Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 107
Filtrar
1.
BMC Plant Biol ; 24(1): 765, 2024 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-39123105

RESUMO

The present study focused on the physiological and biochemical aspects of Tricleocarpa fragilis, red seaweed belonging to the phylum Rhodophyta, along the South Andaman coast, with particular attention given to its symbiotic relationships with associated flora and fauna. The physicochemical parameters of the seawater at the sampling station, such as its temperature, pH, and salinity, were meticulously analyzed to determine the optimal harvesting period for T. fragilis. Seaweeds attach to rocks, dead corals, and shells in shallow areas exposed to moderate wave action because of its habitat preferences. Temporal variations in biomass production were estimated, revealing the highest peak in March, which was correlated with optimal seawater conditions, including a temperature of 34 ± 1.1 °C, a pH of 8 ± 0.1, and a salinity of 32 ± 0.8 psu. GC‒MS analysis revealed n-hexadecanoic acid as the dominant compound among the 36 peaks, with major bioactive compounds identified as fatty acids, diterpenes, phenolic compounds, and hydrocarbons. This research not only enhances our understanding of ecological dynamics but also provides valuable insights into the intricate biochemical processes of T. fragilis. The established antimicrobial potential and characterization of bioactive compounds from T. fragilis lay a foundation for possible applications in the pharmaceutical industry and other industries.


Assuntos
Rodófitas , Alga Marinha , Rodófitas/fisiologia , Rodófitas/metabolismo , Alga Marinha/fisiologia , Alga Marinha/metabolismo , Água do Mar/química , Ecossistema , Biomassa , Ácidos Graxos/metabolismo , Simbiose/fisiologia , Animais
2.
Chem Biodivers ; 21(7): e202400500, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38719739

RESUMO

The Thymus genus includes various medicinal and aromatic species, cultivated worldwide for their unique medicinal and economic value. Besides, their conventional use as a culinary flavoring agent, Thymus species are well-known for their diverse biological effects, such as antioxidant, anti-fungal, anti-bacterial, anti-viral, anti-tumor, anti-inflammatory, anti-cancer, and anti-hypertensive properties. Hence, they are used in the treatment of fever, colds, and digestive and cardiovascular diseases. The pharmaceutical significance of Thymus plants is due to their high levels of bioactive components such as natural terpenoid phenol derivatives (p-cymene, carvacrol, thymol, geraniol), flavonoids, alkaloids, and phenolic acids. This review examines the phytochemicals, biological properties, functional food, and nutraceutical attributes of some important Thymus species, with a specific focus on their potential uses in the nutra-pharmaceutical industries. Furthermore, the review provides an insight into the mechanisms of biological activities of key phytochemicals of Thymus species exploring their potential for the development of novel natural drugs.


Assuntos
Thymus (Planta) , Thymus (Planta)/química , Humanos , Suplementos Nutricionais/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/química
3.
Int J Mol Sci ; 25(2)2024 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-38279323

RESUMO

Natural polysaccharides, which are described in this study, are some of the most extensively used biopolymers in food, pharmaceutical, and medical applications, because they are renewable and have a high level of biocompatibility and biodegradability. The fundamental understanding required to properly exploit polysaccharides potential in the biocomposite, nanoconjugate, and pharmaceutical industries depends on detailed research of these molecules. Polysaccharides are preferred over other polymers because of their biocompatibility, bioactivity, homogeneity, and bioadhesive properties. Natural polysaccharides have also been discovered to have excellent rheological and biomucoadhesive properties, which may be used to design and create a variety of useful and cost-effective drug delivery systems. Polysaccharide-based composites derived from natural sources have been widely exploited due to their multifunctional properties, particularly in drug delivery systems and biomedical applications. These materials have achieved global attention and are in great demand because to their biochemical properties, which mimic both human and animal cells. Although synthetic polymers account for a substantial amount of organic chemistry, natural polymers play a vital role in a range of industries, including biomedical, pharmaceutical, and construction. As a consequence, the current study will provide information on natural polymers, their biological uses, and food and pharmaceutical applications.


