Topical Anti-inflammatory Activity Research Articles

Optimization and Characterization of Thymoquinone-Loaded Liposomes with Enhanced Topical Anti-inflammatory Activity

Thymoquinone, the major constituent of Nigella sativa oil has been found to have a promising topical anti-inflammatory activity; however, exaggerated heat and photo-sensitivity and lipophilicity prevent the best use of this promising product. The present work aimed to formulate an ideal thymoquinone liposomal system for topical delivery. Different liposomal systems were developed using thin film hydration method by applying different cholesterol molar concentrations, different total lipid molar concentrations, and different drug-to-lipid ratios. Morphological characterization of the prepared formulae was performed using polarized light, scanning electron microscope, and transmission electron microscope. The optimized formula (F12) was selected on the basis of enhanced permeation through the skin and was incorporated into chitosan gel for topical application. The gel formulation was clear with suitable skin permeation and exhibited acceptable rheological properties. Using carrageenan-induced paw edema in rats, the developed chitosan gel (F12) showed significant superior in vivo anti-inflammatory activity over the chitosan gel of the TQ (p < 0.05) and comparable effect to the marketed indomethacin gel. As a conclusion, results revealed the potential of formulating thymoquinone as liposomal formulation in enhancing the anti-inflammatory effect compared to the TQ solution.

Development of an effective and safe topical anti-inflammatory gel containing Jatropha gossypiifolia leaf extract: Results from a pre-clinical trial in mice

Ethnopharmacological relevanceJatropha gossypiifolia L. (Euphorbiaceae) is a medicinal plant widely used in traditional medicine as an anti-inflammatory remedy. The topical use of the leaves and/or aerial parts of this plant as anti-inflammatory, analgesic, wound healing and anti-infective in several skin diseases is a common practice in many countries. The use of baths or dressings with this vegetal species is frequently reported in folk medicine. Aim of the studyTo evaluate the topical anti-inflammatory of aqueous extract from leaves of J. gossypiifolia and to develop a safe and effective herbal gel with anti-inflammatory potential. Material and methodsFirst, the topical acute anti-inflammatory activity of J. gossypiifolia extract was evaluated in ear edema induced by single application of croton oil in mice. Then, a polaxamer-based gel containing J. gossypiifolia extract was developed, physicochemically characterized and evaluated in the same model of inflammation to assess whether the extract incorporation in gel would affect its anti-inflammatory potential. The best formulation was then assayed in ear edema induced by multiple applications of croton oil in mice, to evaluate its chronic anti-inflammatory potential. Inflammatory parameters evaluated included edema, nitrite concentration, mieloperoxidase (MPO) activity and oxidative damage in lipids and proteins. Finally, dermal irritation/corrosion test in mice was performed to access the safeness of the developed gel. Phytochemical characterization of J. gossypiifolia extract was performed by high performance liquid chromatography with diode array detector (HPLC-DAD) analysis. ResultsJ. gossypiifolia showed significant acute anti-inflammatory activity in ear edema model, and this activity was significantly increased when equivalent amounts of extract was applied incorporated in the developed polaxamer gels. The gels containing different amounts of extract reduced significantly the levels of edema, nitrite and MPO enzyme in mice ears, with intensity similar to the anti-inflammatory standard drug dexamethasone. The gel containing 1.0% of extract was further evaluated and also showed significant anti-inflammatory activity in chronic inflammation test, reducing significantly ear edema, lipid peroxidation and depletion of reduced glutathione, similarly to dexamethasone. Placebo formulation as well as gel containing extract showed pH compatible to that of human skin and exhibited absence of signs of toxicity in mice, indicating the safeness of the developed product for topical use. HPLC analysis confirmed the presence of C-glycosylflavonoids (orientin, isoorientin, vitexin and isovitexin) as the major compounds of J. gossypiifolia aqueous leaf extract. ConclusionsThe results demonstrate the potentiality of J. gossypiifolia gel as a promising safe and effective topical anti-inflammatory agent for treatment of cutaneous inflammatory diseases.

