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1.
Mar Drugs ; 19(6)2021 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-34204083

RESUMO

We investigated a spray drying process for preparing water-soluble salts of high molecular weight chitosan (CH) intended for pharmaceutical excipient applications. CH was derived from chitin of marine lobster origin (Panulirus argus). The effects of organic acid (acetic or lactic acid) and the ratio (difference) of inlet/outlet air temperature (140/90 °C or 160/100 °C) on spray drying were studied. The yield of spray-dried CH salt powders ranged from 50% to 99% in laboratory and industrial-scale processes. The spray-dried dry powder of CH salts consisted of spherical agglomerated particles with an average diameter of 36.2 ± 7.0 µm (CH acetate) and 108.6 ± 11.5 µm (CH lactate). After dispersing the spray-dried CH salt powder samples in purified water, the mean particle sizes obtained for the CH acetate salts were 31.4 nm (batch A001), 33.0 nm (A002) and 44.2 nm (A003), and for the CH lactate salts 100.8 nm (batch L001), 103.2 nm (L002) and 121.8 nm (L003). The optimum process conditions for spray drying were found: an inlet air temperature of 160 ± 5 °C, an outlet temperature of 100 ± 5 °C and an atomizer disk rotational speed of 18,200 min-1. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) results confirmed the amorphous state of the CH salts. The 1H nuclear magnetic resonance (NMR) and Fourier transform infrared (FT-IR) spectra of CH acetate and lactate salts verified that the spray drying process does not affect the polymer backbone. In conclusion, both laboratory and industrial-scale spray drying methods for preparing water-soluble acid salts of CH are reproducible, and the physicochemical properties of the corresponding CH acid salts are uniform.


Assuntos
Quitosana/síntese química , Excipientes/síntese química , Sais/síntese química , Secagem por Atomização , Animais , Varredura Diferencial de Calorimetria , Química Farmacêutica , Quitosana/química , Excipientes/química , Espectroscopia de Ressonância Magnética , Palinuridae/química , Tamanho da Partícula , Sais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Temperatura , Difração de Raios X
2.
Molecules ; 26(9)2021 Apr 29.
Artigo em Inglês | MEDLINE | ID: mdl-33946815

RESUMO

Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.


Assuntos
Berberina/administração & dosagem , Berberina/química , Composição de Medicamentos , Lipossomos , Nanopartículas , Administração Oral , Fenômenos Químicos , Lipossomos/química , Estrutura Molecular , Nanopartículas/química , Nanopartículas/ultraestrutura , Tamanho da Partícula , Solubilidade
3.
J Nat Prod ; 83(4): 1201-1206, 2020 04 24.
Artigo em Inglês | MEDLINE | ID: mdl-32208696

RESUMO

Six new chiro-inositol derivatives (1-6) were isolated from the leaves of Chisocheton paniculatus collected in Vietnam. Their chemical structures were elucidated by 1D and 2D NMR and HRESIMS analyses. All isolated compounds were evaluated for their inhibitory activity against lipopolysaccharide-induced nitric oxide (NO) production in the RAW 264.7 macrophage cell line. Compound 4 exhibited potent inhibitory activity for NO production with an IC50 value of 7.1 µM.


Assuntos
Inositol/química , Lipopolissacarídeos/farmacologia , Óxido Nítrico/biossíntese , Folhas de Planta/química , Animais , Linhagem Celular , Lipopolissacarídeos/química , Macrófagos/metabolismo , Meliaceae/química , Camundongos , Estrutura Molecular , Óxido Nítrico/química , Células RAW 264.7 , Vietnã
4.
Mol Pharm ; 14(3): 808-820, 2017 03 06.
Artigo em Inglês | MEDLINE | ID: mdl-28195483

RESUMO

Printing technology has been shown to enable flexible fabrication of solid dosage forms for personalized drug therapy. Several methods can be applied for tailoring the properties of the printed pharmaceuticals. In this study, the use of electrospun fibrous substrates in the fabrication of inkjet-printed dosage forms was investigated. A single-drug formulation with lidocaine hydrochloride (LH) and a combination drug system containing LH and piroxicam (PRX) for oromucosal administration were prepared. The LH was deposited on the electrospun and cross-linked gelatin substrates by inkjet printing, whereas PRX was incorporated within the substrate fibers during electrospinning. The solid state analysis of the electrospun substrates showed that PRX was in an amorphous state within the fibers. Furthermore, the results indicated the entrapment and solidification of the dissolved LH within the fibrous gelatin matrix. The printed drug amount (2-3 mg) was in good correlation with the theoretical dose calculated based on the printing parameters. However, a noticeable degradation of the printed LH was detected after a few months. An immediate release (over 85% drug release after 8 min) of both drugs from the printed dosage forms was observed. In conclusion, the prepared electrospun gelatin scaffolds were shown to be suitable substrates for inkjet printing of oromucosal formulations. The combination of electrospinning and inkjet printing allowed the preparation of a dual drug system.