Assuntos
Sistemas de Liberação de Medicamentos , Polissacarídeos , Animais , Humanos , Preparações Farmacêuticas , Polissacarídeos/química , Biopolímeros/química , Polímeros/química
4.
Pharmacol Res ; 197: 106951, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37804927

RESUMO

Echinacoside, a natural phenylethanoid glycoside, was discovered and isolated from the garden plant Echinacea angustifolia DC., belonging to the Compositae family, approximately sixty years ago. Extensive investigations have revealed that it possesses a wide array of pharmacologically beneficial activities for human health, particularly notable for its neuroprotective and anticancer activity. Several crucial concerns surfaced, encompassing the recognition of active metabolites that exhibited inadequate bioavailability in their prototype form, the establishment of precise molecular signal pathways or targets associated with the aforementioned effects of echinacoside, and the scarcity of dependable clinical trials. Hence, the question remains unanswered as to whether scientific research can effectively utilize this natural compound. To support future studies on this natural product, it is imperative to provide a systematic overview and insights into potential future prospects. The current review provides a comprehensive analysis of the existing knowledge on echinacoside, encompassing its wide distribution, structural diversity and metabolism, diverse therapeutic applications, and improvement of echinacoside bioavailability for its potential utilization.


Assuntos
Asteraceae , Produtos Biológicos , Humanos , Glicosídeos/farmacologia , Glicosídeos/uso terapêutico , Disponibilidade Biológica , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico
5.
Crit Rev Food Sci Nutr ; 63(8): 1078-1101, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-34338575

RESUMO

Halophytes are salt-tolerant plants that inhabit environments in which they are exposed to extreme stress, wherefore they exhibit conserved and divergent metabolic responses different from those of conventional plants. Thus, the synthesis and accumulation of metabolites, especially of those oxidative stress-related such as phenolic compounds, should be investigated. The potential of halophytes as a source of phenolics and their prospective industrial applications are evaluated based on a comprehensive review of the scientific literature on the phenolic compounds of more than forty halophytes and their biological activities. Additionally, an overview of the analytical methodologies adopted for phenolics determination in halophytes is provided. Finally, the prospective uses and beneficial effects of the phenolic preparations from these plants are discussed. Halophytes are complex matrices, exhibiting a wide variety of phenolics in their composition, wherefore the results can be greatly affected depending on the organ plant under analysis and the extraction methodology, especially the extraction solvent used. High-performance liquid chromatography, coupled with diode array detection (HPLC-DAD) or mass spectrometry (HPLC-MS), are the most used technique. Halophytes biosynthesize phenolics in concentrations that justify the remarkable antioxidant and antimicrobial activities shown, making them ideal sources of bioactive molecules to be employed in a multitude of sectors.


Assuntos
Fenóis , Plantas Tolerantes a Sal , Plantas Tolerantes a Sal/química , Plantas Tolerantes a Sal/metabolismo , Fenóis/análise , Cromatografia Líquida de Alta Pressão , Antioxidantes/farmacologia , Extratos Vegetais/química
6.
Int J Mol Sci ; 25(1)2023 Dec 29.
Artigo em Inglês | MEDLINE | ID: mdl-38203656

RESUMO

Extracellular vesicles (EVs) are nanoparticles released from various cell types that have emerged as powerful new therapeutic option for a variety of diseases. EVs are involved in the transmission of biological signals between cells and in the regulation of a variety of biological processes, highlighting them as potential novel targets/platforms for therapeutics intervention and/or delivery. Therefore, it is necessary to investigate new aspects of EVs' biogenesis, biodistribution, metabolism, and excretion as well as safety/compatibility of both unmodified and engineered EVs upon administration in different pharmaceutical dosage forms and delivery systems. In this review, we summarize the current knowledge of essential physiological and pathological roles of EVs in different organs and organ systems. We provide an overview regarding application of EVs as therapeutic targets, therapeutics, and drug delivery platforms. We also explore various approaches implemented over the years to improve the dosage of specific EV products for different administration routes.