Topical Anti-inflammatory Activity of Bangle (Zingiber cassumunar Roxb). Ethanolic Extract in Mice Induced By Carrageenan

Rhizome of bangle (Zingiber cassumunar Roxb.) is one of the materials that are traditionally used in the traditional preparation to maintain skin from redness. The content of chemical compound in bangle rhizomes has many benefits, including inhibition of the inflammatory processes. This study aims to determine the topical anti-inflammatory activity of ethanolic extract of bangle rhizomes in mice induced by carrageenan. Thirty five female Swiss mice were used in this study. Animals were divided into 7 group of five: normal group, carrageenan 2% group, carrageenan 2% group plus control of basis (Biocream®), carrageenan 2% group plus 2.5% hydrocortisone cream, and carrageenan 2% group plus cream of ethanolic extract of bangle rhizomes with the concentration of 1%, 2.5% and 5% w/w. Carrageenan 2% was injected subcutaneously in all treatment group except normal group. The skinfold thickness of mice was measured every 1 hour for 6 hours after carrageenan injection. Results of this study shows that there is a significant differences between treatment groups (p &lt;0.05) compared to carrageenan 2% treated group. To conclude, ethanolic extract of bangle rhizomes has topical anti-inflammatory in mice induced by carrageenan.

Topical Anti-Inflammatory and Analgesic Activities of Citrullus colocynthis Extract Cream in Rats.

Background and objectives:Citrullus colocynthis (CC), known as bitter apple, is used to treat diabetes in Iranian traditional medicine. The aim of this study is to evaluate the anti-inflammatory and analgesic activities of CC cream in rats. Materials and Methods: The carrageenan-induced edema in a rat hind paw was carried out to evaluate the topical anti-inflammatory effect of the CC fruit extract cream (2–8%) and the tissue levels of IL-6 and TNF-α were estimated by using a commercial ELISA kit. The topical antinociceptive activity of CC cream (2–8%) was evaluated in the rat formalin test. To determine the role of opioid receptors in the local antinociceptive effect of the CC cream, naloxone (20 μg/paw, i.pl.), a non-selective opioid antagonist, was used. Results: The results showed that the CC cream (2–8%) dose-dependently reduced the carrageenan-induced paw edema and reversed the changes in the level of TNF-α and IL-6 due to carrageenan-induced edema (p < 0.01). The anti-inflammatory effect of CC cream 8% was comparable to that of hydrocortisone ointment 1%. Furthermore, the application of CC cream (2–8%) dose-dependently inhibited both first and second phases of the formalin test (p < 0.05). The antinociceptive effect of the CC cream (8%) was comparable to that of methyl salicylate cream 30%. Moreover, the administration of naloxone significantly reversed the topical antinociceptive effect of the CC cream (p < 0.05). Conclusions: For the first time, this study indicated that the topical application of CC cream possesses significant anti-inflammatory and antinociceptive activities in animal models, which were probably mediated by opioid receptors and the suppression of pro-inflammatory cytokines (TNF-α and IL-6). Thus, the CC cream can be used to treat inflammatory pain and inflammatory diseases.

Copaiba oil enhances in vitro/in vivo cutaneous permeability and in vivo anti-inflammatory effect of celecoxib.

The aim of this article was to use copaiba oil (C.O) to improve skin permeability and topical anti-inflammatory activity of celecoxib (Cxb). Formulations containing C.O (1-50%) were associated with Cxb (2%). In vitro skin permeability studies were conducted using porcine ear skin. Histological analysis of the hairless mice skin samples after application of formulations was achieved with the routine haematoxylin/eosin technique. The anti-inflammatory activity was assessed using the AA-induced ear oedema mice model. The formulation containing 25% C.O promoted the highest levels of in vitro Cxb permeation through pig ear skin, retention in the stratum corneum (SC) and epidermis/dermis of pig ear skin in vitro (~5-fold) and hairless mice skin in vivo (~2.0-fold), as compared with the control formulation. At 25%, C.O caused SC disorganization and increased cell infiltration and induced angiogenesis without clear signs of skin irritation. The formulation added to 25% C.O as adjuvant inhibited ear oedema and protein extravasation by 77.51 and 89.7%, respectively, and that it was, respectively, 2.0- and 3.4-fold more efficient than the commercial diethylammonium diclofenac cream gel to suppress these inflammatory parameters. 25% C.O is a potential penetration enhancer for lipophilic drugs like Cxb that can improve cutaneous drug penetration and its anti-inflammatory activity.

