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The introduction of tablet dosage forms has brought a revolution in the pharmaceutical drug delivery system. Different forms of tablets have been developed based on the target site, the onset of action, and therapeutic drug delivery methods. Fast-disintegrating tablets (FDTs) are the most promising pharmaceutical dosage form, especially for pediatric and geriatric patients having difficulty swallowing. The key feature of FDTs is quick drug release soon after their administration through the oral cavity. With innovations in the formulation of FDTs, the demand for excipients with better functionalities, particularly in terms of flow and compression characteristics, has increased. Co-processed excipients are a mixture of 2 or more conventional excipients that provides significant benefits over the individual excipients while minimizing their shortcomings. Such multifunctional co-processed excipients minimize the number of excipients that are to be incorporated into tablets during the manufacturing process. The present review discusses FTDs formulated from co-processed excipients, their manufacturing techniques, and the latest research, patents and commercially available co-processed FDTs.
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Química Farmacêutica , Excipientes , Humanos , Criança , Idoso , Química Farmacêutica/métodos , Liberação Controlada de Fármacos , Comprimidos , Solubilidade , Composição de Medicamentos/métodosRESUMO
Medicinal plants are considered the reservoir of diverse therapeutic agents and have been traditionally employed worldwide to heal various ailments for several decades. Silymarin is a plant-derived mixture of polyphenolic flavonoids originating from the fruits and akenes of Silybum marianum and contains three flavonolignans, silibinins (silybins), silychristin and silydianin, along with taxifolin. Silybins are the major constituents in silymarin with almost 70-80% abundance and are accountable for most of the observed therapeutic activity. Silymarin has also been acknowledged from the ancient period and is utilized in European and Asian systems of traditional medicine for treating various liver disorders. The contemporary literature reveals that silymarin is employed significantly as a neuroprotective, hepatoprotective, cardioprotective, antioxidant, anti-cancer, anti-diabetic, anti-viral, anti-hypertensive, immunomodulator, anti-inflammatory, photoprotective and detoxification agent by targeting various cellular and molecular pathways, including MAPK, mTOR, ß-catenin and Akt, different receptors and growth factors, as well as inhibiting numerous enzymes and the gene expression of several apoptotic proteins and inflammatory cytokines. Therefore, the current review aims to recapitulate and update the existing knowledge regarding the pharmacological potential of silymarin as evidenced by vast cellular, animal, and clinical studies, with a particular emphasis on its mechanisms of action.
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Silimarina , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Flavonoides/metabolismo , Frutas , Silybum marianum/metabolismo , Silimarina/farmacologia , Silimarina/uso terapêuticoRESUMO
OBJECTIVES: Physicians across the world have been disproportionately affected by the COVID-19 pandemic. This study was designed and conducted to assess the emotional and behavioural reactions of physicians to the initial phase of the COVID-19 pandemic. SUBJECTS AND METHODS: An online survey questionnaire using the google forms platform was constructed by the authors. The items in the questionnaire were based on clinical experience, relevant literature review and discussion with peers. A list of issues that were deemed as essential components of the experience of the pandemic relevant to physicians was arrived at. Thereafter these issues were operationalized into question form and hosted on the google forms platform. The link to this questionnaire was circulated by the authors among their peer groups in the month of April 2020. RESULTS: We received 295 responses and 3 were unusable. Most of the responses were from India, the United States of America, Australia, Canada and the United Kingdom. About 60% of the respondents identified themselves as frontline and had a decade of clinical experience. Most respondents reported being anxious due to the pandemic and also observed the same in their peers and families. A majority also observed changes in behaviour in self and others and advanced a variety of reasons and concerns. A sense of duty was the most commonly employed coping mechanism. CONCLUSION: Physicians are not immune from information and misinformation, or cues in the environment. Behavioural choices are not always predicted by knowledge but by a combination of knowledge, emotional state, personality and environment. Healthcare settings need to be ready for emergencies and should focus on reducing uncertainty in physicians. These factors may also be gainfully used in the mental health promotion of physicians in COVID-19 care roles.
