Polymeric Nanoparticles and Chitosan Gel Loading Ketorolac Tromethamine to Alleviate Pain Associated with Condyloma Acuminata during the Pre- and Post-Ablation

This study describes the preparation and evaluation of two formulations, a hydrogel and a nanostructured system, containing ketorolac tromethamine as an anti-inflammatory agent for the local therapy against the inflammatory process derived from the surgical excision of Condyloma acuminata. Both formulations were physicochemically characterized.In vitrorelease profiles show that the nanoparticles release 92%±2.3 of the total ketorolac tromethamine encapsulated, while the chitosan gel releases 18.6%±0.2. Theex vivo permeation and distribution through human skin were also assayed and was observed how the main amount of ketorolac tromethamine is retained in the epidermis. In vivo studies were accomplished to evaluate the anti-inflammatory efficacy in mice which also involved the histological analysis to confirm thein vivoresults. The nanoparticles present a significantly higher anti-inflammatory efficacy than chitosan gel. The tolerability of developedformulations was assessed by monitoring the biomechanical properties of the skin before and after application of both formulations. No statistical differences in trans-epidermal water loss and skin hydration with respect to the basal values were observed and the formulations exhibited higher anti-inflammatory activity compared to a reference ketotorlac tromethamine solution. Therefore, it can be concluded that both formulations can be proposed as outstanding candidates for offering a local anti-inflammatory therapeutical toolwith potential clinical application.

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Development, Pre-clinical Investigation and Histopathological Evaluation of Metronidazole Loaded Topical Formulation for Treatment of Skin Inflammatory disorders

Drug Delivery Letters ◽

10.2174/2210303110999200821123047 ◽

2020 ◽

Vol 10 ◽

Author(s):

Divya Thakur ◽

Gurpreet Kaur ◽

Sheetu Wadhwa ◽

Ashana Puri

Keyword(s):

Ex Vivo ◽

Clinical Investigation ◽

In Vivo Studies ◽

Tween 20 ◽

Inflammatory Disorders ◽

Rat Paw Edema ◽

Ex Vivo Permeation ◽

Permeation Studies ◽

Anti Inflammatory

Background: Metronidazole (MTZ) is an anti-oxidant and anti-inflammatory agent with beneficial therapeutic properties. The hydrophilic nature of molecule limits its penetration across the skin. Existing commercial formulations have limitations of inadequate drug concentration present at target site, which requires frequent administration and poor patient compliance. Objective: The aim of current study was to develop and evaluate water in oil microemulsion of Metronidazole with higher skin retention for treatment of inflammatory skin disorders. Methods: Pseudo ternary phase diagrams were used in order to select the appropriate ratio of surfactant and co-surfactant and identify the microemulsion area. The selected formulation consisted of Capmul MCM as oil, Tween 20 and Span 20 as surfactant and co-surfactant, respectively, and water. The formulation was characterized and evaluated for stability, Ex vivo permeation studies and in vivo anti-inflammatory effect (carrageenan induced rat paw edema, air pouch model), anti-psoriatic activity (mouse-tail test). Results: The particle size analyses revealed average diameter and polydispersity index of selected formulation to be 16 nm and 0.373, respectively. The results of ex vivo permeation studies showed statistically higher mean cumulative amount of MTZ retained in rat skin from microemulsion i.e. 21.90 ± 1.92 μg/cm2 which was 6.65 times higher as compared to Marketed gel (Metrogyl gel®) with 3.29 ± 0.11 μg/cm2 (p<0.05). The results of in vivo studies suggested the microemulsion based formulation of MTZ to be similar in efficacy to Metrogyl gel®. Conclusion: Research suggests efficacy of the developed MTZ loaded microemulsion in treatment of chronic skin inflammatory disorders.

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Anti-Inflammatory Potential of Daturaolone from Datura innoxia Mill.: In Silico, In Vitro and In Vivo Studies

Pharmaceuticals ◽

10.3390/ph14121248 ◽

2021 ◽

Vol 14 (12) ◽

pp. 1248

Author(s):

Muhammad Waleed Baig ◽

Humaira Fatima ◽

Nosheen Akhtar ◽

Hidayat Hussain ◽

Mohammad K. Okla ◽

...

