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1.
Molecules ; 27(19)2022 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-36234697

RESUMO

The GC-MS analysis of tea tree oil (TTO) revealed 38 volatile components with sesquiterpene hydrocarbons (43.56%) and alcohols (41.03%) as major detected classes. TTO efficacy is masked by its hydrophobicity; nanoencapsulation can address this drawback. The results showed that TTO-loaded solid lipid nanoparticles (SLN1), composed of glyceryl monostearate (2% w/w) and Poloxamer188 (5% w/w), was spherical in shape with a core-shell microstructure. TTO-SLN1 showed a high entrapment efficiency (96.26 ± 2.3%), small particle size (235.0 ± 20.4 nm), low polydispersity index (0.31 ± 0.01), and high negative Zeta potential (-32 mV). Moreover, it exhibited a faster active agent release (almost complete within 4 h) compared to other formulated TTO-SLNs as well as the plain oil. TTO-SLN1 was then incorporated into cellulose nanofibers gel, isolated from sugarcane bagasse, to form the 'TTO-loaded nanolipogel' which had a shear-thinning behavior. Second-degree thermal injuries were induced in Wistar rats, then the burned skin areas were treated daily for 7 days with the TTO-loaded nanolipogel compared to the unmedicated nanolipogel, the TTO-loaded conventional gel, and the normal saline (control). The measurement of burn contraction proved that TTO-loaded nanolipogel exhibited a significantly accelerated skin healing, this was confirmed by histopathological examination as well as quantitative assessment of inflammatory infiltrate. This study highlighted the success of the proposed nanotechnology approach in improving the efficacy of TTO used for the repair of skin damage induced by burns.


Assuntos
Queimaduras , Saccharum , Óleo de Melaleuca , Álcoois , Animais , Queimaduras/tratamento farmacológico , Celulose , Cromatografia Gasosa-Espectrometria de Massas , Lipossomos , Nanopartículas , Ratos , Ratos Wistar , Solução Salina , Óleo de Melaleuca/química , Óleo de Melaleuca/farmacologia
2.
Molecules ; 26(5)2021 Mar 09.
Artigo em Inglês | MEDLINE | ID: mdl-33803294

RESUMO

Tannic acid is a chief gallo-tannin belonging to the hydrolysable tannins extracted from gall nuts and other plant sources. A myriad of pharmaceutical and biological applications in the medical field has been well recognized to tannic acid. Among these effects, potential anticancer activities against several solid malignancies such as liver, breast, lung, pancreatic, colorectal and ovarian cancers have been reported. Tannic acid was found to play a maestro-role in tuning several oncological signaling pathways including JAK/STAT, RAS/RAF/mTOR, TGF-ß1/TGF-ß1R axis, VEGF/VEGFR and CXCL12/CXCR4 axes. The combinational beneficial effects of tannic acid with other conventional chemotherapeutic drugs have been clearly demonstrated in literature such as a synergistic anticancer effect and enhancement of the chemo-sensitivity in several resistant cases. Yet, clinical applications of tannic acid have been limited owing to its poor lipid solubility, low bioavailability, off-taste, and short half-life. To overcome such obstacles, novel drug delivery systems have been employed to deliver tannic acid with the aim of improving its applications and/or efficacy against cancer cells. Among these drug delivery systems are several types of organic and metallic nanoparticles. In this review, the authors focus on the molecular mechanisms of tannic acid in tuning several neoplastic diseases as well as novel drug delivery systems that can be used for its clinical applications with an attempt to provide a systemic reference to promote the development of tannic acid as a cheap drug and/or drug delivery system in cancer management.


Assuntos
Taninos Hidrolisáveis/farmacologia , Neoplasias/tratamento farmacológico , Taninos/farmacologia , Antineoplásicos/farmacologia , Sistemas de Liberação de Medicamentos/tendências , Humanos , Taninos Hidrolisáveis/uso terapêutico , Nanopartículas , Taninos/uso terapêutico
3.
J Liposome Res ; 30(1): 45-53, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30741053

