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Objective: Develop and assess a transdermal emulsion loaded with nanostructured lipid carriers for vitamin D3 supplementation. Methods: Vitamin D3 loaded nanostructured lipid carriers, produced via high shear homogenization and ultrasonication, were assessed for their particle size, distribution, morphology, zeta potential, entrapment efficiency, and cytotoxicity. They were incorporated into a transdermal vehicle, and the stability and ex vivo permeation were evaluated. Results: Spherical nanoparticles were developed with a particle size of 192.5 nm, a polydispersity index of 0.13, a zeta potential of -29.0 mV, and an entrapment efficiency of 99.75%. They were stable (particle size and distribution) for 15 days when stored in a refrigerator, and for 30 days at room temperature and 32 °C. The nanoparticles decreased the drug cytotoxicity against fibroblasts, as shown by IC50 (nanoparticle: 32.48 μg mL−1; vitamin D3: 16.73 μg mL−1). The emulsion loaded with nanoparticles minimized the degradation of vitamin D3 when compared with the nanoparticle dispersion. Additionally, the emulsion provided the skin permeation of vitamin D3 following the recommended daily allowance. Conclusion: To the best of our knowledge, this is the first study to use nanostructured lipid carriers for transdermal delivery of vitamin D. The developed formulation is a promising strategy to overcome the vitamin D3 variable oral bioavailability. It also represents a comfortable route of administration; thus it could be beneficial for patients and clinicians. However, further studies are needed to allow the permeation of larger amounts of vitamin D3, and the combination of these nanoparticles with microneedles would be interesting.

The use of nutraceuticals to improve skin properties and decelerate skin aging has been gaining attention among dermatologists, over the last years. In this article, we are presenting the theoretical scientific support for YulivTM Collagen Drink, a liquid supplement containing bovine type I collagen peptides, ascorbic acid and Camellia sinensis (green tea) extract and its benefits on the skin. The available literature shows that the ingredients contained in the supplement have the potential to improve of skin hydration, dermis collagen density, and decrease the fragmentation of the dermal collagen network—and therefore reduce wrinkles and sagging and improving elasticity. Additionally, other health benefits could also be observed, such as protection against oxidative stress, contribution to the normal function of the immune system and reducing tiredness and fatigue, and reduction of skin inflammation, improvement of elasticity and prevention of oxidation. For those benefits to be visible, it is likely that continuous use of at least 4 weeks is needed.

Summary Objective In this report, we investigated the effects of CitrusiM® (Citrus sinensis (L.) Osbeck dried extract) on body composition, defined in terms of two outcomes: percentage of lean mass and percentage of fat mass. Research methods & procedures A double-blind randomized experiment with overweight and obese volunteers was conducted in which the two variables were measured at baseline and three months afterwards. The treatment levels corresponded to three different daily doses of CitrusiM®: 0 mg (control), 0.5 g, and 1 g. All patients met with a nutritionist, and were given a standardized diet with their assigned treatments. At the end of three months, the intermediate outcomes of diet compliance (in percent) and amount of exercise (either none, low level, or high level) were recorded. The covariates that were collected for each subject were age, height, and sex. We analyzed the effects of the treatments on the two outcomes under a Bayesian framework of the Rubin Causal Model, and accounted for possible relationships between both diet compliance and exercise level and the three outcomes of interest in the analyses. Study registered under Research Ethics Committee of the Faculdade de Ciencias Medicas e da Saude de Juiz de For a (plataformabrasil.gov.br): Identifier no. 2.767.611. Results There was a statistically significant evidence that the treatment may increase lean mass and reduce fat mass. Conclusion A 3-month treatment with CitrusiM® (0.5 g or 1 g, daily) was able to increase lean mass, reduce fat mass, in the participants.

Objective Organic silicon has been linked to positive effects on the skin rejuvenation, mainly by the oral route. Thus, the main objective of the present study was to assess whether monomethylsilanetriol (MMST, a source of organic silicon) can deliver silicon to the epidermis and dermis, when applied topically in a cream. Once the hypothesis was confirmed, the present study also evaluated whether the product was toxic to keratinocytes; additionally, its possible antioxidant activity was assessed. Methods The ex vivo skin permeation profile was determined using human skin in Franz-cells equipment; cytotoxicity was assessed using HaCaT keratinocytes. Antioxidant capacity was determined as scavenging activity, measured according to the 1,1-diphenyl-2-picrylhydrazil free radical method. Results The permeation percentage was almost 60% of the applied MMST, with a large quantity of drug found in the viable epidermis and dermis. The cell viability assay showed no significant difference in the percentage of viable keratinocytes among the treated groups at the doses used. In terms of antioxidant activity, the IC50 value obtained was 2400 μg mL-1 . Low antioxidant activity, negligible toxicity for keratinocytes and a significant percentage of permeation were observed. Conclusion We provide evidence that MMST applied topically can deliver silicon to the skin in biorelevant levels for cosmetic purposes.

In this work, we focus on three ready-to-use vehicles: Fitalite, Versatile, and HRT Supreme Cream Base. Fitalite is a natural, light, hydrophilic gel-cream that contains vitamin E and oil bodies from plant sources (phytosomes), providing antioxidant and skinmoisturizing properties. Versatile is a vanishing oil-inwater cream base which retains its consistency with a broad range and high concentrations of active pharmaceutical ingredients, dermaceutical ingredients, and solvents. Finally, HRT Supreme Cream Base is a paraben-free, dye-free, fragrance-free O/W emulsion base, formulated with a complex of botanical oils to soothe and provide moisture to dry and sensitive skin. In the current study, we evaluated the beyond-use date of formulations containing estradiol, estriol, estrone, progesterone, and testosterone in combination, compounded with these three vehicles. Validated, stability-indicating high-performance liquid chromatography methods were used throughout a 180-day period. A beyond-use date of 180 days was observed for all vehicles stored both at refrigerated and at room temperature. The combination of five ingredients represents a worst-case scenario since there are more possibilities of cross reactions. Therefore, we expect the same or greater stability as individual ingredients are removed from the tested formulation. The extended beyond-use dates provide convenience for both the compounding pharmacist and the patient.

