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1.
J Sci Food Agric ; 2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-38940545

RESUMO

BACKGROUND: Pomegranate peel waste is a valuable reservoir of heat-sensitive total hydrolysable tannins (THT), with potential applications in food and pharmaceuticals. Preserving THT is challenging due to degradation post-extraction. We explore ionic gelation as an encapsulation method to optimize THT utilization. RESULTS: Through external gelation, we optimized the process variables using Box-Behnken design. At 40 g kg-1 sodium alginate, 25 g kg-1 calcium chloride, and 300 g kg-1 pomegranate peel extract (PPE), we achieved an 83.65% encapsulation efficiency. Compared to spray drying, external gelation demonstrated superior performance, with enhanced release percentages and stability. Physical, phytochemical, and release profiles of encapsulates were extensively analysed. External gelation achieved an 87.5% release in 30 min, outperforming spray-dried counterparts (69.7% in 25 min). Encapsulated PPE exhibited robust antibacterial activity against Staphylococcus aureus (ATCC 25923) in powdered infant formula, with a 32 ± 0.01 mm zone of inhibition and 300 µg mL-1 minimum inhibitory concentration. Insights into S. aureus growth curves underlined the mechanism of action via membrane potential alterations. The results of carried investigations also showed that the antibacterial activity of the encapsulated PPE extracts against the targeted organism was identical to the antibacterial activity exhibited by synthetic antibiotics used generally to kill microorganisms in food. Therefore, from the findings, it can be concluded that the PPE encapsulate produced using the external gelation technique at the optimized condition displayed superior storage stability possessing strong antimicrobial activity when compared to encapsulate produced using the spray drying technique. CONCLUSIONS: External gelation emerges as a potent technique for developing effective encapsulates enriched with natural antimicrobials or antibiotics. This approach holds promise for applications in food, pharmaceuticals, and nutraceuticals, enhancing stability and efficacy while reducing reliance on synthetic antibiotics. © 2024 Society of Chemical Industry.

2.
Small ; 19(10): e2206818, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36642817

RESUMO

In this work, the influence of two different types of cations on the gel formation and structure of mixed gel networks comprised of semiconductor (namely CdSe/CdS nanorods NR) and Au nanoparticles (NP) as well as on the respective monocomponent gels is investigated. Heteroassemblies built from colloidal building blocks are usually prepared by ligand removal or cross-linking, thus, both the surface chemistry and the destabilising agent play an essential role in the gelation process. Due to the diversity of the composition, morphology, and optical properties of the nanoparticles, a versatile route to fabricate functional heteroassemblies is of great demand. In the present work, the optics, morphology, and gelation mechanism of pure semiconductor and noble metal as well as their mixed nanoparticle gel networks are revealed. The influence of the gelation agents (bivalent and trivalent cations) on the structure-property correlation is elucidated by photoluminescence, X-ray photoelectron spectroscopy, and electron microscopy measurements. The selection of cations drastically influences the nano- and microstructure of the prepared gel network structures driven by the affinity of the cations to the ligands and the nanoparticle surface. This gelation technique provides a new platform to control the formation of porous assemblies based on semiconductor and metal nanoparticles.

3.
J Microencapsul ; 40(1): 29-36, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36632694

RESUMO

AIM: Silybum marianum extract (SME) possesses neuroprotective potency through its high antioxidant content. We attempted to increase the effectiveness of SME by encapsulating them in chitosan. Neuroprotective potency of SME and SME-loaded chitosan nanoparticles (SME-CNPs) were shown in SH-SY5Y cell line against H2O2-induced oxidative stress. METHODS: We produced CNPs and SME-CNPs by ionic gelation method and properly determined their physical characteristics. Encapsulation efficiency, loading capacity, and in vitro release tests were performed for SME-CNPs. The neurotoxicity and neuroprotective efficiency in SH-SY5Y cell line against H2O2 was also investigated. RESULTS: The size of SME-CNPs was 168.2 ± 11.12 nm with zeta potential 10.6 ± 1.0 mV. The encapsulation efficiency and loading capacity were successfully achieved at 96.6% and 1.89% respectively. SME and SME-CNPs improved cell viability higher than 80%, and SME-CNPs exhibited significant neuroprotective effects against H2O2 damage. CONCLUSIONS: It was concluded that SME and SME-CNPs highly prevent damage caused by H2O2 and reduce cell damage in vitro by their neuroprotective effects.


