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PURPOSE: To compare effect of topical cyclosporine-A 0.05% (CsA) and chloroquine phosphate 0.03% (CHQ) as an adjunct to standard therapy in maintaining post-laser assisted in situ keratomileusis (LASIK) ocular surface stability. METHODS: Randomized controlled trial on 100 eyes undergoing femtosecond-LASIK randomized into three groups: 33 eyes in Group I (Standard Treatment group), 34 eyes in Group II (CsA group) and 33 eyes in Group III (CHQ group). Standard treatment included topical moxifloxacin, topical prednisolone and carboxymethyl cellulose. Group II received topical CsA 0.05% twice daily for three months and group III received topical CHQ 0.03% twice daily for three months in addition to standard treatment. Primary outcome measure was change in ocular surface disease index (OSDI) at 6 months. Secondary outcome measures were tear break up time (TBUT), Schirmer-I score, tear film osmolarity, tear film MMP-9 and visual acuity. Follow-up was performed at postoperative 1, 3 and 6 months. RESULTS: At 6 months, OSDI score, MMP-9, tear osmolarity, TBUT and Schirmer score were significantly better in both CsA and CHQ groups as compared with controls (p < 0.001). OSDI, Tear osmolarity, TBUT, MMP-9 levels were comparable in CsA and CHQ group (p > 0.05). In CsA group, tear film MMP-9 levels at 6 months were comparable to preoperative baseline (p = 0.09). There was no significant change in the Schirmer score from baseline in the CsA group; in addition, the Schirmer score was significantly better than the CHQ group at 6 months (p = 0.02). Visual acuity was comparable in all three groups. Adverse effects including burning sensation, stinging, pain and redness were reported by ten patients (CsA group- 3, CHQ group-7; p = 0.28). CONCLUSION: Both CsA and CHQ are useful adjuncts to standard therapy in maintaining ocular surface stability after refractive surgery. Cyclosporine A has more potent and sustained anti-inflammatory effect with less ocular irritative effects.
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Astigmatismo , Cloroquina , Ciclosporina , Síndromes de Ojo Seco , Queratomileusis por Láser In Situ , Miopía , Humanos , Ciclosporina/administración & dosificación , Cloroquina/administración & dosificación , Administración Tópica , Queratomileusis por Láser In Situ/efectos adversos , Síndromes de Ojo Seco/tratamiento farmacológico , Síndromes de Ojo Seco/etiología , Complicaciones Posoperatorias , Antiinflamatorios/administración & dosificación , Estudios Prospectivos , Astigmatismo/cirugía , Miopía/cirugía , Resultado del Tratamiento , Masculino , Femenino , AdultoRESUMEN
Non-infectious uveitis represents a heterogenous group of immune-mediated ocular diseases, which can be associated with underlying systemic disease. While the initial choice of treatment of non-infectious uveitis depends on a number of factors such as anatomical location and degree of inflammation, topical therapies often remain the initial choice of non-invasive therapy. In this narrative review, we aim to describe the literature on non-infectious uveitis, with specific focus on the current perspective on topical anti-inflammatory therapy.
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PURPOSE: To examine whether "activated" dendritic cells (aDCs) could serve as a biomarker of systemic immune disorders in individuals with dry eye (DE) symptoms. Secondarily, to examine the impact of a topical anti-inflammatory agent on aDC number. METHODS: Retrospective analysis was conducted to identify individuals with DE symptoms who had in-vivo confocal microscopy (IVCM) imaging between October 2018 and July 2020 at the Miami Veterans Hospital. aDCs were manually quantified based on morphology. Receiver operating curve (ROC) analysis examined relationships between aDC number and systemic immune disease status. Individuals were then grouped by aDC number (≥2 versus <2) and demographics and DE parameters were examined. Paired t-test was performed to evaluated aDC number pre-vs post-initiation of an anti-inflammatory agent. RESULTS: 128 individuals were included. Their mean age was 57.1 ± 15.0 years; 71.1% were male, 53.1% self-identified as White and 24.2% as Hispanic. The mean number of aDCs in the central cornea was 1.28 ± 2.16 cells/image. The presence of ≥2 aDCs had a sensitivity of 60% and specificity of 77% for the diagnosis of a systemic immune disorder. Individuals with ≥2 aDCs were more likely to self-identify as Black, have Secondary Sjögren's, and have higher nerve fiber area and fractal dimension. In 12 individuals, aDC number decreased from 2.69 ± 2.36 to 0.58 ± 0.73 cells/image after initiation of an anti-inflammatory agent, p = 0.01. CONCLUSIONS: The presence of ≥2 aDCs in the central cornea suggests a systemic immune disorder in individuals with DE symptoms. Topical anti-inflammatory therapy can reduce the number of aDCs in the central cornea.