Analysis of Solanum Americanum Mill. by Ultrafast Liquid Chromatography with Diode Array and Time-Of-flight Mass Spectrometry Detection with Evaluation of Anti-Inflammatory Properties in Rodent Models

ABSTRACTSolanum americanum Mill. has been traditionally used for the treatment of fever, stomachache, skin diseases, gynecological disorders, and different kinds of inflammation. This study evaluated the anti-inflammatory response of different extracts obtained from ripe fruits of S. americanum Mill., in experimental models and evaluated them qualitatively using ultrafast liquid chromatography with diode array and time-of-flight mass spectrometry (UFLC-DAD/TOF-MS). The inflammatory response of four extracts of ripe fruits was evaluated for the systemic and topical anti-inflammatory activities. The compounds in each extract were identified using UFLC-DAD-TOF/MS. A total of 34 compounds was identified in the four extracts. The best results were obtained in compounds from the aqueous and chloroform extracts. This study demonstrated a significant anti-inflammatory activity for the compounds present in fruit of S. americanum Mill.

Chemical fingerprint, acute oral toxicity and anti-inflammatory activity of the hydroalcoholic extract of leaves from Tocoyena formosa (Cham. & Schlecht.) K. Schum.

Inflammation is a protective response of the organism against damaging agents, this process is considered beneficial, however in some situations, this response can be damage when exacerbated effect are present. This claim objective to evaluate the qualitative and quantitative chemical profile, acute toxic and anti-inflammatory effects of the hydroalcoholic extract of leaves from Tocoyena formosa (Cham. & Schlecht.) K. Schum. (HELTF). Quantitative and qualitative phytochemical analysis was performed by HPLC-DAD and colorimetric assay. The topical anti-inflammatory activity was determined in Croton oil-induced ear edema assay and systemic activity was performed in vascular permeability, paw edema induced by carrageenan and dextran. Phytochemical analysis of leaves from HELTF showed presence of tannin, flavonoid, saponins an other that confirmed by HPLC analysis. The extract did not cause significant with LD50 greater than 5000 mg/kg and did not promote significate reduction in topical inflammatory process. However, HELTF demonstrate significant reduction of paw edema induced by carrageenan and dextran. The HELTF (200 mg/kg) reduced the protein/cell migration in the intradermal carrageenan-induced inflammation. Our results demonstrated that the first time the chemical profile and describe the effective action in systemic anti-inflammatory, antiedematogenic activity and low acute toxicity. This activity presents, supporting its traditional use. However, new studies are necessary for the detection and clarification of the possible mechanism of action.

Efficacy of a polyphenolic extract from silver fir (Abies alba) bark on psoriasis: a randomised, double-blind, placebo-controlled trial.

Silver fir (Abies alba) bark extract contains a mixture of bioactive polyphenols. We tested their effectiveness in the treatment of psoriasis in order to further investigate the potential topical anti-inflammatory activity of polyphenols by means of a randomized, double-blind, placebo-controlled add-on clinical trial, after having examined their ability to downregulate the expression of IL-1β cytokine in monocyte/macrophage primary cell culture. 61 patients with mild psoriasis met the inclusion criteria and were willing to comply with protocol requirements, were enrolled in the study. The severity of the disease was measured by psoriasis area severity index (PASI). Treatment efficacy was evaluated by assessing erythema (E, 0 to 4-point scale), desquamation (D, 0 to 4-point scale) and induration (I, 0 to 4-point scale) of lesions before and after the treatment. All patients enrolled in the study had symmetrical psoriasis plaques on the skin. All patients received O/V ointment with 2% of silver fir bark extract and/or placebo, respectively. We compared medications by right/left intra-patient comparison, so that the control group was always contralateral of the tested one. Location of the tested or control site was randomised, using a computer-generated randomisation schedule. Silver fir extract was well-tolerated. A superiority of active treatment above placebo, based on the clinical investigational PASI score system was observed by 15 % in all volunteers and in 40% regarding the improvement of psoriasis on elbows. However, statistical analysis showed no significant differences between placebo and active treatment with the extract from silver fir bark (p < 0.05).

