RESUMO
The aim of this work is to develop, optimize and characterize cold process emulsions that are stable at acidic pH. The main surfactant was selected according to the hydrophilic lipophilic balance (HLB) concept and surface tension, whereas polymers were selected by viscoelastic measurements and analytical centrifugation. It was showed that the inclusion of methyl vinyl ether/maleic anhydride copolymer crosslinked with decadiene (PVM/MA) increased the storage modulus (G') of the gels (23.9-42.1 Pa) two-fold and the droplet migration decreased from 3.66% to 0.95%/h. Cetrimide was selected as a preservative based on its microbiological results and additional contribution to the stability of the emulsions. Four emulsions were developed that differed by the co-emulsifier used (PEG-20 glyceril laurate and polyglyceryl-4-isostearate) and the glycol (2-methyl-2,4-pentanediol and ethoxydiglycol). Viscoelastic measurements and droplet size/microscopic analysis showed that the structure of PEG-20 glyceril laurate emulsion (η' = 76.0 Pa.s at 0.01 Hz and 32.9 ± 3.7 µm, respectively) was stronger compared to polyglyceryl-4-isostearate (η' = 37.4 Pa.s at 0.01 Hz and 37.8 ± 15.7 µm, respectively). Differential scanning calorimetry (DSC) results were in accordance with the latter and showed that PEG-20 glyceril laurate with 2-methyl-2,4-pentanediol corresponded to the strongest structure (|224.4| W °C g(-1)). This cold process allowed a total production savings of more than 17% when compared to the traditional hot process.
Assuntos
Emulsões/química , Óleos/química , Água/química , Cetrimônio , Compostos de Cetrimônio/química , Química Farmacêutica/métodos , Estabilidade de Medicamentos , Géis/química , Glicóis/química , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Maleatos/química , Tamanho da Partícula , Polietilenoglicóis/química , Polietilenos/química , Polímeros/química , Tensão Superficial , Tensoativos/química , Tecnologia Farmacêutica/métodosRESUMO
Dermatological inflammatory diseases often affect the scalp and the eyebrows. Common dosage forms available on the market for those situations are lotions; however, the presence of hair limits their use. Gels, for their consistency and adhesiveness, are a suitable alternative to the lotions in these situations. The aim of this study was to develop a new stable gel containing mometasone furoate (MF), with anti-inflammatory activity and a controlled delivery, to improve topical treatment of scalp dermatitis. Pharmaceutical development, physical and chemical characterization, stability, in vitro release and permeation studies and in vivo anti-inflammatory activity were performed. The gel presented an acidic pH and an apparent viscosity of 35 Pa.s. The microbiological analysis showed that the results were within the established specification limits. The release and the permeation profiles suggest that the drug is mainly retained in the upper skin layers. MF gel was tested in an animal model of cutaneous inflammation and presented similar anti-inflammatory activity compared to a commercially available MF dosage form. The gel was chemically, physically and microbiologically stable. The results suggest that the developed hydrogel formulation containing MF can be of actual value for improving the clinical effectiveness in the treatment of scalp dermatitis.
Assuntos
Anti-Inflamatórios/administração & dosagem , Preparações de Ação Retardada/química , Hidrogel de Polietilenoglicol-Dimetacrilato/química , Metilcelulose/análogos & derivados , Pregnadienodiois/administração & dosagem , Adesividade , Administração Cutânea , Animais , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/uso terapêutico , Dermatite/tratamento farmacológico , Feminino , Humanos , Derivados da Hipromelose , Metilcelulose/química , Camundongos , Pessoa de Meia-Idade , Furoato de Mometasona , Pregnadienodiois/farmacocinética , Pregnadienodiois/uso terapêutico , Couro Cabeludo/metabolismo , Pele/metabolismo , Absorção CutâneaRESUMO
Wastewater Treatment Plants (WWTPs) are potential sources of microplastics (MPs) in the aquatic environment. This study aimed to investigate the potential of wastewater-native microalgae consortia to remove MPs from the effluent of two different types of WWTPs as a dual-purpose solution for MPs mitigation and biomass production. For that purpose, the occurrence of MPs from two types of WWTP effluents was analysed over one year. MPs were characterized in terms of morphology (microbead, foam, granule, irregular, filament and film), colour and size. The wastewater characterisation was followed by the removal of MP loads, using native microalgae consortia, pre-adapted to the wastewater effluent. Microalgae consortia evolved naturally through four mitigation assays, adapted to seasonal conditions, such as temperature, photoperiod, and wastewater composition. MPs were present in all the effluent samples, ranging from 52 to 233 MP L-1. The characterisation of MPs indicated a predominance of white and transparent particles, with irregular and filament shapes, mainly under 500 µm in size. The µFTIR analysis revealed that 43% of the selected particles were plastic, with a prevalence of polypropylene (PP) (34%) and polyethylene terephthalate (PET) (30 %). In the mitigation experiments, substantial biomass production was achieved (maximum of 2.6 g L-1 (d.w.)), with successful removal of MPs, ranging from 31 ± 25% to 82 ± 13%. These results show that microalgae growth in wastewater effluents efficiently promotes the removal of MPs, reducing this source of contamination in the aquatic environment, while generating valuable biomass. Additionally, the strategy employed, requires minimal control of culture conditions, simplifying the integration of these systems in real-world WWTP facilities for improved wastewater management.
