Prospective computational design and in vitro bio-analytical tests of new chemical entities as potential selective CYP17A1 lyase inhibitors.

The development and advancement of prostate cancer (PCa) into stage 4, where it metastasize, is a major problem mostly in elder males. The growth of PCa cells is stirred up by androgens and androgen receptor (AR). Therefore, therapeutic strategies such as blocking androgens synthesis and inhibiting AR binding have been explored in recent years. However, recently approved drugs (or in clinical phase) failed in improving the expected survival rates for this metastatic-castration resistant prostate cancer (mCRPC) patients. The selective CYP17A1 inhibition of 17,20-lyase route has emerged as a novel strategy. Such inhibition blocks the production of androgens everywhere they are found in the body. In this work, a three dimensional-quantitative structure activity relationship (3D-QSAR) pharmacophore model is developed on a diverse set of non-steroidal inhibitors of CYP17A1 enzyme. Highly active compounds are selected to define a six-point pharmacophore hypothesis with a unique geometrical arrangement fitting the following description: two hydrogen bond acceptors (A), two hydrogen bond donors (D) and two aromatic rings (R). The QSAR model showed adequate predictive statistics. The 3D-QSAR model is further used for database virtual screening of potential inhibitory hit structures. Density functional theory (DFT) optimization provides the electronic properties explaining the reactivity of the hits. Docking simulations discovers hydrogen bonding and hydrophobic interactions as responsible for the binding affinities of hits to the CYP17A1 Protein Data Bank structure. 13 hits from the database search (including five derivatives) are then synthesized in the laboratory as different scaffolds. Ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) in vitro experiments reveals three new chemical entities (NCEs) with half maximal inhibitory concentration (IC50) values against the lyase route at mid-micromolar range with favorable selectivity to the lyase over the hydroxylase route (one of them with null hydroxylase inhibition). Thus, prospective computational design has enabled the design of potential lead lyase-selective inhibitors for further studies.

Alopecia areata totalis and universalis: a multicenter review of 132 patients in Spain.

BACKGROUND: Alopecia areata totalis (AAT) and universalis (AAU) pose a therapeutic challenge. OBJECTIVE: To describe the clinical and epidemiological features, therapeutic response and prognostic factors in a large series of patients diagnosed with AAT and AAU. METHODS: This retrospective multicenter study included patients diagnosed with AAT/AAU with a minimum follow-up of 12 months. Response was assessed based on the regrowth of scalp hair. RESULTS: In all, 132 patients (92 women and 40 men) - 80 (61%) diagnosed with AAU and 52 (39%) diagnosed with AAT - were included. The median time between the presentation of alopecia areata (AA) and the development of extensive AA was 1 year and it was less than 4 years in 121 patients (91%). There was an initial response to treatment in 64% of patients, although only 14% presented a persistent response. Adverse side effects from the medications used were detected in 33% of patients. The prognostic factors associated with poor response were the presence of AAU and a positive family history of AA. CONCLUSIONS: Treatment of AAT and AAU is challenging. Although an initial regrowth may be achieved, the duration of response is usually short. There were no significant differences on the effectiveness or duration of response between the various systemic therapies.

Beard alopecia areata: a multicentre review of 55 patients.

BACKGROUND: Alopecia areata on the beard area (BAA) is a common clinical manifestation, but there are no studies about its characteristics. OBJECTIVE: To describe the epidemiology, comorbidities, clinical presentation, evolution, diagnostic findings and therapeutic choices in a series of patients with BAA. METHODS: This retrospective multicentre review included patients diagnosed with BAA as the first and unique clinical manifestation with at least 12 months of follow-up. Diagnosis was performed based on the typical clinical features. Extra-beard involvement was monitored in all cases. RESULTS: Overall, 55 male patients with a mean age of 39.1 years (range 20-74) were included. Twenty-five patients (45.5%) developed alopecia of the scalp during follow-up and more than 80% of cases appeared in the first 12.4 months. Clinical presentation of AA on the scalp was patchy AA (less than 5 patches) (52%), multifocal AA (28%), AA totalis (12%) and AA universalis (8%). Multivariate analysis revealed a trend of association between scalp involvement and family history of AA without statistical significance. CONCLUSIONS: According to this study, BAA may progress to scalp AA in a significant number of patients (45.5% of the patients with a follow-up interval of at least 12 months). In the group of patients who developed scalp AA, 80% of them did it within the first 12 months, so follow-up of patients with BAA is highly encouraged.