RESUMO

This study was aiming to improve the effect of the water-insoluble drug, resveratrol, by encapsulating it in surfactant-based elastic vesicles (spanlastics). Spanlastics (SLs) were prepared by thin film hydration method using different ratios of Span 60 (S60) and edge activators (EAs). The prepared SLs were subjected to full in-vitro evaluation. All the SLs showed improved properties compared to the drug suspension (p < 0.05). SL5 composed of S60: Brij 35 (7:3) attained the highest drug entrapment efficiency (79.10%±5.56), the smallest particle size (201.30 nm ± 2.45), the best in-vitro anti-oxidant effect and a fast drug release pattern, thus was selected for further investigation. Based on the Draize test, the selected spanlastics (SL5), as well as the drug suspension, showed to be safe to be applied on the skin (PII <2). In-vivo studies were done to test the photoprotective effect of the designed nanovesicles compared to the drug suspension. Evaluation was done based on visual examination and analysis of some anti-oxidant markers (CAT, GSH and SOD), anti-inflammatory markers (IL-6, IL-8 and NF-κB) and anti-wrinkling markers (MMP-1 and GM-CSF) after UVB-irradiation. The drug showed a good prophylactic effect, however, that of SL5 was superior compared to that of the drug suspension as recorded by the level of all biochemical markers (p < 0.05). These results were also confirmed by histopathological examination. This study proves that elastic nanovesicles seem to be a promising approach to overcome the low drug solubility and to improve its efficacy.


Assuntos
Antioxidantes/química , Hexoses/química , Nanocápsulas/química , Resveratrol/química , Pele/efeitos da radiação , Administração Cutânea , Animais , Anti-Inflamatórios/metabolismo , Antioxidantes/administração & dosagem , Biomarcadores/metabolismo , Composição de Medicamentos , Liberação Controlada de Fármacos , Elasticidade , Humanos , Masculino , Polietilenoglicóis/química , Ratos Wistar , Resveratrol/administração & dosagem , Absorção Cutânea , Suspensões/química , Raios Ultravioleta/efeitos adversos
4.
AAPS PharmSciTech ; 17(5): 1159-72, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26589410

RESUMO

Our objective was to prepare nanoparticulate system using a simple yet attractive innovated method as an ophthalmic delivery system for fluocinolone acetonide to improve its ocular bioavailability. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were prepared by adopting thin film hydration method using PLGA/poloxamer 407 in weight ratios of 1:5 and 1:10. PLGA was used in 75/25 and 50/50 copolymer molar ratio of DL-lactide/glycolide. Results revealed that using PLGA with lower glycolic acid monomer ratio exhibited high particle size (PS), zeta potential (ZP) and drug encapsulation efficiency (EE) values with slow drug release pattern. Also, doubling the drug concentration during nanoparticles preparation ameliorated its EE to reach almost 100%. Furthermore, studies for separating the un-entrapped drug in nanoparticles using centrifugation method at 20,000 rpm for 30 min showed that the separated clear supernatant contained nanoparticles encapsulating an important drug amount. Therefore, separation of un-entrapped drug was carried out by filtrating the preparation using 20-25 µm pore size filter paper to avoid drug loss. Aiming to increase the PLGA nanoparticles mucoadhesion ability, surface modification of selected formulation was done using different amount of stearylamine and chitosan HCl. Nanoparticles coated with 0.1% w/v chitosan HCl attained most suitable results of PS, ZP and EE values as well as high drug release properties. Transmission electron microphotographs illustrated the deposition of chitosan molecules on the nanoparticles surfaces. Pharmacokinetic studies on Albino rabbit's eyes using HPLC indicated that the prepared novel chitosan-coated PLGA nanoparticles subjected to separation by filtration showed rapid and extended drug delivery to the eye.


Assuntos
Olho/efeitos dos fármacos , Fluocinolona Acetonida/administração & dosagem , Fluocinolona Acetonida/química , Ácido Láctico/química , Nanopartículas/administração & dosagem , Nanopartículas/química , Ácido Poliglicólico/química , Administração Oftálmica , Animais , Quitosana/química , Estudos Cross-Over , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/química , Portadores de Fármacos/química , Masculino , Tamanho da Partícula , Poloxâmero/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Coelhos
5.
Biomed Environ Sci ; 28(1): 36-43, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25566861

