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1.
Ther Deliv ; : 1-11, 2024 Jun 11.
Artigo em Inglês | MEDLINE | ID: mdl-38888592

RESUMO

Aim: The objective of this study was to develop and characterize the physical properties of fast-melting tablets (FMTs) using cocoa butter as the base and caffeine as the model drug. Method: The simple refrigerator freezing method was employed to prepare caffeine-loaded, FMTs from cocoa butter bases. Results: The F3 chosen formulation achieved a disintegration time of 1.20 min ± 0.035, which falls within the specified limit set by the European Pharmacopoeia. The cumulative drug release data of F3, was 88.52 and 94.08% within 60 and 75 min, respectively (NLT 85% as per US FDA requirement). All the other physical test standards for FMTs met the pharmacopeial specifications. Conclusion: Based on the findings, the simple refrigerator freezing method could be used to formulate FMTs.


Patient-friendly natural caffeine-loaded cocoa butter-based fast-melting tablets with rapid disintegration, affordability, safety and biocompatibility are an efficient base for drug delivery.

2.
Drug Dev Ind Pharm ; 50(1): 36-44, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38149637

RESUMO

INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited. OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs. METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation. RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min. CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.


Assuntos
Excipientes , Xilitol , Humanos , Excipientes/química , Mirtazapina , Composição de Medicamentos/métodos , Solubilidade , Administração Oral , Comprimidos/química , Manitol/química
3.
Int J Pharm Compd ; 27(6): 512-521, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38100669

RESUMO

Memantine hydrochloride is commonly prescribed for Alzheimer's disease and vascular dementia. However, the drug is only available in tablet form, a dosage form which is difficult for geriatrics to swallow. This problem is especially difficult for those patients diagnosed with Alzheimer's. This study was therefore aimed to develop and characterize an oral disintegrating film containing memantine hydrochloride using different types and concentrations of polymers. Using the solvent casting method, twelve formulations were developed, which involved manipulations on the type and concentration of the polymer. Afterwards, six formulations were selected to undergo characterization tests. These tests evaluated the films' tensile strength, Young's Modulus, percent elongation, folding endurance, disintegration and dissolution time, content uniformity, moisture loss, and moisture uptake. Polymers such as polyvinyl alcohol, hydroxypropyl methylcellulose, polyvinyl pyrrolidone, and pullulan gum were respectively incorporated at different concentrations. The study found that only hydroxypropyl methylcellulose and polyvinyl alcohol formulations developed into acceptable oral disintegrating films. Formulation E (hydroxypropyl methylcellulose 50-mg/film), which exhibited optimal mechanical strength, fast disintegration and dissolution, and excellent content uniformity, was identified as the best formula. Although polyvinyl alcohol showed higher mechanical strength, hydroxypropyl methylcellulose films were better at fulfilling the optimal characteristics of an oral disintegrating film. The study showed that the mechanical strength increased proportionally to the polymer concentration in the polyvinyl alcohol film. However, for the hydroxypropyl methylcellulose film, the mechanical strength increased only when hydroxypropyl methylcellulose's concentration was increased from a 40-mg/film to a 50-mg/film but decreased with a 60-mg/film. To summarize, orally disintegrating films containing memantine hydrochloride was developed, characterized, and reasoned to have high potential to be marketed and to increase medication compliance among geriatrics suffering from Alzheimer's disease.


Assuntos
Doença de Alzheimer , Química Farmacêutica , Humanos , Idoso , Memantina/uso terapêutico , Álcool de Polivinil/uso terapêutico , Doença de Alzheimer/tratamento farmacológico , Administração Oral , Derivados da Hipromelose/uso terapêutico , Solubilidade , Polímeros , Composição de Medicamentos/métodos
4.
Int J Pharm Compd ; 27(6): 522-527, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38100670