Assuntos
Quitosana , Nanopartículas , Neuroblastoma , Fármacos Neuroprotetores , Humanos , Quitosana/farmacologia , Fármacos Neuroprotetores/farmacologia , Peróxido de Hidrogênio , Silybum marianum
4.
Molecules ; 28(11)2023 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-37298804

RESUMO

Chitosan nanoparticles (CNPs) are known to have great utility in many fields (pharmaceutical, agricultural, food industry, wastewater treatment, etc.). In this study we aimed to synthesize sub-100 nm CNPs as a precursor of new biopolymer-based virus surrogates for water applications. We present a simple yet efficient synthesis procedure for obtaining high yield, monodisperse CNPs with size 68-77 nm. The CNPs were synthesized by ionic gelation using low molecular weight chitosan (deacetylation 75-85%) and tripolyphosphate as crosslinker, under rigorous homogenization to decrease size and increase uniformity, and purified by passing through 0.1 µm polyethersulfone syringe filters. The CNPs were characterized using dynamic light scattering, tunable resistive pulse sensing, and scanning electron microscopy. We demonstrate reproducibility of this method at two separate facilities. The effects of pH, ionic strength and three different purification methods on the size and polydispersity of CNP formation were examined. Larger CNPs (95-219) were produced under ionic strength and pH controls, and when purified using ultracentrifugation or size exclusion chromatography. Smaller CNPs (68-77 nm) were formulated using homogenization and filtration, and could readily interact with negatively charge proteins and DNA, making them an ideal precursor for the development of DNA-labelled, protein-coated virus surrogates for environmental water applications.


Assuntos
Quitosana , Nanopartículas , Quitosana/química , Reprodutibilidade dos Testes , Nanopartículas/química , Tamanho da Partícula , Alimentos
5.
Molecules ; 28(15)2023 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-37570651

RESUMO

Nanoencapsulation is widely considered as a highly effective strategy to enhance essential oils' (EO) stability by protecting them from oxidative deterioration and evaporation. The present study aims to optimize and characterize an efficient technique for encapsulating Cinnamomum (C.) verum essential oil into chitosan nanoparticles using response surface methodology (RSM). Moreover, the optimized C. verum EO nanoparticle was investigated for its antibacterial (against Gram-positive and Gram-negative bacteria), antifungal (against Candida albicans), and antiparasitic activity (against Leishmania parasites). Five parameters were investigated using a Plackett-Burman and Box-Behnken statistical design: the chitosan molecular weight, TPP concentration, C. verum EO/chitosan ratio, mixing method, and the duration of the reaction. Encapsulation efficiency and anti-candida activity were considered as responses. The antibacterial, anticandidal, and anti-leishmanial activities were also assessed using a standard micro-broth dilution assay and the cytotoxicity assay was assessed against the macrophage cell line RAW 264.7. The optimized nanoparticles were characterized using Fourier transform infrared spectroscopy, Zeta potential, and scanning electron microscopy. The study results indicated that under optimal conditions, the nanoencapsulation of C. verum EO into chitosan nanoparticles resulted in an encapsulation efficiency of 92.58%, with a regular distribution, a nanoparticle size of 480 ± 14.55 nm, and a favorable Zeta potential of 35.64 ± 1.37 mV. The optimized C. verum EO/chitosan nanoparticles showed strong antifungal activity against C. albicans pathogens (CMI = 125 µg mL-1), notable antibacterial activity against both Gram-positive and Gram-negative bacteria (ranging from 125 to 250 µg mL-1), high leishmanicidal potential against the promastigotes form of L. tropica and L. major (IC50 = 10.47 and 15.09 µg mL-1, respectively), and a four-fold cytotoxicity reduction compared to non-encapsulated essential oil. These results suggest that C. verum EO-loaded chitosan nanoparticles could be a promising delivery system for the treatment of cutaneous Candida albicans infections.