Imuno TF® is a nutritional supplement composed of isolated transfer factors (TF) from porcine spleen. It is composed of a specific mixture of molecules that impact functions of the biological systems and historically is linked to the immune system regulation. In this study, we demonstrate for the first time its proteomic analysis, nutritional composition, and safety profile in terms of mutagenic potential and acute oral dose (LD50). The obtained analysis indicated the product is a complex set of oligo- and polypeptides constituted of 163 different peptides which can potentially act on multiple mechanisms on the immune system pathways. The chemical composition showed low fat and low sugar content, saturated fatty acids-free, and the presence of 10 vitamins and 11 minerals. No mutagenic effect was observed, and the LD50 was 5000 mg kg−1 body weight. This accounts for a safe product to be used by the oral route, with potential benefits for the immune system.

The mixing process plays a pivotal role in the quality of pharmaceuticals and food/dietary supplements, as it can impact the homogeneity of the substances in their dosage form and affect characteristics such as dissolution and stability. Thus, the choice of the right mixing device is paramount for compounding pharmacies. In this paper, we evaluated the mixing efficacy of a new 3-axis mixer device and determined its optimal working conditions. Three different formulations were compounded with the device and a total of 540 individual assays were performed by HPLC or ICP-MS to validate its use, in addition to a direct comparison among it and two alternative mixing methods. The 3-axis mixer device was able to provide homogeneous mixtures and finished capsules with adequate content uniformity with a broad range of conditions of use (mixing times from 2 to 8 min, and speed of rotation from 10 to 100 rpm). In addition, the device was superior to classical mixing methods (such as the use of manually shaken plastic bags) and at least equivalent to well-established ones (Y-shaped mixer). Finally, we proposed a cleaning procedure that was also adequate to prevent cross-contamination among products compounded with the same device.

The number of COVID-19 patients is still growing exponentially worldwide due to the high transmissibility of the SARS-CoV-2 virus. Therapeutic agents currently under investigation are antiviral drugs, vaccines, and other adjuvants that could relieve symptoms or improve the healing process. In this review, twelve therapeutic agents that could play a role in prophylaxis or improvement of the COVID-19-associated symptoms (as add-on substances) are discussed. Agents were identified based on their known pharmacologic mechanism of action in viral and/or nonviral fields and are postulated to interact with one or more of the seven known mechanisms associated with the SARS-CoV-2 virus: (i) regulation of the immune system; (ii) virus entrance in the cell; (iii) virus replication; (iv) hyperinflammation; (v) oxidative stress; (vi) thrombosis; and (vii) endotheliitis. Selected agents were immune transfer factor (oligo- and polypeptides from porcine spleen, ultrafiltered at ®), anti-inflammatory natural blend (Uncaria tomentosa, Endopleura uchi and Haematoccocus pluvialis; Miodesin®), zinc, selenium, ascorbic acid, cholecalciferol, ferulic acid, spirulina, N-acetylcysteine, glucosamine sulfate potassium hydrochloride, trans-resveratrol, and maltodextrin-stabilized orthosilicic acid (SiliciuMax®). This review gives the scientific background on the hypothesis that these therapeutic agents can act in synergy in the prevention and improvement of COVID-19-associated symptoms.

Introduction: Cancer is a range of multifactorial diseases which have in common uncontrolled increase in the number of cells invading various tissues and organs. One of its leading etiological agents is sun exposure, and therefore the use of sunscreens plays an important role in cancer prevention. Objective : In this context, the aim of this study was to verify whether the selected naturally-derived raw materials (Oli-ola dry extract, Hibiscus dry extract, Raspberry ketones, Leucoanthocyanidins isolated from grapes and Resveratrol) present adequate photoprotective properties for the development of an innovative broad-spectrum sunscreen. Methods: The determination of sunscreen activity was made in vitro , and the following parameters were obtained: Sun Protection Factor (SPF), UVA Protection Factor (UVAPF), Critical Wavelength and Boots Star Rating. Results: Innovative products showed varied results (maximum SPF=46; maximum UVAPF=22), being that all of them showed to be promising for both parameters. However, the greatest protection was shown in the UVB region. Conclusion: Thus, the Oli-Ola, Hibiscus, Leucoanthocyanidins, Raspberry Ketones and Resveratrol species, grouped in a cosmetic base lotion, showed potential for the development of innovative sunscreen products. Additionally, the SPF should be confirmed in vivo . Key words: Photoprotection, Natural sunscreens, Polyphenols, Flavonoids, Broad spectrum.

Syzygium cumini (L.) Skeels (Myrtaceae) is known to contain phenolic compounds and antioxidant activity of its fruit, bark, and seeds have been investigated...

The purpose of this study was to evaluate the transmucosal permeation of progesterone and testosterone using Pentravan as its vehicle for vaginal delivery. Progesterone deficiency is a hormone imbalance that could lead to luteal-phase deficiency, which is a common problem in assisted reproductive technologies. Testosterone has been explored for treating postmenopausal symptoms, such as vaginal atrophy. The ex vivo experiments were performed using porcine vaginal mucosa and phosphate buffered saline + 0.5% 2-hydroxypropyl-ß-cyclodextrin as the receptor media, which was later quantified through high-performance liquid chromatography. The percentage of the permeated drug was 0.4% and 20.3% for progesterone and testosterone, respectively. The permeation studies revealed that testosterone formulated with Pentravan is potentially effective in reaching the bloodstream and acts locally, whereas progesterone was mostly retained in the mucosa.

