scholarly journals Influence of Inclusion Complexation and Skin Microporation on Enhancement of Transdermal Permeation of Raloxifene Hydrochloride

2019 ◽  
Vol 81 (1) ◽  
Author(s):  
Hetal P. Thakkar ◽  
H. G. Savsani ◽  
P. K. Srivastava
Keyword(s):  
Inclusion Complexation ◽  
Transdermal Permeation ◽  
Raloxifene Hydrochloride

scholarly journals EXTH-65. USING METHYLATION PROFILES TO GUIDE THE REPURPOSING OF CHEMOTHERAPIES AGAINST HIGH-RISK MENINGIOMAS

2020 ◽  
Vol 22 (Supplement_2) ◽  
pp. ii101-ii101
Author(s):  
Anh Tran ◽  
Denise Scholtens ◽  
Lyndsee Zhang ◽  
Jenny Pokorny ◽  
Aneta Baran ◽  
...  
Keyword(s):  
Apoptotic Cell ◽  
Progression Free Survival ◽  
Brain Structures ◽  
Primary Brain Tumor ◽  
Molecular Characteristics ◽  
Cpg Sites ◽  
Hazard Ratios ◽  
The Us ◽  
Patient Prognosis ◽  
Raloxifene Hydrochloride

Abstract Meningioma is the most common primary brain tumor with nearly thirty thousand new cases in the US every year. While most meningiomas grow slowly, hence categorized as benign, they can still impact brain structures and result in disability or lethality. Currently, there is no widely accepted chemotherapy for meningioma, and our understanding of the disease’s molecular characteristics is very limited. In this study, we aimed to identify druggable molecular targets for repurposing of chemotherapies against meningiomas. We analyzed previously published dataset of 493 meningioma patients by Felix Sahm et al (Lancet Oncology, 2017) for association with progression-free survival (PFS) and identified associations of methylation at individual CpG sites as detected by the Illumina 450k platform with PFS. Subsequently, we searched for candidate drugs targeting the pathways linked to poor patient prognosis. Our analyses indicated 981 genes for which methylation of mapped CpG sites was found to be consistently associated with shorter PFS (positive hazard ratios (HRs)) and with longer PFS (negative HRs) at FDR-adjusted p < 0.05. Using Cytoscape/Reactome FI app, we cross-referenced current cancer drugs that target these and identified docetaxel and raloxifene hydrochloride as potential candidates. In our vitro study, docetaxel caused apoptotic cell death in established and primary patient meningioma lines of various grades. IC50s of docetaxel in the sixteen meningioma cell lines tested ranged from 0.8nM to 4.4mM, which partially corresponded to the growth rates of these cells. Our study will advance our understanding of molecular pathways driving meningioma and identify potential targeted therapies to bridge the current gap in treatment of the disease.

scholarly journals Cyclodextrin-Based Supramolecular Complexes of Osteoinductive Agents for Dental Tissue Regeneration

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 136
Author(s):  
Masahiko Terauchi ◽  
Atsushi Tamura ◽  
Yoshinori Arisaka ◽  
Hiroki Masuda ◽  
Tetsuya Yoda ◽  
...  
Keyword(s):  
Growth Factors ◽  
Bone Formation ◽  
Small Molecule ◽  
Tissue Regeneration ◽  
Alveolar Bone ◽  
Inclusion Complexation ◽  
Dental Tissue ◽  
Polyelectrolyte Complexes ◽  
Small Molecule Drugs

Oral tissue regeneration has received growing attention for improving the quality of life of patients. Regeneration of oral tissues such as alveolar bone and widely defected bone has been extensively investigated, including regenerative treatment of oral tissues using therapeutic cells and growth factors. Additionally, small-molecule drugs that promote bone formation have been identified and tested as new regenerative treatment. However, treatments need to progress to realize successful regeneration of oral functions. In this review, we describe recent progress in development of regenerative treatment of oral tissues. In particular, we focus on cyclodextrin (CD)-based pharmaceutics and polyelectrolyte complexation of growth factors to enhance their solubility, stability, and bioactivity. CDs can encapsulate hydrophobic small-molecule drugs into their cavities, resulting in inclusion complexes. The inclusion complexation of osteoinductive small-molecule drugs improves solubility of the drugs in aqueous solutions and increases in vitro osteogenic differentiation efficiency. Additionally, various anionic polymers such as heparin and its mimetic polymers have been developed to improve stability and bioactivity of growth factors. These polymers protect growth factors from deactivation and degradation by complex formation through electrostatic interaction, leading to potentiation of bone formation ability. These approaches using an inclusion complex and polyelectrolyte complexes have great potential in the regeneration of oral tissues.

scholarly journals ß-Cyclodextrin Inclusion Complexes with Catechol-Containing Antioxidants Protocatechuic Aldehyde and Protocatechuic Acid—An Atomistic Perspective on Structural and Thermodynamic Stabilities