RESUMO

OBJECTIVE: The beneficial effects of silymarin have been extensively studied in the context of inflammation and cancer treatment, yet much less is known about its therapeutic effect on diabetes. The present study was aimed to investigate the cytoprotective activity of silymarin against diabetes-induced cardiomyocyte apoptosis. METHODS: Rats were randomly divided into: control group, untreated diabetes group and diabetes group treated with silymarin (120 mg/kg•d) for 10 d. Rats were sacrificed, and the cardiac muscle specimens and blood samples were collected. The immunoreactivity of caspase-3 and Bcl-2 in the cardiomyocytes was measured. Total proteins, glucose, insulin, creatinine, AST, ALT, cholesterol, and triglycerides levels were estimated. RESULTS: Unlike the treated diabetes group, cardiomyocyte apoptosis increased in the untreated rats, as evidenced by enhanced caspase-3 and declined Bcl-2 activities. The levels of glucose, creatinine, AST, ALT, cholesterol, and triglycerides declined in the treated rats. The declined levels of insulin were enhanced again after treatment of diabetic rats with silymarin, reflecting a restoration of the pancreatic ß-cells activity. CONCLUSION: The findings of this study are of great importance, which confirmed for the first time that treatment of diabetic subjects with silymarin may protect cardiomyocytes against apoptosis and promote survival-restoration of the pancreatic ß-cells.


Assuntos
Diabetes Mellitus Experimental/complicações , Cardiomiopatias Diabéticas/prevenção & controle , Miócitos Cardíacos/efeitos dos fármacos , Silimarina/farmacologia , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Glicemia , Colesterol/sangue , Creatinina/sangue , Coração/efeitos dos fármacos , Imuno-Histoquímica , Insulina/sangue , Masculino , Miocárdio/patologia , Ratos , Triglicerídeos/sangue
6.
Int J Biol Macromol ; 265(Pt 2): 130950, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38513911

RESUMO

Due to its outstanding qualities, particularly when it takes the shape of hydrogels, chitosan is a well-known biological macromolecule with many applications. When chitosan hydrogels are modified with other polymers, the desirable function as skin regeneration hydrogels is compromised; nevertheless, the mechanical properties can be improved, which is crucial for commercialization. In this study, for the first time, bimetallic zinc silver metal-organic frameworks (ZAg MOF) loaded with ascorbic acid were added to chitosan/polyethylene oxide (PEO) based interpenetrating polymer network (IPN) hydrogels that were crosslinked with biotin to improve their antimicrobial activity, mechanical characteristics, and sustainable treatment of wounds. Significant changes in the microstructure, hydrophilicity level, and mechanical properties were noticed. Ascorbic acid release patterns were upregulated in an acidic environment pH (5.5) that mimics the initial wound pH. Impressive cell viability (98 %), antimicrobial properties, and almost full skin healing in a short time were achieved for the non-replaceable chitosan/PEO developed hydrogels. Enhancing the wound healing of the treated animals using the prepared CS/PEO hydrogel dressing was found to be a result of the inhibition of dermal inflammation via decreasing IL-1ß, suppressing ECM degradation (MMP9), stimulating proliferation through upregulation of TGF-ß and increasing ECM synthesis as it elevates collagen 1 and α-SMA contents. The findings support the implementation of developed hydrogels as antimicrobial hydrogels dressing for fast skin regeneration.


Assuntos
Quitosana , Animais , Quitosana/farmacologia , Quitosana/química , Polietilenoglicóis/farmacologia , Antibacterianos/química , Hidrogéis/farmacologia , Hidrogéis/química , Polímeros , Ácido Ascórbico
7.
J Liposome Res ; 23(1): 28-36, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23083098

RESUMO

Anorectal diseases, such as hemorrhoids, are bothersome benign conditions that warrant special attention. The design of an optimized vesicular system for localized rectal delivery can be a suitable conservative treatment. The feasibility of preparing proniosomes using different types of Gelucires®, in combination with Span(®) 60 as binary mixtures of nonionic surfactants, was checked, then the prepared proniosomes using Span 60 or Span 60/Gelucire were compared to conventional niosomes through investigations comprising the following: encapsulation efficiency (EE%); particle-size analysis; transmission electron microscopy; zeta potential (Z), and in vitro release study and ex vivo permeation study using excised rat rectum. All preparations showed satisfactory stability (Z >30 mV), particle size <300 nm with niosomes showing the lowest EE%, and the largest particle size, together with the least amount of drug released or accumulated in the rectal walls. Span 60/Gelucire proniosomes exhibited lower particle size as well as better release and permeation results, compared to Span 60 proniosomes. Span 60/Gelucire 44/14 (2:1) proniosomes attained the highest percentage of drug released (98.39%) and drug deposition in the rectal walls (86.26%) after 8 hours, which therefore seems to be the most suitable formula able to achieve targeted therapeutic efficacy, aiming to improve the patient's quality of life.