Chemical form of silicon determines its absorption and bioavailability: particulate and polymerized forms exhibit minimal oral bioavailability, while monomers (maltodextrin-stabilized orthosilicic acid, M-OSA) and organic compounds (monomethylsilanetriol, MMST) may hypothetically be highly absorbed. This study aimed to investigate the dermatological effects of oral ingestion of silicon, either solid (M-OSA&ndash, SiliciuMax&reg, Powder) or liquid (MMST, SiliciuMax&reg, Liquid) on the skin, hair and nails of healthy volunteers, through a clinical trial (Registry number 2,032,724. Full protocol at Plataforma Brasil website). Patients were randomized to receive 5 mg of elemental Si, either M-OSA or MMST (group 1 and 2, n = 17 each) or placebo (group 3, n = 17) twice a day for 150 days. Clinical and patients&rsquo, subjective evaluations were conducted. Multispectral face imaging and hair mineral analysis were also performed. Use of M-OSA and MMST provided significant (p &lt, 0.05) betterment of facial wrinkles and UV spots. Changes were also observed at the end of the study in skin texture and length of eyelashes. Hair aluminum levels decrease with the treatments. Self-reported questionnaire indicated good satisfaction with both M-OSA and MMST. Continuous use of both M-OSA and MMST can provide improvements on skin parameters, as well as act as a detox agent for aluminum.

Background: Transdermal delivery is an alternative route for the administration of drugs. However, it requires the development of vehicles that allow the drugs to cross the layers of the skin and reach the systemic circulation. Objective: In this study, a new transdermal vehicle was evaluated using progesterone, estradiol, estradiol + estriol (Biest) and ketoprofen administered as model drugs. Methods: To evaluate the ex vivo permeation of the drugs, the Franz vertical diffusion cell with human skin was used. Results: After 24 h, the vehicle was able to deliver 18.32 µg/cm2 of progesterone and 92.07 µg/cm2 of ketoprofen through the skin to the receptor medium. The permeation percentages were 91%, 78.8%, 48.5%, 73.2%, and 63.6%, respectively, for estradiol, estradiol (Biest), estriol (Biest), progesterone and ketoprofen. For all drugs, sufficient amounts were delivered to achieve a systemic effect, and it was also possible to decrease the amount of emulsion applied. Thus, the vehicle demonstrated a high performance and the possibility of it being used for drugs that present difficulties in regards to administration by the transdermal route.

The objective of this study was to evaluate the feasibility of 10 commonly used active pharmaceutical ingredients (APIs) compounded in oral suspensions using an internationally used suspending vehicle (SyrSpend(®) SF PH4 liquid): (i) amlodipine, (as besylate) 1.0mg/mL; (ii) chloroquine phosphate,15.0 mg/mL; (iii) dapsone, 2.0 mg/mL; (iv) phenytoin, 15.0 mg/mL; (v) pyridoxine hydrochloride, 50.0 mg/mL; (vi) sulfadiazine, 100.0 mg/mL; (vii) sulfasalazine, 100.0 mg/mL; (viii) tetracycline hydrochloride, 25.0 mg/mL; (ix) trimethoprim, 10.0 mg/mL; and (x) zonisamide, 10.0 mg/mL. All suspensions were stored both at controlled refrigeration (2-8 °C) and controlled room temperature (20-25 °C). Feasibility was assessed by measuring the percent recovery at varying time points throughout a 90-day period. API quantification was performed by high-performance liquid chromatography (HPLC-UV), via a stability-indicating method. Given the percentage of recovery of the APIs within the suspensions, the expiration date of the final products (API+vehicle) was at least 90 days for all suspensions with regard to both the controlled temperatures. This suggests that the vehicle is stable for compounding APIs from different pharmacological classes.

Objective: The present in vitro study aimed to evaluate the photoprotective activity of four plant species from Brazil. Material and Methods: Plants ( Lippia brasiliensis , L. pseudothea , L. rotundifolia and L. rubella ) were collected in Minas Gerais state, Brazil, and ethanolic extracts were obtained. These were incorporated in neutral lotions and their SPF, UVAPF, UVA/ UVB Ratio and Critical Wavelength were determined by diffuse transmittance spectroscopy. Results: The best results were obtained with L. brasiliensis . It was demonstrated that this species generated an estimated in vitro SPF of 9 ± 1.0, and an effective UVAPF of 8 ± 0.7, at 15% in a neutral lotion. Conclusion: Broad spectrum sunscreens were obtained when all of four species were used as single UV filter in the sunscreens formulations, although L. brasiliensis presented the best UVA/UVB balance. Key words: Diffuse transmittance, Lippia , Natural products, Plant extracts, Sunscreens.

Resveratrol is a phenolic compound that has been widely studied in the last years because of its extensive pharmacological properties. It also has physicochemical properties that are adequate for diffusion through the human skin. An analytical method by high performance liquid chromatography was developed and validated for its determination in transdermal emulsion, as well in receptor media and skin layers. The trans-resveratrol release kinetic followed the Higushi's model (R(2) = 0.9926) with steady-state diffusion flux and lag time of 138.5 µg cm(-2) h(-1) and 0.49 h, respectively. It showed a percentage at 64.96 % for permeation. Thus, the results suggest that the emulsion studied is a potential vehicle for transresveratrol administration by transdermal route.

Orodispersible film can be defined as a solid pharmaceutical form intended for the delivery and rapid local or systemic release of active ingredients, consisting of a water-soluble polymer film that hydrates rapidly, adhering and dissolving immediately when placed on the tongue or in the oral cavity (oral, palatal, gingival, lingual, or sublingual), without the need for water administration or mastication. Due to its outstanding importance in cases of emergency, practicality of use by patients in transit, and high adherence, orodispersible film has evolved in popularity and success among consumers. It is a promising dosage form for compounding pharmacies, as simpler technologies are being developed to make the compound process easier and faster for the pharmacist. This article aims to explore some of the basics on orodispersible film and the main possible preparations to be developed in compounding pharmacies worldwide.