Keyword(s):

In Silico ◽

Therapeutic Potential ◽

In Vivo Studies ◽

Metabolic Reaction ◽

Datura Innoxia ◽

In Vivo Models ◽

Immobility Time ◽

Anti Inflammatory

Exploration of leads with therapeutic potential in inflammatory disorders is worth pursuing. In line with this, the isolated natural compound daturaolone from Datura innoxia Mill. was evaluated for its anti-inflammatory potential using in silico, in vitro and in vivo models. Daturaolone follows Lipinski’s drug-likeliness rule with a score of 0.33. Absorption, distribution, metabolism, excretion and toxicity prediction show strong plasma protein binding; gastrointestinal absorption (Caco-2 cells permeability = 34.6 nm/s); no blood–brain barrier penetration; CYP1A2, CYP2C19 and CYP3A4 metabolism; a major metabolic reaction, being aliphatic hydroxylation; no hERG inhibition; and non-carcinogenicity. Predicted molecular targets were mainly inflammatory mediators. Molecular docking depicted H-bonding interaction with nuclear factor kappa beta subunit (NF-κB), cyclooxygenase-2, 5-lipoxygenase, phospholipase A2, serotonin transporter, dopamine receptor D1 and 5-hydroxy tryptamine. Its cytotoxicity (IC50) value in normal lymphocytes was >20 µg/mL as compared to cancer cells (Huh7.5; 17.32 ± 1.43 µg/mL). Daturaolone significantly inhibited NF-κB and nitric oxide production with IC50 values of 1.2 ± 0.8 and 4.51 ± 0.92 µg/mL, respectively. It significantly reduced inflammatory paw edema (81.73 ± 3.16%), heat-induced pain (89.47 ± 9.01% antinociception) and stress-induced depression (68 ± 9.22 s immobility time in tail suspension test). This work suggests a possible anti-inflammatory role of daturaolone; however, detailed mechanistic studies are still necessary to corroborate and extrapolate the findings.

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Su1819 – New Class of Anti-Inflammatory Therapeutics Based on Gold (III) Complexes in Intestinal Inflammation – Proof of Concept Based on in Vitro and in Vivo Studies

Gastroenterology ◽

10.1016/s0016-5085(19)38456-2 ◽

2019 ◽

Vol 156 (6) ◽

pp. S-623

Author(s):

Julia B. Krajewska ◽

Jakub Wlodarczyk ◽

Przemyslaw Taciak ◽

Remigiusz Szczepaniak ◽

Jakub Fichna

Keyword(s):

Intestinal Inflammation ◽

In Vivo Studies ◽

Proof Of Concept ◽

New Class ◽

Anti Inflammatory

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Evaluation of Anti-inflammatory and Anti-nociceptive Potentials of Andrographolide and Forskolin: In vivo Studies

Journal of Biologically Active Products from Nature ◽

10.1080/22311866.2018.1526650 ◽

2018 ◽

Vol 8 (5) ◽

pp. 326-334 ◽

Cited By ~ 1

Author(s):

Velpula Suresh ◽

Godugu Deepika ◽

Veeresh Bantal ◽

Sashidhar Rao Beedu ◽

Karuna Rupula

Keyword(s):

In Vivo Studies ◽

Anti Inflammatory

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Anti-inflammatory effect ofRhus vernivifluaStokes by suppression of iNOS-mediated Akt and ERK pathways: in-vitro and in-vivo studies

Journal of Pharmacy and Pharmacology ◽

10.1111/j.2042-7158.2011.01251.x ◽

2011 ◽

Vol 63 (5) ◽

pp. 679-687 ◽

Cited By ~ 15

Author(s):

Chang Hwa Jung ◽

Jeong-Hyun Kim ◽

Ji Hye Kim ◽

Joo Hee Chung ◽

Han-Seok Choi ◽

...