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COVID-19 , Médicos , Humanos , Internet , Pandemias , SARS-CoV-2 , Inquéritos e QuestionáriosRESUMO
Majority of the representative drugs customarily interact with multiple targets manifesting unintended side effects. In addition, drug resistance and over expression of the cellular efflux-pumps render certain classes of drugs ineffective. With only a few innovative formulations in development, it is necessary to identify pharmacophores and novel strategies for creating new drugs. The conjugation of dissimilar pharmacophoric moieties to design hybrid molecules with an attractive therapeutic profile is an emerging paradigm in the contemporary drug development regime. The recent decade witnessed the remarkable biological potential of 1,3,5-triazine framework in the development of various chemotherapeutics. The appending of the 1,3,5-triazine nucleus to biologically relevant moieties has delivered exciting results. The present review focuses on 1,3,5-triazine based hybrid molecules in the development of pharmaceuticals.
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Triazinas/química , Triazinas/uso terapêutico , Animais , Anti-Infecciosos/química , Anti-Infecciosos/uso terapêutico , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Antineoplásicos/química , Antineoplásicos/uso terapêutico , Desenho de Fármacos , Humanos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/uso terapêuticoRESUMO
BACKGROUND: Co-processing starch with clay nanocomposite has been shown to yield a new class of materials, potentially with better properties than pristine starch, that could be used as directly compressible excipients in tablet formulations. OBJECTIVES: In this study, starches from 3 botanical sources, i.e., millet starch from Pennistum glaucum (L) RBr grains, sorghum starch from Sorghum bicolor L. Moench grains and cocoyam starch from Colocasia esculenta L. Schott tubers, were co-processed with montmorillonite clay (MMT) and evaluated as a directly compressible excipient in tramadol tablet formulations. The effects of different starch-to-clay ratios on the material and drug release properties of the resulting tablets were evaluated. MATERIAL AND METHODS: The starch-clay composites were prepared by heating a dispersion of the starch in distilled water, then precipitating the dispersion with an equal volume of 95% ethanol. The starch-clay composites were characterized and used as direct compression excipients for the preparation of tramadol tablets. The mechanical and drug release properties of the tablets were evaluated. RESULTS: Co-processing MMT with the starches yielded starch-clay composites with different material and tablet properties than the pristine starches. The co-processed starch-MMT biocomposites exhibited improved flowability and compressibility over the pristine starches. The mechanical and drug release properties of tramadol tablets containing starch-clay composites were significantly better than those containing only pristine starches. The properties of the starch-clay composites were not related to the botanical source of the starches. CONCLUSIONS: The study showed that starch-clay biocomposites could be used in the controlled release of tramadol.
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Argila , Excipientes , Amido , Comprimidos , Tramadol , Composição de Medicamentos , SolubilidadeRESUMO
The purpose of the present study was to prepare floating matrix tablets of clarithromycin employing simplex lattice design. Hydroxypropyl methylcellulose (HPMC) and Ethyl Cellulose (EC) were used as matrix forming agents; sodium bicarbonate and citric acid as effervescence producing agents. Simplex lattice design was used as optimization technique employing three independent formulation variables viz. concentration of HPMC (X1), Citric Acid (X2), EC (X3) whereas floating lag time, t50%, t90%, and MDT (Mean Dissolution Time) were the response (dependent) variables. Seven formulations (F1-F7) were prepared and evaluated for dissolution studies, floating characteristics, weight variation, hardness, thickness, friability.t50% of the formulations was found to be ranging from 317±2.54 to 522±2.39 minutes. The t90% and MDT of the tablets were found to be ranging between 659.65±1.89 to 967.35±1.67 minutes and 527.20±1.22 to 846.78±2.61 minutes respectively. Total floating time of the formulations was more than 12 hours and the drug content was in the range of 98.54±0.46 to 99.92±0.32. The amount of both HPMC and EC were found to play a dominating role in controlling the release of the drug from the formulation whereas ratios of sodium bicarbonate and citric acid were showing significant effect on the floating lag time. The release exponent (n) from Korsmeyer-Peppas model was found to be between 0.62 and 0.75 indicating non-Fickian or anomalous drug release behavior from the formulated floating matrix tablets. Simplex lattice design was reported to be an effective optimization technique for optimizing pharmaceutical formulations against desired responses.