Hepatoprotective and Anti‐Inflammatory Activities of the Cnidoscolus chayamansa (Mc Vaugh) Leaf Extract in Chronic Models

Previous report described that CHCl3:MeOH extract of C. chayamansa leaves and pure compounds (moretenol, moretenyl acetate, kaempferol-3,7-dimethyl ether, and 5-hydroxy-7-3′,4′-trimethoxyflavanone) showed important topical and systemic anti-inflammatory activity in acute model, as well as in vitro antimycobacterial and antiprotozoal activities. In this paper, we describe the in vivo hepatoprotective and anti-inflammatory effects of the CHCl3:MeOH extract in chronic model and the isolation of additional compounds (moretenone and lupeol acetate). The hepatoprotective activity was determined at 39 days using Balb/c mice with liver damage induced with an antitubercular drug (RIF/INH/PZA). The anti-inflammatory activity was evaluated in a chronic model induced with CFA and in two acute models (TPA and carrageenan). In addition, moretenone and lupeol acetate were isolated and identified by spectroscopic data. Lupeol acetate is a main compound present in fractions 14-42, and this fraction was the majority fraction from the extract; from this moretenone was obtained. In animals with liver damage, the extract at 200 and 400 mg/kg induced better body weight gain with respect to positive control (Silymarin); in addition, the mice that received the extract at 200 mg/kg and Silymarin exhibited slight steatosis; however, the animals' livers at 400 mg/kg did not show steatosis. The extract and fractions 14-42 showed a good anti-inflammatory activity by TPA model (DE50 = 1.58 and 1.48 mg/ear) and by carrageenan model (DE50 = 351.53 and 50.11 mg/kg). In the chronic inflammatory test, the extract at three doses revealed a similar effect to that of phenylbutazone, although the body weight gain was better in animals that received the extract at 900 mg/kg. Conclusion. The CHCl3:MeOH extract showed significant anti-inflammatory and good hepatoprotective effect on chronic models. The fraction containing moretenone and lupeol acetate as main compounds was more active than extract in both acute models of inflammation.

Identification of compounds from Palicourea rigida leaves with topical anti-inflammatory potential using experimental models.

Palicourea rigida Kunth is traditionally used for the treatment of skin diseases, kidney pains and ovarian inflammation. Based on these traditional uses, this study evaluated the topical anti-inflammatory activity of the ethanol extract from P. rigida leaves (EEPR) and identified bioactive compounds. Ear edema was induced in Swiss mice by the topical application of Croton oil, arachidonic acid, phenol and capsaicin. Histopathological analysis and myeloperoxidase and N-acetyl-β-D-glucosaminidase activities were determined. EEPR was characterized by UHPLC-UV-MS HPLC and the isolated compound was identified through 1H and 13C nuclear magnetic resonance and mass fragmentation. Interaction profiles between quercetin 3-O-β-D-glucoside and cyclooxygenase-1 and -2 were established by molecular docking. EEPR significantly inhibited ear edema induced by Croton oil (p<0.001), arachidonic acid (p<0.01), phenol (p<0.001) and capsaicin (p<0.01 or p<0.001). Histopathological analysis showed a reduction of edema, inflammatory cell infiltration and vasodilation. Additionally, the myeloperoxidase and N-acetyl-β-D-glucosaminidase activities were decreased (p<0.001). From spectroscopic data, quercetin 3-O-β-D-glucoside was the identified compound. This compound can to interact with cyclooxygenase-1 and -2 through van der Waals interactions and dipole-dipole and hydrogen bonding's, demonstrating inhibition of these enzymes. The results indicate that EEPR is a source of active compounds with topical anti-inflammatory activity, justifying the traditional use of P. rigida and showing that this species has a therapeutic potential to treat skin inflammatory processes.