Assuntos
Quitosana , Nanopartículas , Óleos Voláteis , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Candida , Cinnamomum zeylanicum/química , Antifúngicos/farmacologia , Antifúngicos/química , Quitosana/farmacologia , Antibacterianos , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Candida albicans , Nanopartículas/química
6.
Molecules ; 28(13)2023 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-37446946

RESUMO

Grape pomace is a by-product of winemaking characterized by a rich chemical composition from which phenolics stand out. Phenolics are health-promoting agents, and their beneficial effects depend on their bioaccessibility, which is influenced by gastrointestinal digestion. The effect of encapsulating phenol-rich grape pomace extract (PRE) with sodium alginate (SA), a mixture of SA with gelatin (SA-GEL), and SA with chitosan (SA-CHIT) on the bioaccessibility index (BI) of phenolics during simulated digestion in vitro was studied. A total of 27 individual phenolic compounds (IPCs) were quantified by UHPLC. The addition of a second coating to SA improved the encapsulation efficiency (EE), and the highest EE was obtained for SA-CHIT microbeads (56.25%). Encapsulation affected the physicochemical properties (size, shape and texture, morphology, crystallinity) of the produced microbeads, which influenced the delivery of phenolics to the intestine and their BI. Thus, SA-GEL microbeads had the largest size parameters, as confirmed by scanning electron microscopy (SEM), and the highest BI for total phenolic compounds and IPCs (gallic acid, 3,4-dihydroxybenzoic acid and o-coumaric acid, epicatechin, and gallocatechin gallate) ranged from 96.20 to 1011.3%. The results suggest that encapsulated PRE has great potential to be used as a functional ingredient in products for oral administration.


Assuntos
Fenóis , Extratos Vegetais , Vitis , Alginatos/química , Disponibilidade Biológica , Cápsulas , Cromatografia Líquida de Alta Pressão , Digestão , Gelatina/química , Microscopia Eletrônica de Varredura , Microesferas , Tamanho da Partícula , Fenóis/química , Fenóis/farmacocinética , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Vitis/química , Técnicas In Vitro
7.
J Sci Food Agric ; 103(13): 6190-6197, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37139630

RESUMO

BACKGROUND: Monascus pigments (Mps) are easily impacted by heating, pH and light, resulting in degradation. In this study, Mps were encapsulated by the ionic gelation method with sodium alginate (SA) and sodium caseinate (SC), as well as CaCl2 as a crosslinker. The encapsulated Mps SA/SC in four proportions (SA/SC: 1/4, 2/3, 3/2, 4/1, w/w). Then, the encapsulation efficiency and particle size of the SA/SC-Mps system were evaluated to obtain the optimal embedding conditions. Finally, the effects of heating, pH, light and storage on the stability of non-capsulated Mps and encapsulated Mps were assessed. RESULTS: SA/SC = 2/3 (AC2) had higher encapsulation efficiency (74.30%) of Mps and relatively small particle size (2.02 mm). The AC2 gel beads were chosen for further investigating the stability of encapsulated Mps to heating, pH, light and storage. Heat stability experiments showed that the degradation of Mps followed first-order kinetics, and the encapsulated Mps had lower degradation rates than non-capsulated Mps. Encapsulation could reduce the effect of pH on Mps. The effects of ultraviolet light on the stability of Mps were considered, and showed that the retention efficiency of encapsulated Mps was 22.01% higher than that of non-capsulated Mps on the seventh day. Finally, storage stability was also evaluated under dark refrigerated conditions for 30 days, and the results indicated that encapsulation could reduce the degradation of Mps. CONCLUSION: This study has proved that AC2 gel beads can improve the stability of Mps. Thus, the ionic gelation method is a promising encapsulation method to improve the stability of Mps. © 2023 Society of Chemical Industry.


Assuntos
Monascus , Monascus/metabolismo , Alginatos/metabolismo , Extratos Vegetais/metabolismo , Caseínas/metabolismo
8.
Appl Microbiol Biotechnol ; 106(24): 8021-8034, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36370157

RESUMO

In this work, extracellular colored metabolites obtained from the filamentous fungi Talaromyces australis and Penicillium murcianum, isolated in the Andean-Patagonian native forests of Chile, were studied as prospect compounds to increase the sustainability of cosmetic products. The chemical and antioxidant properties of these natural pigments were characterized and strategies for their microencapsulation were also studied. UHPLC/MS-MS analyses indicated that the predominant metabolites detected in the cultures of P. murcianum were monascin (m/z = 411.15) and monashexenone (m/z = 319.10), while athrorosin H (m/z = 458.20) and damnacanthal (m/z = 281.05) were detected in cultures of T. australis. ORAC tests revealed that P. murcianum's metabolites had the greatest antioxidant properties with values higher than 2000 µmol of trolox equivalents/g. The fungal metabolites were successfully microencapsulated by ionic gelation into structures made of 1.3% sodium alginate, 0.2% chitosan, and 0.07% hyaluronic acid. The microencapsulation process generated structures of 543.57 ± 0.13 µm of mean diameter (d50) with an efficiency of 30% for P. murcianum, and 329.59 ± 0.15 µm of mean diameter (d50) and 40% efficiency, for T. australis. The chemical and biological characterization show the biotechnological potential of these fungal species to obtain pigments with antioxidant activity that could be useful in the cosmetic industry. The encapsulation process enables the production of easy-to-handle dry powder from the fungal metabolites, which could be potentially marketed as a functional cosmetic ingredient. KEY POINTS: • The predominant fungal pigments were of azaphilone and anthraquinoid classes. • The fungal pigments showed high antioxidant activity by ORAC assay. • Fungal pigment microcapsules obtained by ionic gelation were characterized.