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Síndromes de Ojo Seco , Síndrome de Sjögren , Adulto , Anciano , Córnea , Células Dendríticas , Síndromes de Ojo Seco/diagnóstico , Síndromes de Ojo Seco/tratamiento farmacológico , Humanos , Masculino , Microscopía Confocal , Persona de Mediana Edad , Fibras Nerviosas , Estudios RetrospectivosRESUMEN
BACKGROUND: Siddha is one of the traditional medical systems of India; previous ethnobotanical survey in Virudhunagar district indicated a high consensus for treating musculoskeletal ailments. OBJECTIVES: This study was aimed to quantitatively document the medicinal plants used to treat musculoskeletal ailments by non-institutionally trained siddha practitioners of Virudhunagar district, Tamil Nadu, India. MATERIALS AND METHODS: This work was the outcome of free-list interviews conducted among 45 informants between April 2016 and January 2017. Sampling sufficiency was assessed by plotting Shannon-Wiener's index and cumulative number of UR. Informant consensus was assessed using Informant Consensus Factor (Fic) and Informant Agreement Ratio (IAR). RESULTS: This study recorded the data regarding 116 plant species which were used to prepare 129 formulations; analysis of the data yielded 490 UR. Among these, 65.3% of UR dealt with internal applications and 34.6% dealt with external applications. In the case of internally used formulations, pain and general musculoskeletal ailments had high Fic values. In the case of externally used formulations, headache and pain had high Fic values. CONCLUSION: Important species prescribed by the informants to treat various musculoskeletal ailments were: Azima tetracantha, Ricinus communis, Sesamum indicum, Moringa oleifera, Cardiospermum halicacabum (internal application), Calophyllum inophyllum, Justicia adhatoda, Curcuma longa, Calotropis gigantea, Zingiber officinale, Withania somnifera, Strychnos nux-vomica, Dodonaea viscosa (external application), Azadirachta indica, Clerodendrum phlomidis,Delonix elata, Pergularia daemia and Vitex negundo (internal and external applications). Robust studies on these local claims will help to improve the community healthcare and will yield some novel agents to treat musculoskeletal ailments.
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PURPOSE: The therapeutic effect of topical nonsteroidal anti-inflammatory drugs (NSAIDs) depends on the drug's ability to penetrate and permeate the skin and subsequently inhibit cyclo-oxygenase (COX) isoforms responsible for pain and inflammation. Most commercially available topical NSAID formulations are clinically effective, but direct comparisons of anti-inflammatory activity including both skin absorption and inhibitory potency are lacking. This study examined the skin absorption of representative commercially available topical diclofenac- and ibuprofen-based formulations along with published potency values to determine formulations with superior anti-inflammatory activity. MATERIALS AND METHODS: Cumulative absorption and flux profiles of 12 commercially available topical NSAIDs (6 diclofenac-based and 6 ibuprofen-based) were evaluated in vitro using human skin in static Franz diffusion cells. Each formulation was applied as a single dose. In vitro permeation parameters and published COX-2 inhibition values were used to calculate a modified index of topical anti-inflammatory activity (mITAA). RESULTS: All diclofenac and ibuprofen formulations permeated human skin in vitro. The rate and degree of absorption differed between diclofenac and ibuprofen formulations and between formulations of the same drug. NSAID concentration within a product was not solely responsible for the permeation flux or degree of absorption. Ibuprofen formulations permeated the skin more rapidly and to a greater degree than diclofenac, but calculated mITAAs were higher for diclofenac. CONCLUSION: Diclofenac exhibited superior anti-inflammatory activity as measured by the index. Differences beyond drug concentration, including excipients, drug salt form, and dosage form, contribute to differences in absorption and thus in anti-inflammatory activity. Both absorption and COX-2 inhibition potency are important for anti-inflammatory activity, but their priority depends upon the products being compared-with the same NSAID, absorption determines superiority; with different NSAIDs, superiority is determined by the balance between absorption and COX-2 potency. These findings should be considered when selecting a topical NSAID for treating patient pain and inflammation.
