scholarly journals In Vivo Bioavailability and Therapeutic Assessment of Host-Guest Inclusion Phenomena for the Hydrophobic Molecule Etodolac: Pharmacodynamic and Pharmacokinetic Evaluation

2010 ◽  
Vol 78 (1) ◽  
pp. 103-115 ◽  
Author(s):  
Vivek Ranjan Sinha
Keyword(s):  
Therapeutic Assessment ◽  
Hydrophobic Molecule ◽  
Inclusion Phenomena ◽  
Pharmacokinetic Evaluation

In-vitro and In-vivo Pharmacokinetic Evaluation of Guar Gum-Eudragit® S100 Based Colon-targeted Spheroids of Sulfasalazine Co-administered with Probiotics

2018 ◽  
Vol 15 (3) ◽  
pp. 367-387 ◽  
Author(s):  
Abhinav Sharma ◽  
Bimlesh Kumar ◽  
Sachin Kumar Singh ◽  
Monica Gulati ◽  
Yogyata Vaidya ◽  
...  
Keyword(s):  
Guar Gum ◽  
Pharmacokinetic Evaluation

scholarly journals The Natural Compound Hydrophobic Usnic Acid and Hydrophilic Potassium Usnate Derivative: Applications and Comparisons

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5995
Author(s):  
Hallysson Douglas Andrade de Araújo ◽  
Hianna Arely Milca Fagundes Silva ◽  
José Guedes da Silva Júnior ◽  
Mônica Camelo Pessoa de Azevedo Albuquerque ◽  
Luana Cassandra Breitenbach Barroso Coelho ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structural Characteristics ◽  
Usnic Acid ◽  
Raw Material ◽  
Structural Modifications ◽  
Hydrophobic Molecule ◽  
Antiparasitic Agents ◽  
Toxic Molecule

Usnic acid is the best-studied lichen metabolite, presenting several biological activities, such as antibacterial, immunostimulating, antiviral, antifungal, anti-inflammatory, and antiparasitic agents; despite these relevant properties, it is a hydrophobic and toxic molecule. In this context, scientific research has driven the development of innovative alternatives, considering usnic acid as a source of raw material in obtaining new molecules, allowing structural modifications (syntheses) from it. The purpose is to optimize biological activities and toxicity, with less concentration and/or response time. This work presents a literature review with an analogy of the hydrophobic molecule of usnic acid with its hydrophilic derivative of potassium usnate, emphasizing the elucidation and structural characteristics, biological activities, and toxicological aspects of both molecules, and the advantages of using the promising derivative hydrophilic in different in vitro and in vivo assays when compared to usnic acid.

Preparation and in vivo pharmacokinetic evaluation of stable microemulsion system of cholecalciferol

2019 ◽  
Vol 41 (11) ◽  
pp. 1589-1595
Author(s):  
Myoung J. Ho ◽  
Sung H. Im ◽  
Hoe T. Jeong ◽  
Hyung T. Kim ◽  
Jeong E. Lee ◽  
...  
Keyword(s):  
Microemulsion System ◽  
Pharmacokinetic Evaluation

scholarly journals Synthesis, Anticancer Activity, and Preliminary Pharmacokinetic Evaluation of 4,4-Disubstituted Curcuminoid 2,2-bis(Hydroxymethyl)Propionate Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 479 ◽  
Author(s):  
Der-Yen Lee ◽  
Yu-Chi Hou ◽  
Jai-Sing Yang ◽  
Hui-Yi Lin ◽  
Tsu-Yuan Chang ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Functional Groups ◽  
Hydrolysis Product ◽  
Structure Activity Relationship ◽  
Ester Hydrolysis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Hct 116 ◽  
Pharmacokinetic Evaluation

Compound 1 is a curcumin di-O-2,2-bis(hydroxymethyl)propionate that shows significant in vitro and in vivo inhibitory activity against MDA-MB-231 cells with eight to ten-fold higher potency than curcumin. Here, we modified the α-position (C-4 position) of the central 1,3-diketone moiety of 1 with polar or nonpolar functional groups to afford a series of 4,4-disubstituted curcuminoid 2,2-bis(hydroxymethyl)propionate derivatives and evaluated their anticancer activities. A clear structure–activity relationship of compound 1 derivatives focusing on the functional groups at the C-4 position was established based on their anti-proliferative effects against the MDA-MB-231 and HCT-116 cell lines. Compounds 2–6 are 4,4-dimethylated, 4,4-diethylated, 4,4-dibenzylated, 4,4-dipropargylated and 4,4-diallylated compound 1, respectively. Compounds 2m–6m, the ester hydrolysis products of compounds 2–6, respectively, were synthesized and assessed for anticancer activity. Among all compound 1 derivatives, compound 2 emerged as a potential chemotherapeutic agent for colon cancer due to the promising in vivo anti-proliferative activities of 2 (IC50 = 3.10 ± 0.29 μM) and its ester hydrolysis product 2m (IC50 = 2.17 ± 0.16 μM) against HCT-116. The preliminary pharmacokinetic evaluation of 2 implied that 2 and 2m are main contributors to the in vivo efficacy. Compound 2 was further evaluated in an animal study using HCT-116 colon tumor xenograft bearing nude mice. The results revealed a dose-dependent efficacy that led to tumor volume reductions of 27%, 45%, and 60% at 50, 100, and 150 mg/kg doses, respectively. The established structure–activity relationship and pharmacokinetic outcomes of 2 is the guidance for future development of 4,4-disubstituted curcuminoid 2,2-bis(hydroxymethyl)- propionate derivatives as anticancer drug candidates.

Design, formulation, in vitro, in vivo, and pharmacokinetic evaluation of nisoldipine-loaded self-nanoemulsifying drug delivery system

2015 ◽  
Vol 17 (1) ◽  
Author(s):  
Balakumar Krishnamoorthy ◽  
S. M. Habibur Rahman ◽  
N. Tamil selvan ◽  
R. Hari prasad ◽  
M. Rajkumar ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Pharmacokinetic Evaluation

Synthesis, Radiolabeling, and In Vivo Pharmacokinetic Evaluation of the Amyloid Beta Radioligand [11C]AZD4694 in Nonhuman Primates

2013 ◽  
Vol 16 (2) ◽  
pp. 173-179 ◽  
Author(s):  
Magnus Schou ◽  
Katarina Varnäs ◽  
Johan Sandell ◽  
Peter Johnström ◽  
Zsolt Cselenyi ◽  
...  
Keyword(s):  
Amyloid Beta ◽  
Nonhuman Primates ◽  
Pharmacokinetic Evaluation

scholarly journals Enhanced Oral Bioavailability of Epalrestat SBE7-β-CD Complex Loaded Chitosan Nanoparticles: Preparation, Characterization and in-vivo Pharmacokinetic Evaluation

2021 ◽  
Vol Volume 16 ◽  
pp. 8353-8373
Author(s):  
Zunaira Alvi ◽  
Muhammad Akhtar ◽  
Arshad Mahmood ◽  
Nisar ur-Rahman ◽  
Imran Nazir ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Chitosan Nanoparticles ◽  
Pharmacokinetic Evaluation
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