scholarly journals Development of Ketoprofen-p-Aminobenzoic Acid Co-Crystal: Formulation, Characterization, Optimization and Evaluation

2021 ◽  
Author(s):  
Meenakshi Bhatia ◽  
Ashwani Kumar ◽  
Vikas Kumar ◽  
Sunita Devi
Keyword(s):  
Experimental Design ◽  
Drug Release ◽  
Wistar Rats ◽  
Inflammatory Activity ◽  
Aminobenzoic Acid ◽  
Standard Drug ◽  
Enhanced Solubility ◽  
Anti Inflammatory

Abstract Co-crystal is a promising class of solids that may provide options for improved properties. In the present study, ketoprofen- p-aminobenzoic acid (KP-PABA) co-crystal were prepared to sought enhanced solubility and dissolution rate of drug. KP-PABA co-crystal were prepared by solvent evaporation technique employing central composite experimental design, selecting independent variables as concentration of drug and PABA whereas dependent variables were assumed to be solubility and % drug release. The optimized batch as suggested by the experimental design was characterized by FTIR, DSC, XRD, SEM and NMR studies and further, evaluated for in-vitro and in-vivo anti-inflammatory and analgesic activities. The solubility and % drug release of different batches of co-crystal was found to be between 34.20-60.11 µg/ml and 68.11–93.45%, respectively. Co-crystal containing ketoprofen and PABA in molar ratio (1:1) was found to be optimized formulation batch. Physical characterization by X-ray diffraction spectra and differential scanning calorimetric studies confirms the crystallinity of prepared co-crystal. The half maximal inhibitory concentration (IC50) values for in-vitro anti-inflammatory activity comes out to be 34.04 µM for ketoprofen and 4.373µM for optimized formulation, exhibiting almost 8-fold amplification indicating higher anti-inflammatory effect of optimized batch as compared to drug ketoprofen. The results of in-vivo anti-inflammatory activity carried out by rat paw edema method revealed that the optimized batch of co-crystal preparation provided a significant % inhibition in paw volume in contrast to standard drug in wistar rats. In this case, a crystalline molecular complex of drug Ketoprofen, that demonstrate poor aqueous solubility, with p-aminobenzoic acid was recognized that further set out an improvement in solubility and also in anti-inflammatory activity of the drug in wistar rats.

scholarly journals Development and Evaluation of Novel Self-Nanoemulsifying Drug Delivery Systems Based on a Homolipid from Capra hircus and Its Admixtures with Melon Oil for the Delivery of Indomethacin

2014 ◽  
Vol 2014 ◽  
pp. 1-9
Author(s):  
Nicholas C. Obitte ◽  
Kenneth C. Ofokansi ◽  
Franklin C. Kenechukwu
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Tween 80 ◽  
Delivery Systems ◽  
Inflammatory Activity ◽  
Capra Hircus ◽  
Anti Inflammatory

In this study, goat fat (Capra hircus) and melon oil were extracted and used to formulate self-nanoemulsifying drug delivery systems (SNEDDS) based on either goat fat alone or its admixture with melon oil by employing escalating ratios of oil(s), surfactant blend (1 : 1 Tween 60 and Tween 80), and cosurfactant (Span 85), with or without carbosil, a glidant, for the delivery of indomethacin. The formulations were encapsulated in hard gelatin capsules and then assessed using isotropicity test, aqueous dilution stability and precipitation propensity, absolute drug content, emulsification time, in vitro drug release, and anti-inflammatory activity. The SNEDDS exhibited low precipitation propensity and excellent stability on copious dilution, as well as high drug release in vitro and in vivo. The inhibition produced by the SNEDDS was comparable to that of indomethacin injection (positive control) for much of the 5 h test period, indicating a high degree of bioavailability of the administered SNEDDS. The absolute drug contents and emulsification times fell within narrow limits. This study has shown that a 1 : 1 ratio of melon oil and goat fat could confer favourable properties with respect to drug release and anti-inflammatory activity on SNEDDS for the delivery of indomethacin, thus encouraging further development of the formulations.

scholarly journals Design and Synthesis of 2-Mercapto Benzoxazole coupled Benzyl Triazoles as Anti-inflammatory Agents Targeting COX-2 Enzyme

2020 ◽  
Vol 32 (12) ◽  
pp. 3209-3218
Author(s):  
K. Praveen Kumar ◽  
Y. Prashanthi ◽  
G. Rambabu ◽  
Md. Ataur Rahman ◽  
J.S. Yadav
Keyword(s):  
Chemical Space ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Design Synthesis ◽  
Standard Drug ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Anti Inflammatory

In this study, we report the design, synthesis and the biological evaluation of 19 analogues of 2-mercapto benzoxazole coupled benzyl triazoles (BOTs) based on analysis of the binding site and literature of chemical space. These BOTs were evaluated both in vitro and in vivo for their anti-inflammatory activity. Eleven compounds showed less than 10 μM in vitro COX-2 enzyme activities. The most potent analogue among the BOT analogues were BOT15, BOT3 and BOT19 with IC50 3.40 μM, 4.50 μM and 4.57 μM respectively against COX-2. The in vivo anti-inflammatory activity of two BOTs has significantly higher than that of standard drug, ibuprofen. 2-Mercapto benzoxazole coupled benzyl triazoles (BOTs) were also tested for their antioxidant capacity and proved to be an as active scavenger, better than ascorbic acid.

scholarly journals In-vitro and in-vivo anti-inflammatory activity of Plumeria indica Linn flowers

2020 ◽  
Vol 10 (5) ◽  
pp. 168-174
Author(s):  
Narendraa Yadav ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Side Effects ◽  
Dose Level ◽  
Ethanolic Extract ◽  
Inflammatory Activity ◽  
Phytochemical Analysis ◽  
Test Protocol ◽  
Standard Drug ◽  
Anti Inflammatory