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BACKGROUND/AIM: natural products are a potential source for drug discovery and development of cancer chemoprevention. Considering that drugs currently available for the treatment of inflammatory and cancer conditions show undesirable side effects, this research was designed to evaluate, for the first time, the in vitro anticancer activity of Algerian Lavandula stoechas essential oil (LSEO) against different cancer cell lines, as well as its in vitro and in vivo topical and acute anti-inflammatory properties. MATERIALS AND METHODS: the LSEO was extracted by steam distillation, and chemical composition analysis was performed using gas chromatography. The main compounds identified in LSEO were oxygenated monoterpenes, such as 1,8-Cineole (61.36%). LSEO exhibited a potent anti-inflammatory activity using the xylene-induced mouse ear edema model. RESULTS: LSEO (200 and 20 mg/kg) was able to significantly reduce (p < 0.05) the carrageenan-induced paw edema with a similar effect to that observed for the positive control. Topical application of LSEO at doses of 82 and 410 mg/kg significantly reduced acute ear edema in 51.4% and 80.1% of the mice, respectively. Histological analysis confirmed that LSEO inhibited the skin inflammatory response. Moreover, LSEO was tested for its antitumor activity against different cancer cell lines. LSEO was found to be significantly active against human gastric adenocarcinoma (AGS), Melanoma MV3, and breast carcinoma MDA-MB-231 cells, with median inhibitory concentration (IC50) values of 0.035 ± 0.018, 0.06 ± 0.022 and 0.259 ± 0.089 µL/mL, respectively. Altogether, these results open a new field of investigation into the characterization of the molecules involved in anti-proliferative processes. CONCLUSION: We suggest that LSEO, with 1,8-Cineole as the major active component, is a promising candidate for use in skin care products with anti-inflammatory and anticancer properties. The results of this study may provide an experimental basis for further systematic research, rational development, and clinical utilization of lavender resources.
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Antiinflamatorios , Antineoplásicos Fitogénicos , Eucaliptol , Lavandula/química , Neoplasias/tratamiento farmacológico , Aceites Volátiles , Aceites de Plantas , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Eucaliptol/química , Eucaliptol/farmacología , Humanos , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Inflamación/patología , Ratones , Neoplasias/metabolismo , Neoplasias/patología , Aceites Volátiles/química , Aceites Volátiles/farmacología , Aceites de Plantas/química , Aceites de Plantas/farmacologíaRESUMEN
Propolis is a natural resinous product and exerts anti-inflammatory properties. The aim of this study is formulation and characterization of solid lipid nanoparticles (SLNs) encapsulating propolis flavonoids (PFs), intended for topical treatment of skin edema. The nanoparticles were prepared and statistically optimized using Box-Behnken response surface methodology. The in vitro release profile of the optimized nanoparticles was investigated. Cytotoxicity of nanoparticles on HSF-PI 18 cell line was determined. Permeation and penetration of nanoparticles across the incised skin were measured. Finally, the nanoparticles were incorporated into a pharmaceutical hydrogel formulation and the in vivo efficacy in reduction of skin edema was determined. The size, PdI, zeta potential, entrapment efficiency (EE%) and loading efficiency (LE %) of the optimized nanoparticles were 111.3 ± 19.35 nm, 0.34 ± 0.005, -24.17 ± 3.3 mV, 73.5 ± 0.86%, and 3.2 ± 0.27%, respectively. Data obtained through in vitro release study suggested a burst release followed by a prolonged release behavior up to 24 h post incubation time interval. The prepared SLNs exhibited no cytotoxicity on HSF-PI 18 cell line. Ex vivo permeation and penetration study of nanoparticles across the incised skin showed approximately a 2.5-fold and a 3-fold increase in cumulative amount of transport and cumulative amount of skin penetration, respectively. Finally, in vivo studies in rat models, showed a threefold reduction in volume of the edema in animals treated with SLNs. The obtained data revealed that the prepared SNs entrapping PFs, exert high skin targeting effects, prolonged anti-inflammatory properties and therefore high efficiency in treatment of skin edema.