Assuntos
Microalgas , Microplásticos , Eliminação de Resíduos Líquidos , Águas Residuárias , Poluentes Químicos da Água , Águas Residuárias/química , Microalgas/metabolismo , Poluentes Químicos da Água/análise , Poluentes Químicos da Água/metabolismo , Eliminação de Resíduos Líquidos/métodos , Biodegradação Ambiental , BiomassaRESUMO
Ultradeformable vesicles (UDV) have recently become a promising tool for the development of improved and innovative dermal and transdermal therapies. The aim of this work was to study three related UDV: transfersomes, ethosomes, and transethosomes for the incorporation of actives of distinct polarities, namely, vitamin E and caffeine, and to evaluate the effect of the carrier on skin permeation and penetration. These actives were incorporated in UDV formulations further characterized for vesicles imaging by transmission electron microscopy; mean vesicle size and polydispersity index by photon correlation spectroscopy; zeta potential by laser-Doppler anemometry; deformability by pressure-driven transport; and incorporation efficiency (IE) after actives quantification by high-performance liquid chromatography. Topical delivery studies were performed in order to compare UDV formulations regarding the release, skin permeation, and penetration profiles. All UDV formulations showed size values within the expected range, except transethosomes prepared by "transfersomal method", for which size was smaller than 100 nm in contrast to that obtained for vesicles prepared by "ethosomal method". Zeta potential was negative and higher for formulations containing sodium cholate. The IE was much higher for vitamin E- than caffeine-loaded UDV as expected. For flux measurements, the following order was obtained: transethosomes (TE) > ethosomes (E) ≥ transfersomes (T). This result was consistent with the release and skin penetration profiles for Vitamin E-loaded UDV. However, the releasing results were totally the opposite for caffeine-loaded UDV, which might be explained by the solubility and thermodynamic activity of this active in each formulation instead of the UDV deformability attending to the higher non-incorporated fraction of caffeine. Anyway, a high skin penetration and permeation for all caffeine-loaded UDV were obtained. Transethosomes were more deformable than ethosomes and transfersomes due to the presence of both ethanol and surfactant in their composition. All these UDV were suitable for a deeper skin penetration, especially transethosomes.
Assuntos
Cafeína/administração & dosagem , Portadores de Fármacos/química , Lipossomos/química , Pele/efeitos dos fármacos , Vitamina E/administração & dosagem , Administração Cutânea , Administração Tópica , Antioxidantes/administração & dosagem , Estimulantes do Sistema Nervoso Central/administração & dosagem , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Sistemas de Liberação de Medicamentos , Humanos , Microscopia Eletrônica de Transmissão , Absorção Cutânea , SolubilidadeRESUMO
It is of crucial importance to evaluate the safety profile of the ingredients used in dermatological emulsions. A suitable equilibrium between safety and efficacy is a pivotal concern before the marketing of a dermatological product. The aim was to assess the safety and biological effects of a new cold processed silicone-based emulsion (SilEmulsion). The hazard, exposure, and dose-response assessment were used to characterize the risk for each ingredient. EpiSkin assay and human repeat insult patch tests were performed to compare the theoretical safety assessment to in vitro and in vivo data. The efficacy of the SilEmulsion was studied using biophysical measurements in human volunteers during 21 days. According to the safety assessment of the ingredients, 1,5-pentanediol was an ingredient of special concern since its margin of safety was below the threshold of 100 (36.53). EpiSkin assay showed that the tissue viability after the application of the SilEmulsion was 92 ± 6% and, thus considered nonirritant to the skin. The human studies confirmed that the SilEmulsion was not a skin irritant and did not induce any sensitization on the volunteers, being safe for human use. Moreover, biological effects demonstrated that the SilEmulsion increased both the skin hydration and skin surface lipids.