Advances of nanotechnology led to the development of nanoparticulate systems with many advantages due to their unique physicochemical properties. The use of iron-oxide magnetic nanoparticles (IOMNPs) ...in pharmaceutical areas increased in the last few decades. This article reviews the conceptual information about iron oxides, magnetic nanoparticles, methods of IOMNP synthesis, properties useful for pharmaceutical applications, advantages and disadvantages, strategies for nanoparticle assemblies, and uses in the production of drug delivery, hyperthermia, theranostics, photodynamic therapy, and as an antimicrobial. The encapsulation, coating, or dispersion of IOMNPs with biocompatible material(s) can avoid the aggregation, biodegradation, and alterations from the original state and also enable entrapping the bioactive agent on the particle via adsorption or covalent attachment. IOMNPs show great potential for target drug delivery, improving the therapy as a consequence of a higher drug effect using lower concentrations, thus reducing side effects and toxicity. Different methodologies allow IOMNP synthesis, resulting in different structures, sizes, dispersions, and surface modifications. These advantages support their utilization in pharmaceutical applications, and getting suitable drug release control on the target tissues could be beneficial in several clinical situations, such as infections, inflammations, and cancer. However, more toxicological clinical investigations about IOMNPs are necessary.
Metronidazole is an antimicrobial agent utilized for the treatment of protozoa and anaerobic bacteria infections. Many times, it is necessary to modify the metronidazole release, and the development ...of modified release systems may be suggested. In this study, we are able to investigate the use of the residue normally thrown out from the preparation of propolis extracts (BP) as strategy to modify the metronidazole release. We prepared films containing polymeric adjuvant (gelatin or ethylcellulose) and metronidazole, by solvent casting method. Density, mechanical properties, water vapor permeability (WVP), moisture uptake capacity (MUC), thermogravimetry, differential scanning calorimetry, Fourier transform infrared spectroscopy (FT-IR), and in vitro metronidazole release were investigated. Thickness and density of the preparations indicated that the compounds were homogeneously dispersed throughout. Mechanical properties were influenced by film composition. Films containing gelatin showed higher resistance to stress while those containing ethylcellulose presented greater flexibility. The greater the adjuvant concentrations lower the resistance to rupture and the elasticity, but higher MUC and WVP of formulations. FT-IR tests suggested interactions between BP and the adjuvants. Films were capable to protect the metronidazole and changed its release profile. BP films are of great practical importance constituting a novel strategy to modify the metronidazole release.
abstract This study investigated the development and characterized the physicochemical properties of films obtained from by-products (BP) from the preparation of propolis extracts. Films were ...produced in the presence and absence of a polymeric adjuvant (gelatin or ethylcellulose) and propylene glycol by a solvent casting method. Density, surface topography by scanning electron microscopy, mechanical properties (folding endurance, tensile strength and percentage elongation), water vapour permeability (WVP), moisture uptake capacity, thermogravimetry, differential scanning calorimetry and Fourier transform infrared spectroscopy (FTIR) were determined. The films were a transparent, light greenish-yellow colour, with a uniform surface, and were flexible and easy to handle. The thickness and density of the preparations indicated that the compounds were homogeneously dispersed throughout the film. Mechanical properties were influenced by the film composition; films containing gelatin were more resistant to stress, while those containing ethylcellulose were more flexible. Increasing the adjuvant concentration decreased the elasticity and the rupture resistance, but increased the moisture uptake capacity and WVP of the formulations. BP was thermally stable as were the films. FTIR tests suggested interactions between BP and the adjuvants. This work could contribute to the utilization of BP to prepare films for food and pharmaceutical uses
resumo Este estudo investigou o desenvolvimento e as características físico-químicas de filmes obtidos com o resíduo (BP), normalmente descartado, advindo da preparação de extratos de própolis. Os filmes foram produzidos com e sem adjuvantes poliméricos (gelatina ou etilcelulose) e propilenoglicol, pelo método de evaporação de solvente. Foram determinadas a densidade, a topografia de superfície usando microscopia eletrônica de varredura, as propriedades mecânicas (resistência à dobra, tensão e elongação), transmissão de vapor de água (WVP), capacidade de absorção de umidade, termogravimetria, calorimetria exploratória diferencial e espectroscopia de infravermelho com transformada de Fourier (FTIR). Os filmes demonstraram coloração verde-amarelada, transparência, uniformidade de superfície, homogeneidade, flexibilidade e fácil manuseio. A espessura e a densidade das preparações indicaram que os compostos estavam dispersos de forma homogênea. As propriedades mecânicas foram influenciadas pela composição dos filmes e aqueles que continham gelatina apresentaram-se mais resistentes enquanto os compostos por etilcelulose demonstraram maior flexibilidade. Com o aumento da concentração polimérica, a resistência e a elasticidade diminuíam, porém aumentou a capacidade de absorção de água e a WVP das formulações. BP apresentou estabilidade térmica assim como os filmes. Os testes de FTIR sugeriram interações entre o BP e os adjuvantes utilizados. Este trabalho pôde contribuir com a utilização de BP na preparação de filmes para uso alimentício e farmacêutico.