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Edema/tratamiento farmacológico , Flavonoides/farmacología , Lípidos/farmacología , Nanopartículas , Própolis , Animales , Portadores de Fármacos , Flavonoides/química , Lípidos/química , RatasRESUMEN
In this study, we isolated from the aerial parts of Baccharis conferta Kunth (i) a new neoclerodane, denominated "bacchofertone"; (ii) four known terpenes: schensianol A, bacchofertin, kingidiol and oleanolic acid; and (iii) two flavonoids: cirsimaritin and hispidulin. All structures were identified by an exhaustive analysis of nuclear magnetic resonance (NMR) and mass spectroscopy (MS). Extracts from aerial parts were screened for anti-inflammatory activity in the mice ear edema model of 12-O-tetradecanoylforbol-13-acetate mice. Dichloromethane extract (BcD) exhibited 78.5 ± 0.72% inhibition of edema, followed by the BcD2 and BcD3 fractions of 71.4% and 82.9% respectively, at a dose of 1 mg/ear. Kingidiol and cirsimaritin were the most potent compounds identified, with a median effective dose of 0.12 and 0.16 mg/ear, respectively. A histological analysis showed that the topical application of TPA promoted intense cell infiltration, and this inflammatory parameter was reduced with the topical application of isolated compounds.
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Antiinflamatorios , Baccharis/química , Enfermedades del Oído , Edema , Flavonas , Terpenos , Acetato de Tetradecanoilforbol/toxicidad , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Modelos Animales de Enfermedad , Enfermedades del Oído/inducido químicamente , Enfermedades del Oído/tratamiento farmacológico , Enfermedades del Oído/metabolismo , Enfermedades del Oído/patología , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/metabolismo , Edema/patología , Flavonas/química , Flavonas/aislamiento & purificación , Flavonas/farmacología , Masculino , Ratones , Ratones Endogámicos ICR , Terpenos/química , Terpenos/aislamiento & purificación , Terpenos/farmacologíaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Baccharis punctulata (Asteraceae), popularly known as "Chíllka saru saru" in Bolivia, has been used by rural communities in Bustillo Province of the Potosi Department for treatment of asthma, luxations and contusions. AIM OF THE STUDY: To analyze the chemical composition of the essential oils obtained from leaves of female (BPF) and male (BPM) specimens and evaluate their anti-inflammatory and antioxidant properties. MATERIAL AND METHODS: Chemical composition analyses of Baccharis punctulata essential oils isolated by hidrodistillation from leaves of male and female specimens were performed by GC-FID-MS. The in vivo anti-inflammatory activity was evaluated using the model of TPA (12-O-tetradecanoylphorbol-13-acetate) induced ear edema, and the polymorphonuclear cell migration was evaluated by mieloperoxidase (MPO) and analyzed histologically. To measure the reactive oxygen species (ROS) in the inflamed tissue, the DCFH-DA fluorescent probe was used. The chemical in vitro antioxidant activity of essential oils was determined using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) free radical assay. RESULTS: The chemical analysis showed high proportion of sesquiterpenes in the volatiles samples obtained from BPM, such as δ-elemene (14.29%), germacrene D (11.29%) and bicyclogermacrene (10.90%), and in the sample from BPF, bicyclogermacrene (42.44%), germacrene D (21.18%) and ß-caryophyllene (14.06%). A statistical difference (pâ¯<â¯0.05) on chemical composition between both essential oils was observed. Topical administration of both BPM and BPF essential oils was able to inhibit the formation of TPA-induced edema in the treated groups. Isolated administration of TPA promoted an increase in MPO enzyme activity, and inhibition of the increase of MPO activity was observed when animals were treated with BFP at concentrations of 0.1â¯mg/ear (13.69⯱â¯0.20%), 0.3â¯mg/ear (22.35⯱â¯0.11%), and 1.0â¯mg/ear (44.98⯱â¯0.27%). Topical treatment with BPM was able to inhibit MPO activity at 22.40⯱â¯0.29% (0.1â¯mg/ear), 36.49⯱â¯0.07% (0.3â¯mg/ear) and 52.19⯱â¯0.28% (1.0â¯mg/ear). The positive control of dexamethasone (DEXA, 0.1â¯mg/ear) was able to revert the increase in the enzymatic activity of MPO caused by TPA (65.16%). Histological analysis showed that topical application of TPA promoted intense cellular infiltration. This inflammatory parameter was reduced with the topical application of the BPF and BPM oil samples as well as with DEXA. The results observed in the ROS and DPPH tests suggest that both samples were able to reduce the inflammatory cells influx and have in vitro antioxidant properties, respectively. CONCLUSIONS: This study presents, for the first time, the chemical composition of the essential oils obtained from leaves of male and female specimens of Baccharis punctulata, and their anti-inflammatory and antioxidant activities. The results presented by the volatile samples in our biotests support traditional uses of this plant species.