RESUMO

Orally disintegrating tablets, which were originally developed in the pharmaceutical field to improve the compliance of patients who had difficulty swallowing tablets, have become a preferable choice in solid dosage forms since it brings advantages to the patients and consumers in the healthcare system. Among the advantages of this novel dosage form are a faster onset of action, improved bioavailability, and the ease of administration as it can be taken without water. However, there are still some limitations of orally disintegrating tablets that need to be overcome, including a lack of mechanical strength, an unpleasant taste of the drug in the mouth, and a stability issue due to its hygroscopicity nature. This objective of this study was to identify the composition of co-processed excipients comprising of mannitol, microcrystalline cellulose, xylitol, and crospovidone or croscarmellose sodium in order to formulate orally disintegrating tablets containing memantine hydrochloride. This study was carried out in two stages. Firstly, orally disintegrating tablets containing memantine hydrochloride with 6 different formulations, which differed in the percentage of crospovidone or croscarmellose sodium, were formulated and manufactured. Secondly, the orally disintegrating tablets obtained were evaluated through pre- and post-compression tests based on the standard for orally disintegrating tablets. Formulation 3, which consisted of 10% xylitol, 10% mannitol, 72% microcrystalline cellulose, and 8% crospovidone, was chosen as the optimum formulation for the co-processed excipient since it was the fastest disintegration process among all the formulations in the study. In addition, Formulation 3 also showed the acceptable and satisfying results in other evaluation tests such as - weight variation test, hardness test, and friability test. The co-processed excipient comprising of 10% xylitol, 10% mannitol, 72% microcrystalline cellulose, and 8% crospovidone, which is characterized by improved functionalities such as a fast disintegration process, plays a crucial role in the application of orally disintegrating tablets.


Assuntos
Manitol , Povidona , Humanos , Manitol/química , Povidona/química , Xilitol , Memantina , Excipientes/química , Carboximetilcelulose Sódica/química , Comprimidos/química , Solubilidade , Composição de Medicamentos , Administração Oral
5.
Heliyon ; 9(11): e21876, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-38034771

RESUMO

Hair shampoos containing botanical ingredients without synthetic additives, such as parabens, petrochemicals, sulfates and silicones are more skin- and environmentally friendly. In recent years, there is a growing demand for shampoo products with botanical extracts. Shampoos with botanical extracts are well-known for their perceived health benefits. They are also generally milder, non-toxic, natural, and less likely to disrupt the hair and scalp's natural pH and oil balance. Many also believe that shampoos with botanical origins have higher standards of quality. Numerous botanical extracts had been used as natural active ingredients in cosmetic formulations to meet consumer demands. In this review, we have revisited six tropical plants commonly added as natural active ingredients in shampoo formulations: Acacia concinna, Camellia oleifera, Azadirachta indica, Emblica officinalis, Sapindus mukorossi, and Garcinia mangostana. These plants have been traditionally used for hair care, and scientific research has shown that they exhibit relevant physicochemical properties and biological activities that are beneficial for hair care and scalp maintenance.

6.
Cancers (Basel) ; 15(14)2023 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-37509402

RESUMO

BACKGROUND: Luteolin is a flavonoid compound that has been widely studied for its various anti-cancer properties and sensitization to multidrug-resistant cells. However, the limited solubility and bioavailability of Lut hindered its potential clinical use. Theoretically, the combination of this compound with vitamin E TPGS and poloxamer 407 can produce a synergistic effect to enhance tumor apoptosis and P-glycoprotein inhibition. This study aimed to develop and optimize vitamin E TPGS/Poloxamer 407 micelles loaded with luteolin through investigating certain factors that can affect the encapsulation efficiency and particle size of the micelle. METHODS: A micelle was prepared using the film hydration method, and the micellar solution was lyophilized. The cake formed was analyzed. The factors investigated include the concentrations of the surfactants, ratio of vitamin E TPGS/Poloxamer 407, temperature of the hydrating solution, duration of hydration, and freezing temperature before lyophilization. The effects of these factors on the encapsulation efficiency and particle size of the micelle were also studied. The encapsulation efficiency was measured using a UV-Vis spectrophotometer, while particle size was measured using dynamic light scattering. RESULTS: The optimized micelle was found to have 90% encapsulation efficiency with a particle size of less than 40 nm, which was achieved using a 10% concentration of surfactants at a vitamin E TPGS/Poloxamer 407 ratio of 3:1. The optimized temperature for hydrating the micellar film was 40 °C, the optimized mixing time was 1 h, and the optimized freezing temperature was -80 °C. The solubility of the luteolin-loaded micelles increased 459-fold compared to pure Lut in water. The critical micelle concentration of the vitamin E TPGS/Poloxamer 407 micelle was 0.001 mg/mL, and the release study showed that luteolin-loaded micelles exhibited sustained release behavior. The release of luteolin from a micelle was found to be higher in pH 6.8 compared to pH 7.4, which signified that luteolin could be accumulated more in a tumor microenvironment compared to blood. CONCLUSION: This study demonstrated that several factors need to be considered when developing such nanoparticles in order to obtain a well-optimized micelle.

