Constructing Anti-Glioma Drug Combination with Optimized Properties through Cocrystallization

Cocrystallization of two anti-glioma agents, Temozolomide (TMZ) and baicalein (BAI), resulted in a cocrystal presenting superior stability for unstable TMZ as well as optimized dissolution and pharmacokinetics for TMZ and BAI. Cocrystallization can be an efficient approach to construct anti-glioma drug combination systems at the molecular level.

[1]  C. Almansa,et al.  Co-crystal of Tramadol Hydrochloride–Celecoxib (ctc): A Novel API–API Co-crystal for the Treatment of Pain , 2017 .

[2]  Bingqing Zhu,et al.  Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability , 2017 .

[3]  Lalit Kumar,et al.  Temozolomide and its stability—A critical factor , 2017 .

[4]  Dinesh Kumar,et al.  Multidrug co-crystals: towards the development of effective therapeutic hybrids. , 2016, Drug discovery today.

[5]  Yong-sheng Jiang,et al.  Effect of treatment with baicalein on the intracerebral tumor growth and survival of orthotopic glioma models , 2015, Journal of Neuro-Oncology.

[6]  G. Desiraju,et al.  Cocrystals of Hydrochlorothiazide: Solubility and Diffusion/Permeability Enhancements through Drug-Coformer Interactions. , 2015, Molecular pharmaceutics.

[7]  Jia Zhou,et al.  Exploring therapeutic potentials of baicalin and its aglycone baicalein for hematological malignancies. , 2014, Cancer letters.

[8]  T. Lu,et al.  Simultaneously enhancing the solubility and permeability of acyclovir by crystal engineering approach , 2013 .

[9]  A. Nangia,et al.  Temozolomide Cocrystals with Carboxamide Coformers , 2013 .

[10]  Chieh-Shan Wu,et al.  Baicalein Triggers Mitochondria-Mediated Apoptosis and Enhances the Antileukemic Effect of Vincristine in Childhood Acute Lymphoblastic Leukemia CCRF-CEM Cells , 2013, Evidence-based complementary and alternative medicine : eCAM.

[11]  A. Nangia,et al.  Crystal engineering of stable temozolomide cocrystals. , 2012, Chemistry, an Asian journal.

[12]  W. Schlindwein,et al.  Pharmaceutical cocrystals: an overview. , 2011, International journal of pharmaceutics.

[13]  Haeyong Lee,et al.  Beta-Catenin mediates the anti-adipogenic effect of baicalin. , 2010, Biochemical and biophysical research communications.

[14]  Sally Freels,et al.  Prevalence estimates for primary brain tumors in the United States by age, gender, behavior, and histology. , 2010, Neuro-oncology.

[15]  F. Lu,et al.  Synergistic anti-cancer effect of baicalein and silymarin on human hepatoma HepG2 Cells. , 2009, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[16]  M. Li‐Weber.  New therapeutic aspects of flavones: the anticancer properties of Scutellaria and its main active constituents Wogonin, Baicalein and Baicalin. , 2009, Cancer treatment reviews.

[17]  L. Reddy,et al.  Polymorphs and polymorphic cocrystals of temozolomide. , 2008, Chemistry, an Asian journal.

[18]  Ning Shan,et al.  The role of cocrystals in pharmaceutical science. , 2008, Drug discovery today.

[19]  Changquan Calvin Sun,et al.  Improving Mechanical Properties of Caffeine and Methyl Gallate Crystals by Cocrystallization , 2008 .

[20]  J. Xing,et al.  Interaction of baicalin and baicalein with antibiotics in the gastrointestinal tract , 2005, The Journal of pharmacy and pharmacology.

[21]  Q. Wang,et al.  Zinc coupling potentiates anti-HIV-1 activity of baicalin. , 2004, Biochemical and biophysical research communications.

[22]  T. Hong,et al.  Evaluation of the Anti-Inflammatory Effect of Baicalein on Dextran Sulfate Sodium-Induced Colitis in Mice , 2002, Planta medica.

[23]  T. Batchelor,et al.  New treatment strategies for malignant gliomas. , 1999, The oncologist.

[24]  M. Stevens,et al.  NMR and molecular modeling investigation of the mechanism of activation of the antitumor drug temozolomide and its interaction with DNA. , 1994, Biochemistry.

[25]  Y. Kimura,et al.  Studies on Scutellariae Radix , 1981 .

[26]  Y. Wang,et al.  Baicalein induces apoptosis via a mitochondrial-dependent caspase activation pathway in T24 bladder cancer cells. , 2013, Molecular medicine reports.

[27]  H. Asaoku,et al.  PPARβ-mediated growth suppression of baicalein and dexamethasone in human myeloma cells , 2007, Leukemia.

[28]  N. Bleehen,et al.  Multicentre CRC phase II trial of temozolomide in recurrent or progressive high-grade glioma , 1997, Cancer Chemotherapy and Pharmacology.

[29]  E. Golovinsky,et al.  Pharmacobiochemistry of arylalkyltriazenes and their application in cancer chemotherapy. , 1985, Pharmacology & therapeutics.