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1.
Acta Cir Bras ; 39: e393324, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39016358

RESUMO

PURPOSE: Bacterial cellulose (BC) has shown high capacity for the treatment of wounds and burns, providing a moisty environment. Calcium alginate can be associated with BC to create gels that aid in wound debridement and contribute to appropriate wound healing. This study is aimed at characterizing and evaluating the use of bacterial cellulose/alginate gel in skin burns in rats. METHODS: Cellulose and cellulose/alginate gels were compared regarding the capacity of liquid absorption, moisture, viscosity, and potential cytotoxicity. The 2nd degree burns were produced using an aluminum metal plate (2.0cm) at 120ºC for 20s on the back of rats. The animals were divided into non-treated, CMC(Carboxymethylcellulose), Cellulose(CMC with bacterial cellulose), and Cellulose/alginate(CMC with bacterial cellulose and alginate). The animals received topical treatment 3 times/week. Biochemical (MPO, NAG and oxidative stress), histomorphometry and immunohistochemical assays (IL-1ß IL-10 and VEGF) were conducted on the 14th, 21st, 28th, and 35th days. RESULTS: Cellulose/Alginate gel showed higher absorption capacity and viscosity compared to Cellulose gel, with no cytotoxic effects. Cellulose/alginate presented lower MPO values, a higher percentage of IL-10, with greater and balanced oxidative stress profile. CONCLUSIONS: The use of cellulose/alginate gel reduced neutrophils and macrophage activation and showed greater anti-inflammatory response, which can contribute to healing chronic wounds and burns.


Assuntos
Alginatos , Queimaduras , Celulose , Hidrogéis , Ratos Wistar , Cicatrização , Animais , Alginatos/uso terapêutico , Celulose/uso terapêutico , Queimaduras/tratamento farmacológico , Queimaduras/terapia , Cicatrização/efeitos dos fármacos , Hidrogéis/uso terapêutico , Masculino , Ratos , Ácido Glucurônico/uso terapêutico , Ácidos Hexurônicos/uso terapêutico , Reprodutibilidade dos Testes , Viscosidade , Estresse Oxidativo/efeitos dos fármacos , Imuno-Histoquímica , Fatores de Tempo , Pele/lesões , Pele/efeitos dos fármacos
2.
Acta cir. bras ; Acta cir. bras;39: e393324, 2024. tab, graf, ilus
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1563651

RESUMO

Purpose: Bacterial cellulose (BC) has shown high capacity for the treatment of wounds and burns, providing a moisty environment. Calcium alginate can be associated with BC to create gels that aid in wound debridement and contribute to appropriate wound healing. This study is aimed at characterizing and evaluating the use of bacterial cellulose/alginate gel in skin burns in rats. Methods: Cellulose and cellulose/alginate gels were compared regarding the capacity of liquid absorption, moisture, viscosity, and potential cytotoxicity. The 2nd degree burns were produced using an aluminum metal plate (2.0cm) at 120ºC for 20s on the back of rats. The animals were divided into non-treated, CMC(Carboxymethylcellulose), Cellulose(CMC with bacterial cellulose), and Cellulose/alginate(CMC with bacterial cellulose and alginate). The animals received topical treatment 3 times/week. Biochemical (MPO, NAG and oxidative stress), histomorphometry and immunohistochemical assays (IL-1ß IL-10 and VEGF) were conducted on the 14th, 21st, 28th, and 35th days. Results: Cellulose/Alginate gel showed higher absorption capacity and viscosity compared to Cellulose gel, with no cytotoxic effects. Cellulose/alginate presented lower MPO values, a higher percentage of IL-10, with greater and balanced oxidative stress profile. Conclusions: The use of cellulose/alginate gel reduced neutrophils and macrophage activation and showed greater anti-inflammatory response, which can contribute to healing chronic wounds and burns.