7.
Nutrients ; 15(10)2023 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-37242265

RESUMO

Research background and Objectives: Age is an independent risk factor for cardiovascular disease (CVD), but CVD risk factors are preventable, and lack of awareness of its risk factors is a contributing factor to CVDs. Middle-aged people may be more likely to engage in unhealthy lifestyle behaviours which can increase the risk of CVD. Health self-assessment is crucial for early detection and management of health issues and early lifestyle intervention for better personalised health management. This study aims to determine the self-assessment of INTERHEART risk classification among the middle-aged community in Malaysia. Method: Local community members aged 40-60 years and who are currently residing in Malaysia were recruited via non-randomised sampling. Sociodemographic characteristics and dietary pattern related to salt, fibre, fat (deep fried/snacks), poultry/meat intakes, and other cardiovascular risk factors (waist-hip ratio, medical history related to diabetes/hypertension, history/exposure of tobacco use, psychosocial status, and level of physical activity) were assessed; INTERHEART risk scores were then computed and stratified into low, medium and high risks. Results: Approximately 45% (n = 273/602) of middle-aged respondents in Malaysia are at moderate-to-high risk of cardiovascular events, with men being more likely to develop CVD compared to women. The results of the survey indicated that poultry/meat intake (61%), physical inactivity (59%), and second-hand smoke (SHS) exposure (54%) are the most prevalent risk factors among the respondents. One-third of the respondents consumed excessive salty food and deep fried foods/snacks/fast food, and only one-third of them consumed vegetables/fruits at a recommended level. It is worrying that about a quarter of the respondents felt several periodical/permanent stresses and even felt sad/blue/depressed for two weeks or more in a row. Males, labour workers, and those with lower educational levels are more likely to develop CVD events. Conclusions: This study found that 45% of the middle-aged respondents were having moderate-to-high risk for cardiovascular events with multiple risk factors related to unhealthy lifestyle habits and environmental factors. In addition to non-modifiable factors such as gender and age, sociodemographic factors, i.e., educational level and occupation, are equally important factors to determine CVD risk. Overall, the findings of this study emphasize the clinical relevance of assessing multiple factors in the determination of CVD risks for early prevention and management of cardiovascular diseases.


Assuntos
Doenças Cardiovasculares , Autoavaliação (Psicologia) , Masculino , Pessoa de Meia-Idade , Humanos , Feminino , Malásia/epidemiologia , Doenças Cardiovasculares/epidemiologia , Doenças Cardiovasculares/etiologia , Doenças Cardiovasculares/prevenção & controle , Fatores de Risco , Frutas , Medição de Risco
8.
Molecules ; 27(17)2022 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-36080243

RESUMO

Traditional medicine is critical in disease treatment and management. Herbs are gaining popularity for disease management and treatment. Therefore, they can be utilised as complementary and alternative treatment (CAT) ingredients. Atopic dermatitis (AD) is one of the common non-communicable diseases. It is characterised by chronic inflammatory skin disease with intense pruritus and eczematous lesions. AD is associated with oxidative stress, microbial infection, and upregulation of inflammatory cytokines. Both children and adults could be affected by this skin disorder. The prevalence of AD is increasing along with the country's level of development. This review revisited the literature on four medicinal herbs widely used as complementary medicine to manage AD. These therapeutic herbs are commonly eaten as food and used as spices in Asian cuisine. The four food herbs reviewed are Cassia alata, Coriandrum sativum, Curcuma longa Linn, and Azadirachta indica. Their traditional uses and phytochemical content will be covered. Four relevant pharmacological and biological activities of the plants crucial in AD management have been reviewed and discussed, including anti-inflammatory, anti-microbial, antioxidant, and wound recovery.