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Antibacterianos/química , Claritromicina/química , Dióxido de Carbono/química , Celulose/análogos & derivados , Celulose/química , Química Farmacêutica , Ácido Cítrico/química , Simulação por Computador , Preparações de Ação Retardada , Excipientes/química , Dureza , Derivados da Hipromelose/química , Cinética , Modelos Químicos , Análise Numérica Assistida por Computador , Bicarbonato de Sódio/química , Solubilidade , Comprimidos , Tecnologia Farmacêutica/métodosRESUMO
BACKGROUND: Starch is a potential biomaterial used for various pharmaceutical applications because of its unique physicochemical and functional characteristics. A number of modification techniques, such as physical, chemical, enzymatic and genetic or a combination of any of these methods have been reported with the aim of enhancing the positive attributes and eliminating the shortcomings of the native starches. OBJECTIVES: The present studies deal with the development of co-precipitates of corn starch with different silicates (Mg, Ca, Al) with an aim of using it as a tablet superdisintegrant. Co-precipitates of starch with different silicates were prepared and FTIR-ATR, XRD and SEM techniques were used for the characterization of conjugates. MATERIAL AND METHODS: The conjugate were analyzed for various powder evaluation test like angle of repose, bulk density, tapped density, Hausner's ratio, Carr's index, swelling index and effective pore radius. RESULTS: The prepared co-precipitates were found to possess good powder flow properties. The swelling and effective pore radius of all co-precipitates (SMgC, SAlC and SCaC) was found in the range between 30-100% and 15.89-21.71 µm respectively. Different ratios of the prepared co-precipitates were used to formulate fast disintegrating tablets. Fast disintegrated tablets formulated using starch silicate conjugates as superdisintegrant were evaluated for diameter, thickness, hardness, friability, tensile strength, in vitro tablet disintegration, water absorption ratio, wetting time and in vitro dissolution studies. The effective pore radius and swelling of the co-precipitates were correlated with the in vitro disintegration, water absorption ratio and wetting time of the tablets. CONCLUSIONS: It was concluded that silicated co-precipitates of starch could be used as superdisintegrants in pharmaceutical tablet formulations.
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Química Farmacêutica/métodos , Silicatos/química , Amido/química , Comprimidos/química , Precipitação Química , Dureza , Metais/química , Pós/química , SolubilidadeRESUMO
The present investigation was aimed at preparation of polymethacrylate(s)- iron oxide conjugates and to evaluate mucoadhesive performance using texture analyzer. Eudragit RL-iron oxide or Eudragit RS-iron oxide conjugate granules were prepared by solvent evaporation technique. The mucoadhesive strength of pure Eudragit RL and RS was found to be 11.25±2.02 and 7.78±0.92 g respectively, whereas the same was found to be 36.42±4.01 and 24.32±4.44 for the iron oxide conjugates of Eudragit RL and RS respectively. Hence, mucoadhesive strength of polymethacrylates was found to be enhanced by this technique while, retaining their pH resistant property. A correlation (p>0.05) of 0.97 between mucoadhesive strength and zeta potential indicated conjugation of iron oxide contributed positive surface charge that causes enhancement of mucoadhesion. Further, the ATR-FTIR spectral analysis as well as DSC analysis supported existence of ionic interactions between conjugates (Eudragit RS or RL with iron oxide) and the tissue surface. Hence, the findings point out toward the expected potential use and application of Eudragit RL-iron oxide conjugate in mucoadhesive drug delivery systems, gastro retentive drug delivery systems, etc.