Assuntos
Animais , Ratos , Queimaduras/terapia , Hidrogéis/uso terapêutico , Alginatos/uso terapêutico , Anti-Inflamatórios/uso terapêutico
3.
Pharmaceutics ; 15(11)2023 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-38004578

RESUMO

Inflammatory bowel disease (IBD) is a chronic inflammatory disorder, most known as ulcerative colitis (UC) and Crohn's disease (CD), that affects the gastrointestinal tract (GIT), causing considerable symptoms to millions of people around the world. Conventional therapeutic strategies have limitations and side effects, prompting the exploration of innovative approaches. Probiotics, known for their potential to restore gut homeostasis, have emerged as promising candidates for IBD management. Probiotics have been shown to minimize disease symptoms, particularly in patients affected by UC, opening important opportunities to better treat this disease. However, they exhibit limitations in terms of stability and targeted delivery. As several studies demonstrate, the encapsulation of the probiotics, as well as the synthetic drug, into micro- and nanoparticles of organic materials offers great potential to solve this problem. They resist the harsh conditions of the upper GIT portions and, thus, protect the probiotic and drug inside, allowing for the delivery of adequate amounts directly into the colon. An overview of UC and CD, the benefits of the use of probiotics, and the potential of micro- and nanoencapsulation technologies to improve IBD treatment are presented. This review sheds light on the remarkable potential of nano- and microparticles loaded with probiotics as a novel and efficient strategy for managing IBD. Nonetheless, further investigations and clinical trials are warranted to validate their long-term safety and efficacy, paving the way for a new era in IBD therapeutics.

4.
Int J Biol Macromol ; 240: 124489, 2023 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-37076077

RESUMO

Nanoparticles and nanoparticle-loaded films based on chitosan/sodium alginate with curcumin (CUR) are promising strategies to improve the efficacy of antimicrobial photodynamic therapy (aPDT) for the treatment of oral biofilms. This work aimed to develop and evaluate the nanoparticles based on chitosan and sodium alginate encapsulated with CUR dispersed in polymeric films associated with aPDT in oral biofilms. The NPs were obtained by polyelectrolytic complexation, and the films were prepared by solvent evaporation. The photodynamic effect was evaluated by counting Colony Forming Units (CFU/mL). Both systems showed adequate characterization parameters for CUR release. Nanoparticles controlled the release of CUR for a longer period than the nanoparticle-loaded films in simulated saliva media. Control and CUR-loaded nanoparticles showed a significant reduction of 3 log10 CFU/mL against S. mutans biofilms, compared to treatment without light. However, biofilms of S. mutans showed no photoinactivation effect using films loaded with nanoparticles even in the presence of light. These results demonstrate the potential of chitosan/sodium alginate nanoparticles associated with aPDT as carriers for the oral delivery of CUR, offering new possibilities to improve the treatment of dental caries and infections. This work will contribute to advances in the search for innovative delivery systems in dentistry.


Assuntos
Quitosana , Curcumina , Cárie Dentária , Nanopartículas , Fotoquimioterapia , Humanos , Curcumina/farmacologia , Alginatos , Cárie Dentária/tratamento farmacológico , Fotoquimioterapia/métodos , Biofilmes
5.
Int J Biol Macromol ; 227: 736-748, 2023 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-36549615

RESUMO

Piperine is an alkaloid mostly found in the fruits of several species of the Piper genus, and its anti-inflammatory potential is already known. However, its therapeutic applications still need to be better explored due to the low aqueous solubility of this active. To overcome this drawback, the objective of this work was to evaluate the efficiency of the nanoencapsulation of the compound as well as its incorporation into hyaluronic acid/alginate-based biomembranes. Polymeric nanoparticles composed of Eudragit S100 and Poloxamer 188 were obtained by the nanoprecipitation technique, obtaining spherical nanosized particles with an average diameter of 122.1 ± 2.0 nm, polydispersity index of 0.266, and encapsulation efficiency of 76.2 %. Hyaluronic acid/sodium alginate membranes were then prepared and characterized. Regarding permeation, a slow passage rate was observed until the initial 14 h, when an exponential increase in the recovered drug concentration began to occur. The in vivo assay showed a reduction in inflammation up to 43.6 %, and no cytotoxicity was observed. The results suggested the potential of the system developed for the treatment of inflammatory skin diseases.