Assuntos
Mucosa Bucal/metabolismo , Piroxicam/química , Administração Oral , Química Farmacêutica/métodos , Formas de Dosagem , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos , Gelatina/química , Lidocaína/química , Impressão/métodos , Propriedades de Superfície , Tecnologia Farmacêutica/métodos
5.
J Nat Prod ; 80(4): 916-924, 2017 04 28.
Artigo em Inglês | MEDLINE | ID: mdl-28333461

RESUMO

The isolation and physical material properties of suberin fatty acids (SFAs) were investigated with special reference to their potential applications as novel pharmaceutical excipients. SFAs were isolated from outer birch bark (OBB) with a new extractive hydrolysis method. The present simplified isolation process resulted in a moderate batch yield and chemical purity of SFAs, but further development is needed for establishing batch-to-batch variation. Cryogenic milling was the method of choice for the particle size reduction of SFAs powder. The cryogenically milled SFAs powder exhibited a semicrystalline structure with apparent microcrystalline domains within an amorphous fatty acids matrix. The thermogravimetric analysis (TGA) of SFAs samples showed a good thermal stability up to 200 °C, followed by a progressive weight loss, reaching a plateau at about 95% volatilization at about 470 °C. The binary blends of SFAs and microcrystalline cellulose (MCC; Avicel PH 101) in a ratio of 25:75 (w/w) displayed good powder flow and tablet compression properties. The corresponding theophylline-containing tablets showed sustained or prolonged-release characteristics. The physicochemical and bulk powder properties of SFAs isolated from OBB are auspicious in terms of potential pharmaceutical excipient applications.


Assuntos
Betula/química , Ácidos Graxos/isolamento & purificação , Lipídeos/isolamento & purificação , Lipídeos/farmacologia , Casca de Planta/química , Celulose , Química Farmacêutica , Excipientes/farmacologia , Ácidos Graxos/química , Lipídeos/química , Estrutura Molecular , Comprimidos/farmacologia , Teofilina/análise
6.
Drug Dev Ind Pharm ; 43(7): 1134-1142, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28277847

RESUMO

OBJECTIVE: Artesunate (ART) is proven to have potential anti-proliferative activities, but its instability and poor aqueous solubility limit its application as an anti-cancer drug. The present study was undertaken to develop coaxial electrospraying as a novel technique for fabricating nanoscale drug delivery systems of ART as the core-shell nanostructures. METHODS: The core-shell nanoparticles (NPs) were fabricated with coaxial electrospraying and the formation mechanisms of NPs were examined. The physical solid state and drug-polymer interactions of NPs were characterized by X-ray powder diffraction (XRPD) and Fourier transform infrared (FTIR) spectroscopy. The effects of materials and electrospraying process on the particle size and surface morphology of NPs were investigated by scanning electron microscopy (SEM). The drug release from NPs was determined in vitro by a dialysis method. RESULTS: The ART/poly(lactic-co-glycolic) acid (PLGA) chitosan (CS) NPs exhibited the mean particle size of 303 ± 93 nm and relatively high entrapment efficiency (80.5%). The release pattern showed an initial rapid release within two hours followed by very slow extended release. The release pattern approached the Korsmeyer-Peppas model. CONCLUSIONS: The present results suggest that the core-shell NPs containing PLGA and CS have a potential as carriers in the anticancer drug therapy of ART.