Assuntos
Antioxidantes , Biotecnologia
9.
Bioprocess Biosyst Eng ; 45(6): 999-1009, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35305152

RESUMO

Isomaltulose is a potential substitute for sucrose, with a high stability and prebiotic potential, for wide use in candies and soft drinks. This sugar is obtained from sucrose through enzymatic conversion using microbial glucosyltransferases. This work aimed to optimize a matrix to immobilize glucosyltransferase producing Erwinia sp. D12 cells using a sequential experimental strategy. The cell mass of Erwinia sp. D12 obtained in a bioreactor was immobilized in beads formed by ionic gelation. The conversion of sucrose into isomaltulose using the beads was performed in batch and continuous processes, and the isomaltulose was recovered through crystallization. The stability of isomaltulose was assessed in beverages of different pH values, and its prebiotic potential was verified with the growth of probiotic microorganisms. The optimized matrix composed of alginate (2.0% w/v), CaCl2 (2.0% w/v), gelatin (2.0% w/v), and transglutaminase (0.2% w/v) showed the highest mean of produced isomaltulose (199.82 g/L) after four batches. In addition, high stability during the continuous process resulted in an isomaltulose production above of 230 g/L for up to 72 h. The produced isomaltulose was more stable than sucrose in lemon soft drink and orange and grape energy drinks after 30 days of storage; and promoted the growth of Bifidobacterium animalis and Lactobacillus lactis. In conclusion, the production of isomaltulose by Erwinia sp. D12 cells immobilized using optimized conditions is recommended, due to its high conversion capacity, high stability, and prebiotic potential of crystals obtained.


Assuntos
Erwinia , Glucosiltransferases/química , Isomaltose/análogos & derivados , Prebióticos , Sacarose
10.
Saudi Pharm J ; 30(4): 454-461, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35527830

RESUMO

Herein we describe the preparation, characterization and the antibacterial effect of Tobramycin-chitosan nanoparticles (TOB-CS NPs) coated with zinc oxide nanoparticles (ZnO NPs). Four formulations of TOB-CS NPs (A-D) were prepared to study the effect of experimental variables on the NPs behavior. Two formulations of ZnO NPs were prepared using the solvothermal and the precipitation methods (ZnO1 and ZnO2), and then characterized. TOB-CS NPs (Formula d) was coated with the ZnO1. Moreover, the antibacterial activity of TOB-CS NPs, ZnO NPs and the coated nanoparticles against S. aureus and E. coli was examined. Changing the variables in preparing TOB-CS NPs resulting in variabilities in sizes (297.6-1116.3 nm), charges (+8.29-+39.00 mV), entrapment (51.95-90.60%). Further, TOB release was sustained over four days. ZnO NPs have sizes of 47.44 and 394.4 nm and charges of -62.3 and 89.4 mV when prepared by solvothermal and precipitation technique, respectively. Coated TOB-CS NPs had a size of 342 nm, a charge of +4.39 and released 100 µg/ mL of the drug after four days. The antimicrobial activity of TOB-CS NPs was lower than free TOB against S. aureus and E. coli. The coated NPs showed higher antimicrobial effect in comparison to formula D and ZnO1. In conclusion, coating TOB-CS NPs with ZnO NPs exhibited a great antibacterial effect that may be sustained for days.