Assuntos
Azadirachta , Cassia , Terapias Complementares , Coriandrum , Dermatite Atópica , Ingredientes de Alimentos , Senna , Curcuma , Dermatite Atópica/tratamento farmacológico
9.
Polymers (Basel) ; 14(15)2022 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-35956565

RESUMO

An excipient intended for direct compression in pharmaceutical tableting must show important features of flowability and compactibility. This study investigated pregelatinised sago starch as an excipient for direct compression tablets. Pregelatinised sago starch was prepared and characterised. Its powder bulk properties and performance in the tablet formulations with paracetamol as a model drug were compared against two commercial, directly compressible excipients, namely Avicel® PH 101 and Spress® B820. The results showed that pregelatinisation did not affect the chemical structure of sago starch, but its degree of crystallinity reduced, and X-ray diffraction pattern changed from C-type to A-type. Powder bulk properties of pregelatinised sago starch and Spress® B820 were comparable, exhibiting better flowability but lower compactibility than Avicel® PH 101. In the formulation of paracetamol tablets, pregelatinised sago starch and Spress® B820 performed equally well, followed by Avicel® PH 101 as indicated in Formulations 3, 2 and 1, respectively.

10.
Int J Pharm Compd ; 26(3): 255-263, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35657749

RESUMO

Co-processed excipients were prepared by incorporating one excipient into the particle structure of another and a combination of two or more compendia or noncompendia excipients to physically modify their properties, which cannot be achievable by simple physical mixing. The co-processed multicomponent-based excipients were introduced to achieve better characteristics and tableting properties. This objective of this study was to develop and evaluate a co-processed excipient for amlodipine orally disintegrating tablets to simplify the compounding process. The co-processed excipients were prepared by wet granulation with 5% of polyvinylpyrrolidone and croscarmellose sodium, five different percentages of microcrystalline cellulose, and lactose monohydrate. After sieving and drying, the co-processed excipients were evaluated for flowability and compressibility. The co-processed excipients were mixed with the amlodipine powder and magnesium stearate and compressed into tablets. The amlodipine tablets were evaluated for weight variation, content uniformity, thickness, hardness, friability, disintegration, and dissolution tests. Formulation 4 was chosen as the optimum formulation because the results showed this formulation had the excellent flowability and compressibility of a co-processed excipient. It showed uniformity of weight, content, thickness, and hardness, weight loss less than 1%, fast disintegration time, and dissolution results. The developed co-processed excipient can be used by the pharmaceutical industry in the future to compound amlodipine orally disintegrating tablets in a fast and economical way.


Assuntos
Anlodipino , Excipientes , Composição de Medicamentos/métodos , Excipientes/química , Pós , Solubilidade , Comprimidos
11.
Molecules ; 27(10)2022 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-35630605

RESUMO

A fast melt tablet (FMT) is well regarded as an alternative delivery system that might help resolve a patient's non-compliance issue. The main objective of this study was to develop a cocoa butter-based FMT. Additives, namely 5-15% of PEG 6000, beeswax, paraffin wax, and corn starch, were incorporated into the cocoa butter-based FMT to study the effects of these additives with the physical characteristic of a cocoa butter FMT. An optimum-based formulation was chosen according to the desired hardness and disintegration time and the taste masking property achieved with the model drug-dapoxetine. The analysis demonstrated that incorporating beeswax (15%) and paraffin wax (15%) could prolong the disintegration time by at least two-fold. On the contrary, the presence of corn starch was found to cause an increase in the hardness and reduction of the disintegration time. The disintegration mechanism might be presumed due to the synergistic effect of starch swelling and cocoa butter melting. The hardness value and in vitro disintegration time of the optimum formulation were recorded at 2.93 ± 0.22 kg and 151.67 ± 6.98 s. In terms of dissolution, 80% of dapoxetine was released within 30 min and the dissolution profile was comparable to the innovator product. The formulation was palatable and stable for at least 1 year. The exposure of the FMT formulation at 30 °C for 12 months was reported to be stable. Along with the sound palatability profile and high drug load capacity, the current formulation possesses the desired characteristics to be scaled up and marketed.