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Compostos Férricos/química , Ácidos Polimetacrílicos/química , Adesivos Teciduais/química , Adesividade , Animais , Varredura Diferencial de Calorimetria , Eletroquímica , Técnicas In Vitro , Mucosa Intestinal , Espectroscopia de Infravermelho com Transformada de Fourier , Suínos , ComprimidosRESUMO
INTRODUCTION: Ferulic acid (FA) is a phenolic phytochemical that has garnered the attention of the research community due to its abundant availability in nature. It is a compound that has been explored for its multifaceted therapeutic potential and benefits in modern and contemporary healthcare. AREAS COVERED: This review furnishes a compilation of the molecular mechanisms underlying the anti-diabetic, anticancer, antioxidant, and anti-inflammatory effects of FA. We also aim to excavate an in-depth analysis of the role of nanoformulations to achieve release control, reduce toxicity, and deliver FA at specified target sites. To corroborate the safety and efficacy of FA, a multitude of pre-clinical studies have also been conducted by researchers and have been discussed comprehensively in this review. The various patented innovations and newer paradigms pertaining to FA have also been presented. EXPERT OPINION: Enormous research has been conducted and should still be continued to find the best possible novel drug delivery system for FA delivery. The utilization of nanocarriers and nanoformulations has intrigued the scientists for delivery of FA, but before that, it is necessary to shed light upon toxicity, safety, and regulatory concerns of FA.
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Ácidos Cumáricos , Sistemas de Liberação de Medicamentos , Nanopartículas , Patentes como Assunto , Ácidos Cumáricos/uso terapêutico , Ácidos Cumáricos/administração & dosagem , Ácidos Cumáricos/farmacologia , Ácidos Cumáricos/química , Humanos , Animais , Portadores de Fármacos/químicaRESUMO
Cutaneous Squamous Cell Carcinoma (cSCC) is a common and potentially fatal type of skin cancer that poses a significant threat to public health and has a high prevalence rate. Exposure to ultraviolet radiation on the skin surface increases the risk of cSCC, especially in those with genetic syndromes like xerodermapigmentosum and epidermolysis bullosa. Therefore, understanding the molecular pathogenesis of cSCC is critical for developing personalized treatment approaches that are effective in cSCC. This article provides a comprehensive overview of current knowledge of cSCC pathogenesis, emphasizing dysregulated signaling pathways and the significance of molecular profiling. Several limitations and challenges associated with conventional therapies, however, are identified, stressing the need for novel therapeutic strategies. The article further discusses molecular targets and therapeutic approaches, i.e., epidermal growth factor receptor inhibitors, hedgehog pathway inhibitors, and PI3K/AKT/mTOR pathway inhibitors, as well as emerging molecular targets and therapeutic agents. The manuscript explores resistance mechanisms to molecularly targeted therapies and proposes methods to overcome them, including combination strategies, rational design, and optimization. The clinical implications and patient outcomes of molecular-targeted treatments are assessed, including response rates and survival outcomes. The management of adverse events and toxicities in molecular-targeted therapies is crucial and requires careful monitoring and control. The paper further discusses future directions for therapeutic advancement and research in this area, as well as the difficulties and constraints associated with conventional therapies.
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INTRODUCTION: Onychomycosis, a multifactorial fungal infection of the nails, shows a global prevalence of about 5.5% and is responsible for 50% of all nail infections. To develop effective management strategies, it is necessary to understand the etiology, pathophysiology, and risk factors of onychomycosis. Oral route of drug delivery is one of the routes utilized to deliver anti-fungal agents, but, has its own limitations like longer duration of treatment, increased adverse effects, and potential for drug interaction. The ungual route has received greater attention due to its localized, non- invasive action and improved patient compliance. AREAS COVERED: This review comprehensively discusses conventional onychomycosis therapies and patented novel drug delivery systems for the management of onychomycosis including chemical permeation enhancers, non-particulate drug delivery systems, penetration enhancing devices etc., Databases such as PubMed, ResearchGate, and Google Patents were searched by using the keywords onychomycosis and trans-ungual drug delivery. EXPERT OPINION: Enormous research has been conducted and is still ongoing to find the best possible novel drug delivery system for onychomycosis management. Approaches like incorporation of herbal constituents in nano-formulations, inkjet printing, laser devices, iontophoretic techniques, etc. can be employed to make safe and effective drug delivery systems which are regulatory compliant.