Background Taxifolin (TAX) is a flavonoid that has numerous pharmacological properties, including an antioxidant ability superior to that of other flavonoids due to its particular structure. Nevertheless, it has low oral bioavailability, which limits its therapeutic application. In this context, potentially important approaches for systemic drug delivery could be by alternative routes such as skin and vaginal mucosa, once both routes have a variety of advantages compared with the oral route, including the ability to bypass both first-pass hepatic metabolism and the consequent degradation in the gastrointestinal tract. Vaginal delivery could also account for a local effect, or an effect on circumvent microregion. Objective The major objective of this study was to develop and validate a high-performance liquid chromatography (HPLC) method for the determination of TAX in a semisolid dosage forms and then to evaluate ex vivo permeations across porcine vaginal mucosa and human skin. Methods TAX was incorporated into an oil-in-water emulsion developed previously by our group. Method for quantification was developed and validated using HPLC. Permeation through human skin and vaginal porcine mucosa were conducted in Franz-type cells. Results The method was precise (CV 0.99), specific, and robust. Permeation experiments through porcine vaginal mucosa and human skin presented permeated percentages equal to 87.43% and 48.09% (per dose), respectively. Conclusion The results suggest that, in the matrixes studied, TAX may be able to exert its biological activities systemically when applied by these routes. Furthermore, it exhibits greater permeability potential when administered by intravaginal route.

BACKGROUND Oxandrolone is a potent synthetic testosterone analogue that possesses strong anabolic property and weak androgenic activity. Apart of their clinical implicances, oral oxandrolone can potentially promote several adverse effects. It is known that the transdermal delivery of drugs may represent a means to avoid or minimize oral adverse effects Thus, the objective of this study was to evaluate the permeability of oxandrolone in human skin on a preliminary basis for possible future determination of the transdermal route as an alternative to oral treatments. METHODS We used a percutaneous absorption assay in Franz diffusion cells coupled with freshly excised human skin. The drug release kinetics were determined to predict the efficiency of this alternative route for the drug. RESULTS Nearly 236 μg (86.7%, in terms of applied dose) of the product was prevented to permeate due to the barrier function of the stratum corneum (SC); 21.6% reached the receptor medium (RM), and the remaining 4.3% were quantified within viable layers of the skin (in vivo, dermis is vascularized). The total amount of drug able to exert effect is the sum of the drug quantified within remained skin (RS) and RM: then, a total of 247.6 μg of oxandrolone (25.9% of the applied dose) would be able to permeate through a non damaged skin. The accuracy of the data is demonstrated by the calculated mass balance (average recovery = 112.6%). CONCLUSION Transdermal oxandrolone could be a viable alternative for traditional oral form, once clinical studies are conducted to prove this hypothesis.

The objective of this study was to evaluate the stability of 10 commonly used active pharmaceutical ingredients compounded in oral suspensions using an internationally used suspending vehicle (SyrSpend SF PH4): alprazolam 1.0 mg/mL, atropine sulfate 0.1 mg/mL, glutamine 250.0 mg/mL, levofloxacin 50.0 mg/mL, metoprolol tartrate 10.0 mg/mL, nitrofurantoin 2.0 mg/mL, ondansetron hydrochloride 0.8 mg/mL, oxandrolone 3.0 mg/mL, pregabaline 20.0 mg/mL, riboflavin 10.0 mg/mL. All suspensions were stored at both controlled refrigeration (2°C to 8°C) and controlled room temperature (20°C to 25°C). Stability was assessed by measuring the percent recovery at varying time points throughout a 90-day period. Active pharmaceutical ingredients quantification was performed by high-performance liquid chromatography via a stability-indicating method. Given the percentage of recovery of the active pharmaceutical ingredients within the suspensions, the beyond-use date of the final products (active pharmaceutical ingredients + vehicle) was at least 90 days for all suspensions with regard to both temperatures. This suggests that the vehicle is stable for compounding active pharmaceutical ingredients from different pharmacological classes.

Introduction Chronic stress and sleeping disorders have long been associated with anxiety. Pharmacological treatment includes benzodiazepines and selective serotonin reuptake inhibitors. The adverse effects associated with these medicines do, however, call for safer alternatives, including aromatherapy. The current study assesses the effect of intranasal administration of essential oils obtained from lavender, French lavender and fennel (Pinetonina™), on chronic stress. Methods Forty-five patients were divided in 3 groups: Group 1 (CTRL) received saline in nasal spray form; Group 2 (P30) received 30 % Pinetonina™ in buffered vehicle for intranasal spray; Group 3 (P50), 50 % Pinetonina™ in the same vehicle. All groups used the product for 3 months, once daily (before bedtime), using a spray-puff in each nostril. Salivary cortisol levels were measured in the beginning and at the end of the study. Quality of sleep, level of anxiety, perceived stress, and overall quality of life were measured through self-reported questionnaires. Results In P30 and P50, total salivary cortisol levels were significantly reduced by 37 % and 54 % respectively. Changes in perceived stress and overall quality of life showed no significant differences among the 3 groups, but P50 showed significant improvement in the quality of sleep index, as evaluated with the PSQI questionnaire. Salivary cortisol levels at time-zero and after 3 months of use were compared. Significant changes in the salivary cortisol levels for 30 % and 50 % of Pinetonina were seen after 3 months, unlike the control that showed no significant changes. Additionally, the Pittsburgh Sleep Quality Index when compared at baseline with the end of the study for the placebo and 30 % and 50 % Pinetonina. Significant changes in the quality of sleep were shown. Conclusions Daily intranasal use of Pinetonina™ before sleep was shown to significantly reduce salivary cortisol levels and improve quality of sleep based upon the significant differences found in the study.

Octocrylene (2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate) is present in several sunscreens and is known to work synergistically with UV filters. We prepared eight octocrylene-related compounds to test their photoprotective activities by measuring diffuse transmittance. The compounds had varied photoprotection profiles, with Sun Protection Factors (SPF) ranging from 1 to 5 and UVA Protection Factors (UVAPF) ranging from 1 to 8. Compounds 4, 5, and 7 showed the best protection against UVB sunrays, while compounds 5, 6, and 7 presented the best results for protection from UVA, so compound 7 had the most balanced protection overall. Results for compounds 4, 8, and 9 are reported for the first time in the literature.