11.
Bioprocess Biosyst Eng ; 44(6): 1109-1118, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33547961

RESUMO

Isomaltulose is an alternative sugar obtained from sucrose using some bacteria producing glycosyltransferase. This work aimed to optimize conditions for the immobilization of Serratia plymuthica through ionic gelation and cross-linking by transglutaminase using the sequential experimental strategy for the conversion of sucrose into isomaltulose. The effect of five variables (concentrations of cell mass, alginate, gelatin, transglutaminase, and calcium chloride) was studied, as well as the interactions between them on the matrix composition for the S. plymuthica immobilization. Three experimental designs were used to optimize the concentrations of each variable to obtain higher concentration of isomaltulose. A high conversion of sucrose into isomaltulose (71.04%) was obtained by the cells immobilized in a matrix composed of alginate (1.7%), CaCl2 (0.25 mol/L), gelatin (0.5%), transglutaminase (3.5%) and cell mass (33.5%). As a result, the transglutaminase application as a cross-linking agent improved the immobilization of Serratia plymuthica cells and the conversion of sucrose into isomaltulose.


Assuntos
Células Imobilizadas , Reagentes de Ligações Cruzadas/química , Isomaltose/biossíntese , Serratia , Sacarose/metabolismo , Transglutaminases/química , Células Imobilizadas/química , Células Imobilizadas/metabolismo , Serratia/química , Serratia/metabolismo
12.
Drug Dev Ind Pharm ; 47(3): 477-483, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33621153

RESUMO

Background: Organ transplantation is an important and critical procedure, which requires the suppression of immunity, and to suppress the immunity, a constant plasma concentration of immunosuppressant is required.Objectives: The said objective can be achieved by formulating a controlled release drug delivery system of the drug. Chitosan (CHT) nanoparticles (NPs) have been revolutionizing the conventional drug delivery system, for the past two decades. The aim of the current research work was to develop and evaluate CHT-based mycophenolate mofetil (MMF) loaded nanoparticles (CHT/MMF-NPs) using different drug to polymer ratios.Methods: The challenge was to entrap a lipophilic drug within NPs by the ionic gelation method of the positively charged CHT, using tripolyphosphate (TPP) as the crosslinking agent. The prepared CHT/MMF-NPs were evaluated for physical and chemical characterizations, including particle size, surface charge, entrapment efficiency (EE), surface morphology by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) for chemical compatibilities, X-ray diffractometry (XRD) and in-vitro dissolution studies.Results: Outcomes of the studies revealed that particles were 260 ± 17 nm in diameter, with the smooth and regular surface. Satisfactory values of EE (99%) have indicated the suitability of selected ingredients and employed methodology. Moreover, FTIR has confirmed the chemical compatibilities of the formulations. In-vitro dissolution studies have indicated diffusion type of controlled and sustained drug release during 24 h, with zero-order, as best fit kinetic model.Conclusion: Conclusively, the successful achievement of objectives has indicated the suitability of excipients and methodology to prepare CHT/MMF-NPs for better therapeutic outcomes.


Assuntos
Quitosana , Nanopartículas , Quitosana/metabolismo , Preparações de Ação Retardada , Portadores de Fármacos , Liberação Controlada de Fármacos , Ácido Micofenólico , Tamanho da Partícula , Espectroscopia de Infravermelho com Transformada de Fourier
13.
J Microencapsul ; 38(2): 100-107, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33245001

RESUMO

Aim: This paper aims to study in-vitro and in-vivo evaluation of chitosan (CHI) biocomposite of gentamicin nanoparticles (GNPs) for wound healing. Methods: In this study, CHI nanoparticles (NPs) were prepared using the ionic gelation technique. GNP biocomposites were examined on the excision wound model in Wistar rats to determine the in-vivo efficiency. Results: The diameter and zeta potential of NPs were between 151-212.9 nm and 37.2 - 51.1 mV, respectively. The entrapment efficiency was in an acceptable range of 36.6-42.7% w/w. The release test information was fitted to mathematical models (Zero, First order, Higuchi, and Korsmeyer-Peppas), and according to calculations, the kinetics of drug release followed the Korsmeyer-Peppas model. A comparison of thermograms revealed that the drug was present in the formulation in a non-crystalline form. Conclusion: Histological studies of the wound showed that the rate of skin tissue repair was higher in the GNP biocomposite treatment group than in the others.