Assuntos
Hemorroidas/tratamento farmacológico , Hexoses/administração & dosagem , Rutina/administração & dosagem , Administração Retal , Animais , Sistemas de Liberação de Medicamentos , Gorduras/administração & dosagem , Ácidos Graxos/administração & dosagem , Ácidos Graxos/química , Hemorroidas/patologia , Humanos , Lipossomos/administração & dosagem , Lipossomos/química , Óleos/administração & dosagem , Polietilenoglicóis/administração & dosagem , Polietilenoglicóis/química , Ratos , Ratos Wistar
8.
Drug Deliv ; 30(1): 51-63, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36474425

RESUMO

Sugarcane bagasse-derived nanofibrillated cellulose (NFC), a type of cellulose with a fibrous structure, is potentially used in the pharmaceutical field. Regeneration of this cellulose using a green process offers a more accessible and less ordered cellulose II structure (amorphous cellulose; AmC). Furthermore, the preparation of cross-linked cellulose (NFC/AmC) provides a dual advantage by building a structural block that could exhibit distinct mechanical properties. 3D aerogel scaffolds loaded with risedronate were prepared in our study using NFC or cross-linked cellulose (NFC/AmC), then combined with different concentrations of chitosan. Results proved that the aerogel scaffolds composed of NFC and chitosan had significantly improved the mechanical properties and retarded drug release compared to all other fabricated aerogel scaffolds. The aerogel scaffolds containing the highest concentration of chitosan (SC-T3) attained the highest compressive strength and mean release time values (415 ± 41.80 kPa and 2.61 ± 0.23 h, respectively). Scanning electron microscope images proved the uniform highly porous microstructure of SC-T3 with interconnectedness. All the tested medicated as well as unmedicated aerogel scaffolds had the ability to regenerate bone as assessed using the MG-63 cell line, with the former attaining a higher effect than the latter. However, SC-T3 aerogel scaffolds possessed a lower regenerative effect than those composed of NFC only. This study highlights the promising approach of the use of biopolymers derived from agro-wastes for tissue engineering.


Assuntos
Quitosana , Saccharum , Ácido Risedrônico , Celulose , Regeneração Óssea
9.
Pharmaceutics ; 15(12)2023 Dec 06.
Artigo em Inglês | MEDLINE | ID: mdl-38140079

RESUMO

Cellulose, the most abundant biopolymer in nature, is derived from various sources. The production of pharmaceutical textiles based on cellulose represents a growing sector. In medicated textiles, textile and pharmaceutical sciences are integrated to develop new healthcare approaches aiming to improve patient compliance. Through the possibility of cellulose functionalization, pharmaceutical textiles can broaden the applications of cellulose in the biomedical field. This narrative review aims to illustrate both the methods of extraction and preparation of cellulose fibers, with a particular focus on nanocellulose, and diverse pharmaceutical applications like tissue restoration and antimicrobial, antiviral, and wound healing applications. Additionally, the merging between fabricated cellulosic textiles with drugs, metal nanoparticles, and plant-derived and synthetic materials are also illustrated. Moreover, new emerging technologies and the use of smart medicated textiles (3D and 4D cellulosic textiles) are not far from those within the review scope. In each section, the review outlines some of the limitations in the use of cellulose textiles, indicating scientific research that provides significant contributions to overcome them. This review also points out the faced challenges and possible solutions in a trial to present an overview on all issues related to the use of cellulose for the production of pharmaceutical textiles.

