Tail-flick Method Research Articles

Unveiling the phytochemical profile, antioxidant and antibacterial activities, acute toxicity insight and analgesic effect of Retama dasycarpa stems: An unexplored endemic plant from Morocco

Retama dasycarpa is an endemic shrubby leguminous plant of Morocco used in traditional folk medicine. The plant has never been studied for either its phytochemical or pharmacological properties. This study represents the first investigation of the phytochemical profile as well as the antioxidant, the antibacterial, the analgesic effects and the oral acute toxicity of Retama dasycarpa. Watery and hydromethanolic stems plant macerates have been investigated. Secondary metabolites quantitative analysis was achieved through spectrophotometric techniques. Antioxidant effect was explored through DPPH, ABTS and FRAP trials. Antibacterial activity was investigated using a micro-plates dilution assay. Analgesic activity was explored through acetic acid-induced writhing and tail-flick methods. Acute oral toxicity was investigated on mice. Phytochemical analysis was achieved through UHPLC connected to diode array and mass spectrometry detectors.The obtained results showed significant contents in total phenolics, flavonoids and tannins in both extracts especially the hydromethanolic extract whose contents were slighlty higher than the aqueous one resulting in a remarkable antioxidant activity. Compared to the aqueous extract, the H2O:MeOH (1:1) one showed notable antibacterial activity against the tested strains. The acute toxicity in mice revealed the non-toxicity of the extracts along with a promised starting material of central and peripheral analgesics. The UHPLC analysis revealed the presence of several bioactive phytochemicals pertaining to phenolic acids, flavonols, flavones and isoflavones.The obtained results demonstrate the richness of this endemic and unexplored plant in terms of bioactive compounds and their associated activities, making it a promising source of pharmacological ingredients.

Spectral characterization, analgesic, and anti-inflammatory effects of ethanolic extract of Calotropis procera leaf and dry latex from Jazan, Kingdom of Saudi Arabia

Traditional healers have used the shrub Calotropis procera (CP) for many years for various therapies. The present study investigated the bioactive constituents of ethanolic extract of CP leaf and dried latex using gas chromatography-mass spectrometry and Fourier transforms infrared spectroscopy. The identification and characterization of the compounds were confirmed by examining the constituents' mass spectrum fragmentations and FT-IR spectra and comparing the results with those in the literature. The tail-flick method was used to investigate the analgesic properties of the extract and its anti-inflammatory activities using a rat model of formalin-induced oedema. Acute oral toxicity in rats was studied per OECD recommendations. Twenty male rats were divided into four groups and received an ethanolic extract of the leaves and dried milky sap of CP (200 mg/Kg) in groups 1, 2, and 3. Group 4 rats were administered aspirin 50 mg/kg as a positive control. The CP dried latex extract has the highest content of lupeol and its acetate derivative compared to its leaf extract. The CP dried latex extract inhibited inflammation more significantly than the ethanolic leaf extract and the drug indomethacin at a higher dosage (200 mg/kg). The ethanolic extracts showed analgesia comparable to aspirin. It suggests that fatty acids and their esters, particularly ethyl linoleate (8.96%), ethyl palmitate (7.99%), ethyl linoleate (6.98%), and palmitic acid (5.18%), may be valuable biomarkers for characterizing leaf and latex samples and describing the medicinal potential of CP.

Effect of electroacupuncture at "Neiguan" (PC6) on pain and brain orexin 1 receptor in mice with inflammatory pain.