Assuntos
Sistemas de Liberação de Medicamentos , Vesículas Extracelulares , Preparações Farmacêuticas , Distribuição Tecidual
7.
Int J Mol Sci ; 23(6)2022 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-35328816

RESUMO

Compounds bearing the phosphorus-carbon (P-C) bond have important pharmacological, biochemical, and toxicological properties. Historically, the most notable reaction for the formation of the P-C bond is the Michaelis-Arbuzov reaction, first described in 1898. The classical Michaelis-Arbuzov reaction entails a reaction between an alkyl halide and a trialkyl phosphite to yield a dialkylalkylphosphonate. Nonetheless, deviations from the classical mechanisms and new modifications have appeared that allowed the expansion of the library of reactants and consequently the chemical space of the yielded products. These involve the use of Lewis acid catalysts, green methods, ultrasound, microwave, photochemically-assisted reactions, aryne-based reactions, etc. Here, a detailed presentation of the Michaelis-Arbuzov reaction and its developments and applications in the synthesis of biomedically important agents is provided. Certain examples of such applications include the development of alkylphosphonofluoridates as serine hydrolase inhibitors and activity-based probes, and the P-C containing antiviral and anticancer agents.


Assuntos
Ácidos de Lewis , Fósforo , Antivirais , Catálise , Micro-Ondas
8.
Appl Microbiol Biotechnol ; 105(3): 899-907, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33427934

RESUMO

Psychrophiles are cold-living microorganisms synthesizing enzymes that are permanently active at almost near-zero temperatures. Psychrozymes are supposed to be structurally more flexible than their homologous proteins. This structural flexibility enables these proteins to undergo conformational changes during catalysis and improve catalytic efficiency at low temperatures. The outstanding characteristics of the psychrophilic enzymes have attracted the attention of the scientific community to utilize them in a wide variety of industrial and pharmaceutical applications. In this review, we first highlight the current knowledge of the cold-adaptation mechanisms of the psychrophiles. In the sequel, we describe the potential applications of the enzymes in different biotechnological processes specifically, in the production of industrial and pharmaceutical products. KEY POINTS: • Methods that organisms have evolved to survive and proliferate at cold environments. • The economic benefits due to their high activity at low and moderate temperatures. • Applications of the psychrophiles in biotechnological and pharmaceutical industry.


Assuntos
Aclimatação , Preparações Farmacêuticas , Adaptação Fisiológica , Temperatura Baixa , Enzimas , Temperatura
9.
Mar Drugs ; 19(11)2021 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-34822499

RESUMO

Alginate, the most abundant polysaccharides of brown algae, consists of various proportions of uronic acid epimers α-L-guluronic acid (G) and ß-D-mannuronic acid (M). Alginate oligosaccharides (AOs), the degradation products of alginates, exhibit excellent bioactivities and a great potential for broad applications in pharmaceutical fields. Alginate lyases can degrade alginate to functional AOs with unsaturated bonds or monosaccharides, which can facilitate the biorefinery of brown algae. On account of the increasing applications of AOs and biorefinery of brown algae, there is a scientific need to explore the important aspects of alginate lyase, such as catalytic mechanism, structure, and property. This review covers fundamental aspects and recent developments in basic information, structural characteristics, the structure-substrate specificity or catalytic efficiency relationship, property, molecular modification, and applications. To meet the needs of biorefinery systems of a broad array of biochemical products, alginate lyases with special properties, such as salt-activated, wide pH adaptation range, and cold adaptation are outlined. Withal, various challenges in alginate lyase research are traced out, and future directions, specifically on the molecular biology part of alginate lyases, are delineated to further widen the horizon of these exceptional alginate lyases.