Study of frontal hairline patterns in Spanish Caucasian women.

BACKGROUND: Anterior hairline measurements and their possible relationship with androgen levels, sebum production, and skin hydration have not been reported in white Spanish women. MATERIAL AND METHODS: This was a prospective descriptive and analytical observational study conducted on 103 healthy premenopausal white Spanish women recruited from the health staff of Hospital Universitario Virgen Macarena in Seville, Spain. Measurements were made of anterior hairline implantation, sebum levels, and the degree of hydration of the stratum corneum. Androgen levels were also determined in 50 volunteers from this group 3 to 5 days after the end of the menstrual cycle. RESULTS: The mean age of the women was 29.7 years. A widow's peak was observed in 94.17% of the group. The mean dimensions of the widow's peak were a height of 1.01 cm and width of 2.13 cm. The mean hormone levels were within normal limits for our hospital's laboratory with the exception of 17-hydroxyprogesterone, with a mean level of 1.39 ng/mL (range, 0.6-5.9ng/mL; normal limits, 0.15-1.10 ng/mL). The mean prostate specific antigen level was 0.04ng/mL (range 0.02-0.08ng/mL; normal limits, 0.00-0.02ng/mL). CONCLUSIONS: The hairline measurements of the white Spanish women in this study differ from those reported in American women. Knowledge of this normal pattern of anterior hairline implantation can be important in the evaluation of women with female androgenetic alopecia with male pattern, frontal fibrosing alopecia, or other established scarring alopecia seeking a surgical solution by hair transplantation.

Hematological and biochemical blood values in wild populations of black howler monkeys (Alouatta pigra) of Campeche, México.

BACKGROUND: The clinical analyses of free-ranging New World primates are extremely limited. The aim of this study was to obtain baseline data of blood chemistry and hematological values of free-ranging Alouatta pigra. METHOD: 17 males and 17 females were captured. We collected blood from the caudal tail vein; conventional techniques were used to analyze the samples RESULTS: Hemoglobin, hematocrit, and erythrocytes were significantly higher in males than in females. In relation to biochemical blood values, albumin/globulin ratio, cholesterol, triglycerides, calcium, phosphorus, magnesium, and iron were significantly higher in males than in females, while creatinine was significantly higher in females than in males. CONCLUSIONS: In general, measured parameters are similar to those of other primates and will be used as reference values for futures studies.

Experimental-like affinity constants and enantioselectivity estimates from flexible docking.

Experimental-like affinity constants and enantioselectivity estimates, not predicted so far computationally, were obtained using a novel flexible modeling/docking combined strategy. The S- and R-warfarin-human serum albumin (HSA, site I) complexes were used as an interaction model. The process for a verified estimation includes the following: (i) ionized open chain forming at physiological pH (a recent focus); (ii) conformational search (molecular mechanics and Monte Carlo methods); (iii) rigid protein-flexible ligand docking (GlideXP) generating low energy paired S- and R-poses; (iv) graphical comparison against the X-ray crystal structure (unsatisfactory verification step); (v) quantum polarized ligand docking (insufficient verification step); (vi) induced fit docking (one pose satisfying the verification criterion; selection step); (vii) converting docking scores to affinity and enantioselectivity estimates (log K(S) = 5.43, log K(R) = 5.34, ES = K(S)/K(R) = 1.23) and numerical comparison against equivalent literature data from bioanalytical techniques (validation step); (viii) intermolecular forces explaining ES (hydrogen bonding and π-π interactions).

Rheological properties of emulsion templated oleogels based on xanthan gum and different structuring agents.

Oleogel design based on emulsions using food grade polymers is a potential strategy for replacing saturated and trans fats. The aim of this paper is the characterization of sunflower oil-based oleogels structured by a non-surface-active polysaccharide, xanthan gum (XG), in combination with different structuring agents, through an emulsion template approach, which consists in the dehydration of the continuous phase of an oil/water emulsion. Four types of molecules with different origins were used: a synthetic one, polysorbate Tween 80, and other three from natural sources: a protein (whey protein, WP), a lipid (soy lecithin, SL) and a polysaccharide (locust bean gum, LBG). All the emulsions had a high shear thinning character (s = 0.45) and a weak gel behaviour (tanδ = 0.2). Only the LBG emulsions presented significant differences, with higher values of viscosity and viscoelastic moduli. The resulting oleogels showed high gel strength, exhibiting a marked elastic behaviour typical of structured solid systems (G'>G'' and tanδ = 0.06). SL oleogels stood out for presenting the lowest firmness, although internal structure seems to be similar to the rest. Regarding to stability, measurements indicated a great oil binding capacity (90% approx.) after 24 h. It is concluded that obtaining stable and solid-like oleogels with liquid oil using a hydrophilic polymer (XG) combined with different food-grade structuring agents was possible. These systems have great potential in food reformulation, especially for saturated fat substitution.