Assuntos
Alcaloides , Dermatite , Nanopartículas , Humanos , Ácido Hialurônico , Alginatos , Alcaloides/farmacologia , Tamanho da Partícula
6.
J Appl Toxicol ; 43(10): 1410-1420, 2023 10.
Artigo em Inglês | MEDLINE | ID: mdl-36579752

RESUMO

Cyclodextrins are nanometric cyclic oligosaccharides with amphiphilic characteristics that increase the stability of drugs in pharmaceutical forms and bioavailability, in addition to protecting them against oxidation and UV radiation. Some of their characteristics are low toxicity, biodegradability, and biocompatibility. They are divided into α-, ß-, and γ-cyclodextrins, each with its own particularities. They can undergo surface modifications to improve their performances. Furthermore, their drug inclusion complexes can be made by various methods, including lyophilization, spray drying, magnetic stirring, kneading, and others. Cyclodextrins can solve several problems in drug stability when incorporated into dosage forms (including tablets, gels, films, nanoparticles, and suppositories) and allow better topical biological effects of drugs at administration sites such as skin, eyeballs, and oral, nasal, vaginal, and rectal cavities. However, as they are nanostructured systems and some of them can cause mild toxicity depending on the application site, they must be evaluated for their nanotoxicology and nanosafety aspects. Moreover, there is evidence that they can cause severe ototoxicity, killing cells from the ear canal even when applied by other administration routes. Therefore, they should be avoided in otologic administration and should have their permeation/penetration profiles and the in vivo hearing system integrity evaluated to certify that they will be safe and will not cause hearing loss.


Assuntos
Produtos Biológicos , Ciclodextrinas , Feminino , Humanos , Ciclodextrinas/toxicidade , Preparações Farmacêuticas , Disponibilidade Biológica , Solubilidade
7.
AAPS PharmSciTech ; 23(7): 269, 2022 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-36171494

RESUMO

Polymeric films are drug delivery systems that maintain contact with the delivery tissue and sustain a controlled release of therapeutic molecules. These systems allow a longer time of drug contact with the target site in the case of topical treatments and allow the controlled administration of drugs. They can be manufactured by various methods such as solvent casting, hot melt extrusion, electrospinning, and 3D bioprinting. Furthermore, they can employ various polymers, for example PVP, PVA, cellulose derivatives, chitosan, gelling gum, pectin, and alginate. Its versatility is also applicable to different routes of administration, as it can be administered to the skin, oral mucosa, vaginal canal, and eyeballs. All these factors allow numerous combinations to obtain a better treatment. This review focuses on exploring some possible ways to develop them and some particularities and advantages/disadvantages in each case. It also aims to show the versatility of these systems and the advantages and disadvantages in each case, as they bring the opportunity to develop different medicines to facilitate therapies for the most diverse purposes .


Assuntos
Quitosana , Alginatos , Celulose , Preparações de Ação Retardada , Sistemas de Liberação de Medicamentos , Feminino , Humanos , Pectinas , Polímeros , Solventes
8.
Life (Basel) ; 12(8)2022 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-36013419

RESUMO

Biotechnology and pharmacy have shown efficient results when combined to generate innovative technological products [...].

9.
ACS Omega ; 7(32): 28238-28247, 2022 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-35990469

RESUMO

The importance of obtaining new compounds with improved antimicrobial activity is a current trend and challenge. Some polymers such as chitosan have shown promising bactericidal properties when they are structurally modified, which is due to the binding versatility provided by their free amines. Likewise, antimicrobial peptides (AMPs) have received attention in recent years because of their bactericidal activity that is similar to or even better than that of conventional drugs, and they exhibit a low induction rate of antimicrobial resistance. Herein, the modified AMP Ctx(Ile21)-Ha-Ahx-Cys was conjugated to chitosan using N-acetylcysteine as an intermediate by the carbodiimide method. Films were prepared using protonated chitosan in 1% acetic acid and Ctx(Ile21)-Ha-Ahx-Cys AMP dissolved in N-acetylcysteine-chitosan; 1.6 mmol of ethylcarbodiimide hydrochloride, 1.2 mmol of N-hydroxysulfosucchimide, and 0.1 mol L -1of N-morpholino)ethanesulfonic acid buffer at pH 6.5 by continuous stirring at 100 × g for 10 min at 37 °C. Physicochemical properties were evaluated by Fourier-transform infrared spectroscopy, differential scanning calorimetry/thermogravimetric analysis, and X-ray diffraction to determine the mechanical properties, solubility, morphology, and thickness. Furthermore, the antimicrobial activities of chitosan-based conjugated films were evaluated againstStaphylococcus aureus,Pseudomonas aeruginosa,SalmonellaTyphimurium, andEscherichia coli. The results showed that the conjugation of a potent AMP could further increase its antibacterial activity and maintain its stable physicochemical properties. Therefore, the developed peptide-chitosan conjugate could be applied as an additive in surgical procedures to prevent and combat bacterial infection.

