Percutaneous absorption of non-steroidal anti-inflammatory drugs from in situ gelling xyloglucan formulations in rats

2002 ◽  
Vol 246 (1-2) ◽  
pp. 179-186 ◽  
Author(s):  
A Takahashi ◽  
S Suzuki ◽  
N Kawasaki ◽  
W Kubo ◽  
S Miyazaki ◽  
...  
Keyword(s):  
Percutaneous Absorption ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
In Situ Gelling

scholarly journals Development of a New Formulation Based on In Situ Photopolymerized Polymer for the Treatment of Spinal Cord Injury

Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4274
Author(s):  
Gabrielle B. Novais ◽  
Stefane dos Santos ◽  
Robertta J. R. Santana ◽  
Rose N. P. Filho ◽  
John L. S. Cunha ◽  
...  
Keyword(s):  
Spinal Cord ◽  
Spinal Cord Injury ◽  
Hydroalcoholic Extract ◽  
Inflammatory Conditions ◽  
Cord Injury ◽  
Light Curing ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
New Formulation

Spinal Cord Injury (SCI) promotes a cascade of inflammatory events that are responsible for neuronal death and glial scar formation at the site of the injury, hindering tissue neuroregeneration. Among the main approaches for the treatment of SCI, the use of biomaterials, especially gelatin methacryloyl (GelMA), has been proposed because it is biocompatible, has excellent mechanical properties, favoring cell adhesion and proliferation. In addition, it can act as a carrier of anti-inflammatory drugs, preventing the formation of glial scars. The present work presents the development and in situ application of a light-curing formulation based on GelMA containing a natural extract rich in anti-inflammatory, antioxidant and neuroprotective substances (hydroalcoholic extract of red propolis—HERP) in an experimental model of SCI in rats. The formulations were prepared and characterized by time of UV exposition, FTIR, swelling and degradation. The hydrogels containing 1 mg/mL of HERP were obtained by the exposure to UV radiation of 2 μL of the formulation for 60 s. The locomotor evaluation of the animals was performed by the scale (BBB) and demonstrated that after 3 and 7 days of the injury, the GelMA-HERP group (BBB = 5 and 7) presented greater recovery compared to the GelMA group (BBB = 4 and 5). Regarding the inflammatory process, using histomorphological techniques, there was an inflammation reduction in the groups treated with GelMA and GelMA-HERP, with decreases of cavitation in the injury site. Therefore, it is possible to conclude that the use of GelMA and GelMA-HERP hydrogel formulations is a promising strategy for the treatment of SCI when applied in situ, as soon as possible after the injury, improving the clinical and inflammatory conditions of the treated animals.

scholarly journals Ratiometric two-photon fluorescent probe for in situ imaging of carboxylesterase (CE)-mediated mitochondrial acidification during medication

2019 ◽  
Vol 55 (76) ◽  
pp. 11358-11361 ◽  
Author(s):  
Ao Jiang ◽  
Guang Chen ◽  
Jie Xu ◽  
Yuxia Liu ◽  
Guanghui Zhao ◽  
...  
Keyword(s):  
Fluorescent Probe ◽  
Hepatoma Cells ◽  
Two Photon ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
In Situ Imaging

A probe for imaging of mitochondrial carboxylesterase and pH has been developed for the visualization of carboxylesterase-mediated acidification in hepatoma cells and hepatic tissues during the administration of antipyretic and anti-inflammatory drugs.

In-Situ Synthesis of Active Pharmaceutical Ingredients Which Content Pyrazole Skeleton

2020 ◽  
Vol 17 (10) ◽  
pp. 743-748
Author(s):  
Sultan Pathan ◽  
Anil Repale ◽  
Girdhar Pal
Keyword(s):  
Aldol Condensation ◽  
Active Pharmaceutical Ingredients ◽  
Reaction Sequence ◽  
One Pot ◽  
Pharmaceutical Ingredients ◽  
One Pot Synthesis ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Work Up