Lesion-associated microglia and macrophages mediate corralling and react with massive phagocytosis for debris clearance and wound healing after LPS-induced dopaminergic depletion.

Neuroinflammation contributes to neuronal degeneration in Parkinson's disease (PD). However, how brain inflammatory factors mediate the progression of neurodegeneration is still poorly understood. Experimental models of PD have shed light on the understanding of this phenomenon, but the exploration of inflammation-driven models is necessary to better characterize this aspect of the disorder. The use of lipopolysaccharide (LPS) to induce a neuroinflammation-mediated neuronal loss is useful to induce reliable elimination of dopaminergic neurons. Nevertheless, how this model parallels the PD-like neuroinflammation is uncertain. In the present work, we used the direct LPS injection as a model inductor to eliminate dopaminergic neurons of the substantia nigra pars compacta (SNpc) in rats and reevaluated the inflammatory reaction. High-resolution 3D histological examination revealed that, although LPS induced a reliable elimination of SNpc dopaminergic neurons, it also generated a massive inflammatory response. This inflammation-mediated injury was characterized by corralling, a damaged parenchyma occupied by a vast population of lesion-associated microglia and macrophages (LAMMs) undertaking wound compaction and scar formation, surrounded by highly reactive astrocytes. LAMMs tiled the entire lesion and engaged in long-standing phagocytic activity to resolve the injury. Additionally, modeling LPS inflammation in a cell culture system helped to understand the role of phagocytosis and cytotoxicity in the initial phases of dopaminergic degeneration and indicated that LAMM-mediated toxicity and phagocytosis coexist during LPS-mediated dopaminergic elimination. However, this type of severe inflammatory-mediated injury, and subsequent resolution appear to be different from the ageing-related PD scenario where the architectural structure of the parenchyma is mostly preserved. Thus, the necessity to explore new experimental models to properly mimic the inflammatory compound observed in PD degeneration.

Presence of Anti-T. cruzi Antibodies in Inhabitants and Dogs of Two Rural Settlements in the Sierra de Los Tuxtlas, Veracruz, Mexico.

PURPOSE: The aim of this study was to identify the risk factors associated with house infestation by Triatoma dimidiata as well as with Trypanosoma cruzi infection in humans and owned dogs in two rural communities from the municipality of Catemaco, Veracruz, Mexico. METHODS: One hundred and 16 human blood samples and 34 dog blood samples were collected. The presence of anti-T. cruzi antibodies was determined using four different ELISA assays. Moreover, reactive ELISA sera from humans and dogs were processed by indirect immunofluorescence (IFI) to confirm the presence of anti-T. cruzi antibodies. RESULTS: Serologic tests for T. cruzi infection showed a prevalence of 5.1% (6/116) in humans and of 50% (17/34) in owned dogs. CONCLUSION: The presence of animals (dogs, chickens and wild animals), as well as some characteristics of house construction were identified as risk factors for infestation and infection. Complementary studies must be carried out to allow a better understanding of the transmission dynamics in the state of Veracruz, Mexico, and the implementation of adequate control programs.

Blood parameters are little affected by time of sampling after the application of ketamine in black howler monkeys (Alouatta pigra).

BACKGROUND: Ketamine hydrochloride is an anesthetic commonly utilized to obtain biological samples in various non-human primates. Its application alters individual hematologic and biochemical values. The aim of this study was to analyze its effect on blood parameters of Alouatta pigra. METHOD: We collected blood samples at 10 and 40 minutes after the application of ketamine in 12 adult female A. pigra living in free-ranging conditions. RESULTS: The analysis showed that 40 minutes after application of ketamine, the number of platelets, lymphocytes and concentration of phosphorus decreased; however, creatinine, cholesterol, triglycerides, and potassium values increased. CONCLUSIONS: Our results suggest that ketamine appears to have little effect on the hematology and blood biochemistry of Alouatta pigra females with respect to those reported for other non-human primates. It is also important to consider the elapsed time after their application when taking blood samples for proper interpretation of the hemogram of Alouatta pigra females.