In Vitro and In Vivo Evaluation of DMSO and Azone as Penetration Enhancers for Cutaneous Application of Celecoxib.

Celecoxib (CXB) has been explored as an anti-inflammatory or chemopreventive drug for topical treatment of skin diseases and cancer. The main aim of this work was to investigate the potential of dimethylsufoxide (DMSO) and Azone (AZ) as penetration enhancers (P.Es) for topical delivery of CXB. The in vitro studies, drug release, skin permeability and potential cytotoxicity/genotoxicity were carried out with formulations containing or not DMSO or AZ (5% and 10%). Skin irritation in rabbits and topical anti-inflammatory activity in mice were assayed in vivo. Skin permeation was minimal while higher retention in stratum corneum (SC) and epidermis plus dermis was found (28.0 and 3-fold respectively) from 10.0% AZ compared to the control indicating a localized CXB effect. CXB associated to 5% or 10% DMSO has shown high drug permeation through skin with low retention. Associations of CXB with both enhancers were not cytotoxic or genotoxic, suggesting safety for cutaneous application. In vivo skin irritation assays of all formulations indicated mild irritation effects and, thus, possible use for longer periods. In vivo anti-inflammatory tests showed that ear edema could be inhibited by CXB associated with 5.0% DMSO (53.0%) or 10.0% AZ (40.0%). These inhibition values were almost 2-fold higher when compared to a commercial formula. Although DMSO- associated CXB is an efficient edema inhibitor its high skin permeation suggests risks of systemic effects, whereas association to 10% AZ may improve topical delivery of the drug with good anti-inflammatory activity and no cytotoxic/genotoxic or significant skin irritation effects.

Study of the non-clinical healing activities of the extract and gel of Portulaca pilosa L. in skin wounds in wistar rats: A preliminary study

IntroductionPortulaca pilosa L., belonging to the family Portulacaceae, is a common herbaceous plant in the Americas and in the Amazon, is popularly known as love-grown and is traditionally used as an aid in the treatment of burns, buds, insect bites and wound healing. This study aims to evaluate the non-clinical topical healing activity of the P. pilosa gel (GPP) and the propyleneglycol extract of P. pilosa (EPP) in Wistar rats. MethodsFor the healing activity, wistar rats were divided into the following groups: negative control (GVE – vehicle, 150mg/kg), positive control (Fibrinase®- FIB, 100U/kg), Portulaca pilosa gel 10%, (GPP, 150mg/kg), and propylenglycollic extract of Portulaca pilosa (EPP, 150 mg/kg), which were submitted to a surgical procedure to obtain the wounds, and were treated topically for 7days. After treatment, the treated area was removed and a histopathological analysis was performed. ResultsThe EPP when analyzed in HPLC was able to identify the presence of gallic acid. EPP significantly modulated the tissue inflammatory response, presenting low number of inflammatory cells in the histopathological study. Treatment with EPP and GPP significantly stimulated angiogenesis and this response was superior to the fibrinase® group. Treatment with EPP and GPP significantly stimulated the proliferation of fibroblasts. The groups treated with EPP and GPP presented an organization pattern of the epidermis and dermis better than the control group, with a mild inflammatory process, with fibroblast proliferation and increased formation of collagen fibers. ConclusionThus, from the results obtained it can be suggested that the phytochemical marker of the P. pilosa species for healing activity is gallic acid and, together with the macroscopic and microscopic findings triggered by the topical applications of EPP and GPP, it can be concluded that this plant species has topical healing activity, with great potential for use, since this pharmacological action is associated with a possible topical anti-inflammatory activity.