Since the designs of optimal formulations for resveratrol permeation via the skin are lacking, the aim of this study was to establish the profile of resveratrol permeability into and across human skin. For that, a laboratory-made chromatographic column was used (Zr-PMODS), with its performance being compared to a traditional C18 column. In vitro drug release was conducted with polysulfone membranes, and the flux (JS) was 30.49 μg cm−2 h−1), with a lag time (LT) of 0.04 h, following a pseudo-first-order kinetics. For ex vivo percutaneous absorption using excised female human skin, the kinetic profile was the same, but JS was 0.87 μg cm−2 h−1 and LT was 0.97 h. From the initials 49.30 μg applied to the skin, 9.50 μg were quantified in the receptor medium, 20.48 μg was retained at the stratum corneum (do not account as permeated) and 21.41 μg was retained at the viable epidermis + dermis (account as permeated), totalizing 30.90 μg of resveratrol permeated after 24 h of application (62.6%). From these results, one can conclude that a person using the 1-g emulsion dose released by the pump containing 20 mg of resveratrol will have, theoretically, 12.53 mg of it liberated into his bloodstream, gradually and continuously for 24 h.

Despite the challenges in producing plant-derived photoprotective products, novel natural, broad-spectrum sunscreens have gained momentum in the cosmetic industry in the past few years. Traditionally, most of these products have been derived from plants producing polyphenolic and flavonoid compounds. In this study, we focused on plants belonging to the genus Lippia. The study aimed to develop a natural broad-spectrum sunscreen from a Lippia species that could be used as a single UV filter in formulation. Initially, UV transmission of sunscreens (10%, w/w) derived from four different Lippia species was determined to estimate their UVB protection factor (SPF). Next, the extract from species showing the best result was subjected to in vivo SPF and in vitro UVA radiation protection factor (UVAPF) determination using diffuse transmittance spectroscopy. The natural sunscreens obtained in vitro SPF values ranging from 1.7 to 7.6. The higher SPF was obtained with L. sericea species; the in vivo SPF of this sunscreen was 7.5 and its UVAPF was 2.97 when used as a single UV filter in a lotion. The photoprotective activity of this sunscreen was found to be related to the total polyphenolic content of the plant and not to its flavonoid content or antioxidant capacity. Thus, the results of this study suggested that the natural sunscreen from L. sericea has the potential to be used commercially.

In vitro release of bioidentical hormones in four different liposomal transdermal emulsions (containing testosterone, progesterone, estradiol, or estradiol and estriol) was assessed. For this purpose, novel high-performance liquid chromatography methods were developed and validated in an eco-friendly manner and used to determine the in vitro release of such products. The methods were suitable for our intended goal, and the emulsions employed were found to be effective as transporting candidates for the efficient release of hormones in the transdermal delivery of human sexual steroids.

Currently, the research and development of sunscreens play an important role on the synthesis of actives that are stable in various kinds of formulations—in addition to their efficiency and broad spectrum of protection against ultraviolet radiation. Our objective here was to synthesize new sunscreening chemical agents using quinoline as a base molecule. Twelve quinoline derivatives were synthesized, four of them novel molecules, and their photoprotective activity was determined in vitro using diffuse transmittance spectrophotometry. We determined their SPF, UVAPF, UVA/UVB ratio, critical wavelength and Boots Star Rating. The quinolines derivatives presented a varied profile of photoprotection, their SPF ranging from 2 to 11 and their UVAPF from 2 to 7. In terms of the critical wavelength, all molecules were considered of broad-spectrum by different classifications. Regarding the Boots Star Rating, one compound received no rating, seven of them received a three stars rating, three received a four stars rating and three were given a five stars rating. The molecules showed in the present work have a wide range of possibilities for creating new sunscreen products, once they have good SPF or UVAPF for single molecules, and they also possess other different qualities that can act synergistically.

Oral liquids are safe alternatives to solid dosage forms, notably for elderly and pediatric patients that present dysphagia. The use of ready-to-use suspending vehicles such as SyrSpend SF PH4 is a suitable resource for pharmacists as they constitute a safe and timesaving option that has been studied often. The objective of this study was to evaluate the stability of 10 commonly used active pharmaceutical ingredients (allopurinol 20 mg/mL; amitriptyline hydrochloride 10 mg/mL; carbamazepine 25 mg/mL; domperidone 5 mg/mL; isoniazid 10 mg/mL; ketoconazole 20 mg/mL; lisinopril 1 mg/mL; naproxen 25 mg/mL; paracetamol [acetaminophen] 50 mg/mL; and sertraline hydrochloride 10 mg/mL) compounded in oral suspensions using SyrSpend SF PH4 as the vehicle throughout the study period and stored both at controlled refrigerated (2°C to 8°C) and room temperature (20°C to 25°C). Stability was assessed by means of measuring the percent recovery at varying time points throughout a 90-day period. The quantification of the active pharmaceutical ingredients was performed by high-performance liquid chromatography through a stability-indicating method. Methods were adequately validated. Forced-degradation studies showed that at least one parameter influenced the stability of the active pharmaceutical ingredients. All suspensions were assayed and showed active pharmaceutical ingredient contents between 90% and 110% during the 90-day study period. Although the forced-degradation experiments led to visible fluctuations in the chromatographic responses, the final preparations were stable in the storage conditions. The beyond-use dates of the preparations were found to be at least 90 days for all suspensions, both for controlled refrigerated temperature and room temperature. This confirms that SyrSpend SF PH4 is a stable suspending vehicle for compounding with a broad range of different active pharmaceutical ingredients for different medical usages.