10.
Drug Dev Ind Pharm ; 38(4): 468-83, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21942308

RESUMO

CONTEXT: Treatment of chronic pain is complicated by the evidence that abuse of prescription opioids is rising; therefore, in many cases, chronic pain remains undertreated. Tramadol is an atypical central analgesic with a mixed mechanism of action offering many advantages over conventional opioids. OBJECTIVE: We exploited the nonopioid action of tramadol, by bypassing the first-pass effect, as well as multiparticulate drug delivery. Our aim was to identify optimal formulation parameters for designing polyvinyl alcohol (PVA), single and mixed dual cross-linked tramadol microspheres-loaded hydrogel with adequate bioadhesion and providing controlled drug release for buccal delivery. METHODS: Microspheres characterization was done by scanning electron microscopy and infrared spectroscopy. Other investigations comprised the evaluation of yield, drug content, particle size, rheology, swelling, mucoadhesion, release, and permeation studies through biological membranes all together with testing the antinociceptive activity and its attenuation by the antagonist naloxone HCl. RESULTS AND CONCLUSION: PVA-alginate microspheres (F3)-loaded carbopol hydrogel attained: the highest mucoadhesion time (1436.67 min ± 5.77) and mucin adsorption capacity, shear thinning thixotropic properties with adequate yield value and hysteresis area, best drug release (RE = 84.20 ± 2.07%) and permeation efficiency (PE = 65.30 ± 7.02%). Dissolution and permeation profiles were compared using similarity factor; F3-loaded carbogel had the lowest value. During in vivo study, the nonsignificant difference between the AUC of the groups receiving F3-loaded carbogel buccally with (group 5) and without (group 4) administration of naloxone, and between group 4 and the oral group, showed that the buccal route may arguably provide an alternative safer route of tramadol administration.


Assuntos
Analgésicos Opioides/administração & dosagem , Materiais Biocompatíveis/administração & dosagem , Preparações de Ação Retardada/química , Hidrogéis/administração & dosagem , Álcool de Polivinil/administração & dosagem , Tramadol/administração & dosagem , Administração Bucal , Animais , Disponibilidade Biológica , Galinhas , Dor Crônica/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Humanos , Masculino , Microesferas , Transtornos Relacionados ao Uso de Opioides/prevenção & controle , Tamanho da Partícula , Ratos , Ratos Wistar
11.
Antioxidants (Basel) ; 11(5)2022 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-35624887

RESUMO

ß-Sitosterol glucoside (SG), isolated from Senecio petasitis (Family Asteraceae), was loaded in self-nanoemulsifying drug delivery systems (SEDDS) in a trial to enhance its solubility and biological effect. Various co-surfactants were tested to prepare a successful SEDDS. The selected SG-loaded SEDDS had a droplet size of 134 ± 15.2 nm with a homogenous distribution (polydispersity index 0.296 ± 0.02). It also demonstrated a significant augmentation of SG in vitro release by 4-fold compared to the free drug suspension. The in vivo insulin sensitivity and antidiabetic effect of the prepared SG-loaded SEDDS were further assessed in streptozotocin-induced hyperglycemic rats. The hypoglycemic effect of SG-loaded nanosystem was evidenced by decreased serum glucose and insulin by 63.22% and 53.11%, respectively. Homeostasis model assessment-insulin resistance (HOMA-IR) index demonstrated a significant reduction by 5.4-fold in the diabetic group treated by SG-loaded nanosystem and exhibited reduced glucagon level by 40.85%. In addition, treatment with SG-loaded nanosystem significantly decreased serum MDA (malondialdehyde) and increased catalase levels by 38.31% and 64.45%, respectively. Histopathological investigations also supported the protective effect of SG-loaded nanosystem on the pancreas. The promising ability of SG-loaded nanosystem to ameliorate insulin resistance, protect against oxidative stress, and restore pancreatic ß-cell secretory function warrants its inclusion in further studies during diabetes progression.

12.
Gels ; 8(9)2022 Sep 16.
Artigo em Inglês | MEDLINE | ID: mdl-36135305

RESUMO

The pharmaceutical application of biomaterials has attained a great success. Rapid wound healing is an important goal for many researchers. Hence, this work deals with the development of nanocellulose crystals/lipid nanogels loaded with ofloxacin (OFX) to promote skin repair while inhibiting bacterial infection. Ofloxacin-loaded hybridized nanocellulose/lipid nanogels (OFX-HNCNs) were prepared and evaluated adopting a computational method based on regression analysis. The optimized nanogels (OFX-HNCN7) showed a spherical outline with an encapsulation efficiency (EE), particle size (PS) and zeta potential (ZP) values of 97.53 ± 1.56%, 200.2 ± 6.74 nm and -26.4 ± 0.50 mV, respectively, with an extended drug release profile. DSC examination of OFX-HNCN7 proved the amorphization of the encapsulated drug into the prepared OFX-HNCNs. Microbiological studies showed the prolonged inhibition of bacterial growth by OFX-HNCN7 compared to the free drug. The cytocompatibility of OFX-HNCN7 was proved by Sulforhodamine B assay. Tissue repair was evaluated using the epidermal scratch assay based on cell migration in human skin fibroblast cell line, and the results depicted that cell treated with OFX-HNCN7 showed a faster and more efficient healing compared to the control. In overall, the obtained findings emphasize the benefits of using the eco-friendly bioactive nanocellulose, hybridized with lipid, to prepare a nanocarrier for skin repair.