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•Effect of propolis (PRP) and polymer content on physicochemical and biological properties of film forming systems (FFS) was evaluated.•Propolis presence and different acrylic acid ...derivatives influenced on the morphological, mechanical, bioadhesive and biological properties of FFS.•PRP and C974P or PCB resulted the nanostructured FFS displaying controlled PRP release and enhanced skin permeation.•Optimized FFS showed in-vitro antitumor activity, no cell toxicity and improved the migration of these cells in wound.
Film form systems (FFS) composed of thermoresponsive and bioadhesive polymers have shown properties for the improvement of topical application. FFS are easy for administration, can increase the local residence time, control the drug delivery and improve the skin permeation. Propolis displays important biological properties like anticancer, healing, antimicrobial, antioxidant and can improve the structuring of FFS. It is a safe bioactive compound for wound healing and the treatment of skin diseases. However, propolis displays drawbacks for administration. The aim of this work was to evaluate the effect of polymeric and propolis composition on morphological, rheological, bioadhesive, drug release and skin permeation properties of designed FFS. In-vitro cytotoxicity, antitumoral and wound healing activity were also evaluated. Formulations composed of different amounts of polymers and propolis were proposed. The presence of propolis enhanced the bioadhesiveness and structuring of FFS. They displayed excellent capacity to form nanostructured film, displaying controlled propolis delivery and improved skin permeation. FFS were not cytotoxic and displayed in-vitro antitumoral activity and stimulated the cell migration. The selected preparations containing propolis extract (12%, w/w) and carbomer 974P or polycarbophil (0.25%, w/w) indicate a potentially advantageous role to be topically administered and suggest they are promissory formulations for clinical evaluation.
The use of propolis by-product (PBP) microparticles (MP) as delivery systems can be a promising tool to surpass drawbacks related to low stability of ascorbic acid (AA). The objective of this study ...was to develop and characterize MP prepared with PBP containing AA. The MP was characterized regarding morphology, particle size, polydispersity index (PDI), association efficiency (AE), drug loading (DL), infrared and Raman spectroscopy as well as antioxidant and radical scavenging activity,
in vitro
release, and cellular studies. MP was shown to be spherical with some agglomeration. Its particle size was 1654 ± 0.210 nm with a PDI of 0.7. The AE and DL were, respectively, 100.30 ± 2.66% and 13.16 ± 0.59. Spectroscopic studies indicated a possible interaction between the PBP and AA. 2,2-Diphenyl-1-picrylhydrazyl (DPPH&z.rad;), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and ferric reducing antioxidant power (FRAP) assays demonstrated that the MP containing AA have an excellent antioxidant capacity as well as a considerable scavenging activity against reactive oxygen and nitrogen species. The
in vitro
release profile showed a slow pattern of drug release of AA from MP. Viability studies with intestinal cells revealed that MP did not present toxicity in Caco-2 and HT29-MTX. Moreover, AA could permeate Caco-2 monolayers and triple co-culture substantially at the end of 8 h, opposite to the MP. Therefore, the proposed MP formulation represents a promising platform for oral delivery of AA with a local effect on intestines.
The use of propolis by-product (PBP) microparticles (MP) as delivery systems can be a promising tool to surpass drawbacks related to low stability of ascorbic acid (AA).
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•Nanostructured lipid systems containing propolis and its by-product are proposed.•All systems show good morphology, size, and X-ray diffractometry characteristics.•Solid lipid ...nanoparticles (SLN) display the best size stability result.•The occlusive capacity, drug content and release profile show the best formulations.•The systems SLN display no toxicity in HaCaT cells and accelerate wound healing.
Propolis, a natural compound that can accelerate the wound healing process, is mainly used as ethanolic extract. The extractive solution may also be obtained from the propolis by-product (BP), transforming this waste material into a pharmaceutical active ingredient. Even if propolis does not show toxicity, when used as an extract over harmed skin or mucosa, the present ethanol content may be harmful to the tissue recovering, besides hindering the drug release. This study describes the development of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) as topical propolis delivery systems and the investigation of their in vitro and in vivo activities. The extracts were evaluated to guarantee their quality, and the lipid dispersions were characterized with respect to morphology (cryo-TEM), size and diffractometry (X-ray) properties. The occlusive capacity of formulations was also evaluated by an in vitro technique, which determines the occlusion factor. The drug entrapment efficiency (EE), as well as the in vitro drug release profile from the nanoparticulate systems was investigated as well. The size analysis performed through 90days was favorable to a topical administration and the polydispersity index, though not ideal in all cases due to the high content of resins and gums from the extracts, were relatively stable for the SLN. The propolis extract contributes to the occlusive potential of the formulations. The human immortalized keratinocytes presented good cell viability when tested with both extracts (propolis and BP) freely or entrapped in the systems. SLN modified with propolis material provided an acceleration of the in vivo wound healing process.