To observe the effect of electroacupuncture (EA) at "Neiguan" (PC6) on pain response in mice injected with complete Freund's adjuvant (CFA) in the hind paw, so as to investigate the mechanism of orexin 1 receptor (OX1R) -endogenous cannabinoid 1 receptor (CB1R) pathway in acupuncture analgesia. A total of 48 male C57BL/6 mice were used in the present study. In the first part of this study, 18 mice were randomized into control, model and EA groups, with 6 mice in each group. In the second part of this study, 30 mice were randomized into control, model, EA, EA+Naloxone, EA+OX1R antagonist (SB33486) groups, with 6 mice in each group. Inflammatory pain model was established by subcutaneous injection of 20 μL CFA solution in the left hind paw. EA (2 Hz, 2 mA ) was applied to bilateral PC6 for 20 min, once a day for 5 consecutive days. The mice in the EA+Naloxone and EA+SB33486 groups were intraperitoneally injected with naloxone (10 mg/kg) or SB33486 (15 mg/kg) 15 min before EA intervention on day 5, respectively. Tail-flick method and Von Frey method were used to detect the thermal pain threshold and mechanical pain threshold of mice. Quantitative real-time PCR was used to detect the expression level of β-endorphin mRNA in periaqueductal gray (PAG) of mice. The expression of OX1R positive cells in the lateral hypothalamic area (LH) and CB1R positive cells in the ventrolateral periaqueductal gray (vlPAG) were detected by immunofluorescence. Compared with the control group, the thermal pain threshold and mechanical pain threshold of the model group were decreased (P<0.001), the expression level of β-endorphin mRNA in PAG was decreased (P<0.001), and the numbers of OX1R positive cells in LH and CB1R positive cells in vlPAG were decreased (P<0.05, P<0.001). Compared with the model group, the thermal pain threshold and mechanical pain threshold of the EA group were significantly increased (P<0.001), and the numbers of OX1R positive cells in LH and CB1R positive cells in vlPAG were increased (P<0.01, P<0.001). Compared with the EA group, the mechanical pain threshold in the EA+SB33486 group was significantly decreased (P<0.01), but there was no significant difference in the mechanical pain threshold between the EA+Naloxone group and EA group, and the numbers of OX1R positive neurons in LH and CB1R positive neurons in vlPAG were decreased in the EA+SB33486 group (P<0.001). EA at PC6 can achieve analgesic effect on CFA mice by activating the OX1R-CB1R pathway in the brain, and this effect is opioid-independent.

Screening for Antinociceptive Action of Gastroretentive Drug delivery System of Tramadol hydrochloride in Mice

The floating drug delivery system is to avoid the problem of drug waste and to limit the frequency of administration. Here the drug Tramadol is being centrally acting opioid analgesic can be formulated as sustained release formulation by adopting the method gastroretentive drug delivery system through effervescent floating drug delivery system with different grades of polymer Hyperomellose. The Pharmacological activity on Mice by both Hot Plate and Tail Flick Methods also suggest that when the Tramadol Hcl increased with its dosage form shows significant Analgesic Activity in animals which shows a spontaneous dose dependent increase in Analgesic activity was found it shows that the dosage form deserve for designed method of gastroretentive drug delivery system.

Evaluation of analgesic and anti-inflammatory activities of ethanolic fruit extract of Terminalia chebula

Analgesic and Anti-inflammatory activities of ethanolic fruit extract of Terminalia chebula was evaluated using tail-flick method, eddy’s hot plate method, acetic acid induced writhing responses and in-vivo anti-inflammatory property was determined using carrageenan rat paw edema. The ethanolic fruit extract of Terminalia chebula at different concentrations significantly inhibited the nociception in comparision with different standard drugs that showed anti-nociception. The test extract also reduced the edema induced in rats using carrageenan paw edema method as compared with the standard drug Diclofenac sodium 10mg/kg. The results obtained in this research study found to be very significant when compared to standard reference drug.