The ethanol extract of Leonurus sibiricus L. induces antioxidant, antinociceptive and topical anti-inflammatory effects

Ethnopharmacological relevanceLeonurus sibiricus L. (Lamiaceae), popularly known as motherwort, or “erva-de-macaé” or “rubim” in Brazil, is a plant used for the treatment of inflammatory conditions, but few studies have evaluated this anti-inflammatory activity or other activities that may be relevant. Aim of the studyThis study was undertaken to investigate the antioxidant, antinociceptive and topical anti-inflammatory effects of the ethanol extract of L. sibiricus (EELs). Materials and methodsChromatographic analysis, determination of total phenolic and flavonoid contents and in vitro antioxidant assays were performed, while the formalin test and ear inflammation induced by 12-0-tetradecanoylphorbol-13-acetate (TPA) were performed in mice. ResultsWe observed that total phenolic and flavonoids content in EELs were respectively 60.1mg of gallic acid equivalent/g of extract and 15.4mg of catechin equivalent/g of extract. Chlorogenic, caffeic, p-coumaric and ferulic acids, as well as quercetin were identified in EELs. This extract also led to the consumption of the radicals 2,2-diphenyl-1-picrylhydrazyl, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and nitric oxide, increased the ferric reducing/antioxidant power (FRAP) and inhibited the spontaneous or FeSO4-induced in vitro lipid peroxidation. In the formalin test, oral pretreatment with EELs (400mg/kg) reduced (p<0.001) the licking/biting time in the second phase, but not in the first phase. In the ear inflammation induced by TPA, the concomitant topical administration of EELs (0.3–3mg/ear) significantly reduced the edema, myeloperoxidase activity, levels of tumoral necrosis factor-α and interleukin-1β and lipoperoxidation, as well as increased FRAP in ear tissue when compared to vehicle-treated ears. ConclusionsThese results indicate that EELs has antioxidant, antinociceptive and topical anti-inflammatory activities, supporting the use of this plant in folk medicine.

22 5α-tetrahydrocortisone exhibits topical anti-inflammatory action with limited adverse effects on angiogenesis

Glucocorticoids (GC) are potent anti-inflammatory drugs but have debilitating side effects. A safer alternative is required and 5α-tetrahydrocorticosterone (5αTHB, a metabolite of the natural rodent glucocorticoid corticosterone) may provide a solution. 5αTHB is anti-inflammatory in vivo but with fewer systemic adverse effects. It is rapidly cleared from systemic circulation and is therefore being investigated for topical application. Topical steroids additionally impair wound healing, largely due to the inhibition of angiogenesis and of collagen deposition. Here, the effects of 5αTHB on processes involved with wound repair were investigated. Angiogenesis was assessed using two murine models. In the first, sponges containing vehicle, 5αTHB (3 mg or 15 mg), or corticosterone (3 mg) were implanted subcutaneously in C57Bl6 mice (male, aged 8–12 weeks, 8–12/group). After 21 days sponges were excised and fixed, and vessel growth and collagen deposition were assessed by counting and picro-sirius red staining, respectively. At equipotent anti-inflammatory doses, corticosterone decreased the amount of collagen in sponges (3 mg changing to 30%±8% of control; p In the second model, vessel growth was stimulated from mouse aortic rings (C57Bl6 mice, male, age 8–10 weeks) and attenuation of growth was assessed following incubation with steroid (dose ranges 1 nM–10 μM, n=6–8/dose). Angiogenesis was suppressed to a lesser extent by 5αTHB (EC50 2399 nM) than by dexamethasone (8 nM) or hydrocortisone (675 nM; n=6–8/dose). These data suggest that 5αTHB could provide a safer anti-inflammatory treatment for topical application. It has fewer adverse effects on angiogenesis and collagen deposition than hydrocortisone and is thus likely to be less detrimental during wound repair.

