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The wound healing potential of a topical herbal formulation containing “buriti” oil (Mauritia flexuosa L.f., Arecaceae) in a liquid crystalline phase consisting of “murumuru” (Astrocaryum murumuru Mart., Arecaceae) butter was evaluated. The fatty acid composition of “buriti” oil and murumuru butter was determined by gas chromatography coupled with flame ionization detection, which revealed that the major component of Mauritia flexuosa oil was oleic acid (70.4%), followed by palmitic acid (17.4%), whereas Astrocaryum murumuru butter contained lauric acid (40%) and myristic acid (29.3%). The ternary phase diagram was constructed from the mixture of the components (murumuru butter/Procetyl®/water) in order to obtain the Astrocaryum murumuru butter–based liquid crystal phase and two new herbal formulations containing 1% and 15% of Mauritia flexuosa oil. The phase behaviors were characterized by polarized light microscopy which showed that the analyzed formulations exhibited a hexagonal liquid crystalline phase. The designed formulations were subjected to physicochemical analysis and showed appropriate pH ranging from 5.90 to 6.45 and desirable rheological properties for skin application, such as pseudoplasticity. The wound healing potential of the topical herbal formulation was evaluated in Wistar rats over a period of 21 days. The formulations containing 15% of Mauritia flexuosa oil showed a significant effect (p < 0.05) on the epithelial regeneration process, causing early re-epithelialization of the injured tissue. The in silico prediction of skin sensitization showed that none of the identified compounds had any potential skin toxicity for humans.

A new consumer profile for pharmaceutical and cosmetic products has motivated research into natural raw materials in the development of “green” products such as herbal medicines and biocosmetics. However, various limitations have been encountered in the marketing of these products, for example the quality control of the natural raw materials used by the industrial market. This study aims to evaluate the sensory and physicochemical parameters of murumuru (Astrocaryum murumuru Mart.), bacuri (Platonia insignis Mart.), tucuma (Astrocaryum vulgare Mart.), and ucuuba (Virola sebifera Aubl.) butters for applications in pharmaceutical and cosmetic bioproducts. The acidity and saponification as well as the iodine and peroxide indexes were evaluated and fatty acid profiles for the samples obtained by GC-MS. The sensory properties of the butters showed the appearance of solid to soft cream, color (yellow, brown, buttercup, and ochre), and characteristic odor. The melting temperatures of all butters ranged between 31 oC and 49 °C. The acidity, saponification, iodine and peroxide indexes for the butters were of 5.82 – 17.73 mg (NaOH or KOH) g−1, 181.10 – 573.55 mg KOH g−1, 2.78 – 44.96 gl2 100 g−1, and 1.39 – 9.30 meq kg−1, respectively. From analyses of the fatty acid profiles, the major components identified were lauric acid in murumuru (40%) and ucuuba butters (73%), myristic acid in tucuma butter (53%), and palmitic acid in bacuri butter (42%). In general, the results of the analyses differed from the specifications of the supplier reports and official compendia. These findings highlight the importance of quality control in natural raw materials to ensure their functionality in pharmaceutical and cosmetic bioproducts.

We comparatively evaluate two distinct formulations containing 5% of Jucá (Libidibia ferrea) for wound healing in dogs. An excision model study was performed in 11 dogs with three dermal wounds in each animal, which were treated with: (1) topical phytopharmaceutical based on Carbopol (PyC) containing 5% Jucá ethanolic extract; (2) topical phytopharmaceutical based on Astrocaryum murumuru butter (PyM) containing 5% Jucá ethanolic extract; and (3) commercial ointment (control). Wound treatment was carried out on alternated days starting at day (D) one until D21. Macroscopic (all time-points) and histological (D0 and D21) analyses were performed. The antimicrobial activity of Jucá was evaluated through Minimal Inhibitory Concentration (MIC). Phytochemical analysis of Jucá revealed 3.1% phenolic compound content expressed in rutin and the presence of hydrolyzable tannins and flavonoids. The mean wound retraction was 33.7 ± 5.5, 34.0 ± 4.7, and 28.4 ± 4.9 % for PyC, PyM, and control groups, respectively, with higher wound retraction for both herbal-treated groups compared to the control (P < 0.05). Alcoholic extract of Jucá had antimicrobial activity against the microorganisms Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida krusei at different degrees, with MIC ranging from 250 to 16.625 μg/ml. Microscopic evaluation showed that the phytotherapic formulations contributed to better dermal wound healing through wound fibroplasia. The alcoholic extract of Jucá pods has great potential for wound healing in dogs and can be used in the development of commercially viable phytotherapic formulations.

Made available in DSpace on 2018-12-11T17:29:07Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-08-01 This article reports the development of a precursor liquid crystalline system based on a mixture of monoglycerides (MO) and Cremophor® (CREM) that exhibits in situ gelation to a liquid crystalline phase. The effects of different MO/CREM ratios and the water content (WC) on several performance characteristics were investigated with a full factorial design. The formulations were characterized by polarized light microscopy, small-angle X-ray scattering, and water uptake assays. Rheological, syringeability, and mucoadhesion evaluation were also performed. The polarized light microscopy and small-angle X-ray scattering results for average and high MO/CREM ratios (2.1 and 4.0, respectively) indicated the coexistence of phases in transition to the liquid crystalline phase, independently of the WC. These systems became more viscous after taking up water, showing peaks characteristic of a cubic phase. Systems that had average and high MO/CREM ratios also exhibited shear-thinning behavior and high elasticity. Most systems showed suitable mucoadhesion for buccal purposes. Response surface methodology results demonstrated that the relative contribution of MO was the principal factor that affected the performance of the system. Accordingly, these precursor systems with average to high MO/CREM ratios and an average WC (10% w/w) demonstrated physicochemical and mucoadhesive properties that could enable them to be used as an in situ-gelling controlled drug delivery platform. Department of Pharmaceutical Sciences of Ribeirão Preto USP—University of São Paulo Department of Chemistry UFS—Federal University of Sergipe Department of Pharmaceutical Sciences Health Science Center UEL—State University of Londrina Department of Pharmaceutical Sciences Chemistry Institute of Araraquara UNESP—São Paulo State University Department of Pharmaceutical Sciences Chemistry Institute of Araraquara UNESP—São Paulo State University