Assuntos
Parafina , Amido , Gorduras na Dieta , Humanos , Polietilenoglicóis , Comprimidos , Ceras
12.
Chem Biol Drug Des ; 100(2): 185-217, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35490393

RESUMO

Cheminformatics utilizing machine learning (ML) techniques have opened up a new horizon in drug discovery. This is owing to vast chemical space expansion with rocketing numbers of expected hits and lead compounds that match druggable macromolecular targets, in particular from natural compounds. Due to the natural products' (NP) structural complexity, uniqueness, and diversity, they could occupy a bigger space in pharmaceuticals, allowing the industry to pursue more selective leads in the nanomolar range of binding affinity. ML is an essential part of each step of the drug design pipeline, such as target prediction, compound library preparation, and lead optimization. Notably, molecular mechanic and dynamic simulations, induced docking, and free energy perturbations are essential in predicting best binding poses, binding free energy values, and molecular mechanics force fields. Those applications have leveraged from artificial intelligence (AI), which decreases the computational costs required for such costly simulations. This review aimed to describe chemical space and compound libraries related to NPs. High-throughput screening utilized for fractionating NPs and high-throughput virtual screening and their strategies, and significance, are reviewed. Particular emphasis was given to AI approaches, ML tools, algorithms, and techniques, especially in drug discovery of macrocyclic compounds and approaches in computer-aided and ML-based drug discovery. Anthraquinone derivatives were discussed as a source of new lead compounds that can be developed using ML tools for diverse medicinal uses such as cancer, infectious diseases, and metabolic disorders. Furthermore, the power of principal component analysis in understanding relevant protein conformations, and molecular modeling of protein-ligand interaction were also presented. Apart from being a concise reference for cheminformatics, this review is a useful text to understand the application of ML-based algorithms to molecular dynamics simulation and in silico absorption, distribution, metabolism, excretion, and toxicity prediction.


Assuntos
Produtos Biológicos , Antraquinonas/farmacologia , Inteligência Artificial , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Quimioinformática , Aprendizado de Máquina , Simulação de Dinâmica Molecular
13.
J Med Life ; 15(3): 328-335, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35449993

RESUMO

Antimicrobials are widely used to treat bacteria, viruses, fungi, and protozoa. Therefore, research and development of newer types of antimicrobials are important. Antimicrobial resistance has emerged as a major challenge to the healthcare system, although various alternative antimicrobials have been proposed. However, none of these show consistent and comparable efficacy to antimicrobials in clinical trials. More recently, nanoparticles have emerged as a potential solution to antimicrobial agents to overcome antimicrobial resistance. This article revisits and updates applications of various types of nanoparticles for the delivery of antimicrobial agents and their characterization. Though nanoparticle technology has some limitations, it provides an innovative approach to pharmaceutical technology. Furthermore, nanoparticles offer a variety of advantages, such as enhancement of solubility and permeation, leading to better efficacy. In this article, approaches commonly employed to improve antimicrobial therapy are discussed. These approaches have advantages and applications and provide a broader opportunity for pharmaceutical scientists to choose the proper method per the desired outcome.


Assuntos
Anti-Infecciosos , Nanopartículas , Antibacterianos , Anti-Infecciosos/uso terapêutico , Bactérias , Sistemas de Liberação de Medicamentos , Humanos
14.
J Med Life ; 15(3): 313-318, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35449999

RESUMO

The COVID-19 pandemic has tremendously increased the production and sales of disinfectants. This study aimed to systematically review and analyze the efficacy and safety of chlorine dioxide as a disinfectant. The literature relating to the use of chlorine dioxide as a disinfectant was systematically reviewed in January 2021 using databases such as PubMed, Science Direct, and Google Scholar. Inclusion criteria were studies that investigated the use of chlorine dioxide to assess the efficacy, safety, and impact of chlorine dioxide as a disinfectant. Out of the 33 included studies, 14 studies focused on the disinfectant efficacy of chlorine dioxide, 8 studies expounded on the safety and toxicity in humans and animals, and 15 studies discussed the impact, such as water treatment disinfection using chlorine dioxide. Chlorine dioxide is a safe and effective disinfectant, even at concentrations as low as 20 to 30 mg/L. Moreover, the efficacy of chlorine dioxide is mostly independent of pH. Chlorine dioxide can be effectively used to disinfect drinking water without much alteration of palatability and can also be used to destroy pathogenic microbes, including viruses, bacteria, and fungi from vegetables and fruits. Our review confirms that chlorine dioxide is effective against the resistant Mycobacterium, H1N1, and other influenza viruses. Studies generally support the use of chlorine dioxide as a disinfectant. The concentration deemed safe for usage still needs to be determined on a case-by-case basis.