Agomelatine alleviates pain-related behaviour in ovariectomized rats

Aim: Menopause is a physiological process that results in the cessation of ovarian follicle activity. Research suggests that postmenopausal women may experience changes in pain sensitivity. Ovariectomized (Ovx) rats are commonly used to mimic postmenopausal pain symptoms in research. Agomelatine is a unique antidepressant that acts as both a melatonergic receptor agonist and a 5-HT2C receptor antagonist. Preclinical studies have suggested potential analgesic effects associated with Agomelatine. This study aims to investigate the influence of agomelatine on pain behavior in Ovx rats. Materials and Methods: Forty female Sprague Dawley rats were divided into four groups: Sham, Ovx, Ago20 and Ago40. The Ovx, Ago20 and Ago40 groups underwent bilateral ovariectomy, while the Sham group underwent all surgical procedures except ovarian ligation. After four months, the Sham and Ovx groups received vehicle, while the Ago20 (20mg/kg) and Ago40 (40mg/kg) groups received agomelatine by oral gavage for two months. Pain sensitivity assessments were conducted using electronic von Frey, hot plate, tail flick, and tail immersion methods after the final drug administration. Results: In the Ovx group, there was an increase in pain sensitivity observed in the hot plate, electronic von Frey, tail flick, and tail immersion tests (p &lt; 0.05). Agomelatine treatment significantly reduced the heightened nociceptive response (p &lt; 0.05). Conclusion: Agomelatine effectively attenuates the increased sensitivity to pain observed in Ovx rats.

Characterization of microencapsulated Saga Leaves Extract (Abrus precatorius L.) and Analgetic Activity Tests in Male Mice (Mus musculus)

Background: Saga leaves are one of the plants that have analgesic activity. Saga leaves contain phenol compounds, flavonoids, tannins, alkaloids, and saponins. Phenol has instability with oxygen, light, and high temperatures. Therefore, the microencapsulation process is necessary. Microcapsule characterization in this study included encapsulation efficiency, particle size, distribution value and morphology. Objective: This research was to determine the characterization of microcapsules and the analgesic activity of saga leaf extract microcapsules in male mice. Methods: The microencapsulation process conducted in this study was carried out using the spray drying method. Saga leaf extract was coated with the coating material in the ratio of 1:20. Several ratios of maltodextrin (MD) and soy protein isolate (SPI) (100%:0%); (75%%:25); (50%:50%); (25%:75%) were applied as the coating material. The encapsulation efficiency was determined by comparing the total phenol content of the extract and microcapsule. Particle size and distribution values were tested using a particle size analyzer. Microcapsule morphology was seen using scanning electron microscopy. Analgesic activity test using the tail-flick method with mice as test animals. Data analysis in this study used one-way ANOVA. Results: The encapsulation efficiency obtained was 31.40-80.29%. The particle size obtained in the microcosm was 17.70-30.90 µm. The distribution value obtained was 1.42-2.45. The morphology of the microcapsule obtained was round and had wrinkles. The analgesic activity obtained in this study resulted in significantly different pain inhibition values before and after microencapsulation. Conclusion: The characteristics of microcapsule preparations are well-known, and the analgesic activity of various microcapsules was 42.43-57.15%.

Experimental evaluation of analgesic activity of Naga Parpam: An Siddha formulation

Background : Prolonged usage of NSAIDs and corticosteroids was associated with serious side effects. Siddha is an ancient system of medicine, promotes the utilization of herbal anad elemental formulations. Interestingly, certain elements considered toxic in modern medicine, such as Arsenic (As), Cadmium (Cd), Mercury (Hg), Iron (Fe), Silver (Ag), Gold (Au), etc., have been employed in Siddha herbo mineral formulation for the treatment of illness, a practice that dates back to ancient times. Introduction Pain is a widely recognized indicator of poor health, the analgesic medications are employed to alleviate it. In Siddha classics, pain is considered a separate disease called Soolai. Naga Parpam is one of the herbo metal preparations with analgesic potential but no scientific evaluation there. Aim: To evaluate the analgesic activity of Naga parpam in experimental rats using Tail immersion method. Materials and methods : After obtaining permission from the IAEC, the animals were separated into 5 groups of 6 animals Each Group 1 (control) received ghee orally, and Group 2 (standard) received Pentazocine in dose 10 mg/kg intraperitoneally. The test drug Naga parpam was mixed with the adjuvant Ghee and administrated per oral route to three groups (Group 3,4,5), Group 3 (test) received Naga Parpam in low dose 6 mg/kg, Group 4 (test) received mid dose 12 mg/kg, Group 5 (test) received high dose – 24 mg/kg ). Statistical analysis : One-way ANOVA followed by the Dunnett test P &lt; 0.05 was considered to be significant. Results : The test drug Naga parpam has significant analgesic activity in the tail flick method (P &lt;0.01) by increasing the reaction time of the rats. Conclusion : The present study indicates that the test drug Naga parpam possesses significant central analgesic activity in the tail flick method.