10.
Life (Basel) ; 12(7)2022 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-35888137

RESUMO

Vitamins are widely found in nature, for example, in plants and fruits. Ascorbic acid and nicotinamide are examples of these compounds that have potent antioxidant properties, besides stimulating collagen production and depigmenting properties that protect the skin from premature aging. To overcome the skin barrier and reduce the instability of antioxidant compounds, alternative systems have been developed to facilitate the delivery of antioxidants, making them efficiently available to the tissue for an extended time without causing damage or toxicity. The objective of this study was to obtain chitosan biodegradable microparticles containing ascorbic acid and nicotinamide for topical delivery. The microparticles were obtained by spray drying and characterized chemically by means of scanning electron microscopy, infrared spectroscopy, X-ray diffraction, and differential exploratory calorimetry. The drugs were successfully encapsulated and the microparticles showed positive zeta potential. In vitro release assays showed a sustained release profile. The evaluation of ex vivo skin permeation and retention demonstrated low permeation and adequate retention of the compounds in the epidermis/dermis, suggesting the efficient delivery from the obtained microparticles. Antibacterial assays have shown that microparticles can inhibit the growth of microorganisms in a time- and dose-dependent manner, corroborating their use in cosmetic products for application on the skin.

11.
Pharmaceutics ; 14(6)2022 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-35745722

RESUMO

Trans-resveratrol can promote various dermatological effects. However, its high crystallinity decreases its solubility and bioavailability. Therefore, solid dispersions have been developed to promote its amorphization; even so, they present as powders, making cutaneous controlled drug delivery unfeasible and an alternative necessary for their incorporation into other systems. Thus, polyvinylpyrrolidone (PVP) films were chosen with the aim of developing a controlled delivery system to treat inflammation and bacterial infections associated with atopic dermatitis. Four formulations were developed: two with solid dispersions (and trans-resveratrol) and two as controls. The films presented with uniformity, as well as bioadhesive and good barrier properties. X-ray diffraction showed that trans-resveratrol did not recrystallize. Fourier-transform infrared spectroscopy (FT-IR) and thermal analysis evidenced good chemical compatibilities. The in vitro release assay showed release values from 82.27 ± 2.60 to 92.81 ± 2.50% (being a prolonged release). In the in vitro retention assay, trans-resveratrol was retained in the skin, over 24 h, from 42.88 to 53.28%. They also had low cytotoxicity over fibroblasts. The in vivo assay showed a reduction in inflammation up to 66%. The films also avoided Staphylococcus aureus's growth, which worsens atopic dermatitis. According to the results, the developed system is suitable for drug delivery and capable of simultaneously treating inflammation and infections related to atopic dermatitis.

12.
Biofouling ; 38(1): 71-83, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-34906018

RESUMO

This study aimed to evaluate the antimicrobial and anti-biofilm activity of morin on polymicrobial biofilms and its cytotoxicity in controlled-release films and tablets based on gellan gum. Polymicrobial biofilms were formed from saliva for 48 h under an intermittent exposure regime to 1% sucrose and in contact with films or tablets of gellan gum containing 2 mg of morin each. Acidogenicity, bacterial viability, dry weight and insoluble extracellular polysaccharides from biofilms were evaluated. The cytotoxicity of morin was evaluated in oral keratinocytes. Morin released from the systems reduced the viability of all the microbial groups evaluated, as well as the dry weight and insoluble polysaccharide concentration in the matrix and promoted the control of acidogenicity when compared with the control group without the substance. Morin was cytotoxic only at the highest concentration evaluated. In conclusion, morin is an effective agent and shows antimicrobial and anti-biofilm activity against polymicrobial biofilms.