Assuntos
COVID-19 , Compostos Clorados/farmacologia , Desinfetantes , Vírus da Influenza A Subtipo H1N1 , Animais , Cloro , Desinfetantes/farmacologia , Humanos , Óxidos , Pandemias
15.
Int J Mol Sci ; 23(5)2022 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-35270025

RESUMO

Sunlight is an important factor in regulating the central circadian rhythm, including the modulation of our sleep/wake cycles. Sunlight had also been discovered to have a prominent influence on our skin's circadian rhythm. Overexposure or prolonged exposure to the sun can cause skin photodamage, such as the formation of irregular pigmentation, collagen degradation, DNA damage, and even skin cancer. Hence, this review will be looking into the detrimental effects of sunlight on our skin, not only at the aspect of photoaging but also at its impact on the skin's circadian rhythm. The growing market trend of natural-product-based cosmeceuticals as also caused us to question their potential to modulate the skin's circadian rhythm. Questions about how the skin's circadian rhythm could counteract photodamage and how best to maximize its biopotential will be discussed in this article. These discoveries regarding the skin's circadian rhythm have opened up a completely new level of understanding of our skin's molecular mechanism and may very well aid cosmeceutical companies, in the near future, to develop better products that not only suppress photoaging but remain effective and relevant throughout the day.


Assuntos
Cosmecêuticos , Envelhecimento da Pele , Dermatopatias , Ritmo Circadiano/fisiologia , Cosmecêuticos/metabolismo , Humanos , Pele/metabolismo , Dermatopatias/metabolismo
16.
Molecules ; 27(6)2022 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-35335312

RESUMO

Common wheat (Triticum aestivum), one of the world's most consumed cereal grains, is known for its uses in baking and cooking in addition to its medicinal uses. As this plant's medical benefits are enormous and scattered, this narrative review was aimed at describing the pharmacological activities, phytochemistry, and the nutritional values of Triticum aestivum. It is a good source of dietary fiber, resistant starch, phenolic acids, alkylresorcinols, lignans, and diverse antioxidant compounds such as carotenoids, tocopherols and tocotrienols. These constituents provide Triticum aestivum with a wide range of pharmacological properties, including anticancer, antimicrobial, antidiabetic, hypolipemic, antioxidant, laxative, and moisturizing effects. This review summarized the established benefits of wheat in human health, the mode of action, and different clinical, in vitro and in vivo studies for different varieties and cultivars. This review also gives an insight for future research into the better use of this plant as a functional food. More clinical trials, in vivo and in vitro studies are warranted to broaden the knowledge about the effect of Triticum aestivum on nutrition-related diseases prevention, and physical and mental well-being sustenance.


Assuntos
Antioxidantes , Triticum , Antioxidantes/química , Antioxidantes/farmacologia , Fibras na Dieta , Grão Comestível , Alimento Funcional , Humanos , Triticum/química
17.
Polymers (Basel) ; 13(17)2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34502895

RESUMO

Polymeric colloidal nanocarriers formulated from hydrophobically grafted carbohydrates have been the subject of intensive research due to their potential to increase the percutaneous penetration of hydrophilic actives. To this goal, a series of hydrophobically grafted pullulan (BMO-PUL) derivatives with varying degree of grafting (5-64%) was prepared through functionalisation with 2-(butoxymethyl)oxirane. The results demonstrated that monodispersed BMO-PUL nanocarriers (size range 125-185 nm) could be easily prepared via nanoprecipitation; they exhibit close-to-spherical morphology and adequate stability at physiologically relevant pH. The critical micellar concentration of BMO-PUL was found to be inversely proportional to their molecular weight (Mw) and degree of grafting (DG), with values of 60 mg/L and 40 mg/L for DG of 12.6% and 33.8%, respectively. The polymeric nanocarriers were loaded with the low Mw hydrophilic active α-arbutin (16% loading), and the release of this active was studied at varying pH values (5 and 7), with a slightly faster release observed in acidic conditions; the release profiles can be best described by a first-order kinetic model. In vitro investigations of BMO-PUL nanocarriers (concentration range 0.1-4 mg/mL) using immortalised skin human keratinocytes cells (HaCaT) evidenced their lack of toxicity, with more than 85% cell viability after 24 h. A four-fold enhance in arbutin permeation through HaCaT monolayers was recorded when the active was encapsulated within the BMO-PUL nanocarriers. Altogether, the results obtained from the in vitro studies highlighted the potential of BMO-PUL nanocarriers for percutaneous delivery applications, which would warrant further investigation in vivo.