Exploring the Potential of Crude Methanolic Leaf Extract of Gossypium Hirsutum in Malaria Treatment, Pain Relief, and Inflammation Reduction

The increasing resistance of Plasmodium falciparum to standard anti-malarial drugs has led to a search for new compounds with antimalarial properties. Throughout history, various plants have been used for the treatment of malaria. Gossypium hirsutum, a plant commonly used in Ondo state for malaria treatment, was the focus of this study. The crude extracts of Gossypium hirsutum were evaluated for their anti-plasmodial, analgesic, and anti-inflammatory properties. To assess the anti-plasmodial effect, Plasmodium berghei was inoculated into 12 mice divided into four groups, with three mice in each group. Groups 1 and 2 were treated with doses of 200mg/kg.bw and 400mg/kg.bw of the crude plant extract, respectively. Group 3 received 5mg/kg.bw of chloroquine phosphate, while group 4 received normal saline. The analgesic effects were evaluated using the Eddy's hot plate method and the Tail flick method in mice. The anti- inflammatory effect was assessed using egg albumin-induced paw edema in rats. The crude methanolic extracts of Gossypium hirsutum demonstrated activity against Plasmodium parasites and a significant anti-inflammatory effect, suppressing paw edema by 49.7%. Animals administered with the extracts showed increased resptime to thermal pain induction in both the hot plate and tail flick methods, similar to the effect oonse bserved with the standard drug. The crude plant extract reduced parasitemia in mice by 79.2%, accompanied by a slight but statistically insignificant decrease in packed cell volume (PCV) and the weight of treated animals. Overall, the crude extract of Gossypium hirsutum exhibited effectiveness in managing malaria, along with a moderate analgesic and anti-inflammatory potential. These findings suggest that the plant contains active compounds with promising antimalarial effects, which could be further isolated and studied.

Evaluation of Analgesic activity of Schiff base Coumarins with metal complex

Purpose: The metal complexes of schiff bases have essential task during the field of chemistry and possess diverse pharmacological activities. Coumarin containing synthesized derivatives or plant extract may show analgesic effects Objective: Evaluating the analgesic activity of schiff base coumarins with metal complex. Materials and Methods: The study was conducted using Wister rats (150-250g) in both central and peripheral screening models of analgesics such as hot plate method, tail flick method (central) and writhing test (peripheral). The rats were pre administered with different derivatives of coumarins such as copper complex of schiff base of 2,5-dimethoxybenzaldehyde (Compound I), copper complex of schiff base of 4-dimethylaminobenzaldehyde (Compound II) and copper complex of the schiff base of 3-nitrobenzaldehyde (Compound III) for 14 days orally at the dose of 200mg/kg. Body weight, food and water consumption were continuously noted in chronic model. After the fourteen days rats were subjected to different screening models of pain and noted the reaction time. Gastro intestinal (GI) histopathological study was carried out to evaluate the GI toxicity. Results: Pretreatment with the different coumarin derivatives showed analgesic effect by increasing the reaction time to pain. In hot plate method, Compound II and III exhibited significant analgesic activity compared to Compound I whereas all three compounds showed significant increase in reaction time for tail flick method. In writhing test all compounds showed significant activity by reducing the pain perception induced by acetic acid. In histopathological study all compounds showed protective effect by reducing the ulceration and congestion of gastric mucosa. Conclusion: The screening model results and histopathological data evidently substantiate the analgesic effect of schiff base coumarins with metal complex.