Assuntos
Alginatos/farmacologia , Phaeophyceae , Polissacarídeos/farmacologia , Alginatos/química , Animais , Organismos Aquáticos , Humanos , Polissacarídeos/química , Relação Estrutura-Atividade , Especificidade por Substrato
10.
Mar Drugs ; 19(3)2021 Mar 08.
Artigo em Inglês | MEDLINE | ID: mdl-33800149

RESUMO

There are several reviews that separately cover different aspects of fish gelatin including its preparation, characteristics, modifications, and applications. Its packaging application in food industry is extensively covered but other applications are not covered or covered alongside with those of collagen. This review is comprehensive, specific to fish gelatin/hydrolysate and cites recent research. It covers cosmetic applications, intrinsic activities, and biomedical applications in wound dressing and wound healing, gene therapy, tissue engineering, implants, and bone substitutes. It also covers its pharmaceutical applications including manufacturing of capsules, coating of microparticles/oils, coating of tablets, stabilization of emulsions and drug delivery (microspheres, nanospheres, scaffolds, microneedles, and hydrogels). The main outcomes are that fish gelatin is immunologically safe, protects from the possibility of transmission of bovine spongiform encephalopathy and foot and mouth diseases, has an economic and environmental benefits, and may be suitable for those that practice religious-based food restrictions, i.e., people of Muslim, Jewish and Hindu faiths. It has unique rheological properties, making it more suitable for certain applications than mammalian gelatins. It can be easily modified to enhance its mechanical properties. However, extensive research is still needed to characterize gelatin hydrolysates, elucidate the Structure Activity Relationship (SAR), and formulate them into dosage forms. Additionally, expansion into cosmetic applications and drug delivery is needed.


Assuntos
Proteínas de Peixes/química , Gelatina/química , Hidrolisados de Proteína/química , Animais , Cosméticos , Sistemas de Liberação de Medicamentos , Humanos , Reologia , Relação Estrutura-Atividade
11.
Mar Drugs ; 19(2)2021 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-33530360

RESUMO

Biotechnology is an essential tool for the sustainable exploitation of marine resources, although the full development of their potential is complicated by a series of cognitive and technological limitations. Thanks to an innovative systematic approach that combines the meta-analysis of 620 articles produced worldwide with 29 high TRL (Technology Readiness Level) European funded projects, the study provides an assessment of the growth prospects of blue biotechnologies, with a focus on pharmaceutical and food applications, and the most promising technologies to overcome the main challenges in the commercialization of marine products. The results show a positive development trend, with publications more than doubled from 2010 (36) to 2019 (70). Biochemical and molecular characterization, with 150 studies, is the most widely used technology. However, the emerging technologies in basic research are omics technologies, pharmacological analysis and bioinformatics, which have doubled the number of publications in the last five years. On the other hand, technologies for optimizing the conditions of cultivation, harvesting and extraction are central to most business models with immediate commercial exploitation (65% of high-TRL selected projects), especially in food and nutraceutical applications. This research offers a starting point for future research to overcome all those obstacles that restrict the marketing of products derived from organisms.


Assuntos
Biotecnologia/métodos , Indústria Farmacêutica/métodos , Tecnologia de Alimentos/métodos , Biologia Marinha/métodos , Marketing/métodos , Animais , Biotecnologia/tendências , Biologia Computacional/métodos , Biologia Computacional/tendências , Indústria Farmacêutica/tendências , Tecnologia de Alimentos/tendências , Humanos , Biologia Marinha/tendências , Marketing/tendências , Preparações Farmacêuticas/análise , Preparações Farmacêuticas/química
12.
BMC Med Inform Decis Mak ; 21(1): 217, 2021 07 16.
Artigo em Inglês | MEDLINE | ID: mdl-34271932

RESUMO

BACKGROUND: Most mobile pharmaceutical applications produced for people with visual disabilities in Thailand fail to meet the required standard due to poor-quality regulations, defective design, lack of user support and impracticality; as a result, visually-impaired people are unable to use them. This research is motivated by the limited use of this technology in primary medical services and its aim is to enable people with disabilities to access effective digital health information. The research objective is to analyse, design and develop a mobile pharmaceutical application with functions that are appropriate for visually-impaired users, and test its usability. RESULTS: Based on the design and development of the application, it contained five necessary functions. When testing the usability and users' satisfaction, it was found that the input or fill of information in the application was of low usability. According to the test results, the medicinal database function was missing 71 times and the voice command function was missing 34 times. Based on users' satisfaction results, users who had the highest level of usage gave higher average scores to users' attitude, users' confidence, user interface and system performance than those with lower levels of usage. The scores of both groups were found to be the same when discussing the implementation of the development. CONCLUSIONS: This mobile application, which was developed based on the use of smart technology, will play an important role in supporting visually-impaired people in Thailand by enhancing the efficacy of self-care. The design and development of the application will ensure the suitability of many functions for visually-impaired users. However, despite the high functional capacity of the application, the gap in healthcare services between the general public and disabled groups will still exist if users have inadequate IT skills.