Inflammation is a reaction of a living vascularised tissue to an injury. Conventional or synthetic drugs used in the treatment of inflammatory diseases are inadequate, it sometimes have serious side effects. So, number of herbal medicines is recommended for the treatment of inflammation that has no side effects. Hence our study focused to investigate the physicochemical, qualitative phytochemical analysis of bioactive compounds and In-vitro and In-vivo anti-inflammatory activity of Plumeria indica Linn (P. Indica) flowers extract which has boundless medicinal properties. The physicochemical evaluations carried out in terms of loss on drying, ash value, extractive values and acid insoluble ash value ect. Qualitative analysis of various phytochemical constituents was determined by the well-known test protocol available in the literature. The aqueous and ethanolic extract of P. Indica flowers was screened for in-vivo anti-inflammatory activity by carrageenan induced paw edema in rat model and in-vitro anti-inflammatory activity by human red blood cell membrane stabilization method. Phytochemical analysis revealed the presence of phenols, flavonoids, tannins, saponins, alkaloids ect. Ethanolic extract showed best in vitro anti-inflammatory activity was screened for in vivo anti-inflammatory activity at the dose level of 250 and 500mg/kg. Indomethacin at the dose level of 10 mg/kg was used as reference standard drug. Both the extracts showed a dose dependent anti-inflammatory potential which provide scientific basis for the traditional claims of P. Indica flowers as an anti-inflammatory drug. Keywords: Plumeria indica Linn, Anti-inflammatory activity, Carrageenan, Human red blood cells membrane

scholarly journals In vitro and In vivo Anti-inflammatory Activities of Mesua ferrea Linn

2018 ◽  
Vol 10 (03) ◽  
Author(s):  
Krishna Chaithanya K ◽  
Gopalakrishnan V K ◽  
ZenebeHagos . ◽  
Nagaraju B ◽  
Kamalakararao K ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Wistar Rats ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Bark Extract ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Anti Inflammatory

Objective: Mesuaferrea L is a medicinal plant belongs to the family Clusiace, it is extensively used in folk medicine for treatment of chronic inflammatory diseases.The present study was aimed to evaluate in vitro and in vivo anti-inflammatory activity of M. ferrea L. Methods: The in vitro anti-inflammatory activities such as nitric oxide, PGE2, pro-inflammatory cytokines (TNF-α and IL-1β) were studied in RAW 264.7 cells and in vivo studies were carried out on carrageenan -induced inflammation in Wistar rats. The sequentially extracted M. ferreaL bark extracts (MFBHE, MFBEE, and MFBME) exhibited inhibitory effects on pro-inflammatory mediators such as nitric oxide, prostaglandin E2, tumour necrosis factorαandinterleukin-1βproduction in concentration dependent manner in LPS induced RAW 264.7 cells andCarrageenan induced paw oedema in Wistar rats. Conclusion: The result of the present study indicated that M. ferrea L ethyl acetate bark extract exhibited significant in vitroand in vivoanti-inflammatory activity.

scholarly journals NARINGENIN-LOADED D-Α-TOCOPHERYL POLYETHYLENE GLYCOL SUCCINATE 1000 POLYMERIC NANOSUSPENSION: AN IN VITRO AND IN VIVO ANTI-INFLAMMATORY ACTIVITY

2019 ◽  
pp. 459-463
Author(s):  
SUMATHI RAJAMANI ◽  
GOBINATH KALYANA SUNDARAM ◽  
TAMIZHARASI SENGODAN ◽  
SIVAKUMAR THANGAVELU ◽  
NIKHITHA K SHANMUKHAN ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
Pharmacological Action ◽  
Inflammatory Activity ◽  
In Vivo Studies ◽  
Glycol Succinate ◽  
Albino Rats ◽  
Standard Drug ◽  
Anti Inflammatory

Objective: Naringenin (NAR) a flavonoid, exhibits extensive pharmacological action, fails to attain a significance in application due to low aqueous solubility (~ 0.214 mg/mL) which results in low bioavailability (5.8%). Nanosuspension of NAR (NARNS) was prepared in our previous studies using high-pressure homogenization employing various polymers. All these formulations were characterized and as a continuation of our work formulations was further evaluated for their anti-inflammatory activity by in vitro and in vivo methods. Methods: Denaturation of protein method and membrane stabilization methods was chosen for in vitro evaluation. In vivo studies performed were acute inflammatory studies (carrageenan-induced paw edema) and chronic inflammatory studies (cotton pellet granuloma) on Wistar albino rats. Results: The studies demonstrated that the NAR and NARNS at a dose of 50mg/kg P.O. have a potent activity compared to the standard drug diclofenac. Conclusion: The percentage of protection against inflammation exhibited by NARNS was highly significant compared to NAR.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF CURCUMIN AND CAPSAICIN AUGMENTED IN COMBINATION

2017 ◽  
Vol 9 (6) ◽  
pp. 145
Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp
Keyword(s):  
Acetic Acid ◽  
Protective Effect ◽  
Vascular Permeability ◽  
Diclofenac Sodium ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
The Individual

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.

Anti-Inflammatory Activity in Vitro and in Vivo of the Protein Farnesyltransferase Inhibitor Tipifarnib

2005 ◽  
Vol 317 (1) ◽  
pp. 53-60 ◽  
Author(s):  
Xiaohua Xue ◽  
Kuei-Tai A. Lai ◽  
Jing-Feng Huang ◽  
Yin Gu ◽  
Lars Karlsson ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Farnesyltransferase Inhibitor ◽  
Protein Farnesyltransferase ◽  
Anti Inflammatory
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