Piperidine Derivatives: Synthesis, Pharmacological Evaluation and Insilico Approach of Novel Potential Analgesics in 4-amino Methyl Piperidine Series

Piperidine is an essential moiety of morphine, responsible for the analgesic activity. Among number of other analgesic targets, µ-opioid receptor is still the most focused and therapeutically important in the management of pain. In this study, a series of novel derivatives of 4 amino methyl piperidine were synthesized and explored for analgesic potential against mu opioid receptor. Their structures were elucidated by FT-IR, 1H NMR, and LC-MS followed by in vivo analgesic evaluation by tail-flick method and writhing test. Among all derivatives, HN58 showed excellent analgesic activity (100% inhibition) in writhing test. Furthermore, reduction of HN58 analgesic effect by naloxone suggests its involvement with µ-OR. Molecular docking approach was also utilized to compare the analgesic potential of synthesized derivatives in order to find potent µ-OR inhibitors, we designed five piperidine derivatives with analgesic activity. We have elucidated the binding affinities and binding modes of these piperidine derivatives including standard molecules Morphine, Fentanyl Pethidine and DAMGO revealed a well-known µ-O inhibitor (having binding affinity ranges from −8.13 to −13.37 kcal/mol). All novel derivatives exhibited the remarkable binding score and encapsulated in the binding pocket of transmembraneous helices engaged by the residues Q124, W133, I144, D147, Y148, M151, V236, I296, H297, W318, I322, and Y236. All derivatives revealed excellent binding scores and interaction mechanism as compared to morphine, pethidine, and fentanyl respectively.

Anti-inflammatory and Analgesic Activity of Cleome brachycarpa Ethanolic Extract in Lower Mammals and Effects on Blood and Liver Enzymes

Background: Cleome brachycarpa, magical species full of phytochemicals, has magical medicinal properties and should be evaluated extensively. Objectives: We evaluated the anti-inflammatory and analgesic activity of Cleome brachycarpa and the effect of its extract on various hematological parameters, cholesterol levels, and liver enzymes to ensure the safe use of this natural product. Methods: Cleome brachycarpa was evaluated for its anti-inflammatory and analgesic effects at 200 mg/kg compared to diclofenic sodium and morphine, respectively. For anti-inflammatory activity, Wistar strain albino rats were pooled and divided into four groups: Negative control (normal saline), positive control (2% acetic acid), standard (Diclofenic sodium 10 mg/kg), and test (Cleome brachycarpa extract orally) groups for 10 days. For analgesic evaluation, mice were divided into control (normal saline), standard (morphine 10 mg/kg), and test (Cleome brachycarpa extract 200 mg/kg) groups and analyzed by the tail-flick method from zero to six hours. An assortment of blood parameters was evaluated, including white cells, red cells, hemoglobin level, hematocrit value, mean corpuscular volume, and mean corpuscular hemoglobin concentration. Besides, we computed the number of platelets, cholesterol, and enzyme (liver) level to ensure the safe use of this natural product. For this purpose, 60 rabbits were collected and divided into groups: Group A (control group) of 30 rabbits pooled without any treatment and Group B (treated group) of 30 rabbits receiving 200 mg/kg of Cleome brachycarpa. After 30 days, 4 mL blood sample was obtained by cardiac puncture. Results: Plethysmometer evaluation of anti-inflammatory effects showed maximum inflammatory inhibition of 29.42% at the sixth hour. Moreover, tail flick analysis showed maximum pain inhibition of 55.10% at the sixth hour, comparable to the standard drug. Furthermore, hematological data were analyzed statistically and showed insignificant results (P ≥ 0.05), indicating no prominent changes in hematological parameters, except for SGPT, a liver enzyme that increased after 30 days of treatment (P ≤ 0.05). Elevated levels of SGPT are usually reported with several drug administrations like NSAIDs and anti-TB drugs, but still, it should be further investigated. Conclusions: Cleome brachycarpa showed promising anti-inflammatory and analgesic effects without producing any potent change in enzymes except SGPT, which would be evaluated further.