Assuntos
Biofilmes , Streptococcus mutans , Antibacterianos , Preparações de Ação Retardada/farmacologia , Flavonoides , Comprimidos
13.
Crit Rev Anal Chem ; 52(5): 1000-1014, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33258695

RESUMO

Five-aminosalicylic acid (5-ASA) is an anti-inflammatory drug indicated in the treatment of inflammatory bowel diseases such as ulcerative colitis and Crohn's disease. Among the analytical methods of quantification of 5-ASA described in the literature, the High Efficiency Liquid Chromatography stands out, a sensitive technique but with a high cost. In recent years, alternative methods have been developed, presenting efficiency and reduced cost, such as UV/visible spectrophotometric, spectrofluorescent, and electrochemical methods, techniques recommended for the application in quality control and quantification of 5-ASA in pharmaceutical forms and biological fluids. This article aims to review the physicochemical characteristics, pharmacokinetics, mechanisms of action, controlled release systems, and the different analytical and bioanalytical methods for the quantification of 5-ASA.


Assuntos
Colite Ulcerativa , Doença de Crohn , Colite Ulcerativa/tratamento farmacológico , Doença de Crohn/tratamento farmacológico , Fezes , Humanos , Mesalamina/uso terapêutico
14.
Pharmaceutics ; 13(9)2021 Sep 19.
Artigo em Inglês | MEDLINE | ID: mdl-34575591

RESUMO

Cellulose nanofibers (CNF) were employed as the nanoreinforcement of a retrograded starch/pectin (RS/P) excipient to optimize its colon-specific properties. Although starch retrogradation ranged from 32 to 73%, CNF addition discretely disfavored the RS yield. This result agrees with the finding that in situ CNF reduces the presence of the RS crystallinity pattern. A thermal analysis revealed that the contribution of pectin improves the thermal stability of the RS/CNF mixture. Through a complete factorial design, it was possible to optimize the spray-drying conditions to obtain powders with high yield (57%) and low moisture content (1.2%). The powders observed by Field Emission Gum Scanning Electron Microscopy (FEG-SEM) had 1-10 µm and a circular shape. The developed methodology allowed us to obtain 5-aminosalicilic acid-loaded microparticles with high encapsulation efficiency (16-98%) and drug loading (1.97-26.63%). The presence of CNF in RS/P samples was responsible for decreasing the burst effect of release in simulated gastric and duodenal media, allowing the greatest mass of drug to be targeted to the colon. Considering that spray-drying is a scalable process, widely used by the pharmaceutical industry, the results obtained indicate the potential of these microparticles as raw material for obtaining other dosage forms to deliver 5-ASA to the distal parts of gastrointestinal tract, affected by inflammatory bowel disease.

15.
Pharmaceutics ; 13(7)2021 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-34209453

RESUMO

BACKGROUND: Probiotic bacteria have been emerging as a trustworthy choice for the prevention and treatment of Candida spp. infections. This study aimed to develop and characterize an orodispersible film (ODF) for delivering the potentially probiotic Enterococcus faecium CRL 183 into the oral cavity, evaluating its in vitro antifungal activity against Candida albicans. METHODS AND RESULTS: The ODF was composed by carboxymethylcellulose, gelatin, and potato starch, and its physical, chemical, and mechanical properties were studied. The probiotic resistance and viability during processing and storage were evaluated as well as its in vitro antifungal activity against C. albicans. The ODFs were thin, resistant, and flexible, with neutral pH and microbiologically safe. The probiotic resisted the ODF obtaining process, demonstrating high viability (>9 log10 CFU·g-1), up to 90 days of storage at room temperature. The Probiotic Film promoted 68.9% of reduction in fungal early biofilm and 91.2% in its mature biofilm compared to the group stimulated with the control film. Those results were confirmed through SEM images. CONCLUSION: The probiotic ODF developed is a promising strategy to prevent oral candidiasis, since it permits the local probiotic delivery, which in turn was able to reduce C. albicans biofilm formation.