Celecoxib containing pyrazole derivatives were synthesized by path aldol condensation of substituted ketone with trifluoroethyl acetate subsequently by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine. Here, a one-pot synthesis of celecoxib and substituted analogues have been reported which are nonsteroidal anti-inflammatory drugs for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. In order to intermediate work-up, a continuous one-pot synthesis has been developed, performing the entire reaction sequence that results in a shorter time with good yield.

scholarly journals Gelucire BasedIn SituGelling Emulsions: A Potential Carrier for Sustained Stomach Specific Delivery of Gastric Irritant Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Ashwin Saxena ◽  
Arun K. Mishra ◽  
Navneet Verma ◽  
Shiv S. Bhattacharya ◽  
Amitava Ghosh ◽  
...  
Keyword(s):  
Crosslinking Agent ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Albino Rats ◽  
Low Viscosity ◽  
Release Studies ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Non steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed medications to the geriatric patients for the treatment of arthritis and other painful disorders. The major side effects of NSAIDs are related to their effects on the stomach and bowels. The present study concerns assessment of the potential of liquidin situgelling emulsion formulations (emulgels) as patient compliant stomach specific sustained release carrier for the delivery of highly gastric irritant drug, Piroxicam. Emulgels were prepared, without using any emulgent, by mixing different concentrations of molten Gelucire 39/01 with low viscosity sodium alginate solution prepared in deionized water at 50°C. CaCO3was used as buoyancy imparting as well as crosslinking agent. Emulgels so prepared were homogenous, physically stable, and rapidly formed into buoyant gelled mass when exposed to simulated gastric fluid (SGF, pH 1.2). Drug release studies carried out in SGF revealed significant retardation (P<0.05) of Piroxicam release from emulgels compared to conventionalin situgelling formulations prepared without Gelucire 39/01. Pharmacodynamic studies carried out inalbino ratsrevealed significantly increased analgesic/anti-inflammatory response fromin situemulgels compared to conventionalin situgelling formulations. Further,in vivotoxicity studies carried out inalbino ratsrevealed no signs of gastric ulceration upon prolonged dosing.

scholarly journals Development of a Mucoadhesive and an in Situ Gelling Formulation Based on κ-Carrageenan for Application on Oral Mucosa and Esophagus Walls. II. Loading of a Bioactive Hydroalcoholic Extract

Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 153 ◽  
Author(s):  
Barbara Vigani ◽  
Silvia Rossi ◽  
Matteo Gentile ◽  
Giuseppina Sandri ◽  
Maria Bonferoni ◽  
...  
Keyword(s):  
Protective Action ◽  
Extraction Yield ◽  
Dermal Fibroblasts ◽  
Ultrasound Assisted Extraction ◽  
Hydroalcoholic Extract ◽  
Assisted Extraction ◽  
Anti Inflammatory ◽  
In Situ Gelling

The aim of the present work was to load a Hibiscus sabdariffa (HS) hydroalcoholic extract into in situ gelling formulations for the treatment of oral mucositis and esophagitis. Such formulations, selected as the most promising options in a previous work of ours, were composed by κ-carrageenan (κ-CG), a sulfated marine polymer able to gelify in presence of saliva ions, hydroxypropyl cellulose (HPC), used as mucoadhesive agent, and CaCl2, salt able to enhance the interaction κ-CG/saliva ions. HS extract, which is rich in phytochemicals such as polyphenols, polysaccharides and organic acids, was selected due to its antioxidant and anti-inflammatory properties. For HS extraction, three different methodologies (maceration, Ultrasound Assisted Extraction (UAE) and Microwave Assisted Extraction (MAE)) were compared in terms of extraction yield and extract antioxidant activity, revealing that MAE was the best procedure. Rheological and mucoadhesive properties of HS-loaded formulations were investigated. Such formulations were characterized by a low viscosity at 25 °C, guaranteeing an easy administration, a proper in situ gelation behavior and marked elastic and mucoadhesive properties at 37 °C, functional to a protective action towards the damaged mucosa. Finally, the biocompatibility and the proliferative effect of HS-loaded formulations, as well as their antioxidant and anti-inflammatory properties, were proved in vitro on human dermal fibroblasts.

scholarly journals Nonsteroidal anti-inflammatory drugs alter vasa recta diameter via pericytes