BACKGROUND Dentin hypersensitivity is a short, severe pain with fast onset. Therapy aims to either prevent or decrease neural transmission or physically occlude the dentinal tubules. This study aimed to evaluate the effectiveness of commercial desensitizing dentifrice by means of an ex vivo method. MATERIAL AND METHODS Samples (n=8 lower human premolars for each group) were randomly allocated into: G1- brushing with Colgate®Sensitive Pro-Relief; G2- brushing with Sensodyne®Rapid Relief; G3- brushing with Sensodyne®Repair & Protect; and G4- brushing with Colgate®Maximum Cavity Protection. The test bodies were submitted to simulated toothbrushing and dentifrices were analyzed regarding their hydrodynamic size, polydispersity index (PI) and zeta potential. Specimens were evaluated using: scanning electron microscopy (SEM); spectroscopy energy dispersive X-ray (EDS); and profilometry. A qualitative analysis of the photomicrographs and topographies was performed. RESULTS The dentifrices showed statistical similar physical and chemical characteristics. They also demonstrated obliteration of dentinal tubules when micrographs were observed. Regarding the chemical elements present in the dentin samples, there was a statistically significant difference between the control and experimental surfaces in the four groups. CONCLUSIONS Joint data analysis shows that the desensitizing dentifrice showed better results with regards to the obliteration of dentinal tubules compared to positive and negative controls. Key words:Dentin hypersensitivity, dentin desensitizing agents, toothpastes.

Resveratrol is a promising agent for protecting human skin from UV radiation and to reduce the occurrence of cutaneous malignancies. We describe the photoprotective activity of six resveratrol analogues using the diffuse transmittance technique to determine the SPF and the protection against UVA radiation. The analogues presented a varied profile of photoprotection, the SPF ranging from 2 to 10 and the UVAPF from 0 to 9. Among the six compounds tested, the protection against UVB sunrays provided by compound B was more significant than the protection provided by resveratrol; compounds C, D, E and F show photoprotection similar to resveratrol.

Background Resveratrol is a polyphenol that has gained momentum in therapeutics in the last few years. Objective In this study, we hypothesised that resveratrol could act prophylactically and/or treat inflammatory lesions of the oral cavity after being delivered by two different formulations of buccal mucoadhesive tablets (F1 and F2, which differed in terms of viscosity agents used). Methods This hypothesis was assessed through permeation studies, to verify diffusion of the drug through the buccal mucosa using a porcine model to predict human in vivo behaviour. Results F2 (tablet with less viscosity agent) presented better permeation than F1, but the amount of drug that crossed the mucosa was still low compared to the amount retained within it (35.90 µg found in the receptor medium and 15.63 mg quantified within the mucosa). Conclusion This accounted for a local effect rather than a systemic one, which is desirable for local processes, such as oral mucositis, lichen planus, erythema multiforme, nicotinic stomatitis, recurrent aphthous stomatitis, among others. In this sense, resveratrol-loaded mucoadhesive tablets appear to be a prominent alternative to prevent and/or cure inflammatory lesions of the oral cavity.

Objectives To evaluate the microbiological and physicochemical compatibility of commonly used proton pump inhibitors (PPIs) esomeprazole, lansoprazole, omeprazole and pantoprazole compounded at a single concentration using SyrSpend SF Alka and stored at refrigerated temperatures (omeprazole was also stored at room temperature because it has the most widespread use). Methods Compatibility was assessed by measuring the per cent recovery at varying time points throughout a 90-day period. Quantification of the APIs was performed by a validated high performance liquid chromatography (HPLC-UV) method. This same assay was also used to determine the dosage content uniformity of the suspensions. Microbiological stability (‘test in use’) was assessed during 60 days and total aerobic microbial count (TAMC), total combined yeasts and moulds count (TYMC), detection of Escherichia coli and pH determination were performed. Antimicrobial effectiveness testing was determined following European Pharmacopoeia guidelines. Results Beyond-use dates of maximum 60 days for omeprazole (5 mg/mL), pantoprazole (3 mg/mL) and esomeprazole (3 mg/mL) were established. All suspensions that met the physicochemical criteria for stability also met the content uniformity criteria. The suspensions showed no antimicrobial efficiency against bacteria, yeasts and moulds as SyrSpend SF Alka is an unpreserved vehicle, but the ‘test in use’ showed that the suspensions can remain microbiologically stable for up to 60 days. Conclusions SyrSpend SF Alka can be used to compound palatable (taste-masking properties) preservative-free oral suspensions with almost all commonly used PPIs.

The objective of this study was to evaluate the stability of 10 commonly used active pharmaceutical ingredients compounded in oral suspensions using SyrSpend SF PH4 (atenolol 1.0 and 5.0 mg/mL, clonazepam 0.2 mg/mL, dexamethasone 1.0 mg/mL, diclofenac sodium 5.0 mg/mL, diltiazem 12.0 mg/mL, enalapril maleate 1.0 mg/mL, ketoprofen 20.0 mg/mL, lamotrigine 1.0 mg/mL, penicillamine-D 50.0 mg/mL, thiamine 100 mg/m) and stored both at controlled refrigerated (2°C to 8°C) and room temperature (20°C to 25°C). Stability was assessed by means of measuring percent recovery at varying time points throughout a 90-day period. The quantification of the active pharmaceutical ingredients was performed by a stability-indicating, high-performance liquid chromatographic method. The beyond-use date of the products was found to be at least 90 days for all suspensions (except atenolol 1 mg/mL, which was stable up to 60 days), both for controlled refrigerated temperature and room temperature. This confirms that SyrSpend SF PH4 is a stable suspending vehicle for compounding with a broad range of different active pharmaceutical ingredients.

Background: The transdermal pharmaceutical forms had a limited usage for a long time, for it was believed that the stratum corneum, the outermost layer of epidermis, made it impracticable the permeation of medications through the skin. However, studies exploring this area of research came up and it was discovered that there are strategies to overcome this barrier, for example, creating a transdermal vehicle able to facilitate the drug absorption. Objective: This study aimed to develop a new transdermal vehicle and compare the permeation flux between products compounded with the innovative vehicle and commercial products, using nimesulide and piroxicam, non steroidal anti-inflammatory, as model drugs. Methods: Four different products were evaluated, two of them were the innovative containing the developed vehicle, and the other two were the commercial products, through ex vivo permeation experiment using Franz-type diffusion cell equipment, and as a membrane, human skin. For evaluation of permeated active pharmaceutical ingredients concentrations, we performed quantification from the receptor solution, stratum corneum and viable epidermis + dermis, through high-performance liquid chromatography analyses. Results: The innovative vehicle promoted increased permeation of active pharmaceutical ingredients through the viable epidermis and dermis, when compared to commercial products, but the stratum corrneum continued to keep the highest retention. Conclusion: The innovative vehicle was capable of enhancing the transdermal absorption of active pharmaceutical ingredients from the manipulated formulations, thus, demonstrating the capability thereof to improve the permeability of active pharmaceutical ingredients by transdermal use.