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Onicomicose , Humanos , Onicomicose/tratamento farmacológico , Onicomicose/metabolismo , Antifúngicos/farmacologia , Administração Tópica , Patentes como Assunto , Unhas/metabolismo , Sistemas de Liberação de MedicamentosRESUMO
Co-processing involves the incorporation of one excipients into the particle structure of other excipients to overcome the deficiencies of each excipients. The current patent describes the co-processing of microcrystalline cellulose and mannitol via fluid bed agglomeration with an aim to limit the use of lubricant in tablet composition. The co-processed excipients blend was compared with the physical blend of excipients and characterized for scanning electron microscopy, disintegration and hardness. The average particle size of co-processed excipients was less than 0.55 mm, characterized by large individual lactose-coated particles whereas, the physical blend particles are uncoated and irregular in shape. Tablets made from both physical blend and co-processed excipients were compared. As per the hardness and disintegration studies, with increase in mixing time of excipients both hardness and disintegration time decreases.
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Excipientes , Lactose , Excipientes/química , Composição de Medicamentos , Comprimidos/química , Dureza , Lactose/químicaRESUMO
In the past, wounds were treated with natural materials, but modern wound dressings include functional elements to expedite the process of healing and to improve skin recovery. Due to their exceptional properties, nanofibrous wound dressings are now the most cutting-edge and desirable option. Similar in structure to the skin's own extracellular matrix (ECM), these dressings can promote tissue regeneration, wound fluid transportation, and air ductility for cellular proliferation and regeneration owing to their nanostructured fibrous meshes or scaffolds. Many academic search engines and databases, such as Google Scholar, PubMed, and Sciencedirect, were used to conduct a comprehensive evaluation of the literature for the purposes of this investigation. Using the term "nanofibrous meshes" as a keyword, this paper focuses on the importance of phytoconstituents. This review article summarizes the most recent developments and conclusions from studies on bioactive nanofibrous wound dressings infused with medicinal plants. Several wound-healing methods, wound-dressing materials, and wound-healing components derived from medicinal plants were also discussed.
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Polyglycolic acid (PGA) nanoparticles show promise in biomedical applications due to their exceptional biocompatibility and biodegradability. These nanoparticles can be readily modified, facilitating targeted drug delivery and promoting specific interactions with diseased tissues or cells, including imaging agents and theranostic approaches. Their potential to advance precision medicine and personalized treatments is evident. However, conventional methods such as emulsification solvent evaporation via batch synthesis or tubular reactors via flow chemistry have limitations in terms of nanoparticle properties, productivity, and scalability. To overcome these limitations, this study focuses on the design and development of a 3D-printed vortex tube reactor for the continuous synthesis of PGA nanoparticles using flow chemistry. Computer-aided design (CAD) and the design of experiments (DoE) optimize the reactor design, and computational fluid dynamics simulations (CFD) evaluate the mixing index (MI) and Reynolds (Re) expression. The optimized reactor design was fabricated using fused deposition modeling (FDM) with polypropylene (PP) as the polymer. Dispersion experiments validate the optimization process and investigate the impact of input flow parameters. PGA nanoparticles were synthesized and characterized for size and polydispersity index (PDI). The results demonstrate the feasibility of using a 3D-printed vortex tube reactor for the continuous synthesis of PGA nanoparticles through flow chemistry and highlight the importance of reactor design in nanoparticle production. The CFD results of the optimized reactor design showed homogeneous mixing across a wide range of flow rates with increasing Reynolds expression. The residence time distribution (RTD) results confirmed that increasing the flow rate in the 3D-printed vortex tube reactor system reduced the dispersion variance in the tracer. Both experiments demonstrated improved mixing efficiency and productivity compared to traditional tubular reactors. The study also revealed that the total flow rate had a significant impact on the size and polydispersity index of the formulated PGA nanoparticle, with the optimal total flow rate at 104.46 mL/min, leading to smaller nanoparticles and a lower polydispersity index. Additionally, increasing the aqueous-to-organic volumetric ratio had a significant effect on the reduced particle size of the PGA nanoparticles. Overall, this study provides insights into the use of 3D-printed vortex tube reactors for the continuous synthesis of PGA nanoparticles and underscores the importance of reactor design and flow parameters in PGA nanoparticle formulation.