Central and Peripheral Analgesic Activities of Aqueous Extract of Centella Asiatica (AECA) Leaves in Rats and Mice

The demand of herbal based medicines are increasing all over the world and the focus on plant research has increased. Centella asiatica (CA) is a medicinal herb used in traditional medicine as remedy for a variety of diseases. It is widely used in Ayurvedic medicines. The present study evaluated the Analgesic Activity of Aqueous Extract of the leaves of Centella asiatica (AECA). Acute oral toxicity test was performed according to Organization for Economic Cooperation and Development, 2008 (OECD) guidelines. The tail flick method and glacial acetic acid-induced writhing tests were used to study the central and peripheral analgesic activities of AECA, respectively. AECA (200mg/kg) produced significant analgesia in both central and peripheral mechanisms compared to the control. The maximal analgesic effect was observed after 90 minutes of drug administration in the tail-flick method. In the glacial acetic acid-induced writhing test, AECA (200 mg/kg, p.o) produced a significant decrease (71.07%) in the number of writhes (p&lt;0.01) when compared to the control. Therefore, CA can be a very promising herbal-based medicine for treatment of various painful conditions. Further investigations are needed to determine the precise mechanism and site of action of AECA.

UHPLC-MS and GC-MS phytochemical profiling, amelioration of pain and inflammation with chloroform extract of Funaria hygrometrica Hedw. via modulation of inflammatory biomarkers.

People of Pakistan have undisturbed customs for the employment of medicinal plants for healthcare requisites. Chloroform extract of F. hygrometrica (CE FH) was examined for its ability to reduce inflammation and to produce analgesia. Carrageenan and formalin-induced paw edema model for inflammatory activity, hot-plate and tail-flick methods to assess analgesic activity were executed. Phytochemical analysis was done by UHPLC-MS and GC-mass spectrometer. The results demonstrated that in carrageenan-induced paw edema, maximum reduction in inflammation was observed at 5th hour at the dose 100mg/kg; while at doses 250 and 500mg/kg, maximum response was observed at 5th and 6th hours. Analgesic activity results indicated that maximum analgesia was observed up to 120min at 100mg/kg, while up to 90min in case of 250 and 500mg/kg doses. The formalin-induced rat paw edema showed significant (p < 0.05) anti-inflammatory activity after 5days treatment. After, testing period of 10days, the biochemical parameters such as CBC, CRP, serum enzymes like CAT, SOD, GSH and inflammatory mediators like TNF-α, IL-6, IL-4 and IL-10 were estimated. The administration of formalin resulted in an increase in the level of leucocytes, total WBC, CRP, serum enzymes and in the diameters of paw thickness, while pre-treatment with CE FH at dose levels of 100, 250 and 500mg/kg exhibited a diminution in the levels of SOD, GSH, CAT, total RBC and HB. Acute inflammatory mediators such as TNFα, IL -6 and IL-4 were reduced, and IL-10 was upregulated in the treated group as compared to the control. Many phytoconstituents, i.e., chitobiose, chlorovulone III, γ-tocotrienol, emmotin, cassine, hexacosanedioic acid, neophytadiene, fumaric acid, neophytadiene, hexadecanoic acid, phytol and stigmasterol were detected during UHPLC-MS and GC-MS analysis seems to be responsible for the said activity in correlation with the already reported data about these compounds. The results concluded that CE FH possess noteworthy anti-inflammatory and central analgesic action at different doses (100, 250 and 500mg/kg).