A doença periodontal é uma patogenia que afeta as estruturas de suporte dos dentes com formação da bolsa periodontal, e caso não tratada, em estágios mais avançados o periodonto é destruído, ocasionando perda do dente. O tratamento concerne em duas etapas, à remoção mecânica do biofilme e cálculo dentário por raspagem e alisamento radicular e utilização de antimicrobianos. Ainda é comum a utilização de antimicrobiano de ação sistêmica, embora, tenha eficácia reduzida e frequentes efeitos adversos. Em face disto, justifica-se o desenvolvimento de sistemas de liberação sustentada de fármaco intrabolsa periodontal a fim de sanar os inconvenientes da terapia sistêmica. Contudo, aspectos como espaço anatomofisiológico e fluído gengival crevicular intrínsecos à bolsa, são limitações pertinentes durante o desenvolvimento. Portanto, este trabalho teve como objetivo desenvolver sistemas e formulações precursoras de fase líquido cristalina baseados em monolinoleato de glicerila (MLG) e cremophor (CREM) com gelificação in situ em fase líquido cristalina. Por meio de planejamento fatorial 32 foram obtidos 9 sistemas sem adição de fármaco e 9 formulações contendo metronidazol com diferentes razões de MLG/CREM e %H2O. Quando caracterizados por microscopia de luz polarizada e espalhamento de raios-X a baixo ângulo, os sistemas e formulações com menor razão MLG/CREM e conteúdos de água de 5, 10 e 15% apresentaram organização micelar isotrópica. Eles também apresentaram rápida erosão no ensaio de captação de água, inviabilizando sua transição para mesofase. Os sistemas e formulações com média e alta razão MLG/CREM e conteúdos de água de 5, 10 e 15% apresentaram coexistência de fases em transição líquido cristalina. Apresentaram rápida captação de água com transição para fase cúbica. Contudo, com exceção do sistema e formulação com alta razão MGL/CREM e 15% de água, os demais sistemas e formulações, apresentaram propriedades de fluxo ideais para fácil aplicação por seringa acoplada a agulha, e comportamento viscoelástico adequado para promover espalhabilidade e retenção no interior da bolsa. Os sistemas e formulações com média e alta razão de MLG/CREM apresentaram melhor mucoadesão. Dentre as formulações, apenas a com média razão de GML/CREM e 5% de água, apresentou perfil bi-modal de liberação mantendo concentrações de metronidazol acima do MIC por 6 dias, característica desejável para sistemas de liberação intrabolsa periodontal. Portanto, todos os resultados advogam a favor desta formulação como potencial candidata ao emprego clínico como sistema de liberação de fármaco intrabolsa periodontal. Periodontal disease is a chronic infection that affects the structural supports of the tooth with periodontal pocket formation. If untreated, the periodontium may be destroyed, which can cause the tooth loss in the latest stages of the disease. The treatment for this infection comprises two stages, the mechanical removal of plaque and calculus by scaling and root planing and the use of antimicrobials. It is still common to use systemic antimicrobials, even though it has a reduced efficacy and frequent adverse effects. For the reason, justified the development of systems for sustained release of drug intra-pocket periodontal in order to solve the drawbacks of systemic therapy. The main limitations for the development of these systems are the anatomical and physiological aspects of the periodontal pocket, which includes the limited size and the depth area and the natural irrigate flow of the gingival crevice fluid (GCF). So, this study aimed to develop precursor liquid crystalline systems and formulations based on glyceryl monolinoleate (GML) and cremophor (CREM), with in situ gelation to liquid crystalline phases. Through a 32 factorial design 9 systems without drug and 9 formulations containing metronidazole were obtained. Different ratios of GML / CREM and water percentage were evaluated. When characterized by Small-Angle X-ray Scattering and Polarized Light Microscopy, lower ratio GML / CREM with 5, 10 and 15% H2O produce isotropic micellar organization. They also showed high erosion during water uptake, thus, precluding in situ crystalline transition. Medium and high ratio GML / CREM with 5, 10 and 15% H2O indicated the coexistence of regions in transition to the crystalline phase. They showed characteristic peaks of cubic phases, rapid water uptake, higher viscosity and increased mucoadhesion. Moreover, with the exception of the formulation containing high ratio and high water content, other systems and formulations with medium ratio GML / CREM and 5, 10, 15% of water and high ratio and 5 and 10% of water had flow properties ideal for easy application through needle fitted syringes, viscoelastic behavior appropriate to promote spreadability and might favor retention within the periodontal pocket. However, only the formulation with higher ratio and the lowest water content presented a bimodal release profile of metronidazole, maintaining concentrations above the MIC for 5 days, with the release of 100% of the drug added to the formulation. These are desirable features for delivery systems designed for periodontal pockets. Therefore, all results advocate in favor of the formulation with high ratio of GML / CREM and 5% of water as a potential candidate for clinical use as drug delivery system for the periodontal pocket.