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Numerous compounds, with extensive applications in biomedical and biotechnological fields, are present in the oceans, which serve as a prime renewable source of natural substances, further promoting the development of novel medical systems and devices. Polysaccharides are present in the marine ecosystem in abundance, promoting minimal extraction costs, in addition to their solubility in extraction media, and an aqueous solvent, along with their interactions with biological compounds. Certain algae-derived polysaccharides include fucoidan, alginate, and carrageenan, while animal-derived polysaccharides comprise hyaluronan, chitosan and many others. Furthermore, these compounds can be modified to facilitate their processing into multiple shapes and sizes, as well as exhibit response dependence to external conditions like temperature and pH. All these properties have promoted the use of these biomaterials as raw materials for the development of drug delivery carrier systems (hydrogels, particles, capsules). The present review enlightens marine polysaccharides providing its sources, structures, biological properties, and its biomedical applications. In addition to this, their role as nanomaterials is also portrayed by the authors, along with the methods employed to develop them and associated biological and physicochemical properties designed to develop suitable drug delivery systems.
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Ecossistema , Polissacarídeos , Animais , Polissacarídeos/química , Sistemas de Liberação de Medicamentos , Carragenina/química , Materiais Biocompatíveis/químicaRESUMO
Wounds represent various significant health concerns for patients and also contribute major costs to healthcare systems. Wound healing comprises of overlapped and various coordinated steps such as homeostasis, inflammation, proliferation, and remodeling. In response to the failure of many strategies in delivering intended results including wound closure, fluid loss control, and exhibiting properties such as durability, targeted delivery, accelerated action, along with histocompatibility, numerous nanotechnological advances have been introduced. To understand the magnitude of wound therapy, this systematic and updated review discussing the effectiveness of nanoemulsions has been undertaken. This review portrays mechanisms associated with wound healing, factors for delayed wound healing, and various technologies utilized to treat wounds effectively. While many strategies are available, nanoemulsions have attracted the tremendous attention of scientists globally for the research in wound therapy due to their long-term thermodynamic stability and bioavailability. Nanoemulsions not only aid in tissue repair, but are also considered as an excellent delivery system for various synthetic and natural actives. Nanotechnology provides several pivotal benefits in wound healing, including improved skin permeation, controlled release, and stimulation of fibroblast cell proliferation. The significant role of nanoemulsions in improved wound healing along with their preparation techniques has also been highlighted with special emphasis on mechanistic insights. This article illustrates recent research advancements for the utilization of nanoemulsions in wound treatment. An adequate literature search has been conducted using the keywords 'Nanoemulsions in wound healing', 'Wound therapy and nanoemulsions', 'Herbal actives in wound therapy', 'Natural oils and wounds treatment' etc., from PubMed, Science Direct, and Google Scholar databases. Referred and original publications in the English language accessed till April 2022 has been included, whereas nonEnglish language papers, unpublished data, and nonoriginal papers were excluded from the study.
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Atenção à Saúde , Cicatrização , HumanosRESUMO
Anti-cancer drugs are mostly limited in their use due to poor physicochemical and biopharmaceutical properties. Their lower solubility is the most common hurdle limiting their use upto their potential. In the recent years, the cyclodextrin (CD) complexation have emerged as existing approach to overcome the problem of poor solubility. CD-based nano-technological approaches are safe, stable and showed well in vivo tolerance and greater payload for encapsulation of hydrophobic drugs for the targeted delivery. They are generally chosen due to their ability to get self-assembled to form liposomes, nanoparticles, micelles and nano-sponges etc. This review paper describes a birds-eye view of the various CD-based nano-technological approaches applied for the delivery of anti-cancer moieties to the desired target such as CD based liposomes, niosomes, niosoponges, micelles, nanoparticles, monoclonal antibody, magnetic nanoparticles, small interfering RNA, nanorods, miscellaneous formulation of anti-cancer drugs containing CD. Moreover, the author also summarizes the various shortcomings of such a system and their way ahead.