2015 ◽  
Vol 309 (7) ◽  
pp. F648-F657 ◽  
Author(s):  
Teresa Kennedy-Lydon ◽  
Carol Crawford ◽  
Scott S. Wildman ◽  
Claire M. Peppiatt-Wildman
Keyword(s):  
Rat Kidney ◽  
Tubular Damage ◽  
Endogenous Production ◽  
Primary Mechanism ◽  
Cyclooxygenase 1 ◽  
Vasa Recta ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Prostacyclin Analog

We have previously shown that vasa recta pericytes are known to dilate vasa recta capillaries in the presence of PGE2 and contract vasa recta capillaries when endogenous production of PGE2 is inhibited by the nonselective nonsteroidal anti-inflammatory drug (NSAID) indomethacin. In the present study, we used a live rat kidney slice model to build on these initial observations and provide novel data that demonstrate that nonselective, cyclooxygenase-1-selective, and cyclooxygenase -2-selective NSAIDs act via medullary pericytes to elicit a reduction of vasa recta diameter. Real-time images of in situ vasa recta were recorded, and vasa recta diameters at pericyte and nonpericyte sites were measured offline. PGE2 and epoprostenol (a prostacyclin analog) evoked dilation of vasa recta specifically at pericyte sites, and PGE2 significantly attenuated pericyte-mediated constriction of vasa recta evoked by both endothelin-1 and ANG II. NSAIDs (indomethacin > SC-560 > celecoxib > meloxicam) evoked significantly greater constriction of vasa recta capillaries at pericyte sites than at nonpericyte sites, and indomethacin significantly attenuated the pericyte-mediated vasodilation of vasa recta evoked by PGE2, epoprostenol, bradykinin, and S-nitroso- N-acetyl-l-penicillamine. Moreover, a reduction in PGE2 was measured using an enzyme immune assay after superfusion of kidney slices with indomethacin. In addition, immunohistochemical techiques were used to demonstrate the population of EP receptors in the medulla. Collectively, these data demonstrate that pericytes are sensitive to changes in PGE2 concentration and may serve as the primary mechanism underlying NSAID-associated renal injury and/or further compound-associated tubular damage.

scholarly journals An In Situ Gelling System for the Local Treatment of Inflammatory Bowel Disease (IBD). The Loading of Maqui (Aristotelia Chilensis) Berry Extract as an Antioxidant and Anti-Inflammatory Agent

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 611 ◽  
Author(s):  
Tenci ◽  
Rossi ◽  
Giannino ◽  
Vigani ◽  
Sandri ◽  
...  
Keyword(s):  
Human Fibroblasts ◽  
Local Treatment ◽  
Antioxidant Properties ◽  
Viscoelastic Behavior ◽  
Distal Colon ◽  
Quantitative Composition ◽  
Anti Inflammatory ◽  
Maqui Berry ◽  
In Situ Gelling

The aim of the present work was the development of an innovative in situ gelling system, to be applied on the mucosa of the distal colon via rectal route. The system consisted of three polymers having different functions: gellan (GG), able to jellify in presence of ions; methylcellulose (MC), a thermosensitive polymer with a gelation temperature close to 50 °C; and hydroxypropylcellulose (HPC), a mucoadhesive polymer. The three polymers were able to act synergistically, increasing the permanence of the vehicle on the mucosa and forming a protective gel layer. A DoE approach, “simplex centroid mixture design,” was used to identify the optimal quantitative composition of the vehicle. The response variables considered were: vehicle viscosity at room temperature; increase in vehicle viscosity on increasing temperature (from room to physiological value) and upon dilution with simulated colonic fluid (SCF); and viscoelastic behavior, thixotropic area, and mucoadhesion properties of the gel formed at 37 °C upon dilution in SCF. The optimized vehicle was loaded with maqui berry extract (MBE), known for its antioxidant and anti-inflammatory properties. MBE loading (0.5% w/w) into the vehicle improved rheological and mucoadhesive properties of the formulation. Both MBE and the optimized vehicle were not cytotoxic towards human fibroblasts and Caco-2 cells. Moreover, the optimized vehicle did not affect MBE antioxidant properties.

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