16.
Antibiotics (Basel) ; 10(6)2021 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-34064051

RESUMO

The constant use of synthetic antibiotics as growth promoters can cause bacterial resistance in chicks. Consequently, the use of these drugs has been restricted in different countries. In recent years, antimicrobial peptides have gained relevance due to their minimal capacity for bacterial resistance and does not generate toxic residues that harm the environment and human health. In this study, a Ctx(Ile21)-Ha antimicrobial peptide was employed, due to its previously reported great antimicrobial potential, to evaluate its application effects in laying chicks challenged with Salmonella Enteritidis, resistant to nalidixic acid and spectinomycin. For this, Ctx(Ile21)-Ha was synthesized, microencapsulated and coated with hypromellose phthalate (HPMCP) to be released in the intestine. Two different doses (20 and 40 mg of Ctx(Ile21)-Ha per kg of isoproteic and isoenergetic poultry feed) were included in the chick's food and administered for 28 days. Antimicrobial activity, effect and response as treatment were evaluated. Statistical results were analyzed in detail and indicate that the formulated Ctx(Ile21)-Ha peptide had a positive and significant effect in relation to the reduction of chick mortality in the first days of life. However, there was moderate evidence (p = 0.07), not considered statistically significant, in the differences in laying chick weight between the control and microencapsulation treatment groups as a function of time. Therefore, the microencapsulated Ctx(Ile21)-Ha antimicrobial peptide can be an interesting and promising option in the substitution of conventional antibiotics.

17.
Int J Biol Macromol ; 183: 1236-1247, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-33965488

RESUMO

Microencapsulation is a potential biotechnological tool, which can overcome antimicrobial peptides (AMP) instabilities and reduce toxic side effects. Thus, this study evaluates the antibacterial activities of the Ctx(Ile21)-Ha AMP against multidrug-resistant (MDR) and non-resistant bacteria and develop and characterize peptide-loaded microparticles coated with the enteric polymers hydroxypropylmethylcellulose acetate succinate (HPMCAS) and hydroxypropylmethylcellulose phthalate (HPMCP). Ctx(Ile21)-Ha was obtained by solid phase peptide synthesis (SPPS) method, purified and characterized by HPLC and Mass Spectrometry. The peptide exhibited potent antibiotic activities against Salmonella enteritidis, Salmonella typhimurium, Pseudomonas aeruginosa (MDR), Acinetobacter baumannii (MDR), and Staphylococcus aureus (MDR). Ctx(Ile21)-Ha microencapsulation was performed by ionic gelation with high efficiency, maintaining the physical-chemical stability. Ctx(Ile21)-Ha coated-microparticles were characterized by DSC, TGA, FTIR-Raman, XRD and SEM. Hemolytic activity assay demonstrated that hemolysis was decreased up to 95% compared to single molecule. In addition, in vitro release control profile simulating different portions of gastrointestinal tract was performed and showed the microcapsules' ability to protect the peptide and release it in the intestine, aiming pathogen's location, mainly by Salmonella sp. Therefore, use of microencapsulated Ctx(Ile21)-Ha can be allowed as an antimicrobial controller in monogastric animal production as an oral feed additive (antimicrobial controller), being a valuable option for molecules with low therapeutic indexes or high hemolytic rates.


Assuntos
Alginatos/química , Metilcelulose/análogos & derivados , Proteínas Citotóxicas Formadoras de Poros/farmacologia , Acinetobacter baumannii/efeitos dos fármacos , Composição de Medicamentos , Aditivos Alimentares/química , Aditivos Alimentares/farmacologia , Hemólise , Metilcelulose/química , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Proteínas Citotóxicas Formadoras de Poros/química , Pseudomonas aeruginosa/efeitos dos fármacos , Salmonella/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
18.
J Drug Target ; 29(10): 1029-1047, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-33729081