[Quality of home medication collection in the Emergency Department: reconciliation discrepancies]. / Calidad de la recogida de la medicación domiciliaria en urgencias: discrepancias en la conciliación.

INTRODUCTION: The objective of the study was to assess home medication data collected at the Emergency Department in a tertiary hospital. It also aimed to identify whether any possible deficiencies in this collection were translated as reconciliation errors on admission, to analyse and classify these data and identify the pharmacological groups involved. METHOD: A prospective observational study was carried out which analysed the pharmacotherapeutic data collected at the Emergency Department. Patients who were admitted to the Pneumology and Internal Medicine wards at the Miguel Servet University Hospital in Zaragoza were included. A list of the home drugs taken before the hospital stay was compiled, assessing whether the quality deficiencies in data collected in the emergency department translated as reconciliation errors at admission. Unjustified discrepancies were considered and classified in line with the criteria of the consensus document on terminology, classification and assessment of the drug reconciliation programmes for 2009. RESULTS: We included 136 patients, finding reconciliation errors in 86.8%. The total number of reconciliation errors found was 519. The most frequent types were: omitting a drug, missing dose information, missing administration frequency information. Almost 40% of the reconciliation errors found in the Internal Medicine ward were not resolved, which was double that of the Pneumology ward. Most discrepancies were found for the Digestive System and Metabolism group (24%). CONCLUSIONS: The percentage of patients that experienced reconciliation errors was high (86%), observing an important opportunity to improve at patient admission to the Emergency Department.

Natural infection with Trypanosoma cruzi in three species of non-human primates in southeastern Mexico: A contribution to reservoir knowledge.

The mechanisms of infection and dispersion of Trypanosoma cruzi among animals, especially in the sylvatic environment, are still not entirely clear, and various aspects of the transmission dynamics of this parasite in the sylvatic environment are still unknown. T. cruzi is a parasite with a great biological and genetic diversity that infects a wide variety of hosts, therefore, transmission cycles of this parasite are complex. The objective of this study was to determine the prevalence of T. cruzi infection and analyze the genetic variability of the discrete typing units (DTUs) of the parasite in three non-human primate species (Alouatta palliata, Alouatta pigra, and Ateles geoffroyi) in southeastern Mexico. A total of one hundred sixty-four serum samples (42 samples of A. pigra, 41 samples of A. palliata (free-ranging) and 81 samples of A. geoffroyi (hosted in care centers)) were analyzed for the detection of anti-T. cruzi antibodies by ELISA assays. The seroprevalence of infection was 23.39% in A. palliata, 21.40% in A. pigra and 16.27% in A. geoffroyi. Additionally, presence of parasite DNA was assessed by PCR, and the identification of DTUs was performed by real-time PCR coupled to High Resolution Melting (qPCR-HRM). Different DTUs (TcI, TcII, TcIII, TcV and TcVI) were found in the analyzed monkeys. In addition, infection of monkeys was not associated with age or gender, but it was associated with the species. This study reveals the risk of infection in the study area and that the different DTUs of the parasite can coexist in the same habitat, indicating that T. cruzi transmission in the study area is very complex and involves many ecological factors. However, there is a need for long-term studies of host-parasite interactions to provide a solid understanding of the ecology of these species and to understand the dispersion strategies of T. cruzi.

Economic burden of recurrent Clostridioides difficile infection in adults admitted to Spanish hospitals. A multicentre retrospective observational study.

OBJECTIVE: Clostridioides difficile infection (CDI) is associated with increased hospital stays and mortality and a high likelihood of rehospitalization, leading to increased health resource use and costs. The objective was to estimate the economic burden of recurrent CDI (rCDI). METHODS: Observational, retrospective study carried out in six hospitals. Adults aged ≥18 years with ≥1 confirmed diagnosis (primary or secondary) of rCDI between January 2010 and May 2018 were included. rCDI-related resource use included days of hospital stay (emergency room, ward, isolation and ICU), tests and treatments. For patients with primary diagnosis of rCDI, the complete hospital stay was attributed to rCDI. When diagnosis of rCDI was secondary, hospital stay attributed to rCDI was estimated using 1:1 propensity score matching as the difference in hospital stay compared to controls. Controls were hospitalizations without CDI recorded in the Spanish National Hospital Discharge Database. The cost was calculated by multiplying the natural resource units by the unit cost. Costs (euros) were updated to 2019. RESULTS: We included 282 rCDI episodes (188 as primary diagnosis): 66.31% of patients were aged ≥65 years and 57.80% were female. The mean hospital stay (SD) was 17.18 (23.27) days: 86.17% of rCDI episodes were isolated for a mean (SD) of 10.30 (9.97) days. The total mean cost (95%-CI) per episode was €10,877 (9,499-12,777), of which the hospital stay accounted for 92.56. CONCLUSIONS: There is high cost and resource use associated with rCDI, highlighting the importance of preventing rCDI to the Spanish National Health System.