Assuntos
Antibacterianos/administração & dosagem , Quitosana/química , Portadores de Fármacos/química , Gentamicinas/administração & dosagem , Nanopartículas/química , Cicatrização/efeitos dos fármacos , Animais , Antibacterianos/química , Antibacterianos/uso terapêutico , Liberação Controlada de Fármacos , Gentamicinas/química , Gentamicinas/uso terapêutico , Ratos Wistar , Pele/efeitos dos fármacos , Pele/lesões , Pele/patologia
14.
Pharm Dev Technol ; 26(2): 181-192, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33213232

RESUMO

Co-loaded isoniazid and pyrazinamide chitosan nanoparticles were formulated using the ionic gelation method. The formulations were adjusted to five mass ratios of tripolyphosphate (TPP) and chitosan at three TPP concentrations. Particle size, polydispersity index, zeta potential, and encapsulation efficiency were used to evaluate all formulations. The results revealed that the ratio of TPP to chitosan had the highest impact in generating chitosan nanoparticles. The selected nanoparticle formulations were freeze-dried, and the obtained dry powders were characterized using scanning electron microscopy, differential scanning calorimetry, X-ray diffraction, and Fourier-transform infrared spectroscopy to confirm the interaction of loaded drug and formulation excipients. The aerosolized performance of dry powders was also evaluated using the Andersen cascade impactor. A mass median aerodynamic diameter of 3.3-3.5 µm, % fine particle fraction of 30-44%, and 92-95% emitted dose were obtained from all formulations. The dry powder formulations were not toxic to the respiratory tract cell lines. Furthermore, they did not provoke alveolar macrophages into producing inflammatory cytokines or nitric oxides, indicating that the formulations are safe and could potentially be used to deliver to respiratory tract for tuberculosis treatment.


Assuntos
Quitosana/química , Isoniazida/administração & dosagem , Nanopartículas , Pirazinamida/administração & dosagem , Administração por Inalação , Animais , Antituberculosos/administração & dosagem , Antituberculosos/toxicidade , Linhagem Celular , Química Farmacêutica , Combinação de Medicamentos , Inaladores de Pó Seco , Excipientes/química , Liofilização , Humanos , Isoniazida/toxicidade , Macrófagos Alveolares/efeitos dos fármacos , Macrófagos Alveolares/metabolismo , Tamanho da Partícula , Polifosfatos/química , Pirazinamida/toxicidade , Ratos
15.
Drug Dev Ind Pharm ; 46(10): 1604-1612, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32812474

RESUMO

Biodegradable nanoparticulate carriers are potentially applicable compounds in the administration of therapeutic agents and drug delivery. They have received much attention due to their biological characteristics such as biodegradability, biocompatibility, and bioadhesive. The objectives of this work are first, investigating the impact of two important parameters (i.e. chitosan or sodium tripolyphosphate (TPP) solution concentration and chitosan to TPP mass ratio) on the chitosan nanoparticles (CNPs) formation by ionic-gelation method and then, the synthesis and characterization of chitosan-based, biodegradable drug-loaded nanoparticles in the encapsulation of novel 4'-(4-(methylsulfonyl)phenyl)-3'-(3,4,5-trimethoxyphenyl)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one (MTS) indanonic tricyclic spiroisoxazoline, which is a potent anticancer drug. The particle size, shape, zeta potential, drug loading capacity, in vitro release characteristics, and stability of the formulated drug-loaded nanoparticles of the different drug:carrier ratio has been studied. The results indicated that the particle size increased at the higher chitosan or TPP concentration while the mass ratio did not appear to be a significant parameter during the cross-linking process. The particle diameter and zeta potential of CNPs including MTS were approximately in the range of 256-350 nm and 24.08-38.70 mV, respectively. The entrapment efficiency steadily increased with increasing the concentration of the polymer in formulizations. Throughout 24 h, the in vitro release behavior was provided a sustained release from all the drug-loaded formulizations. The optimal formulization of CNPs based on drug content with a drug:carrier ratio of 1:2 did not change appreciably during 60-day storage at either 4 °C or the ambient temperature.


Assuntos
Quitosana , Nanopartículas , Polifosfatos/química , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Tamanho da Partícula
16.
Molecules ; 25(5)2020 Mar 02.
Artigo em Inglês | MEDLINE | ID: mdl-32131498

RESUMO

Breast cancer ranks as the fifth leading cause of death worldwide. Chemotherapy is commonly used directly or as neo-adjuvant therapy for the management of breast cancer with its attendant adverse effects, underscoring the need to develop biocompatible bioactive compounds for pharmacological applications. The aim of this study is to encapsulate carboplatin (CP) with silk fibroin protein (SF) by using an ionic gelation method as a drug carrier system and assess the apoptotic effect on MCF-7 breast cancer cells during in vitro studies. The characterization of silk fibroin encapsulated carboplatin (SFCP) microparticles was analyzed by FTIR spectrophotometer, SEM, Mastersizer, and biodegradation methods. The encapsulation efficiency and release profile of SFCP microparticles were analyzed by an indirect UV-Vis spectrophotometric method. An apoptotic screening of MCF-7 cells was carried out with 10-200 µg/mL CP loaded SFCP, which were cultured for 24, 48, and 72 h. Data were analyzed using the Student's t test and analysis of variance. FTIR and drug release studies confirmed an interaction of silk fibroin with the carboplatin moiety. SFCP showed successful encapsulation of the carboplatin moiety. Apoptotic screening showed a dose dependent increase in absorbance, indicating significant cell death (p < 0.05). Thus, the direct apoptotic effect of SFCP microparticles on MCF-7 was confirmed.