Topical anti-inflammatory activity test and identification of anti-inflammatory active compounds of ether extract of stem bark and leaves resin of tenggulun protium javanicum burm

Topical anti-inflammatory activity test and identification of anti-inflammatory active compounds of ether extract of stem bark and leaves resin of tenggulun protium javanicum burm

Ipomoea pes-caprae (L.) R. Br (Convolvulaceae) relieved nociception and inflammation in mice – A topical herbal medicine against effects due to cnidarian venom-skin contact

Ethnopharmacological relevanceIpomoea pes-caprae is known as bayhops, beach morning glory or goat's foot, and in Brazil as salsa-de-praia. Its leaves are used in worldwide folk medicine for the relief of jellyfish-stings symptoms. The literature only reports the neutralizing effects of nonpolar plant derived over jellyfish venoms, without validating the popular use or exploring the mechanism of action. Aim of the studyThis study aimed to evaluate and validate the topical effects of a semisolid containing hydroethanolic extract obtained from the aerial parts of I. pes-caprae using different models of paw- and ear-oedema and spontaneous nociception in mice, attempting to better understand the mechanism involved in its effect. Materials and methodsLeaf and stem of I. pes-caprae were extracted by ethanol 50% (v/v) and the soft-extract was incorporated in Hostacerin® cream base at 0.5%, 1.0% and 2% (w/w). The anti-hypersensitivity effects were evaluated by injecting the Physalia physalis venom into the right mice’s hindpaw pre-treated either with the semisolid containing the I. pes-caprae extract or with the isolated majority compound 3,5-Di-O-caffeoylquinic acid (ISA). The topical anti-inflammatory activity was investigated using both preclinical models: paw oedema induced by trypsin, bradykinin (BK), histamine and carrageenan, and ear oedema induced by capsaicin. Additionally, the model of spontaneous nociception induced by trypsin and capsaicin were used to verify the topical antinociceptive activity. ResultsThe animals pre-treated with the semisolid containing I. pes-caprae extract or with the intraplantar injection of the major component (ISA) had the mechanical hypersensitivity induced by P. physalis venom significantly reduced. Significant inhibition was also observed in paw-oedema induced by trypsin, histamine and BK, and in a less extent in carrageenan-induced paw oedema. Similar effect was observed in mice challenged to the capsaicin-induced ear-oedema. Besides the vascular effects, the extract interfered with leukocyte migration induced by histamine injection. Finally, the semisolid presented significant inhibition in trypsin- and capsaicin-induced spontaneous nociception. ConclusionsThe hydroethanolic extract of I. pes-caprae showed compliance with the topical popular use of the herbal product to relieve the symptoms evoked by the cnidarian venom-skin contact, such as neurogenic oedema and nociception. The extract components seem to interfere with the effects resulting from the TRPV1, B2R and PAR-2 activation, once it interfered with painful-behaviour and oedema induced by capsaicin, BK and trypsin, pointing the histaminergic system as the main target, once it is an important mediator in the signalling pathway of the aforementioned receptors.

English

Croton cordiifolius is widely used in Brazilian Caatinga folk medicine to treat general inflammation, pain, and gastrointestinal disturbances. Currently, its medicinal properties are not well understood, owing to the absence of chemical and pharmacological studies. The aims of this work were to analyze the chemical composition of C. cordiifolius stem bark and evaluate its in vitro antioxidant and in vivo anti-inflammatory activities. C. cordiifolius ethanolic extract (CcEE) was obtained by maceration, while essential oil (CcEO) was extracted by hydrodistillation in a Clevenger-type apparatus. The chemical composition was evaluated by thin-layer chromatography and GCMS. Total phenolics, flavonoids, and antioxidant activity were quantitated by spectrophotometry. Topical anti-inflammatory activity was evaluated by different ear edema models in mice. The major compounds in CcEO were α-pinene (51.76%) and β-pinene (19.08%). CcEE analysis indicated the presence of alkaloids, mono- and sesquiterpenes, flavonoids, phenylpropanoids, triterpenes, steroids, and coumarins. CcEE showed antioxidant activity in vitro. In a topical anti-inflammatory assay, CcEO showed no activity. On the contrary, CcEE inhibited ear edema induced by phorbol 12-myristate 13-acetate (PMA), arachidonic acid (AA), ethyl phenylpropriolate (EPP), and phenol. Probable mechanisms include inhibition of AA metabolite biosynthesis, vasoactive amine activity, and cytokine release/activity. These results corroborate the popular reputation of C. cordiifolius as an anti-inflammatory remedy. Key words: Croton cordiifolius, Euphorbiaceae, caatinga, topical anti-inflammatory activity, ear edema.