Assuntos
Pessoas com Deficiência , Aplicativos Móveis , Preparações Farmacêuticas , Humanos , Autocuidado , Tailândia
13.
Ann Pharm Fr ; 79(4): 335-345, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33383021

RESUMO

Carbon quantum dots (CQDs, C-dots, or CDs), are generally small carbon nanoparticles having a size less than 10nm. Carbon dots (CDs) were accidentally discovered during the purification of single-walled carbon nanotubes through preparative electrophoresis in 2004. Carbon is an organic material having poor water solubility that emits less fluorescence. However, CDs have good aqueous solubility and excellent fluorescent property, hence more attention has been given to the synthesis of CDs and their applications in chemistry and allied sciences. CDs being easily accessible for in-house synthesis, simpler fabrication as per compendial requirements are wisely accepted. In addition, since CDs are biocompatible, of low toxicity, and of biodegradable nature, they appear as a promising tool for the health care sector. Furthermore, owing to their capabilities of expressing significant interaction with biological materials, and their excellent photoluminescence (PL), CDs have been emerging as novel pioneered nanoparticles useful for pharmaceutical and theranostic applications. Also, CDs are more eco-friendly in synthesis and therefore can be favorably consumed as alternatives in the further development of biological, environmental, and food areas. A massive study has been performed dealing with different approaches which are adopted for CDs synthesis and their applications as, filters for the separation of pollutants from polluted water, food safety, toxicological studies, and optical properties, etc. While still less emphasis is given on the applications of CDs in pharmaceuticals like for sustained and targeted drug delivery systems, theranostic study, etc. Hence, in the present review, we are exploring CQDs as a boon to pharmaceutical concerns.


Assuntos
Nanotubos de Carbono , Preparações Farmacêuticas , Pontos Quânticos , Sistemas de Liberação de Medicamentos , Solubilidade
14.
Rocz Panstw Zakl Hig ; 72(2): 203-208, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34114779

RESUMO

Objectives: Antimicrobial efficacy and toxicity analysis of 5 different concentrations of silver zeolite (SZ) compound against 5 common oral pathogens Streptococcus mutans, Streptococcus pyogenes, Lactobacillus sp., Staphylococcus aureus, Candida albicans. Material and methods: The antimicrobial efficacy of 5 different concentrations of SZ was tested against 5 common oral pathogens using the agar well diffusion method and the MIC and MBC values were determined using the micro broth dilution method. The toxicity of all 5 different concentrations was evaluated using brine shrimp assay and lethal concentration (Lc50) value was determined. Results: At 10 µg/mL the antimicrobial activity of SZ was almost negligible. The antimicrobial activity was observed in an increasing trend against all the test microorganisms as the concentration increased. At 75 & 100 µg/mL the zone of inhibitions was more than the control. Furthermore, MIC and MBC values of SZ with concentrations 25, 50, 75, and 100 µg/mL were determined and recorded. SZ was equally effective against all the test organisms. The LC25 (lethal concentration25) value was 1.6 µg/mL, whereas the LC50 value was 1.77 µg/mL and the LC75 value was 1.90 µg/mL, calculated from the probit computational method. Conclusion: SZ has the potential to change the ongoing system and bring about a revolution as an antimicrobial drug. However, the dose must be regulated as it can be toxic in higher concentrations. SZ compounds with the correct study of physicochemical properties and toxicity analysis can increase their pharmacological use and market value.