13.
Int J Pharm ; 616: 121549, 2022 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-35131357

RESUMO

Recycling of agro-wastes presents a great economic and ecologic value. In this study, TEMPO-oxidized nanofibrillated cellulose (TONFC) originating from sugarcane bagasse pulp was exploited in regenerative medicine. TONFC in combination with glucosamine HCl (G) were used to prepare a 3D aerogel implant loaded with rosuvastatin as an integrative approach for extraction-socket healing. Comparing the prepared devices, aerogel composed of TONFC: G (4:1 wt ratio) had the best mechanical properties and integrity. Strontium borate-based bioactive ceramic particles were prepared and characterized for crystal structure, shape, porosity, and zeta potential. The particles had a crystalline diffraction pattern relative to Sr3B2O6, and they were rod in shape with nanopores with a zeta potential value of -16 mV. The prepared bioactive ceramic (BC) was then added in different concentrations (3 or 6% w/w) to the selected aerogel implant. The BC had a concentration-dependent effect on the aerogel properties as it ameliorated its mechanical performance (compressive strength = 90 and 150 kPa for 3 and 6%, respectively) and retarded drug release (mean release time = 2.34 and 3.4 h for 3 and 6%, respectively) (p < 0.05). The microphotograph of the selected aerogel implant loaded with BC showed a rough surface with an interconnective porous structure. During cell biology testing, the selected implant loaded with the lower BC concentration had the highest ability to increase MG-63 cells proliferation. In conclusion, TONFC is a promising material to formulate rosuvastatin-loaded aerogel implant with the aid of glucosamine and bioactive ceramic for dental socket preservation.


Assuntos
Celulose , Saccharum , Celulose/química , Cerâmica , Glucosamina , Rosuvastatina Cálcica
14.
Int J Nanomedicine ; 16: 6807-6824, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34675509

RESUMO

PURPOSE: TEMPO-oxidized nanofibrillated cellulose (TONFC) originating from an agricultural waste (sugar cane) was utilized to prepare injectable in-situ forming hydrogel scaffolds (IHS) for regenerative medicine. METHODS: TONFC was prepared and characterized for its morphology and chemical structure using TEM and FT-IR, respectively. The cold method was applied to prepare hydrogels. Various concentrations of poloxamer 407 were added to the prepared TONFC (0.5%w/w). Different sources of calcium, Fujicalin® (DCP) or hydroxyapatite (TCP), were used to formulate the aimed calcium-enriched raloxifene hydrochloride-loaded IHS. Gelation temperature, drug content, injectability and in-vitro drug release were evaluated along with the morphological characters. Cytocompatibility studies and tissue regeneration properties were assessed on Saos-2 cells. RESULTS: TEM photograph of TONFC showed fibrous nanostructure. The selected formulation "Ca-IHS4" composed of TONFC+15% P407+10% TCP showed the most prolonged release pattern for 12 days with the least burst effect (about 25% within 24 h). SEM micro-photographs of the in-situ formed scaffolds showed a highly porous 3D structure. Cytocompatibility studies of formulation "Ca-IHS4" revealed the biocompatibility as well as improved cell adhesion, alkaline phosphatase enzyme activity and calcium ion deposition. CONCLUSION: The outcomes suggest that Ca-IHS4 presents a simple, safe-line and non-invasive strategy for bone regeneration.


Assuntos
Hidrogéis , Cloridrato de Raloxifeno , Cálcio , Celulose , Poloxâmero , Espectroscopia de Infravermelho com Transformada de Fourier , Engenharia Tecidual , Alicerces Teciduais
15.
Food Funct ; 12(11): 4738-4748, 2021 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-34100507

RESUMO

Mucilage is a soluble dietary fiber used as a food additive to give foods a firmer texture, aside from its many health benefits and pharmacological properties. It is a polysaccharide in nature, composed of large molecules of sugars and uronic acid moieties. The extraction of mucilage is achieved from a wide variety of plant parts, including rhizomes, roots, and seeds, and it has also been reported from microorganisms. In this review, the nutritional and medicinal applications of mucilage are described in the context of the different mucilage types. The current article highlights state-of-the-art valorization practices relating to mucilage and its potential novel usages in the food industry and nutraceuticals, and as a prebiotic, in addition to its nutritional and anti-nutritional values. Analysis of the prebiotic action of mucilage with respect to its structure activity relationship, as well as how it modulates gut bacteria, is presented for the first time and in the context of its known health benefits inside the colon. It is recommended that more investigations are carried out to maximize the health benefits of mucilage and ensure its safety, especially upon long-term usage.


