4, and was not cytotoxic at the tested thymoquinone concentrations (0.125-4 µg/mL) indicating the inclusion complex possibly had better antiallergic effects. Our finding suggested that the inclusion complex achieved prolonged action and reduced side-effect of thymoquinone.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzoquinonas / Sistemas de Liberación de Medicamentos / Antialérgicos / 2-Hidroxipropil-beta-Ciclodextrina Límite: Animals Idioma: En Revista: Eur J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Malasia Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzoquinonas / Sistemas de Liberación de Medicamentos / Antialérgicos / 2-Hidroxipropil-beta-Ciclodextrina Límite: Animals Idioma: En Revista: Eur J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Malasia Pais de publicación: Países Bajos