The present work at hands deals with physicochemical properties of an organogel composed of non-ionic triblock copolymer poloxamer 188 and passion fruit oil. To provide the characterization it was ...investigated the rheological (continuous shear and oscillatory) properties, sol-gel transition temperature, mechanical properties (hardness, compressibility, adhesiveness, cohesiveness and elasticity) and softness index. Moreover, we investigated the possible correlation between the rheological and mechanical characteristics to study the structuring of formulations and to select the best organogel for pharmaceutical applications. Mechanical and rheological characteristics showed to be temperature, polymer and oil concentration dependent. The increase of poloxamer 188 and passion fruit oil amounts in formulations displayed more expressive textural properties and softness. The organogels exhibited plastic flow with higher yield value, consistency index and thixotropic behavior at higher poloxamer 188 concentrations. All formulations showed viscoelastic properties and the sol-gel transition temperature was dependent of polymer and oil concentration in formulations. Rheological-mechanical correlation coefficient evidenced that rheological methods were more sensible than the mechanical ones. Considering the mechanical and rheological characteristics, the organogel composed of poloxamer 188 (35%, w/w) and passion fruit oil (16.7%, w/w) can be considered potentially promising as a drug delivery platform for pharmaceutical applications.
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•Physicochemical properties of an organogel composed of poloxamer 188 and passion fruit oil were investigated.•Mechanical and rheological characteristics of systems showed to be temperature, polymer and oil concentration dependent.•Increased poloxamer 188 and passion fruit oil amounts in systems displayed more expressive textural properties and softness.•Viscoelasticity and the sol-gel transition temperature of systems were dependent of polymer and oil concentration.•The system containing poloxamer 188 (35%, w/w) and passion fruit oil (16.7%, w/w) is potentially promising.
Correction for 'Development of a microparticulate system containing Brazilian propolis by-product and gelatine for ascorbic acid delivery: evaluation of intestinal cell viability and radical ...scavenging activity' by Lizziane Maria Belloto de Francisco
et al.
,
Food Funct.
, 2018, DOI: 10.1039/c8fo00863a.
Intra-periodontal pocket drug delivery systems, such as liquid crystalline systems, are widely utilized improving the drug release control and the therapy. Propolis is used in the treatment of ...periodontal diseases, reducing the inflammatory and infectious conditions. Iron oxide magnetic nanoparticles (MNPs) can improve the treatment when an alternating external magnetic field (AEMF) is applied, increasing the local temperature. The aim of this study was to develop a liquid crystalline system containing MNPs for intra-periodontal pocket propolis release. MNPs were prepared using iron salts and the morphological, size, thermal, x-ray diffraction, magnetometry, and Mössbauer spectroscopy analyses were performed. Cytotoxicity studies using
Artemia salina
and fibroblasts were also accomplished. The systems were prepared using polyoxyethylene (10) oleyl ether, isopropyl myristate, purified water, and characterized by polarized optical microscopy, rheometry, and
in vitro
drug release profile using a periodontal pocket simulator apparatus. The antifungal activity of the systems was investigated against
Candida
spp. using an AEMF. MNPs displayed nanometric size, were monodisperse, and they displayed very low cytotoxicity. Microscopically homogeneous formulations were obtained displaying important physicochemical and biological properties. The system displayed prolonged release of propolis and important
in vitro
fungicide activity, which was increased when the AEMF was applied, indicating a potentially alternative therapy for the treatment of the periodontal disease.
The use of iron oxide magnetic nanoparticles (IMNP) in medical and pharmaceutical areas dates to the beginning of the 1970s, as carriers. Some other uses to these nanoparticles are in vitro ...separation, magnetic resonance imaging and drug targeting agent. Many preparations containing IMNP have been described and used in drug delivery, hyperthermia, in vitro separation, tissue repair, cellular therapy, for magnetic separation, magnetic resonance imaging, as spoilers for magnetic resonance spectroscopy, and more recently as sensors for metabolites and other biomolecules. The use of these nanostructures as antibacterial agents has also been reported, which could kill some bacteria species causing no damage to the human host cells. Recently, they have been used as hyperthermia agents to treat infections or cancer, which are more susceptible than the healthy host's cells. Engineering designs, physiochemical characteristics, biomedical applications of IMNP, toxicity and magnetic nanotoxicology have been discussed. However, the application of IMNP as antimicrobials is very important. Thus, this review explores the therapeutic activities of IMNP and their use as antimicrobial agents. These nanoparticles can be efficient for the treatment of microbial infections, probably acting as membrane permeability enhancer, damaging the cell wall or by generating reactive oxygen species.
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