18.
Mar Drugs ; 19(6)2021 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-34070821

RESUMO

Air pollution has recently become a subject of increasing concern in many parts of the world. The World Health Organization (WHO) estimated that nearly 4.2 million early deaths are due to exposure to fine particles in polluted air, which causes multiple respiratory diseases. Algae, as a natural product, can be an alternative treatment due to potential biofunctional properties and advantages. This systematic review aims to summarize and evaluate the evidence of metabolites derived from algae as potential anti-inflammatory agents against respiratory disorders induced by atmospheric particulate matter (PM). Databases such as Scopus, Web of Science, and PubMed were systematically searched for relevant published full articles from 2016 to 2020. The main key search terms were limited to "algae", "anti-inflammation", and "air pollutant". The search activity resulted in the retrieval of a total of 36 publications. Nine publications are eligible for inclusion in this systematic review. A total of four brown algae (Ecklonia cava, Ishige okamurae, Sargassum binderi and Sargassum horneri) with phytosterol, polysaccharides and polyphenols were reported in the nine studies. The review sheds light on the pathways of particulate matter travelling into respiratory systems and causing inflammation, and on the mechanisms of actions of algae in inhibiting inflammation. Limitations and future directions are also discussed. More research is needed to investigate the potential of algae as anti-inflammatory agents against PM in in vivo and in vitro experimental models, as well as clinically.


Assuntos
Poluentes Atmosféricos/efeitos adversos , Anti-Inflamatórios/uso terapêutico , Material Particulado/efeitos adversos , Phaeophyceae , Doenças Respiratórias/tratamento farmacológico , Animais , Humanos
19.
Arch Pharm Res ; 44(8): 1-10, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25579848

RESUMO

Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.


Assuntos
Benzilaminas/administração & dosagem , Excipientes/química , Naftalenos/administração & dosagem , Polímeros/química , Amido/química , Acrilatos/química , Administração Oral , Adulto , Benzilaminas/química , Química Farmacêutica/métodos , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Liofilização , Dureza , Humanos , Derivados da Hipromelose/química , Pessoa de Meia-Idade , Naftalenos/química , Ácidos Polimetacrílicos/química , Comprimidos , Paladar , Adulto Jovem
20.
Clin Exp Vaccine Res ; 9(1): 8-14, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32095436

RESUMO

PURPOSE: The objective of this research was to examine the cold chain temperature maintenance for the supply of vaccines and other biological products by pharmaceutical wholesaler. MATERIALS AND METHODS: In this study, six configurations using cold vaccine boxes or bags made with different materials, with and without insulation, of different sizes, and number of coolant-packs were used to simulate the configuration used by the pharmaceutical wholesalers for transportation of vaccine. Model vaccines (vial, n=10) were packed using these six configurations which then stored in an incubator at 38℃ and monitored for 24 hours. Each configuration was tested repeatedly for 5 times. RESULTS: In term of compliance to 2℃-8℃, four out of six tested configurations are effective in cold chain transportation. The effectiveness is highly dependent on the type of passive containers used, size of cold boxes, insulation, and number of coolant-packs. The configuration with a larger polystyrene foam box with five coolant-packs maintained the required temperature up to 23 hours. In contrast, configurations using a polystyrene foam box with four coolant-packs and a large vaccine cold box with two coolant-packs failed to reach below 8℃ throughout the 24 hours. CONCLUSION: Packaging method, the material and size of the container could have a direct impact on the effectiveness of cold chain temperature maintenance. Polystyrene foam box, cold box with polyethylene interior lining and polypropylene insulation, a cooler bag with proper number of ice packs could be effectively used for transportation of vaccines within their respective transportation duration allowance.

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