Assuntos
Coloides , Suplementos Nutricionais , Alimento Funcional , Mucilagem Vegetal/química , Prebióticos , Valor Nutritivo
16.
Sci Rep ; 10(1): 10435, 2020 06 26.
Artigo em Inglês | MEDLINE | ID: mdl-32591621

RESUMO

The use of (PEG)-grafted materials has a positive impact on drug delivery. In this study we designed PEGylated lipid nanocarriers (PLN) loaded with curcumin (Cur) to target skin cancer by photodynamic therapy. Cur is a polyphenolic compound having vast biological effects masked due to its low aqueous solubility. PLN were prepared using Tefose 1500 with different surfactants. PLN3, containing Tween 80, had the smallest particle size (167.60 ± 15.12 nm), Z = - 26.91 mV and, attained the highest drug release (Q24 = 75.02 ± 4.61% and Q48 = 98.25 ± 6.89%). TEM showed spherical, well-separated nanoparticles. The dark and photo-cytotoxicity study on a human skin cancer cell line (A431) revealed that, at all tested concentrations, the viability of cells treated with PLN3 was significantly lower than those treated by Cur suspension and, it decreased upon irradiation by blue light (410 nm). The amount of Cur extracted from the skin of mice treated by PLN3 was twice that of mice treated by aqueous drug suspension, this was confirmed by the increase in fluorescence intensity measured by confocal laser microscopy. Histopathological studies showed that PLN3 could extend Cur effect to deeper skin layers, especially after irradiation. This study highlights the possible efficacy of curcumin-loaded PEGylated lipidic nanoparticles to combat skin cancer by photodynamic therapy.


Assuntos
Curcumina/administração & dosagem , Sistemas de Liberação de Medicamentos , Lipídeos/administração & dosagem , Nanopartículas/administração & dosagem , Fotoquimioterapia , Animais , Portadores de Fármacos/administração & dosagem , Masculino , Camundongos
17.
Food Funct ; 11(6): 5357-5376, 2020 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-32463028

RESUMO

The chemical constituents of Allium sativum (garlic) oil were investigated using the GC/MS technique after silylation, and the presence of several fatty acids and their esters was revealed. The most dominant was 9,12-octadecadienoic acid (linoleic acid), a precursor of arachidonic acid, which is essential for brain development. Garlic oil-loaded chitosan nanoparticles (GCNs) were prepared to enhance its cerebral effects, and to mask its odor and taste. Two-level orthogonal factorial design, followed by regression analysis, was used to study the influence of different formulation variables. GCN3, the formula with the smallest particle size and the highest mucoadhesion, was selected as the optimized one. Transmission electron microscopy showed that GCN3 has a short nanorod-shape outline. We aimed to investigate the influence of orally administered GCN3 compared to the plain garlic oil (GO), on ciprofloxacin-induced (CPX) neurotoxicity in rats and the probable underlying mechanisms. The results show the significantly higher neurological curative effect of GCN3 compared to GO, and its greater antidepression-like and antianxiety-like potential via the alteration of brain neurotransmitter levels and inhibition of oxidative stress and inflammatory pathways. The histopathological examination showed the higher capability of GCN3 to repair the damage induced by CPX in the cerebral cortex, hippocampus area and substantia nigra brain sections. Similar results were proved immunohistochemically using Cox-2 antibody. The nanoencapsulation of GO represents a promising strategy for brain-targeting.