RESUMO

Peptic ulcer disease (PUD) is a common condition that is induced by acid and pepsin causing lesions in the mucosa of the duodenum and stomach. The pathogenesis of PUD is a many-sided scenario, which involves an imbalance between protective factors, such as prostaglandins, blood flow, and cell renewal, and aggressive ones, like alcohol abuse, smoking, Helicobacter pylori colonisation, and the use of non-steroidal anti-inflammatory drugs. The standard oral treatment is well established; however, several problems can decrease the success of this therapy, such as drug degradation in the gastric environment, low oral bioavailability, and lack of vectorisation to the target site. In this way, the use of strategies to improve the effectiveness of these conventional drugs becomes interesting. Currently, the use of drug delivery systems is being explored as an option to improve the drug therapy limitations, such as antimicrobial resistance, low bioavailability, molecule degradation in an acid environment, and low concentration of the drug at the site of action. This article provides a review of oral drug delivery systems looking for improving the treatment of PUD.


Assuntos
Antiulcerosos/administração & dosagem , Sistemas de Liberação de Medicamentos , Úlcera Péptica/tratamento farmacológico , Administração Oral , Animais , Antiulcerosos/farmacocinética , Disponibilidade Biológica , Mucosa Gástrica/patologia , Humanos , Úlcera Péptica/etiologia , Úlcera Péptica/patologia , Fatores de Proteção , Fatores de Risco
19.
Curr Med Chem ; 28(16): 3216-3248, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32867631

RESUMO

Administration of substances through the skin represents a promising alternative, in relation to other drug administration routes, due to its large body surface area, in order to offer ideal and multiple sites for drug administration. In addition, the administration of drugs through the skin avoids the first-pass metabolism, allowing an increase in the bioavailability of drugs, as well as reducing their side effects. However, the stratum corneum (SC) comprises the main barrier of protection against external agents, mainly due to its structure, composition and physicochemical properties, becoming the main limitation for the administration of substances through the skin. In view of the above, pharmaceutical technology has allowed the development of multiple drug delivery systems (DDS), which include liquid crystals (LC), cubosomes, liposomes, polymeric nanoparticles (PNP), nanoemulsions (NE), as well as cyclodextrins (CD) and dendrimers (DND). It appears that the DDS circumvents the problems of drug absorption through the SC layer of the skin, ensuring the release of the drug, as well as optimizing the therapeutic effect locally. This review aims to highlight the DDS that include LC, cubosomes, lipid systems, PNP, as well as CD and DND, to optimize topical skin therapies.


Assuntos
Sistemas de Liberação de Medicamentos , Nanopartículas , Administração Cutânea , Portadores de Fármacos , Humanos , Lipossomos , Nanotecnologia , Pele
20.
Int J Biol Macromol ; 162: 1944-1958, 2020 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-32791274

RESUMO

The use of controlled drug delivery systems represents an alternative and promising strategy for the use of antimicrobials in the oral cavity. Microparticles, films and oral tablets based on alginate and gellan gum were developed also as a strategy to overcome the low aqueous solubility of morin. The systems were characterized in terms of morphological characteristics, mucoadhesion and in vitro drug release. Antibiofilm activity was analyzed for acidogenicity, microbial viability and the composition of the extracellular matrix of single-species biofilms. Scanning Electron Microscopy demonstrated that the microparticles were spherical, rough and compact. The film and the tablet presented smooth and continuous surface and in the inner of the tablet was porous. These systems were more mucoadhesive compared to the microparticles. The in vitro morin release profiles in artificial saliva demonstrated that the microparticles controlled the release better (39.6%), followed by the film (41.1%) and the tablet (91.4%) after 20 h of testing. The morin released from the systems reduced the acidogenicity, microbial viability, concentration of insoluble extracellular polysaccharides and dry weight of biofilms, when compared to the control group. The findings of this study showed that the morin has antibiofilm activity against cariogenic microorganisms.


Assuntos
Alginatos/química , Biofilmes/efeitos dos fármacos , Placa Dentária/tratamento farmacológico , Portadores de Fármacos , Desenho de Fármacos , Flavonoides/farmacologia , Polissacarídeos Bacterianos/química , Actinomyces/efeitos dos fármacos , Administração Oral , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Humanos , Streptococcus mutans/efeitos dos fármacos , Comprimidos/uso terapêutico
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