Assuntos
Antineoplásicos/administração & dosagem , Artemisininas/administração & dosagem , Quitosana/química , Sistemas de Liberação de Medicamentos/métodos , Nanopartículas/química , Ácido Poliglicólico/química , Antineoplásicos/química , Artemisininas/química , Artesunato , Liberação Controlada de Fármacos , Microscopia Eletrônica de Varredura , Tamanho da Partícula , Difração de Raios X
7.
Drug Dev Ind Pharm ; 42(3): 378-88, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26065533

RESUMO

Amorphous solid dispersions (SDs) open up exciting opportunities in formulating poorly water-soluble active pharmaceutical ingredients (APIs). In the present study, novel catalytic pretreated softwood cellulose (CPSC) and polyvinylpyrrolidone (PVP) were investigated as carrier polymers for preparing and stabilizing cryogenic co-ground SDs of poorly water-soluble piroxicam (PRX). CPSC was isolated from pine wood (Pinus sylvestris). Raman and Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) were used for characterizing the solid-state changes and drug-polymer interactions. High-resolution scanning electron microscope (SEM) was used to analyze the particle size and surface morphology of starting materials and final cryogenic co-ground SDs. In addition, the molecular aspects of drug-polymer interactions and stabilization mechanisms are presented. The results showed that the carrier polymer influenced both the degree of amorphization of PRX and stabilization against crystallization. The cryogenic co-ground SDs prepared from PVP showed an enhanced dissolution rate of PRX, while the corresponding SDs prepared from CPSC exhibited a clear sustained release behavior. In conclusion, cryogenic co-grinding provides a versatile method for preparing amorphous SDs of poorly water-soluble APIs. The solid-state stability and dissolution behavior of such co-ground SDs are to a great extent dependent on the carrier polymer used.


Assuntos
Química Farmacêutica/métodos , Portadores de Fármacos/química , Piroxicam/química , Polímeros/química , Água/química , Criopreservação/métodos , Portadores de Fármacos/análise , Piroxicam/análise , Polímeros/análise , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Difração de Raios X/métodos
8.
Plants (Basel) ; 13(6)2024 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-38592748

RESUMO

The pharmaceutical industry usually utilizes either hydrophobic or hydrophilic substances extracted from raw plant materials to prepare a final product. However, the waste products from the plant material still contain biologically active components with the opposite solubility. The aim of this study was to enhance the comprehensive usability of plant materials by developing a new no-waste extraction method for eucalypt leaves and by investigating the phytochemical and pharmacological properties of eucalypt extracts and their 3D-printed dosage forms. The present extraction method enabled us to prepare both hydrophobic soft extracts and hydrophilic (aqueous) dry extracts. We identified a total of 28 terpenes in the hydrophobic soft extract. In the hydrophilic dry extract, a total of 57 substances were identified, and 26 of them were successfully isolated. The eucalypt extracts studied showed significant antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Candida albicans, Corynebacterium diphtheriae gravis, and Corynebacterium diphtheriae mitis. The anti-inflammatory activity of the dry extract was studied using a formalin-induced-edema model in mice. The maximum anti-exudative effect of the dry extract was 61.5% at a dose of 20 mg/kg. Composite gels of polyethylene oxide (PEO) and eucalypt extract were developed, and the key process parameters for semi-solid extrusion (SSE) 3D printing of such gels were verified. The SSE 3D-printed preparations of novel synergistically acting eucalypt extracts could have uses in antimicrobial and anti-inflammatory medicinal applications.

9.
Int J Pharm ; 653: 123890, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38346601

RESUMO

In this work, the optical imaging based single particle analysis (SPA) and the gold standard shake-flask (SF) solubility methods are compared. We show that to analyze pharmaceutical compounds spanning 7 log units in solubility and a diverse chemical space with limited resources, several analytical techniques are required (HPLC-UV, LC-MS, refractometry and UV-Vis spectrometry), whereas solely the SPA method is able to analyze all the same compounds. SPA experiments take only minutes, while for SF, it may take days to reach thermodynamic equilibration. This decreases the time span needed for the solubility experiment from initial preparations to obtaining the result from roughly three days to less than three hours. The optimal particle size for SPA ranges from approximately one to hundreds of microns. Challenges include measuring large particles, very fast dissolving compounds and handling small sample sizes. Inherent exclusion of density from the SPA measurement is a potential source of error for compounds with very low or high density values. The average relative difference of 37 % between the two methods is very good in the realm of solubility, where 400 % interlaboratory reproducibility can be expected.