Assuntos
Apoptose/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Carboplatina , Portadores de Fármacos , Fibroínas , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Cápsulas , Carboplatina/química , Carboplatina/farmacologia , Portadores de Fármacos/química , Portadores de Fármacos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Fibroínas/química , Fibroínas/farmacologia , Humanos , Células MCF-7
17.
J Sci Food Agric ; 100(5): 2018-2026, 2020 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-31858600

RESUMO

BACKGROUND: Spirulina microalgae have been added to food; however, there have been few reports on the methods used to protect the antioxidant potential against process conditions, and the effects on the sensory characteristics of products need to be better described. The aim of this study was to evaluate the influence on the technological properties, sensory profile, and acceptability of the pasta with free or microencapsulated Spirulina biomass added. Pasta formulations included: free Spirulina (FSP), microencapsulated Spirulina (MSP), and empty microspheres (EMP), which were compared with the control pasta (CP). RESULTS: The microencapsulation protected the antioxidant potential of Spirulina in 37.8% of the pasta cooking conditions. The microspheres presented low solubility in water (86 g.kg-1 ) and high encapsulation efficiency (87.6%), this being appropriate for addition to products that need cooking in water. The technological properties of pasta (water absorption, weight gain, firmness, and adhesiveness) were affected, but the overall acceptability index (85.13%) was not influenced by the addition of microspheres, despite changes observed in the sensory profile obtained by the CATA (check-all-that-apply). CONCLUSIONS: Spirulina could be added to pasta even without microencapsulation but the microencapsulation in alginate allows for the protection of the antioxidant potential of the biomass, representing a potential alternative for the bakery industry. © 2019 Society of Chemical Industry.


Assuntos
Aditivos Alimentares/análise , Alimento Funcional/análise , Spirulina/química , Triticum/química , Antioxidantes/análise , Antioxidantes/metabolismo , Culinária , Farinha/análise , Aditivos Alimentares/metabolismo , Análise de Alimentos , Manipulação de Alimentos , Humanos , Spirulina/metabolismo , Paladar , Triticum/metabolismo
18.
J Food Sci Technol ; 57(11): 4171-4181, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33071338

RESUMO

Research into characterization and storage stability of carrot powders encapsulated in soy protein isolate and cassava starch based film solutions via ionic gelation method was performed. Carotene a major antioxidant presents in carrot powders plays a beneficial role in preventing some health problems such as cancer, and cardiovascular/coronary heart diseases. Consequently, the carotene contains a hydrocarbon with an unsaturated double bond or its oxygen derivatives, which makes it unstable and sensitive to moisture, heat, oxygen, light, and acid. There is therefore the need for encapsulation of this nutritive and healthy component of carrot powders to extend its stability. Film solutions required for encapsulation of the carrot powders were prepared from soy protein isolate, cassava starch and their combinations, and were as well categorized into plasticized and non-plasticized using glycerol in combination with sorbitol as plasticizer. Ionic encapsulation was achieved using sodium alginate for gelation of carrot powder beads in 5% calcium chloride solution for curing. Distinction in gelation features of the film solutions as a result of blend compositions as well as the addition of plasticizers substantially influenced the quality criteria of encapsulated carrot powder beads such as encapsulation efficiency, encapsulation yield, moisture content, hygroscopicity, particle size, and also their sensory qualities. Their values varied between 70.93-82.59%, 70.35-75.35%, 9.88-13.04%, 40.00-49.00 g/100 g, and 2.18-2.64 mm respectively. 100% soy protein isolate based film solution performed much better than 100% cassava starch based film solutions in preventing degradation of carotene content of the encapsulated carrot powder beads. Plasticization of the membrane solutions caused greater carotene degradation. Combination of soy-protein isolate (50%) and cassava starch (50%) composite based film solutions gave the best protection for carotene degradation having shelf life of 106 days while plasticized cassava starch based was the least with the shelf life of 13 days which is closed to that of the control (carrot powders).