Comparative assessment of analgesic activity between whole plant and parts of Azadirachta Indica

Azadirachta Indica is a most common medicinal plant which is use for Antibacterial, Antifungal, Antiulcer, Antiviral, Analgesic, sedative properties. Objective: The aim of the study was Comparative Assessment of Analgesic Activity between whole plant and parts of Azadirachta Indica in experimental animal model. Methods: The extracts were prepared by maceration method. Analgesic activity was assessed by tail flick method and hot plate method (for central action) and acetic acid-induced writhing test (for peripheral action). Results: Seed extract, whole plant extract and aspirin showed significant analgesic activity, both central and peripheral, as compared to control (p&lt; 0.01). Although Whole plant extract at dose of 500 mg/kg showed better activity than 250 mg/kg (p &lt;0.05).

Preclinical evaluation of analgesic activities of Barringtonia Racemosa

Background: Pain is the major devastating health problems. Barringtonia racemosa Roxb. (Lecythidaceae) is the one which is frequently used to treat pain by traditional healers in Ethiopian folk medicine. However, the plant has not been scientifically evaluated for its traditionally claimed use. The present study aimed at the investigation of analgesic activities of ethanol root extract of Barringtonia racemosa Roxb in Albino rats (Wistar) model. Methods: Successive maceration was used as a method of extraction using solvents ethanol. After extraction of the roots, the crude extract was evaluated for its analgesic activities using tail flick and hot plate method. The extract was evaluated at 100, 200 and 400 mg/kg doses. The positive control groups were treated with Aspirin 20 mg/ kg i.p, distilled water (10 mL/kg) treated rat were assigned as negative controls. Results: Barringtonia racemosa Roxb root extract at all test doses showed statistically significant antinociceptive activity in both model in a dose dependent manner (p &lt; 0.01 and p &lt; 0.001). The greater analgesic activity was observed by the maximum dose of the extract (400 mg/kg) in both tail flick and hot plate method method. Conclusion: In general, the data obtained from the present study elucidated that the extract possessed a significant analgesic activities and recommended for further studies.

Anti-inflammatory and Analgesic Studies of 2-aryl-3-(5-alkyl-1, 3, 4-thiadiazol-2-yl) 4-thiazolidinones

Any damage and bad stimulus causes pain and inflammation. The compound used for pain is known as analgesic and for inflammation is known as anti-inflammatory. The title compounds were evaluated for analgesic activity using Tail-Flick method and anti-inflammatory activity using Carrgenan Induced Rat Paw Edema. Diclofenac Sodium used as standard drug. The chloro, fluro and nitro containg derivatives showed best activity as compared to methyl, methoxy and hydroxy derivatives.

Superporous acrylic acid and HPMC hydrogels of mefenamic acid: Formulation, characterization and optimization by central composite design.

The purpose of the study was to devise the superporous hydrogels (SPHs) of mefenamic acid (MA) to acquire the sustained action of the MA in the body. The superporous hydrogels of mefenamic acid were formulated by employing the gas blowing method. The central composite rotatable design (CCRD) was applied to optimize the effect of independent formulation factors like acrylic acid (AC), HPMC and glycerol (GLY) over dependent variables like porosity, viscosity, drug content and swelling ratio of superporous hydrogels in water, phosphate buffer (pH 6.8) and in 0.1N HCl (pH 1.2). A number of characteristics such as void fraction, surface morphology by Scanning electron microscopy (SEM) and in vitro drug release study were governed along with physico-chemical analysis by Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and appraised statistically by employing the ANOVA. The comparative analgesic activity of optimized superporous hydrogel formulation SPH17 was also analyzed by using tail flick method. The Fourier transform infrared spectroscopy and Differential scanning calorimetry studies approved the physical compatibility between the polymers and the drug. The Scanning electron microscopy study specified micrographic insight about the structure of formed formulations comprising presence of pores, fibers and drug-hole aggregates. The superporous hydrogels were detected to be low dense as they expressed density lower than 0.75g/cc. The decrease in concentration of the polymers and cross linker contributed towards the increase in the void fraction of the superporous hydrogel formulations. The optimized formulation SPH 17 exhibited a highly sustained release of MA for up to 10h in the both 0.1N HCl and phosphate buffer (66.6%) media. The non-fickian release of drug revealed the coupling of the diffusion and polymer relaxation mechanism of the drug release from the formulations. The obtained outcomes suggested that analgesic effect of SPH 17 was significantly (p < 0.05) higher than that of simple suspension of mefenamic acid and total analgesic effect duration for superporous hydrogel was also doubled as compared to the duration of analgesic effect produced by drug suspension. The successfully formulated SPH with HPMC K100M as a gelling agent had sustained the action of the mefenamic acid (MF) by improving its poor solubility and permeability. The introduction of inter-penetrating polymeric network (acrylic acid) using glycerol as a cross linker impart increased residence time to superporous hydrogels which ultimately enhanced the feasibility of using superporous hydrogel as oral sustained release devices particularly for gastric retention.