Assuntos
Solubilidade , Reprodutibilidade dos Testes , Cromatografia Gasosa-Espectrometria de Massas , Cromatografia Líquida de Alta Pressão , Termodinâmica , Preparações Farmacêuticas
10.
Eur J Pharm Sci ; 195: 106712, 2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38290611

RESUMO

Anxiety disorders are highly prevalent worldwide and can affect people of all ages, genders and backgrounds. Much efforts and resources have been directed at finding new anxiolytic agents and drug delivery systems (DDSs) especially for cancer patients to enhance targeted drug delivery, reduce drug adverse effects, and provide an analgesic effect. The aim of this study was (1) to design and develop novel nanofiber-based DDSs intended for the oral administration of new 1,2,3-triazolo-1,4-benzodiazepines derivatives, (2) to investigate the physical solid-state properties of such drug-loaded nanofibers, and (3) to gain knowledge of the anxiolytic activity of the present new benzodiazepines in rodents in vivo. The nanofibers loaded with 1,2,3-triazolo-1,4-benzodiazepine derivatives were prepared by means of electrospinning (ES). Field-emission scanning electron microscopy and attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy were used for the physicochemical characterization of nanofibers. The anxiolytic activity of new derivatives and drug-loaded nanofibers was studied with an elevated plus maze test and light-dark box test. New 1,2,3-triazolo-1,4-benzodiazepine derivatives showed a promising anxiolytic effect in mice with clear changes in behavioral reactions in both tests. The nanofiber-based DDS was found to be feasible in the oral delivery of the present benzodiazepine derivatives. The nanofibers generated by means of ES presented the diameter in a nanoscale, uniform fiber structure, capacity for drug loading, and the absence of defects. The present findings provide new insights in the drug treatment of anxiety disorders with new benzodiazepine derivatives.


Assuntos
Ansiolíticos , Nanofibras , Humanos , Feminino , Masculino , Camundongos , Animais , Nanofibras/química , Benzodiazepinas , Hipnóticos e Sedativos , Anticonvulsivantes , Sistemas de Liberação de Medicamentos
11.
Plants (Basel) ; 13(3)2024 Jan 24.
Artigo em Inglês | MEDLINE | ID: mdl-38337883

RESUMO

Galenic preparations of German chamomile are used to treat mild skin diseases, inflammation, and spasms, and they have also been reported to have anxiolytic and sedative effects. The medicinal use of chamomile is well known in ethnomedicine. After obtaining its galenic preparations, there is lots of waste left, so it is expedient to develop waste-free technologies. The aims of this study were to gain knowledge of the ethnomedical status of chamomile in the past and present, develop methods for preparing essential oils and dry extracts from German chamomile flowers using complex processing, reveal the phytochemical composition of such extracts, and verify the analgesic and soporific activity of the extracts. Two methods for the complex processing of German chamomile flowers were developed, which allowed us to obtain the essential oil and dry extracts of the tincture and aqueous extracts as byproducts. A total of 22 phenolic compounds (7 hydroxycinnamic acids, 13 flavonoids, and 2 phenolic acids) were found in the dry extracts by using UPLC-MS/MS. In total, nine main terpenoids were identified in the chamomile oil, which is of the bisabolol chemotype. During the production of chamomile tincture, a raw material-extractant ratio of 1:14-1:16 and triple extraction are recommended for its highest yield. In in vivo studies with mice and rats, the extracts showed analgesic activity and improvements in sleep. The highest sedative and analgesic effects in rodents were found with the dry extract prepared by using a 70% aqueous ethanol solution for extraction at a dose of 50 mg/kg. The developed methods for the complex processing of German chamomile flowers are advisable for implementation into the pharmaceutical industry to reduce the volume of waste during the production of its essential oil and tincture, and to obtain new products.

12.
Biomolecules ; 14(3)2024 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-38540779

RESUMO

Pineapple weed (Matricaria discoidea DC.) is a widespread plant in Europe and North America. In ethnomedicine, it is well-known for its anti-inflammatory and spasmolytic activities. The aim of this research was to develop novel methods of M. discoidea processing to obtain essential oil and dry extracts and to investigate their phytochemical compositions. Moreover, the molecular docking of the main substances and the in vivo studies on their soporific and analgesic activities were conducted. The essential oil and two dry extracts from M. discoidea were prepared. A total of 16 phenolic compounds (seven flavonoids, seven hydroxycinnamic acids, and two phenolic acids) in the dry extracts were identified by means of UPLC-MS/MS. In the essential oil, nine main terpenoids were identified by gas chromatography (GC). It was shown that phenolic extraction from the herb was successful when using 70% ethanol in a triple extraction method and at a ratio of 1:14-1:16. The in vivo studies with rodents demonstrated the analgesic activity of the M. discoidea extracts and improvements in the sleep of animals. The dry extracts of M. discoidea did not show any toxicity. The molecular docking analysis showed a high probability of COX-1,2 inhibition and NMDA receptor antagonism by the extracts.