Assuntos
Compostos Alílicos/análise , Compostos Alílicos/farmacologia , Quitosana/farmacologia , Alho/química , Nanotubos/química , Sulfetos/química , Sulfetos/farmacologia , Animais , Encéfalo/patologia , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/patologia , Ciprofloxacina/efeitos adversos , Sistemas de Liberação de Medicamentos , Cromatografia Gasosa-Espectrometria de Massas , Hipocampo/efeitos dos fármacos , Hipocampo/patologia , Masculino , Síndromes Neurotóxicas , Estresse Oxidativo/efeitos dos fármacos , Tamanho da Partícula , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Ratos
18.
Int J Biol Macromol ; 163: 1579-1590, 2020 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-32755697

RESUMO

Cellulose was and still is the most abundant biopolymer generated from all plant fibers including agricultural wastes. Using this waste as a starting material in the production of new products is a field of great interest. The demand for renewable and available resources in combination with advanced technologies is a necessity to develop new generations of advanced nanomaterials. This review aims to present integrated details on the extraction techniques and structure of nanofibrillated cellulose as well as cellulose nanocrystals derived from agricultural wastes besides the different treatment methods used to be suitable for several pharmaceutical applications. Different pharmaceutical applications are described, including controlled, sustained or rapid drug delivery, stabilizing agent, and its use as safe and sustained environment for cell culture allowing its use in tissue engineering field.


Assuntos
Celulose/química , Nanoestruturas/química , Preparações Farmacêuticas/química , Animais , Biopolímeros/química , Sistemas de Liberação de Medicamentos/métodos , Humanos , Nanotecnologia/métodos , Engenharia Tecidual/métodos
19.
Int J Biol Macromol ; 156: 704-716, 2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32289405

RESUMO

This study intended to design novel nanofibrillated cellulose/cyclodextrin-based 3D scaffolds loaded with raloxifene hydrochloride for bone regeneration. The scaffolds were prepared using two different types of cyclodextrins namely; beta-cyclodextrin and methyl-beta-cyclodextrin. The prepared scaffolds were evaluated by characterizing their porosity, compressive strength, in-vitro drug release, FT-IR and XRD as well as their morphological properties using SEM. Results presented that the prepared scaffolds were highly porous, additionally, the scaffold containing drug/beta-cyclodextrin kneaded complex (SC5) showed the most controlled drug release pattern with the least burst effect and reached almost complete release at 480 h. The in-vitro cytocompatibility and regenerative effect of the chosen scaffold (SC5) was assessed using Saos-2 cell line. Results proved that SC5 was biocompatible. Moreover, it enhanced the cell adhesion, alkaline phosphatase enzyme expression and calcium ion deposition which are essential factors for bone mineralization. The obtained observations presented a novel, safe and propitious approach for bone engineering.


Assuntos
Conservadores da Densidade Óssea/administração & dosagem , Regeneração Óssea , Celulose/química , Ciclodextrinas/química , Cloridrato de Raloxifeno/administração & dosagem , Engenharia Tecidual , Alicerces Teciduais/química , Biomarcadores , Conservadores da Densidade Óssea/farmacocinética , Diferenciação Celular , Sobrevivência Celular , Humanos , Porosidade , Cloridrato de Raloxifeno/farmacocinética , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
20.
Int J Biol Macromol ; 165(Pt B): 2550-2564, 2020 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-33115647

RESUMO

Demand for safe, environmentally friendly and minimally processed food additives with intrinsic technological (stabilizing, texturizing, structuring) and functional potential is already on the rise. There are actually several natural excipients eligible for pharmaceutical formulation. Mucilage, as a class constitutes arabinoxylan and rhamnogalacturonan-based biomolecules used in the pharmaceutical, environmental as well as phytoremediation industries owing to its particular structure and properties. These compounds are widely used in pharmaceutical, food and cosmetics, as well as, in agriculture, paper industries. This review emphasizes mucilage valuable applications in the pharmaceutical and industrial fields. In this context, much focus has recently been given to the valorization of mucilage as an ingredient for food or nutraceutical applications. Furthermore, different optimization and extraction techniques are presented to develop better utilization and/or enhanced yield of mucilage. The highlighted mucilage extraction methods warrant assessing up-scale processes to encourage for its industrial applications. The current article capitalizes on cutting-edge characteristics of mucilage and posing for other possible innovative applications in non-food industries. Here, the first holistic overview of mucilage with regards to its physicochemical properties and potential novel usages is presented.


Assuntos
Biodegradação Ambiental , Mucilagem Vegetal/química , Polissacarídeos/química , Xilanos/química , Aditivos Alimentares/química , Aditivos Alimentares/uso terapêutico , Humanos , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Mucilagem Vegetal/uso terapêutico , Polissacarídeos/uso terapêutico , Viscosidade , Xilanos/uso terapêutico
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