Investigation of biological activities of Xeromphis uliginosa (Retz.) root extracts in Swiss-albino mice model, an extinctive medicinal plant of Bangladesh

Xeromphis. uliginosa (Retz.) is an extinctive Bangladeshi medicinal plant that is locally used for the treatments of pain, diabetes, diarrhea, depressant, and other diseases. The present study was conducted to evaluate the peripheral analgesic activity (PAA), central analgesic activity (CAA), central nervous system antidepressant activity (CNS-AD), antidiarrheal activity (ADA), and hypoglycaemic activity (HGA) of methanolic root extract of X. uliginosa (MREXU) in a mice model. The acetic acid-induced writhing inhibition and tail flick method were applied to determine the PAA and CAA of MREXU. The CNS-AD was measured using the phenobarbitone sodium-mediated sleeping method whereas, the castor oil-induced antidiarrheal method was used to determine the ADA of the crude extracts. To determine the HGA of MREXU crude extract, the tail tipping technique was conducted in a mice model. The MREXU displayed potential PAA and CAA in mice models. The MREXU 200 and 400 mg/kg significantly inhibit the number of writings along with diclofenac sodium. On the other hand, MREXU both doses significantly inhibit thermal stimulus after 60 and 90 minutes respectively. In the CNS-AD study, crude extract of 200 and 400 mg/kg significantly increase the onset of sleep by decreasing the duration of sleep. Similarly, the dose of 200 mg/kg significantly reduced diarrheal faeces for the whole 4 hours of experiments. The heartiest outcome of MREXU was displayed in the HGA assay. Both doses of MREXU significantly reduced the blood sugar level for the entire 3 hours of the experiments. In this study, it is revealed that the root of MREXU has extremely significant blood sugar-reducing activity, potential CNS-AD and mild to moderate nociceptive activity in the mice model

Development of Bioadhesive Transdermal Patches of Bupivacaine for the Enhancement of Anaesthetic Effect: Study in Rat Model

The topical route for local anaesthesia including ointments and creams can be easily washed off by wetting agents or with contact or movement. The goal and objective of the present study was to develop and formulate a transdermal patch for local anaesthesia. These patches were formulated by solvent casting method by the use of Hydroxypropyl Methylcellulose (HPMC) polymer, different enhancers, and vasoconstrictor which is the key ingredient for enhancing aesthetic activity. Formulated patches were evaluated for the physical and physicochemical parameters like moisture content, moisture uptake, folding endurance, water vapour permeability, drug content, and drug release, and in vivo study was done on rats. Amongst all the formulations, F7 was considered the ideal formulation which is the combination of HPMC polymer, polyoxyethylene 2-oleyl ether as an enhancer, and vasoconstrictor Tetrahydrozoline. For in vivo testing Tail flick method was applied and the effect of anaesthesia was maximum as compared to other formulations. In comparison to the control formulation, there was a 2.34-fold increase in aesthetic activity. When compared to the control formulation, the F7 formulation exhibited improved and longer efficacy. A transdermal bupivacaine patch incorporating a penetration enhancer and a vasoconstrictor could be created to improve the local cosmetic effects of bupivacaine.