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Antiinflamatorios/farmacología , Antioxidantes/farmacología , Baccharis/química , Aceites Volátiles/farmacología , Administración Tópica , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/aislamiento & purificación , Antioxidantes/administración & dosificación , Antioxidantes/aislamiento & purificación , Dexametasona/farmacología , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Edema/tratamiento farmacológico , Femenino , Masculino , Ratones , Aceites Volátiles/administración & dosificación , Aceites Volátiles/aislamiento & purificación , Hojas de la Planta , Especies Reactivas de Oxígeno/metabolismoRESUMEN
The topical application of linoleic and linolenic acids is a potential prophylactic approach to migraine via an anti-inflammatory mechanism. We present a 45-year-old woman with chronic migraine without aura. Previous use of abortive or prophylactic therapies including sumatriptan, amitriptyline and topiramate had failed due to lack of efficacy or side-effects, especially vomiting. In search of a topical agent she performed an n-of-1 trial comparing application of linoleic acid (safflower oil) versus oleic acid (olive oil) for migraine relief. She found safflower oil to be effective. Topically applied safflower oil rich in linoleic and linolenic acids may offer a safe, easily applied, well-tolerated, effective anti-inflammatory approach for the prophylactic treatment of chronic migraine.
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Ácido Linoleico/administración & dosificación , Ácidos Linolénicos/administración & dosificación , Trastornos Migrañosos/tratamiento farmacológico , Animales , Femenino , Humanos , Masculino , Persona de Mediana Edad , Aceite de Oliva/administración & dosificación , Aceite de Cártamo/administración & dosificación , Aceite de Cártamo/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Jatropha 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 STUDY: To 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 METHODS: First, 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. RESULTS: J. 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. CONCLUSIONS: The results demonstrate the potentiality of J. gossypiifolia gel as a promising safe and effective topical anti-inflammatory agent for treatment of cutaneous inflammatory diseases.
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Antiinflamatorios/uso terapéutico , Edema/tratamiento farmacológico , Jatropha , Extractos Vegetales/uso terapéutico , Administración Tópica , Animales , Aceite de Crotón , Edema/inducido químicamente , Femenino , Geles , Masculino , Ratones , Fitoterapia , Hojas de la Planta , Pruebas de Irritación de la PielRESUMEN
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 ß-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.(AU)
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Humanos , Animales , Masculino , Ratones , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Croton , Edema/tratamiento farmacológico , Antiinflamatorios/química , Antioxidantes/química , Croton/química , Modelos Animales de Enfermedad , Oído , Aceites Volátiles/química , Aceites Volátiles/farmacología , Corteza de la Planta/química , Plantas MedicinalesRESUMEN
An extract of Zingiber cassumunar Roxb. (ZC) was encapsulated in niosomes of which a topical gel was formed. (E)-4-(3',4'-dimethoxyphenyl)but-3-en-1-ol or compound D detected by a gradient HPLC was employed as the marker and its degradation determined to follow zero-order kinetics. Niosomes significantly retarded thermal-accelerated decomposition of compound D in the gel (p < 0.05) but did not change the activation energy of compound D. Niosomes enhanced in vitro permeation rate of compound D from the gel. Topical applications of ZC noisome gel gave a faster change in tail flick latency than piroxicam gel and hydrocortisone cream (p < 0.05) while there were insignificant differences in anti-inflammatory activity up to 6 h using croton oil-induced ear edema model in mice (p > 0.05). Thus, encapsulation of ZC extract in niosomes enhanced chemical stability and skin permeation with comparable topical anti-inflammatory effects to steroid and NSAID.
