Vladi Olga Consiglieri

Effects of caffeine and siloxanetriol alginate caffeine, as anticellulite agents, on fatty tissue: histological evaluation

Background  Cellulite is a physiological condition that presents etiologic plurality. Caffeine and its derivatives are used in anticellulite cosmetics due to their lipolytic activity on fatty cells. Siloxanetriol alginate caffeine (SAC) is a silanol derived from organic silicon. Radicals primarily from SAC are caffeine and the mannuronic acid.

Functional photostability and cutaneous compatibility of bioactive UVA sun care products

Sunscreens are the most-established approach for photoprotection. The strategy of providing antioxidant properties to sun care products by addition of natural and potent anti-free radical compounds has led to the development of bioactive sunscreens, able to neutralize the harmful effects of ultraviolet (UV) radiation. UVA filters, such as benzophenone-3 (BP) and butyl methoxydibenzoylmethane (BMDBM), can exhibit photodegradation which limits the development of broad spectrum sunscreens. Previous research verified that rutin interacts with filters incorporated in sunscreens. In this work, we focused on the development and evaluation of the efficacy of the sunscreens containing either BP or BMDBM with and without rutin. The addition of rutin to the UVA filters afforded antioxidant properties to the formulations and they were considered safe for human use. Additionally, rutin in combination with either BP or BMDBM increased the antioxidant activity about 40 times when compared with the UVA filters alone. Remarkably, the addition of rutin 0.1% (w/w) to BP 6.0% (w/w) raised the SPF from 24.3±1.53 to 33.3±2.89. In conclusion, these findings demonstrated that the addition of rutin into sunscreens can markedly improve the antioxidant properties of the formulation as well as photostabilize some of the UVA filters.

Optimization of Pothomorphe umbellata (L.) Miquel topical formulations using experimental design

Pothomorphe umbellata is a native plant widely employed in the Brazilian popular medicine. This plant has been shown to exert a potent antioxidant activity on the skin and to delay the onset and reduce the incidence of UVB-induced skin damage and photoaging. The aim of this work was to optimize the appearance, the centrifuge stability and the permeation of emulsions containing P. umbellata (0.1% 4-nerolidylchatecol). Experimental design was used to study ternary mixtures models with constraints and graphical representation by phase diagrams. The constraints reduce the possible experimental domain, and for this reason, this methodology offers the maximum information while requiring the minimum investment. The results showed that the appearance follows a linear model, and that the aqueous phase was the principal factor affecting the appearance; the centrifuge stability parameter followed a mathematic quadratic model and the interactions between factors produced the most stable emulsions; skin permeation was improved by the oil phase, following a linear model generated by data analysis. We propose as optimized P. umbellata formulation: 68.4% aqueous phase, 26.6% oil phase and 5.0% of self-emulsifying phase. This formulation displayed an acceptable compromise between factors and responses investigated.

Derivative spectrophotometric method for determination of acyclovir in polymeric nanoparticles

A derivative spectrophotometric method was validated for quantification of acyclovir in poly ( n-butylcyanoacrylate) (PBCA) nanoparticles. Specificity, linearity, precision, accuracy, recovery, detection (LOD) and quantification (LOQ) limits were established for method validation. First-derivative at 295.2 nm eliminated interferences from nanoparticle ingredients and presented linearity for acyclovir concentrations ranging from 1.25 to 40.0 µg/mL (r = 0.9999). Precision and accuracy data demonstrated good reproducibility. Recovery ranged from 99.3 to 101.2. LOD was 0.08 µg/mL and LOQ, 0.25 µg/mL. Thus, the proposed method proved to be easy, low cost, and accurate, and therefore, an useful alternative to quantify acyclovir in nanoparticles.

Formulation and in vitro evaluation of theophylline-Eudragit® sustained-release tablets

Comprimidos contendo teofilina (66.67%) e polimeros de Eudragit® NE 30D e RS 30D entre 10 e 30% foram produzidos por compressao. A influencia das diferentes proporcoes de esteres do acido metacrilico, uso da lactose e fosfato de calcio tribasico como diluente, bem como os efeitos da adicao de estearato de magnesio como agente lubrificante hidrofobico na liberacao da teofilina foram estudados. Analises fisico-quimicas e teor de farmaco foram avaliados. Estudos da liberacao do farmaco in vitro foram conduzidos em fluido gastrico simulado (pH 1,2) e fluido intestinal simulado sem pancreatina (pH 7,5). Observou-se liberacao prolongada relativa de teofilina partindo de polimeros matriciais, em 7 horas de dissolucao. Estearato de magnesio a 0,5% e de Eudragit® NE 30D a 10% foi considerado o sistema de liberacao adequado para comprimidos matriciais comparado com de Eudragit® RS 30D nas mesmas condicoes (USP). Os resultados das analises fisico-quimicas apresentaram-se dentro das especificacoes. Modelos matematicos de ordem zero, primeira ordem e Higuchi foram aplicados para estudar a liberacao de teofilina nos comprimidos. Adicionalmente, foram calculadas a meia-vida (Td50%) e a velocidade de dissolucao (kd). O modelo de liberacao de Higuchi foi o que melhor representou a liberacao do farmaco nos comprimidos, sendo demonstrado que o principal mecanismo de liberacao foi a difusao.