Assuntos
Anti-Infecciosos , Zeolitas , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Humanos , Testes de Sensibilidade Microbiana , Prata/química , Prata/farmacologia , Zeolitas/farmacologia
15.
Drug Dev Res ; 81(1): 3-22, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31800139

RESUMO

Crystallization is an important and difficult to control unit operation in the pharmaceutical industry. Crystallization can control molecular (i.e., polymorphism) and particulate (i.e., particle size and crystal habit) properties of active pharmaceutical ingredient (API). Moreover, these molecular and particulate properties govern the manufacturability, stability, and biopharmaceutical performance of the API and drug product. Nucleation is a key step and primary heterogeneous nucleation is a common mode of nucleation during crystallization. Hence, it is important to understand the parameters affecting primary heterogeneous nucleation, to achieve desirable properties in crystalline APIs. Primary heterogeneous crystallization has usually been linked to the surface characteristics like topography and functionality of the heteronucleant. The review outlines recent findings in the primary heterogeneous crystallization with specific emphasis on its pharmaceutical applications including regulatory considerations. Molecular-level mechanisms governing heteronucleation and subsequent outcome in terms of molecular as well as particulate-level properties of API have also been discussed. Moreover, general guidance for the selection of heteronucleant has also been included. Heterogeneous crystallization is a promising tool for efficient crystallization of API having properties for optimal pharmaceutical performance.


Assuntos
Preparações Farmacêuticas/química , Cristalização , Estrutura Molecular , Tamanho da Partícula , Tecnologia Farmacêutica
16.
Int J Mol Sci ; 21(5)2020 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-32155742

RESUMO

Acacia dealbata biomass, either from forest exploitation or from the management of invasive species, can be a strategic topic, namely as a source of high-value compounds. In this sense, the present study aimed at the detailed characterization of the lipophilic components of different morphological parts of A. dealbata and the evaluation of their cytotoxicity in cells representative of different mammals' tissues. The chemical composition of lipophilic extracts from A. dealbata bark, wood and leaves was evaluated using gas chromatography-mass spectrometry (GC-MS). Terpenic compounds (representing 50.2%-68.4% of the total bark and leaves extracts, respectively) and sterols (60.5% of the total wood extract) were the main components of these extracts. Other constituents, such as fatty acids, long-chain aliphatic alcohols, monoglycerides, and aromatic compounds were also detected in the studied extracts. All the extracts showed low or no cytotoxicity in the different cells tested, demonstrating their safety profile and highlighting their potential to be used in nutraceutical or pharmaceutical applications. This study is therefore an important contribution to the valorization of A. dealbata, demonstrating the potential of this species as a source of high value lipophilic compounds.


Assuntos
Acacia/química , Ácidos Graxos/isolamento & purificação , Ácidos Graxos/farmacologia , Neoplasias/patologia , Fitosteróis/farmacologia , Extratos Vegetais/farmacologia , Animais , Sobrevivência Celular , Humanos , Camundongos , Neoplasias/tratamento farmacológico , Folhas de Planta/química , Células Tumorais Cultivadas
17.
Molecules ; 25(12)2020 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-32570958

RESUMO

Bisphosphonates (BPs), well-known medicinal compounds used for osteoporosis management, are currently the target of intensive research, from basic pre-formulation studies to more advanced stages of clinical practice. The high demand by the pharmaceutical industry inherently requires an easy, efficient and quick preparation of BPs. Current synthetic procedures are, however, still far from ideal. This work presents a comprehensive compilation of reports on the synthesis of the commercially available bisphosphonates that are pharmaceutical active ingredients. Current limitations to the conventional synthesis are assessed, and paths towards their improvement are described, either through the use of alternative solvents and/or by selecting appropriate ratios of the reactants. Innovative processes, such as microwave-assisted synthesis, are presented as more environmental-friendly and effective methods. The main advantages and setbacks of all syntheses are provided as a way to clarify and promote the development of simpler and improved procedures. Only in this way one will be able to efficiently respond to the future high demand of BPs, mostly due to the increase in life span in occidental countries.