Com o intuito de se tratar problemas dermatológicos de hiperpigmentação, há uma tendência mundial no desenvolvimento de cosméticos que possuam propriedades despigmentantes, os quais agem inibindo a biossíntese de melanina. O objetivo deste trabalho foi avaliar in vitro a atividade de inibição da tirosinase de cogumelo de cinco óleos de plantas nativas da Amazônia e, desta forma, verificar a possibilidade de sua incorporação em produtos cosméticos. Ainda, a composição de ácidos graxos dos óleos foi determinada por cromatografia gasosa com detecção por ionização de chama, no intuito de determinar os principais componentes destes óleos. A atividade de inibição da tirosinase dos óleos testados foi encontrada na seguinte ordem: açaí (IA50 = 66,08 µg mL-1) >; tucumã >; patauá >; pracaxi >; castanha do Brasil. Este estudo sugere que o óleo de açaí possui grande potencial para o tratamento da hiperpigmentação cutânea e doenças correlatas, devido à sua considerável atividade de inibição da tirosinase. In order to treat hyperpigmentation-related problems, there has been a global trend in developing cosmetics claiming to have skin-whitening properties, which act by inhibiting melanin biosynthesis. The objective of this work was to evaluate the in vitro mushroom tyrosinase inhibitory activity of five Amazonian native flora oils, and so to verify the possibility of their incorporation into cosmetic products. In addition, the fatty acid composition of the essential oils was determined by gas chromatography-flame ionisation detection in order to determine the main components of these oils. The tyrosinase inhibitory activity of the tested oils was found to be in the following order: açaí (IA50 = 66.08 µg mL-1) >; tucumã >; patauá >; pracaxi >; castanha do Brasil. This study suggests that açaí oil has great potential in the treatment of hyperpigmentation and other related disorders, due to its considerable tyrosinase inhibitory activity.

In this work, a dissolution test for oxcarbazepine capsules was developed and validated. For the screening study, a mixed-level factorial design containing factors at three and two levels (3² × 2) was used in order to select the stirring speed, the dissolution medium and the dissolution apparatus. This strategy is needful for reducing the time of method development and to provide less ambiguous data. The best in vitro percentage dissolution was obtained using apparatus paddle at 80 rpm and sodium lauryl sulfate 1% m/v aqueous solution as the dissolution medium. The quantification of the mass dissolved was obtained by UV-Vis spectrophotometric analysis at 304 nm. The validation results demonstrate that the method was precise and linear over the range of 83-249 µg mL-1 of oxcarbazepine. Thus, the method is useful and adequate for oxcarbazepine capsules dissolution test, once there is no official monograph regarding it. Neste trabalho foi desenvolvido e validado um teste de dissolução para cápsulas de oxcarbazepina. Para o estudo de triagem, foi utilizado um planejamento experimental de níveis mistos composto de fatores com dois e três níveis (3² × 2), de modo a selecionar a velocidade de agitação, o meio de dissolução e o aparato. Esta estratégia é útil, pois reduz o tempo de desenvolvimento do método e também gera resultados mais exatos. A melhor porcentagem de dissolução foi obtida utilizando o aparato pá a 80 rpm e com solução aquosa de laurilsulfato de sódio a 1% m/v como meio de dissolução. A quantificação da massa dissolvida foi realizada por análise espectrofotométrica UV-Vis a 304 nm. Os resultados do estudo da validação demonstraram que o método é preciso e linear no intervalo de 83-249 µg mL-1 de oxcarbazepina. Os resultados evidenciaram que o método apresenta utilidade e adequabilidade para o estudo da dissolução de cápsulas de oxcarbazepina, uma vez que não existe método oficial com este propósito.

Objectives The objective of this study was to evaluate the compatibility of 10 commonly used active pharmaceutical ingredients (APIs) compounded in oral suspensions using a globally available suspending vehicle (SyrSpend SF PH4 liquid): caffeine 10.0 mg/mL, carvedilol 1.0 mg/mL, clomipramine hydrochloride 5.0 mg/mL, folic acid 1.0 mg/mL, hydrochlorothiazide 5.0 mg/mL, loperamide hydrochloride 1.0 mg/mL, methotrexate 2.5 mg/mL, nadolol 10.0 mg/mL, naltrexone hydrochloride 1.0 mg/mL and pentoxifylline 20.0 mg/mL, stored at both controlled refrigerated (2–8°C) and room (20–25°C) temperature. Methods Compatibility was assessed by measuring the per cent recovery at different time points throughout a 90-day period. Quantification of the APIs was performed by high performance liquid chromatography (HPLC-UV) using a stability-indicating method. Results Methods were adequately validated. Forced degradation studies showed that at least one parameter influenced the stability of the APIs. All suspensions were assayed and showed API contents of between 90% and 110% over 90 days. Discussion Given the percentage of recovery of the APIs within the suspensions, the expiration date of the final products (API+vehicle) was found to be at least 90 days for all suspensions, for both controlled refrigerated and room temperature. Conclusions The results suggest that SyrSpend SF PH4 liquid is a stable suspending vehicle for compounding APIs from different pharmacological classes.