Assuntos
Matricaria , Óleos Voláteis , Animais , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cromatografia Líquida , Espectrometria de Massas em Tandem , Analgésicos/farmacologia , Analgésicos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Óleos Voláteis/farmacologia , Etanol , Fenóis/farmacologia , Antioxidantes/química
13.
Drug Dev Ind Pharm ; 39(3): 489-98, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22458299

RESUMO

To date, little is known on applicability of different types of pharmaceutical dosage forms in an automated high-speed multi-dose dispensing process. The purpose of the present study was to identify and further investigate various process-induced and/or product-related limitations associated with multi-dose dispensing process. The rates of product defects and dose dispensing errors in automated multi-dose dispensing were retrospectively investigated during a 6-months follow-up period. The study was based on the analysis of process data of totally nine automated high-speed multi-dose dispensing systems. Special attention was paid to the dependence of multi-dose dispensing errors/product defects and pharmaceutical tablet properties (such as shape, dimensions, weight, scored lines, coatings, etc.) to profile the most suitable forms of tablets for automated dose dispensing systems. The relationship between the risk of errors in dose dispensing and tablet characteristics were visualized by creating a principal component analysis (PCA) model for the outcome of dispensed tablets. The two most common process-induced failures identified in the multi-dose dispensing are predisposal of tablet defects and unexpected product transitions in the medication cassette (dose dispensing error). The tablet defects are product-dependent failures, while the tablet transitions are dependent on automated multi-dose dispensing systems used. The occurrence of tablet defects is approximately twice as common as tablet transitions. Optimal tablet preparation for the high-speed multi-dose dispensing would be a round-shaped, relatively small/middle-sized, film-coated tablet without any scored line. Commercial tablet products can be profiled and classified based on their suitability to a high-speed multi-dose dispensing process.


Assuntos
Rotulagem de Medicamentos/métodos , Prescrições de Medicamentos/normas , Erros de Medicação/prevenção & controle , Preparações Farmacêuticas/normas , Relação Dose-Resposta a Droga , Rotulagem de Medicamentos/normas , Embalagem de Medicamentos , Seguimentos , Humanos , Polimedicação , Estudos Retrospectivos
14.
AAPS PharmSciTech ; 14(3): 1129-36, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23867979

RESUMO

Tablet compression of softwood cellulose and lignin prepared by a new catalytic oxidation and acid precipitation method were investigated and compared with the established pharmaceutical direct compression excipients. Catalytic pretreated softwood cellulose (CPSC) and lignin (CPSL) were isolated from pine wood (Pinus sylvestris). The compaction studies were carried out with an instrumented eccentric tablet machine. The plasticity and elasticity of the materials under compression were evaluated using force-displacement treatment and by determining characteristic plasticity (PF) and elasticity (EF) factors. With all biomaterials studied, the PF under compression decreased exponentially as the compression force increased. The compression force applied in tablet compression did not significantly affect the elasticity of CPSC and microcrystalline cellulose (MCC) while the EF values for softwood lignins increased as compression force increased. CPSL was clearly a less plastically deforming and less compactable material than the two celluloses (CPSC and MCC) and hardwood lignin. CPSL presented deformation and compaction behaviour almost identical to that of lactose monohydrate. In conclusion, the direct tablet compression behaviour of native lignins and celluloses can greatly differ from each other depending on the source and isolation method used.