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Antiinflamatorios no Esteroideos/metabolismo , Butanoles/metabolismo , Liposomas/metabolismo , Extractos Vegetales/metabolismo , Absorción Cutánea/efectos de los fármacos , Zingiber officinale , Administración Tópica , Animales , Animales Recién Nacidos , Antiinflamatorios no Esteroideos/administración & dosificación , Estabilidad de Medicamentos , Edema/tratamiento farmacológico , Edema/metabolismo , Geles , Liposomas/administración & dosificación , Masculino , Ratones , Ratones Endogámicos ICR , Técnicas de Cultivo de Órganos , Dimensión del Dolor/efectos de los fármacos , Dimensión del Dolor/métodos , Extractos Vegetales/administración & dosificación , Extractos Vegetales/aislamiento & purificación , Distribución Aleatoria , Absorción Cutánea/fisiología , PorcinosRESUMEN
Curcuma longa is a ginger family aromatic herb (Zingiberaceae) whose rhizomes contain curcuminoid pigments, including curcumin, a compound known for its anti-inflammatory effects. The objective of this study was to obtain curcuminoid-rich extracts, develop topical formulations thereof, and assess the stability and skin permeation of these formulations. Curcuma longa extracts were obtained and used to develop formulations. Skin permeation studies were conducted in a modified Franz diffusion cell system, and skin retention of curcuminoid pigments was quantified in pig ear membrane. Prepared urea-containing gel-cream formulations were unstable, whereas all others had satisfactory stability and pseudoplastic rheological behavior. The amount of curcuminoid pigments recovered from the receptor solution was negligible. The skin concentration of curcuminoid pigments retained was positive (>20 µg/g of skin, mostly in the stratum corneum), considering the low skin permeability of curcumin. We conclude that development of topical formulations containing curcumin or Curcuma longa extract is feasible, as long as adjuvants are added to improve preservation and durability. The formulations developed in this study enabled penetration of curcumin limited to the superficial layers of the skin and then possibly without a risk of systemic action, thus permitting local use as a topical anti-inflammatory.
Curcuma longa é uma erva aromática, pertencente à família Zingiberaceae e seus rizomas contêm pigmentos curcuminoides, dentre eles a curcumina, conhecida por seu efeito anti-inflamatório. O objetivo deste trabalho foi obter extratos ricos nestes pigmentos, desenvolver e avaliar a estabilidade de formulações tópicas e realizar o estudo da penetração cutânea. Extratos de Curcuma longa foram obtidos e utilizados no desenvolvimento de formulações. A penetração e retenção cutâneas de pigmentos curcuminoides foi avaliada em pele de orelha de porco, utilizando célula de difusão de Franz modificada. As formulações de gel creme preparadas que continham ureia foram instáveis e as demais apresentaram estabilidade satisfatória e comportamento reológico pseudoplástico. A quantidade de pigmentos curcuminoides encontrada na solução receptora foi insignificante, enquanto que a quantidade retida na pele foi superior a 20 µg/g de pele. Concluiu-se como possível o desenvolvimento de formulações tópicas contendo curcumina ou extrato de Curcuma longa, conciliando a adição de adjuvantes para a preservação e maior durabilidade da mesma. As formulações promoveram a penetração da curcumina limitada às camadas superiores da pele, possivelmente sem o risco de ocorrência de ação sistêmica sendo possível a sua utilização para ação local com atividade anti-inflamatória.