Rutin increases critical wavelength of systems containing a single UV filter and with good skin compatibility

Ultraviolet (UV) radiation is responsible for sunburns, skin cancer, photoaging, and the production of reactive oxygen species (ROS). The awareness on preventing these deleterious effects made the use of anti‐UVB formulations an important part of population habits; however, despite the availability of several antioxidants capable of ROS scavenging, the pharmaceutical market lacks products associating UV filters with natural compounds of proven efficacy. Here, we investigated the effect of rutin, a flavonoid with antioxidant activity, associated with UVB filters in dermocosmetic preparations.

Influence of particle size on appearance and in vitro efficacy of sunscreens

A nanotecnologia se aplica a diversos setores da ciencia. Na area de cosmeticos, os investimentos tem reforcado a ideia de que nanoprodutos oferecem inumeros beneficios para os consumidores. A exposicao excessiva a luz solar pode causar efeitos indesejaveis, logo, a adicao de filtros UV em produtos cosmeticos e frequentemente usada como prevencao. O p-metoxicinamato de octila e a benzofenona-3 sao filtros UV amplamente utilizados em formulacoes de proteccao solar, que absorvem radiacoes UVB e UVA, respectivamente. Neste estudo, desenvolveram-se formulacoes de protetores solares na forma de nano e macroemulsao, mas compostos pelas mesmas materias-primas. A nanoemulsao foi obtida pelo metodo da temperatura de inversao de fases (PIT). As propriedades fisicas e funcionais foram avaliadas por analise visual, distribuicao de tamanho de particulas e por espectrofotometria de reflectância difusa. A nanoemulsao obtida apresentou brilho azulado, menor consistencia aparente quando comparada `a macroemulsao, estabilidade superior a 48 horas (22,0 ± 2,0 ° C) e distribuicao de tamanhos de particula bimodal, com media (media) de tamanhos ao redor de 10 nm (61%) e 4,5 µm (39%) . A macroemulsao apresentou aspecto leitoso, maior consistencia aaprente do que nanoemulsao, instabilidade apos 48 horas (22,0 ± 2,0 oC) e distribuicao de tamanhos de particula bimodal, com media (media) de tamanhos ao redor de 202 nm (9%) e 10,4 µm (91%). O perfil de eficacia das formulacoes fotoprotetoras permaneceu aparentemente similar, com base em resultados obtidos por ensaios de FPS in vitro, relacao UVA/UVB e comprimento de onda critico.

Dissolution Enhancement and Characterization of Nimodipine Solid Dispersions with Poloxamer 407 or PEG 6000

The solid dispersion approach is an alternative to increase drug solubility. Many carriers have been studied, but there is few information about poloxamer 407 (P407). Consequently, the objective of this study was to evaluate P407 as a carrier for nimodipine solid dispersions and to compare its solubility and dissolution rates with those from polyethylene glycol (PEG 6000). The solid dispersions were prepared by the hot melting and solvent methods and they were characterized by FTIR, DSC, solubility, and dissolution tests. The results indicated a three-fold increase in solid dispersions solubility in the presence with P407 than those prepared with PEG.

Physical and physicochemical stability evaluation of cosmetic formulations containing soybean extract fermented by Bifidobacterium animalis

Peel off facial masks, based on polyvinyl alcohol (PVA), are formulations that, after application and drying, form an occlusive film over the face. After removing, they provide cleanness, tensor and moisturizing effects, removing dead cells, residues and other materials deposited on the stratum corneous. The soybean extract fermented by Bifidobacterium animalis has sugars, amino acids, peptides, proteins and free isoflavonoids in high concentrations, when compared to the unfermented extract, providing benefits to the cosmetic formulations like anti-aging effect, moisture, tensor action and emollience. The cosmetic bases of peel off facial masks, added with 5.0% w/w of fermented soybean extract, were submitted to Preliminary and Accelerated Stability Studies. Eight (8) preparations were evaluated in several conditions of temperature (-10.0, 5.0, 22.0 and 45.0 oC) and time (maximum of 15 days), comparing the results with the initial condition (48 h after preparation). The variables observed were: organoleptic characteristics, pH and appearing viscosity value and film drying time. The preparation containing 17.0% w/w of PVA and 0.5% w/w of guar gum was selected between the eight preparations initially prepared, because it presented the best performance in the stability test, being recommended storage at low temperatures (5.0 oC).

Using fluid bed granulation to improve the dissolution of poorly water-soluble drugs

In this study, fluid bed granulation was applied to improve the dissolution of nimodipine and spironolactone, two very poorly water-soluble drugs. Granules were obtained with different amounts of sodium dodecyl sulfate and croscarmellose sodium and then compressed into tablets. The dissolution behavior of the tablets was studied by comparing their dissolution profiles and dissolution efficiency with those obtained from physical mixtures of the drug and excipients subjected to similar conditions. Statistical analysis of the results demonstrated that the fluid bed granulation process improves the dissolution efficiency of both nimodipine and spironolactone tablets. The addition of either the surfactant or the disintegrant employed in the study proved to have a lower impact on this improvement in dissolution than the fluid bed granulation process.