Assuntos
Celulose/química , Química Farmacêutica , Excipientes/química , Lignina/química , Catálise , Microscopia Eletrônica de Varredura , Pinus/química , Comprimidos
15.
Eur J Pharm Sci ; 187: 106487, 2023 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-37277046

RESUMO

Overcoming the health threatening consequences of staphylococcal infections and their negative socio-economic effects have become a priority in the medical, pharmaceutical, food and many other sectors globally. Staphylococcal infections are a big challenge for a global health care, since they are difficult to be diagnosed and treated. Therefore, the development of new medicinal products of plant-origin is timely and important, because bacteria have a limited ability to develop resistance to such products. In the present study, a modified eucalypt (Eucalyptus viminalis L.) extract was prepared and further enhanced by using different excipients (surface active agents) to obtain a water-miscible 3D-printable extract (nanoemulsified aqueous eucalypt extract). Phytochemical and antibacterial studies of the eucalypt leaves extracts were conducted as a preliminary investigation for 3D-printing experiments of the extracts. The nanoemulsified aqueous eucalypt extract was mixed with polyethylene oxide (PEO) to form a gel applicable for semi-solid extrusion (SSE) 3D printing. The key process parameters in a 3D-printing process were identified and verified. The printing quality of the 3D-lattice type eucalypt extract preparations was very good, demonstrating the feasibility of using an aqueous gel in SSE 3D printing also exhibiting compatibility of the carrier polymer (PEO) with the plant extract. The SSE 3D-printed eucalypt extract preparations presented a rapid dissolution in water within 10-15 min, suggesting the applicability of these preparations e.g., in oral immediate-release applications.


Assuntos
Anti-Infecciosos , Infecções Estafilocócicas , Humanos , Liberação Controlada de Fármacos , Polietilenoglicóis , Impressão Tridimensional , Preparações Farmacêuticas , Tecnologia Farmacêutica , Comprimidos
16.
J Funct Biomater ; 14(7)2023 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-37504859

RESUMO

Derived Hench bioactive glass (BaG) containing boron (B) is explored in this work as it plays an important role in bone development and regeneration. B was also found to enhance BaG dissociation. However, it is only possible to incorporate a limited amount of B. To increase the amount of B in BaG, bioactive borosilicate glasses (BaG-Bx) were fabricated based on the use of the solution-gelation process (sol-gel). In this work, a high B content (20 wt.%) in BaG, respecting the conditions of bioactivity and biodegradability required by Hench, was achieved for the first time. The capability of BaG-Bx to form an apatite phase was assessed in vitro by immersion in simulated body fluid (SBF). Then, the chemical structure and the morphological changes in the fabricated BaG-Bx (x = 0, 5, 10 and 20) were studied. The formation of hydroxyapatite (HAp) layer was observed with X-ray diffraction (XRD) and infrared (IR) spectroscopy. The presence of HAp layer was confirmed using scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Enhanced bioactivity and chemical stability of BaG-Bx were evaluated with an ion exchange study based on Inductively Coupled Plasma-Optical Emission Spectrometry (ICP-OES) and energy dispersive spectroscopy (EDS). Results indicate that by increasing the concentration of B in BaG-Bx, the crystallization rate and the quality of the newly formed HAp layer on BaG-Bx surfaces can be improved. The presence of B also leads to enhanced degradation of BaGs in SBF. Accordingly, BAG-Bx can be used for bone regeneration, especially in children, because of its faster degradation as compared to B-free glass.

17.
Pharmaceutics ; 15(11)2023 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-38004508

RESUMO

One of the key pathogenetic links in type 2 diabetes mellitus (T2DM) is the formation of insulin resistance (IR). Besides a wide selection of synthetic antidiabetic drugs, various plant-origin extracts are also available to support the treatment of T2DM. This study aimed to investigate and gain knowledge of the chemical composition and potential IR correction effect of American cranberry (Vaccinium macrocarpon Aiton) leaf extracts and formulate novel 3D-printed oral dosage forms for such extracts. The bioactivity and IR of L-arginine-loaded cranberry leaf extracts were studied in vivo in rats. The cranberry leaf extracts consisted of quinic, 3-caffeoylquinic (chlorogenic), p-coumaroylquinic acids, quercetin 3-O-galactoside, quercetin-3-O-glucoside, quercetin-3-xyloside, quercetin-3-O-arabino pyranoside, quercetin-3-O-arabinofuranoside, quercetin 3-O-rhamnoside, and quercetin-O-p-coumaroyl hexoside-2 identified by HPLC. In vivo studies with rats showed that the oral administration of the cranberry leaf extracts had a positive effect on insulin sensitivity coefficients under the insulin tolerance test and affected homeostasis model assessment IR levels and liver lipid content with experimental IR. A novel 3D-printed immediate-release dosage form was developed for the oral administration of cranberry leaf extracts using polyethylene oxide as a carrier gel in semi-solid extrusion 3D printing. In conclusion, American cranberry leaf extracts loaded with L-arginine could find uses in preventing health issues associated with IR.