19.
Drug Dev Ind Pharm ; 45(8): 1342-1350, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31094571

RESUMO

Objective: High lipophilicity and extensive hepatic metabolism limits the oral application of risperidone in the treatment of CNS disorders. In order address this limitation, risperidone (RS) loaded chitosan nanoparticles (CS-NPs) were processed for intranasal administration in the management of schizophrenia. Methods: RS loaded CS-NPs were prepared by ionic gelation of chitosan with tripolyphosphate and stabilized by tween 80/ poloxamer 188. The CS-NPs were characterized by FTIR, DSC, particle size, zeta potential and surface morphology. Entrapment efficiency, mucoadhesive strength, in vitro drug release, and release kinetics of CS-NPs were evaluated. Pharmacokinetics and pharmacodynamics of RS loaded CS-NPs were studied using Wistar rats. Stereotypy behavior and swimming normalization tests were conducted in amphetamine induced psychosis in animals. Results: Risperidone nanoparticles (RP12) were produced with an average size of 86 nm, polydispersity index of 0.287, zeta potential of +36.6 mV, mucoadhesion of 68.9% and entrapment efficiency of 77.96%. CS-NPs released the RS in controlled manner with Fickian diffusion mode. Maximum concentration of RS in plasma was 1240 ng/ml at 4 h for RP12, and 403.8 ng/ml at 2 h for RS sample. RS loaded CS-NPs significantly reduced the stereotypy score in experimental animals that indicated the efficiency of CS-NPs in delivery of RS at brain tissues and moreover amphetamine effect was reversed. Thus, RS loaded CS-NPs proved as potential delivery systems against induced psychotic disorders. Conclusion: Risperidone loaded chitosan nanoparticles were effective against schizophrenia via intranasal route.


Assuntos
Quitosana/química , Nanopartículas/química , Risperidona/química , Administração Intranasal/métodos , Animais , Disponibilidade Biológica , Encéfalo/efeitos dos fármacos , Química Farmacêutica/métodos , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Nanopartículas/administração & dosagem , Tamanho da Partícula , Poloxâmero/química , Polifosfatos/química , Polissorbatos/química , Ratos , Ratos Wistar , Esquizofrenia/tratamento farmacológico
20.
Drug Dev Ind Pharm ; 45(7): 1130-1139, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30884977

RESUMO

Objective: Control the release and enhance the bioavailability of chitosan-doxazosin mesylate nanoparticles (DM-NPs). Significance: Improve DM bioavailability for the treatment of benign prostatic hyperplasia and hypertension. Methods: Plackett-Burman design was utilized to screen the variables affecting the quality of DM-NPs prepared by ionic gelation method. The investigated variables were initial drug load (X1), chitosan percentage (X2), tripolyphosphate sodium (TPP) percentage (X3), poloxamer percentage (X4), homogenization speed (X5), homogenization time (X6) and TPP addition rate (X7). The prepared DM-loaded NPs have been fully evaluated for particle size (Y1), Zeta potential (Y2), production yield (Y3), entrapment efficiency (Y4), loading capacity (Y5), initial burst (Y6), and cumulative drug release (Y7). Finally, DM pharmacokinetic has been investigated on healthy albino male rabbits by means of non-compartmental analysis. Results: The combination of variables showed variability of Y1, Y2, and Y3 equal to 122-710 nm, 3.49-23.63 mV, and 47.31-92.96%, respectively. While Y4 and Y5, reached 99.87%, and 8.53%, respectively. The prepared NPs revealed that X2, X3, and X4 are the variables that play the important role in controlling the release behavior of DM from the NPs. The in vivo pharmacokinetic results indicated the enhancement in bioavailability of DM by 7 folds compared to drug suspension and the mean residence time prolonged to 23.72 h compared to 4.7 h of drug suspension. Conclusion: The study proved that controlling the release of DM from NPs enhance its bioavailability and improve the compliance of patients with hypertension or benign prostatic hyperplasia.


Assuntos
Quitosana/análogos & derivados , Quitosana/química , Doxazossina/química , Nanopartículas/química , Poloxâmero/química , Polifosfatos/química , Administração Oral , Animais , Disponibilidade Biológica , Química Farmacêutica/métodos , Portadores de Fármacos/química , Liberação Controlada de Fármacos/efeitos dos fármacos , Masculino , Tamanho da Partícula , Coelhos , Suspensões/química
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