Anti-Inflammatory Activity of Babassu Oil and Development of a Microemulsion System for Topical Delivery.

Babassu oil extraction is the main income source in nut breakers communities in northeast of Brazil. Among these communities, babassu oil is used for cooking but also medically to treat skin wounds and inflammation, and vulvovaginitis. This study aimed to evaluate the anti-inflammatory activity of babassu oil and develop a microemulsion system with babassu oil for topical delivery. Topical anti-inflammatory activity was evaluated in mice ear edema using PMA, arachidonic acid, ethyl phenylpropiolate, phenol, and capsaicin as phlogistic agents. A microemulsion system was successfully developed using a Span® 80/Kolliphor® EL ratio of 6 : 4 as the surfactant system (S), propylene glycol and water (3 : 1) as the aqueous phase (A), and babassu oil as the oil phase (O), and analyzed through conductivity, SAXS, DSC, TEM, and rheological assays. Babassu oil and lauric acid showed anti-inflammatory activity in mice ear edema, through inhibition of eicosanoid pathway and bioactive amines. The developed formulation (39% A, 12.2% O, and 48.8% S) was classified as a bicontinuous to o/w transition microemulsion that showed a Newtonian profile. The topical anti-inflammatory activity of microemulsified babassu oil was markedly increased. A new delivery system of babassu microemulsion droplet clusters was designed to enhance the therapeutic efficacy of vegetable oil.

Topical antiedematogenic and anti-inflammatory effect of Scutia buxifolia Reissek gel and stability study

Scutia buxifolia Reissek (Rhamnaceae), popularly known in Brazil as “coronilha”, is a plant species used in folk medicine for several disorders, including inflammation. However, no studies have been done with this species to confirm its topical anti-inflammatory action. In this study we evaluate the topical antiedematogenic and anti-inflammatory effects of the gel containing crude extract (CE) and the gel containing ethyl acetate (EtOAc) fraction of S. buxifolia on croton oil or UVB radiation-induced ear edema in mice, and perform gel stability study. Antiedematogenic and anti-inflammatory effects were evaluated through ear edema induced by irritant agent croton oil, UVB irradiation-induced skin injury model and neutrophil infiltration. The gel stability study was performed by analyzing organoleptical aspects, pH, viscosity, and quantification of quercetin and rutin by HPLC. The topical treatment with S. buxifolia gel reduced the ear edema and myeloperoxidase activity. Antiedematogenic and anti-inflammatory effects of S. buxifolia were obtained with concentrations of 0.3, 1 and 3%, with maximal inhibition in the concentration of 1% for gel containing CE (inhibitions of 100, 73±0.05 and 97±0.08% for croton oil- or UVB irradiation-induced ear edema and myeloperoxidase activity, respectively) and EtOAc fraction (inhibitions of 79±0.05, 73±0.05 and 89±0.04% for croton oil- or UVB irradiation-induced ear edema and myeloperoxidase activity, respectively). Such effects may be attributed, at least in part, to rutin and quercetin, as well as other compounds found in this species. No important changes were detected in the stability study, in all aspects analyzed in temperature below 25°C. Our results demonstrate that topically applied S. buxifolia gel presented anti-inflammatory effects, provided that it was maintained at a temperature below 25°C.

Alfred Wilson McKenzie

Alfred Wilson McKenzie (“Freddie”) was a consultant dermatologist of international repute. He was responsible for creating a revolutionary method for assessing and quantifying topical anti-inflammatory activity through the application of...