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3574
Author(s):  
Thammarat Aree
Keyword(s):  
Inclusion Complexes ◽  
Protocatechuic Acid ◽  
Inclusion Complexation ◽  
Geometry Optimization ◽  
Therapeutic Effects ◽  
Full Geometry Optimization ◽  
Oh Groups ◽  
X Ray ◽  
Protocatechuic Aldehyde ◽  
Crystal Contacts

Protocatechuic aldehyde (PCAL) and protocatechuic acid (PCAC) are catechol derivatives and have broad therapeutic effects associated with their antiradical activity. Their pharmacological and physicochemical properties have been improved via the cyclodextrin (CD) encapsulation. Because the characteristics of b-CD inclusion complexes with PCAL (1) and PCAC (2) are still equivocal, we get to the bottom of the inclusion complexation by an integrated study of single-crystal X-ray diffraction and DFT full-geometry optimization. X-ray analysis unveiled that PCAL and PCAC are nearly totally shielded in the b-CD wall. Their aromatic rings are vertically aligned in the b-CD cavity such that the functional groups on the opposite side of the ring (3,4-di(OH) and 1-CHO/1-COOH groups) are placed nearby the O6–H and O2–H/O3–H rims, respectively. The preferred inclusion modes in 1 and 2 help to establish crystal contacts of OH×××O H-bonds with the adjacent b-CD OH groups and water molecules. By contrast, the DFT-optimized structures of both complexes in the gas phase are thermodynamically stable via the four newly formed host–guest OH⋯O H-bonds. The intermolecular OH×××O H-bonds between PCAL/PCAC 3,4-di(OH) and b-CD O6–H groups, and the shielding of OH groups in the b-CD wall help to stabilize these antioxidants in the b-CD cavity, as observed in our earlier studies. Moreover, PCAL and PCAC in distinct lattice environments are compared for insights into their structural flexibility.

NMR studies of inclusion complexation of the pyrrolizidine alkaloid retronecine and p-sulfonic acid calix[6]arene

2010 ◽  
Vol 69 (1-2) ◽  
pp. 149-155 ◽  
Author(s):  
Daniel Leite Silva ◽  
Eder Couto Tavares ◽  
Leila Souza Conegero ◽  
Ângelo Fátima ◽  
Ronaldo Aloise Pilli ◽  
...  
Keyword(s):  
Sulfonic Acid ◽  
Pyrrolizidine Alkaloid ◽  
Inclusion Complexation ◽  
Nmr Studies

Enhanced photocatalytic activity of CeO2 using β-cyclodextrin on visible light assisted decoloration of methylene blue

2013 ◽  
Vol 69 (1) ◽  
pp. 113-119 ◽  
Author(s):  
Sakthivel Pitchaimuthu ◽  
Ponnusamy Velusamy
Keyword(s):  
Methylene Blue ◽  
Photocatalytic Activity ◽  
Visible Light ◽  
Inclusion Complexation ◽  
Processing Parameters ◽  
Operational Parameters ◽  
Illumination Time ◽  
Operational Conditions ◽  
Electron Microscopy Analysis ◽  
Initial Ph

An attempt has been made to enhance the photocatalytic activity of CeO2 for visible light assisted decoloration of methylene blue (MB) dye in aqueous solutions by β-cyclodextrin (β-CD). The inclusion complexation patterns between host and guest (i.e., β-CD and MB) have been confirmed with UV–visible spectral data. The interaction between CeO2 and β-CD has also been characterized by field emission scanning electron microscopy analysis. The photocatalytic activity of the catalyst under visible light was investigated by measuring the photodegradation of MB in aqueous solution. The effects of key operational parameters such as initial dye concentration, initial pH, CeO2 concentration as well as illumination time on the decolorization extents were investigated. Among the processing parameters, the pH of the reaction solution played an important role in tuning the photocatalytic activity of CeO2. The maximum photodecoloration rate was achieved at basic pH (pH 11). Under the optimum operational conditions, approximately 99.6% dye removal was achieved within 120 min. The observed results indicate that the decolorization of the MB followed a pseudo-first order kinetics.

Exploring unsaturated fatty acid cholesteryl esters as transdermal permeation enhancers

2017 ◽  
Vol 7 (2) ◽  
pp. 333-345 ◽  
Author(s):  
Sanjeev Rambharose ◽  
Rahul S. Kalhapure ◽  
Mahantesh Jadhav ◽  
Thirumala Govender
Keyword(s):  
Fatty Acid ◽  
Unsaturated Fatty Acid ◽  
Cholesteryl Esters ◽  
Permeation Enhancers ◽  
Transdermal Permeation

scholarly journals Inclusion complexation of .BETA.-cyclodextrin with some sulfonamides in aqueous solution.

1978 ◽  
Vol 26 (4) ◽  
pp. 1162-1167 ◽  
Author(s):  
KANETO UEKAMA ◽  
FUMITOSHI HIRAYAMA ◽  
MASAKI OTAGIRI ◽  
YOUKO OTAGIRI ◽  
KEN IKEDA
Keyword(s):  
Aqueous Solution ◽  
Inclusion Complexation ◽  
Beta Cyclodextrin
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