Assuntos
Difosfonatos , Osteoporose/tratamento farmacológico , Difosfonatos/síntese química , Difosfonatos/química , Difosfonatos/uso terapêutico , Humanos , Micro-Ondas , Solventes
18.
Molecules ; 25(12)2020 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-32575617

RESUMO

Drug concentration plays an important role in the interaction with drug carriers affecting the kinetics of release process and toxicology effects. Cyclodextrins (CDs) can solubilize hydrophobic drugs in water enhancing their bioavailability. In this theoretical study based on molecular mechanics and molecular dynamics methods, the interactions between ß-cyclodextrin and piroxicam, an important nonsteroidal anti-inflammatory drug, were investigated. At first, both host-guest complexes with native ß-CD in the 1:1 and in 2:1 stoichiometry were considered without assuming any initial a priori inclusion: the resulting inclusion complexes were in good agreement with literature NMR data. The interaction between piroxicam and a ß-CD nanosponge (NS) was then modeled at different concentrations. Two inclusion mechanisms were found. Moreover, piroxicam can interact with the external NS surface or with its crosslinkers, also forming one nanopore. At larger concentration, a nucleation process of drug aggregation induced by the first layer of adsorbed piroxicam molecules is observed. The flexibility of crosslinked ß-CDs, which may be swollen or quite compact, changing the surface area accessible to drug molecules, and the dimension of the aggregate nucleated on the NS surface are important factors possibly affecting the kinetics of release, which shall be theoretically studied in more detail at specific concentrations.


Assuntos
Anti-Inflamatórios não Esteroides/química , Portadores de Fármacos/química , Simulação de Dinâmica Molecular , Piroxicam/química , beta-Ciclodextrinas/química , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas
19.
Ann Pharm Fr ; 78(1): 1-11, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31564424

RESUMO

Development of tailor-made pharmaceutical nanofibers has gained vital prominence due to ease of fabrication and versatility of electrospinning (ES). ES is one of the flexible and, wonderful strategies for the fabrication of nanofibers. ES unit comprises a supplier of high voltage current, a syringe (pump), spinneret and a metal plate collector. The obtained nanofibers are optimized by manipulating process and formulation variables Viz: polymer/drug resolution (viscosity, concentration, physical phenomenon, molecular mass) and the environmental conditions (humidity, temperature). The electrospun nanofibers can be used for loading of the drug, amorphization of a crystalline API and an increase in its physical storage stability. ES technique enables mixing of two or more API and may facilitate or inhibit the burst release of a drug, along with attainment of modified release. Additionally, nanofibers demonstrate a reduction in overall dose needed for the therapeutic activity, by improving dissolution and bioavailability of the drugs. The current review is an attempt to focus on ES method, the optimization parameters, and pharmaceutical applications of the electrospun nanofibers.


Assuntos
Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Nanofibras , Nanotecnologia/métodos , Fármacos Anti-HIV/administração & dosagem , Anti-Infecciosos/administração & dosagem , Anti-Inflamatórios/administração & dosagem , Anti-Hipertensivos/administração & dosagem , Antineoplásicos/administração & dosagem , Preparações de Ação Retardada , Implantes de Medicamento , Fármacos Hematológicos/administração & dosagem , Nanotecnologia/instrumentação
20.
Ann Pharm Fr ; 78(6): 469-486, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32569621

RESUMO

Silk sericin is an applicable protein extracted from dried silk cocoons, which are composed of a polar amino acid chain with hydroxyl, carboxyl, and amino functional groups. It anticipated that the functionality present in sericin provides excellent assets such as stability, release-modifying capacity, interaction with molecules, etc. It has various significant properties like biocompatibility, biodegradability, non-toxicity, hydrophilicity, etc. Besides, sericin exhibits the capability to form gels, nanoparticles, micro-particles, and keen bioengineered materials. Sericin also offers stability by strong affinity to the drug substance/molecules. Currently, sericin reconnoitered for a variety of pharmaceutical applications including solubility enhancement, release modifications, formulation stabilization, and as a drug carrier, etc. The focus of the review is to deliver an impression of the sericin based pharmaceutical applications including nanocrystal and nanoparticle stabilization, inhibition of devitrification, solubility enhancement, controlled and the extended-release formulation, targeted drug delivery, wound healing applications and as a suitable carrier.


Assuntos
Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Sericinas/química , Animais , Materiais Biocompatíveis , Bioengenharia , Humanos , Nanopartículas , Seda
SELEÇÃO DE REFERÊNCIAS
Detalhe da pesquisa