Gallium-assisted growth of silicon nanowires by electron cyclotron resonance plasmas.

The use of gallium droplets for growing Si nanowires (SiNWs) by electron cyclotron resonance plasmas is investigated. First, the relationship between evaporation time and resultant size of the gallium droplets is studied. Through the use of spectroscopic ellipsometry, the dependence of the surface plasmon resonance (SPR) energy on the droplet size is determined. From these gallium droplets, SiNWs were grown at 300 and 550 °C in electron cyclotron resonance plasmas containing SiH(4), Ar, and H(2). Scanning electron microscopy results show that tapered NWs are obtained for a wide range of growth conditions. Besides, it is found that H(2) plays an important role in the parasitic axial growth of the SiNWs. Namely, H(2) inhibits the radial growth and contributes dramatically to increasing the SiNW defects.

Modified Gaussian models applied to the description and deconvolution of peaks in chiral liquid chromatography.

The description of the profiles of chromatographic peaks has been studied extensively, with a large number of proposed mathematical functions. Among them, the accuracy achieved with modified Gaussian models that describe the deviation of an ideal Gaussian peak as a change in the peak variance or standard deviation over time, has been highlighted. These models are, in fact, a family of functions of different complexity with great flexibility to adjust chromatographic peaks over a wide range of asymmetries and shapes. However, an uncontrolled behaviour of the signal may occur outside the region being fitted, forcing the use of different strategies to overcome this problem. In this work, the performance of the LMG (Linear Modified Gaussian), PVMG (Parabolic Variance Modified Gaussian), and PLMG (Parabolic-Lorentzian Modified Gaussian) models is compared with variants obtained by combination of the modified Gaussian models with an equation that adds an exponential tail and with other functions that limit the growth of the independent variable. The behaviour of the approaches is checked through the simultaneous fitting of enantiomeric peaks showing a wide range of characteristics, obtained in the separation of drugs with chiral activity by liquid chromatography using enantioselective columns. The study is also carried out with the purpose of performing the deconvolution of the peaks of the enantiomers, when these are not completely resolved, in order to evaluate the enantiomeric fraction.

Antifungal susceptibility of oral isolates of Candida species from chronic kidney disease patients on chronic dialysis.

Chronic renal disease patients under chronic dialysis (CRDD) have a multifactorial immunological deterioration with an increased risk of Candida infections. Incidence of Candida infections is increasing. Choice of suitable antifungal agents is limited due to the resistance of some species to several antifungals. Aim of the present study was to identify the distribution and antifungal susceptibility patterns of oral isolated Candida species from infected and colonized patients, as well as to investigate the risk factors for oral infection in patients on dialysis. Cross-sectional study, approved by the institutional bioethics committees was performed in CRDD patients. Demographic, clinic data, and oral mucosa samples were obtained. Infection diagnosis was established clinically and confirmed with exfoliative cytology, each sample was plated on CHROMagar Candida and incubated at 36°C for 2 days. Yeast species were identified by carbohydrate assimilation ID 32C AUX system and the apiweb database. For the antifungal susceptibility test, the M44 A-3 method (CLSI) using fluconazole (FCZ), miconazole (MCZ), nystatin (NYS), and voriconazole (VCZ). Study included 119 participants, the main cause of CRD was nephropathy due to DM2 (58%), and three-fourths of the patients were under hemodialysis. Candida prevalence was 56.3% of 67 colonized or infected patients, 88 isolates were obtained. Principal identified species were C. albicans (51.1%), C. glabrata (25%), and C. tropicalis (14.8%). C. glabrata showed a reduced response to FCZ in 50% of isolates and C. albicans had a reduced response in 16% of the isolates. Antifungal agent with the least efficacious response or with the lowest susceptibility in the isolates of these patients was MCZ, followed by VCZ and FCZ, whereas NYS induced the best antifungal response.

Strongyloides stercoralis hyperinfection transmitted by liver allograft in a transplant recipient.