Keyword(s):

In Vivo Studies ◽

Anti Inflammatory ◽

Inflammatory Effect

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Trajectory-Based Tissue Engineering for Cartilage Repair: Correlation Between Maturation Rate and Integration Capacity

Volume 1A: Abdominal Aortic Aneurysms; Active and Reactive Soft Matter; Atherosclerosis; BioFluid Mechanics; Education; Biotransport Phenomena; Bone, Joint and Spine Mechanics; Brain Injury; Cardiac Mechanics; Cardiovascular Devices, Fluids and Imaging; Cartilage and Disc Mechanics; Cell and Tissue Engineering; Cerebral Aneurysms; Computational Biofluid Dynamics; Device Design, Human Dynamics, and Rehabilitation; Drug Delivery and Disease Treatment; Engineered Cellular Environments ◽

10.1115/sbc2013-14572 ◽

2013 ◽

Author(s):

Matthew B. Fisher ◽

Nicole Söegaard ◽

David R. Steinberg ◽

Robert L. Mauck

Keyword(s):

Tissue Engineering ◽

Time Course ◽

Biomechanical Properties ◽

Time Dependent ◽

In Vivo Studies ◽

Surgical Approaches ◽

General Hypothesis ◽

Vitro Assay

Given the limitations of current surgical approaches to treat articular cartilage injuries, tissue engineering (TE) approaches have been aggressively pursued over the past two decades. Although biochemical and biomechanical properties on the order of the native tissue have been achieved (1–5), several in-vitro and in-vivo studies indicate that increased tissue maturity may limit the ability of engineered constructs to remodel and integrate with surrounding cartilage, although results are highly variable (2, 6–8). Thus, “static” measures of construct maturity (e.g. compressive modulus) upon implantation may not be the best indicators of in-vivo success, which likely requires implanted TE constructs to mature, remodel, and integrate with the host over time to achieve optimal results. We recently introduced the concept of “trajectory-based” tissue engineering (TB-TE), which is based on the general hypothesis that time-dependent increases in construct maturation in-vitro prior to implantation (i.e. positive rates) may provide a better predictor of in-vivo success (9). As a first step in evaluating this concept, in the current study we hypothesized that time-dependent increases in equilibrium modulus (a metric of growth) would be correlated to ability of constructs to integrate to cartilage using an in-vitro assay. To test this hypothesis, the current objective was to determine and model the time course of maturation of TE constructs during in-vitro culture and to assess the ability of these constructs to integrate to cartilage at various points during their maturation.

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In Vitro and in Vivo Studies on Anti-Inflammatory Effects of Traditional Okinawan Vegetable Methanol Extracts

ACS Omega ◽

10.1021/acsomega.9b02178 ◽

2019 ◽

Vol 4 (13) ◽

pp. 15660-15664

Author(s):

Junichi Nagata ◽

Hiroyuki Yokodera ◽

Goki Maeda

Keyword(s):

In Vivo Studies ◽

Methanol Extracts ◽

Anti Inflammatory

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Evaluation of the Biocompatibility of CS-Graphene Oxide Compounds In Vivo

International Journal of Molecular Sciences ◽

10.3390/ijms20071572 ◽

2019 ◽

Vol 20 (7) ◽

pp. 1572 ◽

Cited By ~ 4

Author(s):

Diego López Tenorio ◽

Carlos Valencia ◽

Cesar Valencia ◽

Fabio Zuluaga ◽

Mayra Valencia ◽

...

Keyword(s):

Graphene Oxide ◽

Bone Regeneration ◽

Wistar Rats ◽

Biomechanical Properties ◽

Cellular Membrane ◽

In Vivo Studies ◽

New Bone Formation ◽

Critical Size Defects ◽

Tissue Recovery

In the last few years, graphene oxide (GO) has gained considerable importance in scaffold preparation for tissue engineering due to the presence of functional groups that allow the interaction between the extracellular matrix and the components of the cellular membrane. The interaction between GO and chitosan (CS) can not only improve the biomechanical properties of the scaffold but also generate a synergistic effect, facilitating tissue recovery. In vivo studies on GO are scarce; therefore, biocompatibility tests on CS-GO scaffolds and bone regeneration experiments on critical size defects were carried out on Wistar rats. Scaffolds made of CS, CS-GO 0.5%, and CS-GO 1% were prepared and implanted on Wistar rats cranial bones for three months. Scaffold samples were analyzed through histochemistry and scanning electron microscopy. The analysis performed showed reabsorption of the material by phagocytic activity and new bone formation. The CS-GO 0.5% formulation gave the best performance in bone regeneration, with excellent biocompatibility. These results show the potential of this compound for tissue regeneration opening and medical applications.

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