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Antineoplásicos , Ciclodextrinas , Nanopartículas , Humanos , Ciclodextrinas/química , Lipossomos , Micelas , Nanopartículas/química , SolubilidadeRESUMO
Curcumin has been used in traditional medicine forages. The present study aimed to develop a curcumin-based hydrogel system and assess its antimicrobial potential and wound healing (WH) activity on an invitro and in silico basis. A topical hydrogel was prepared using chitosan, PVA, and Curcumin in varied ratios, and hydrogels were evaluated for physicochemical properties. The hydrogel showed antimicrobial activity against both gram-positive and gram-negative microorganisms. In silico studies showed good binding energy scores and significant interaction of curcumin components with key residues of inflammatory proteins that help in WH activity. Dissolution studies showed sustained release of curcumin. Overall, the results indicated wound healing potential of chitosan-PVA-curcumin hydrogel films. Further in vivo experiments are needed to evaluate the clinical efficacy of such films for wound healing.
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The direct compression suitability of active pharmaceutical ingredients could be studied by SeDeM diagram method. Cefuroxime axetil (CfA) and paracetamol (PCM) were employed for SeDeM studies as these powders are well-characterized and known to be particularly difficult with respect to flowability and compactibility. Twelve different selected pharmacotechnical parameters were determined experimentally and were treated mathematically for being expressed in graphic representation as SeDeM diagram. Parameter index, parameter profile index and good compression index were calculated for both the selected drugs. Good compression index was found to be 2.19 and 1.36 for CfA and PCM, respectively, indicating poor direct compression characteristics of the selected drugs. The results from this SeDeM diagram method are in line with the previously reported studies where it was established as a reliable method for preformulation studies and as a quality control tool for studying batch-to-batch reproducibility of API's. Furthermore, it once again established the notion that blending poorly compressible drugs with suitable ingredients followed by SeDeM studies could be used as method for identifying best excipient and calculating maximum amount of excipient required for direct compression of API.
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Acetaminofen/química , Cefuroxima/análogos & derivados , Gráficos por Computador , Sistemas Inteligentes , Tecnologia Farmacêutica/métodos , Cefuroxima/química , Química Farmacêutica , Composição de Medicamentos , Excipientes/química , Tamanho da Partícula , Porosidade , Pós , Pressão , Reologia , MolhabilidadeRESUMO
The objective of this study was to extend the GI residence time of the dosage form and to control the release of domperidone using directly compressible sustained release mucoadhesive matrix (SRMM) tablets. A 2-factor centre composite design (CCD) was employed to study the influence of independent variables like gum ghatti (GG) (X1) and hydroxylpropylmethyl cellulose K 15M (HPMC K 15M) (X2) on dependent variable like mucoadhesive strength, tensile strength, release exponent (n), t50 (time for 50% drug release), rel(10 h) (release after 10 h) and rel(18 h) (release after 18 h). Tablets were prepared by direct compression technology and evaluated for tablet parametric test (drug assay, diameter, thickness, hardness and tensile strength), mucoadhesive strength (using texture analyzer) and in vitro drug release studies. The tensile strength and mucoadhesive strength were found to be increased from 0.665 +/- 0.1 to 1.591 +/- 0.1 MN/cm2 (Z1 to Z9) and 10.789 +/- 0.985 to 50.924 +/- 1.150 N (Z1 to Z9), respectively. The release kinetics follows first order and Hixson Crowell equation indicating drug release following combination of diffusion and erosion. The n varies between 0.834 and 1.273, indicating release mechanism shifts from non fickian (anomalous release) to super case II, which depict that drug follows multiple drug release mechanism. The t50 time was found to increase from 5 +/- 0.12 to 11.4 +/- 0.14 h (Z1 to Z9) and release after 10 and 18 h decreases with increasing concentration of both polymers concluding with release controlling potential of polymers. The accelerated stability studies were performed on optimized formulation as per ICH guideline and the result showed that there was no significant change in tensile strength, mucoadhesive strength and drug assay.