We describe a case of Strongyloides stercoralis hyperinfection in a liver allograft recipient 2.5 months after transplantation. The patient lives in Spain, which is not considered an endemic country for strongyloidiasis, and denied prior residence or travel to any known endemic area. The initial symptoms were fever and vomiting, and he subsequently developed a severe respiratory disease. An endoscopic biopsy of ulcerative lesions of the duodenum revealed massive mucosa infiltration by larvae and adult worms, which were also found in respiratory samples. The patient was successfully treated with combined therapy with albendazole and ivermectin. The strongyloides infection was transmitted by the liver allograft. The donor was from Ecuador and, retrospectively, his serum tested positive for S. stercoralis IgG antibodies. Additionally, the pancreas-left kidney allograft recipient from the same donor later developed an intestinal strongyloidiasis without hyperinfection syndrome. To our knowledge, this is the first confirmed case of S. stercoralis infection transmission from the same donor to two solid allograft recipients.

Risk factors for multidrug-resistant tuberculosis in a tuberculosis unit in Madrid, Spain.

The setting for this retrospective cohort study was a specialised tuberculosis unit in Madrid, Spain. The objective was to describe the risk factors for multidrug-resistant tuberculosis (MDR-TB). The medical records of all patients admitted to the unit were reviewed retrospectively to identify factors associated with multidrug resistance. Patients with positive culture for M. tuberculosis and with available drug-susceptibility tests were included. The variables assessed were age, gender, country of origin, homelessness, alcohol consumption, intravenous drug use, methadone substitution therapy, contact with a tuberculosis patient, sputum smear, site of disease, previous tuberculosis treatment, HIV infection, history of imprisonment, diabetes mellitus and chronic obstructive pulmonary disease. Thirty patients with MDR-TB and 666 patients with non-MDR-TB were included from the years 1997 to 2006. The only factors associated with MDR-TB in multivariate analysis were previous tuberculosis treatment (OR: 3.44; 95% CI: 1.58-7.50; p = 0.003), age group 45-64 years (OR: 3.24; 95% CI: 1.34-7.81; p = 0.009) and alcohol abuse (OR: 0.12; 95% CI: 0.03 to 0.55; p = 0.003). In our study, patients who had had previous treatment for tuberculosis, who were 45-64 years of age or who had no history of alcohol abuse were more likely to have MDR-TB.

Permeability and toxicological profile estimation of organochlorine compounds by biopartitioning micellar chromatography.

This paper points out the usefulness of biopartitioning micellar chromatography (BMC) as a high-throughput primary screening tool providing key information about the oral absorption, skin permeability (K(p)), brain-blood distribution coefficient (BB) and ecotoxicological parameters such as median lethal concentration (LC(50)) and bioconcentration factors of 15 organochloride compounds. The retention data of compounds in BMC conditions were interpolated in previously developed quantitative-retention activity relationships by our research group. Results show that the compounds studied readily cross the intestinal barrier (oral absorption > 90%) and the blood-brain barrier (log BB > 0.4). In addition, the organochlorines DDE, chlorobenzene, 1,3-dichlorobenzene and 1,2-dichlorobenzene are the compounds which can more quickly cross the skin barrier (log K(p ) > -0.74 cm/h). From a ecotoxicological point of view, it can be concluded that the most retained compounds, DDE, DDD, hexachlorobenzene and dicofol, are the most toxic and bioacumulative.

Mangiferin nanoemulsions in treatment of inflammatory disorders and skin regeneration.

In this paper mangiferin nanoemulsions were developed using hyaluronic acid of different molecular weight, in absence or presence of Transcutol-P. An extensive study was carried out on the physico-chemical properties of nanoemulsions. Nanosizer and transmission electron microscopy showed oil droplets average size 296 nm with monodisperses distribution (PI ≤ 0.30). The zeta potential was highly negative (-30 mV). FTIR analysis confirms the existence of physical interactions among compounds. Rheological measurements allowed to conclude that all formulations present a pseudoplastic behavior (s ∼ 0.4) in presence of the biopolymer. Moreover, mangiferin release depends on the molecular weight of the polymer. Permeability assays on pig epidermis showed that nanoemulsions with low molecular weight hyaluronic acid improve the permeation, being this effect more pronounced in nanoemulsions with Transcutol-P. Administration of mangiferin nanoemulsions on TPA-inflamed skin mice model provided an attenuation of oedema and leucocyte infiltration. Macroscopic appearance of mice skin lesions has a good correlation with the histological study. The topical application of these formulations shows an appropriate anti-inflammatory effect.