Trans-resveratrol affects biological systems in a multitude of ways, but its oral bioavailability is remarkably poor due to in vivo metabolization. This drawback has fomented the development of new strategies for systemic delivery, such as transmucosal delivery via the vaginal route, which is our main focus here. In this sense, our pioneering study purposed to evaluate the trans-resveratrol permeation efficacy through this route. For that, we used a previously validated method and tested it with three different stationary phases: a commercial C18 column and two laboratory-made chromatographic columns containing poly(methyloctadecylsiloxane) (PMODS) thermally immobilized onto zirconized silica (Zr-PMODS) or titanized silica (Ti-PMODS). The permeation experiments showed that resveratrol, in the formulation used, was not successfully delivered to the bloodstream - it was actually retained within the vaginal mucosa, which suggests a local use rather a systemic one.

International audience; Studies have been demonstrating that smaller particles can lead to unexpected and diverse ecotoxico-logical effects when compared to those caused by the bulk material. In this study, the chemical composition, size and shape, state of dispersion, and surface's charge, area and physicochemistry of micro (BT MP) and nano barium titanate (BT NP) were determined. Green algae Chlorella vulgaris grown in Bold's Basal (BB) medium or Seine River water (SRW) was used as biological indicator to assess their aquatic toxicology. Responses such as growth inhibition, cell viability, superoxide dis-mutase (SOD) activity, adenosine-5-triphosphate (ATP) content and photosynthetic activity were evaluated. Te-tragonal BT (*170 nm, 3.24 m 2 g-1 surface area) and cubic BT (*60 nm, 16.60 m 2 g-1) particles were negative , poorly dispersed, and readily aggregated. BT has a statistically significant effect on C. vulgaris growth since the lower concentration tested (1 ppm), what seems to be mediated by induced oxidative stress caused by the particles (increased SOD activity and decreased photo-synthetic efficiency and intracellular ATP content). The toxic effects were more pronounced when the algae was grown in SRW. Size does not seem to be an issue influencing the toxicity in BT particles toxicity since mi-cro-and nano-particles produced significant effects on algae growth.

Manufactured nanomaterials are used in many commercially available consumer products, such as cosmetics, textiles, and paints. Due to the increasing production volumes, environmental exposure to these materials is evident. Here, we will discuss the toxicological impact of some nanomaterials, such as ZnO, TiO2, and BaTiO3 nanoparticles on aquatic microorganisms by giving some examples. It is clear that the physicochemical properties as well as the structure and morphology of nanomaterials have a high influence on toxicity. We will emphasize the importance of nanomaterial characterization before biological tests.

A monolithic stationary phase based on 3-(methacryloxypropyl)trimethoxysilane monomer, prepared within a fused silica capillary externally coated with a UV-transparent fluoropolymer was employed for separation of estriol, 17-b-estradiol and progesterone by capillary electrochromatography in a standard mixture. A 23 factorial design was used to optimize the separation system. The optimized condition containing 30% (v/v) of acetonitrile and 10 mmol L-1 aqueous ammonium acetate presented a total run time less than 10 min by applying 25 kV. The resolution between adjacent peaks ranged from 1.8 up to 2.9 and the plate numbers per column meter in this condition was 1873, 3631 and 3886 for the estriol, 17-b-estradiol and progesterone peaks, respectively. The optimized method was employed in the quantitative analysis of a commercial transdermal emulsion formulation.

Resveratrol is a natural substance that has been the target of many researchers over the years since it presents a variety of potential applications in the areas of cosmetics and medicine as a treatment for some diseases. Due to its high antioxidant capacity but low bioavailability, we evaluated the antiaging potential of resveratrol as a liotropic liquid crystal emulsion. Initially, we performed in vitro assays to quantify both the organoleptic characteristics and stability of the emulsion. Next, an in vivo trial was performed on the faces of 30 volunteers to determine the cream’s cosmetic potential and to measure porphyrins, skin barrier function, skin pigmentation, expression lines, and porosity. The emulsion maintained its characteristics during the in vitro assays and, in the in vivo trial, it had some effect only on pore size in forehead, without any significant effects on the other parameters. We had 6 dropouts throughout the study, then the final number of volunteers was 24. Most volunteers did not show any changes in skin pigmentation throughout the study. Similarly, there was not any noticeable improvement on any other parameters evaluated. However, volunteers related a high level of satisfaction with the product.

There is a lack of studies on Pentravan cream, a widespread transdermal vehicle which is used by compounding pharmacies. The purpose of this study was to evaluate this transdermal vehicle. The permeation performance for progesterone, estradiol, and estriol in formulations containing each of those drugs separately, as well as an association of estradiol + estriol (Biest), was evaluated regarding their compounding process and their potential biological application. An excised female human skin model was used to predict the permeation and the retention of the active compounds in every skin layer in lieu of conventional tape stripping. Progesterone was the drug with the highest permeation (37.02 mcg cm(-2) at the end of the experiment). Estradiol and estriol in Biest had permeations approximately 4-fold lower (9.44 mcg cm(-2) for estradiol-Biest and 14.02 mcg cm(-2) for estriol-Biest), and the profiles of estradiol in Eemuls and in Biest were almost the same (9.46 mcg cm(-2) for Eemuls). All permeations followed pseudo- first order kinetics. For progesterone, using the percentage of permeation by dose, one can infer that a patient using the 1-g emulsion dose released by the pump containing 50 mg of progesterone will have 38.4 mg of progesterone liberated into his bloodstream, gradually and continuously for 48 hours. The results indicate that the vehicle was able to provide percutaneous absorption rates compatible with and higher than clinical treatment needs. Using the same rationale, the Eemuls would deliver practically the entire amount of estradiol load per dose (1.0 mg), approximately 0.5 mg of estradiol per day. As for the Biest, the dosing used would deliver almost 0.5 mg estradiol/day and 2.0 mg estriol/ day. Thus, according to the results, human female sexual hormones incorporated in the oil-in-water vanishing cream base and applied topically are expected to exert their biological activities systemically with good efficacy due to their satisfactory permeation through human skin. However, one must take into account that a high quantity of drug was delivered. Thus, to avoid patient overdose, care has to be taken regarding the quantity of emulsion used.