18.
Front Pharmacol ; 13: 761787, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35418859

RESUMO

Background: Drug-related problems (DRPs) which arise from potentially inappropriate medications (PIMs) are a common problem in older people with multi-morbidity and polypharmacy. Aim: To develop an integrated PIM clinical decision support tool for identification of DRPs in geriatric multi-morbid polypharmacy patients, using the EU(7)-PIM and EURO-FORTA lists, with a focus on high-risk medications. Methods: The integrated PIM tool used the information on PIMs in both databases-the EU(7)-PIM and EURO-FORTA. PIMs were classified into four color groups based on risk profile: high-risk PIMs (should be avoided in older patients) as red, moderate-risk PIMs (require dose and/or treatment duration adjustment) as yellow, low-risk PIMs (low DRP risk) as green, and questionable PIMs (incomplete/missing information) as grey. Results: The summarized list of the high-risk (red and some grey) PIMs contained 81 active substances and medication classes. According to the ATC classification, most of the high-risk PIMs (n = 60, 74.1%) belong to the A, C, and N medication groups and 50.6% (n = 41) of the high-risk PIMs have currently marketing authorization in Estonia. The preliminary list of the moderate- and low-risk (yellow, green, and other grey) PIMs contained 240 active substances and medication classes, but sub-classification of this category into one or another group depends mainly on an individual patient´s clinical characteristics in a concrete analyzed study sample and needs further research. Conclusion: The integrated clinical decision support tool based on the EU(7)-PIM and EURO-FORTA criteria addresses the need for more efficient identification of DRPs. It can be applied to identify PIMs and geriatric prescribing problems in different health care settings, and also in a context of little clinical information available.

19.
Int J Pharm ; 616: 121558, 2022 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-35143904

RESUMO

Theophylline (TEO) nanofibers with polyethylene oxide (PEO) were prepared by conventional electrospinning (ES) and novel needleless ultrasound-enhanced electrospinning (USES). They were compared for Young's modulus, elongation at rupture and rupture stress, tabletability and drug release. Placebo (PEO) or drug-loaded (PEO/TEO 90:10) nanofibers were examined by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and infrared spectroscopy (ATR-FTIR). Nanofibers prepared by USES were thinner than ES nanofibers and drug-loaded nanofibers thinner than placebo. Drug was mostly amorphous and interacted weakly with PEO. Mats generated by USES and also drug-loaded mats demonstrated higher Young's modulus (stiffness) and higher rupture stress. Under compression, USES and drug-loaded nanofibers demonstrated greater compaction work, higher yield pressure (Heckel and K-L models), and produced stronger tablets than ES and placebo respectively. Principal Component Analysis revealed two significant components explaining 91.05% of the variance. The first comprised the compaction work, yield pressure (ductility) and Young's modulus that were positively intercorrelated and elongation at rupture that was correlated negatively. The second comprised the mat rupture stress and tablet breaking load. Drug release from nanofibrous tablets was faster than tablets of physical mixture but there was no difference between the tablets of the two electrospinning methods.


Assuntos
Nanofibras , Liberação Controlada de Fármacos , Nanofibras/química , Polietilenoglicóis/química , Comprimidos , Teofilina
20.
Pharmaceutics ; 14(9)2022 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-36145548

RESUMO

Essential oils (EOs) have been widely exploited for their biological properties (mainly as antimicrobials) in the food industry. Encapsulation of EOs has opened the way to the utilization of EOs in the pharmaceutical and biomedical fields. Electrospinning (ES) has proved a convenient and versatile method for the encapsulation of EOs into multifunctional nanofibers. Within the last five years (2017-2022), many research articles have been published reporting the use of ES for the fabrication of essential oil-loaded nanofibers (EONFs). The objective of the present mini-review article is to elucidate the potential of EONFs in the pharmaceutical and biomedical fields and to highlight their advantages over traditional polymeric films. An overview of the conventional ES and coaxial ES technologies for the preparation of EONFs is also included. Even though EONFs are promising systems for the delivery of EOs, gaps in the literature can be recognized (e.g., stability studies) emphasizing that more research work is needed in this field to fully unravel the potential of EONFs.

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