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The prevalence of polymer usage in everyday activities has emerged as a detriment to both human life and the environment. A large number of studies describe severe impacts of micropolymers (MP) and nanopolymers (NP) on various organ systems, including the endocrine system. Additionally, plasticizers utilized as additives have been identified as endocrine-disrupting chemicals (EDCs). MP/NP, along with associated plasticizers, affect principal signalling pathways of endocrine glands such as the pituitary, thyroid, adrenal, and gonads, thereby disrupting hormone function and metabolic processes crucial for maintaining homeostasis, fertility, neural development, and fetal growth. This review delves into the sources, distribution, and effects of micropolymers, nanopolymers, and associated plasticizers acting as EDCs. Furthermore, it provides a detailed review of the mechanisms underlying endocrine disruption in relation to different types of MP/NP.
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BACKGROUND: The tear ferning test can be an easy clinical procedure for the evaluation and characterization of the ocular tear film. OBJECTIVE: The objective of this study was to examine the restoration of tear ferning patterns and reduction of glycosylation peak after amlodipine application in carrageenan-induced conjunctivitis. METHODS: At the rabbit's upper palpebral region, carrageenan was injected for cytokine-mediated conjunctivitis. Ferning pattern and glycosylation of the tear fluid were characterized using various instrumental analyses. The effect of amlodipine was also examined after ocular instillation and flexible docking studies. RESULTS: Optical microscopy showed a disrupted ferning of the tear collected from the inflamed eye. FTIR of the induced tear fluid exhibited peaks within 1000-1200 cm-1, which might be due to the protein glycosylation absent in the normal tear spectrogram. The glycosylation peak reduced significantly in the tear sample collected from the amlodipine-treated group. Corresponding energy dispersive analysis showed the presence of sulphur, indicating protein leakage from the lacrimal gland in the induced group. The disappearance of sulphur from the treated group indicated its remedial effect. The flexible docking studies revealed a stronger binding mode of amlodipine with Interleukin-1ß (IL-1ß). The reduction in the intensity of the glycosylated peak and the restoration offering are probably due to suppression of IL-1ß. CONCLUSION: This study may be helpful in obtaining primary information for drug discovery to be effective against IL-1ß and proving tear fluid as a novel diagnostic biomarker.
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Anlodipino , Carragenina , Interleucina-1beta , Simulação de Acoplamento Molecular , Lágrimas , Lágrimas/metabolismo , Lágrimas/química , Anlodipino/administração & dosagem , Anlodipino/química , Animais , Coelhos , Glicosilação , Interleucina-1beta/metabolismo , Administração Oftálmica , MasculinoRESUMO
The study explores anticancer potential of telmisartan (TS) loaded lipid nanocarriers (TLNs) in glioma cells as a potential repurposing nanomodality along with estimation of drug availability at rat brain. Experimental TLNs were produced by previously reported method and characterized.In vitroanticancer efficacy of experimental TLNs was estimated by MTT, confocal microscopy, and FACs analysis in glioma cells. Plasma and brain pharmacokinetic (PK) parameters were also analysed by LCMS/MS. Spherical, nanosized, homogenous, unilamellar, TLNs were reported having desirable drug loading (9.5% ± 0.6%), negative zeta potential and sustained TS release tendency. FITC-TLNs were sufficiently internalized into U87MG cells line within 0.5 h incubation period. IC50for TLNs was considerably higher than free TS in the tested glioma cell lines. Further, TLNs induced superior apoptotic effect in U87MG cells than TS. PK (plasma/brain) data depicted higher AUC,Vss, MRT with lower Cltfor TLNs suggesting improved bioavailability,in vivoresidence and sustained drug availability than free TS administration. Docking studies rationalizedin vitro/in vivoresults as preferably higher binding affinity (docking score:12.4) was detected for TS with glioma proteins. Further,in vivostudies in glioma bearing xenograft model is underway for futuristic clinical validation of TLNs.
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Apoptose , Portadores de Fármacos , Glioma , Lipídeos , Nanopartículas , Telmisartan , Telmisartan/farmacocinética , Telmisartan/farmacologia , Telmisartan/química , Telmisartan/administração & dosagem , Glioma/tratamento farmacológico , Glioma/patologia , Glioma/metabolismo , Humanos , Animais , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Ratos , Nanopartículas/química , Lipídeos/química , Simulação de Acoplamento Molecular , Reposicionamento de Medicamentos , Masculino , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/administração & dosagem , Neoplasias Encefálicas/tratamento farmacológico , Neoplasias Encefálicas/patologia , Neoplasias Encefálicas/metabolismo , Liberação Controlada de FármacosRESUMO
The current study describes the efficacy of B. acutangula fruit extract in wound healing via incorporation within topical gels. B. acutangula fruit extract was produced by solvent extraction method. The bioactive extract was incorporated within Carbopol 940-based topical gels, which were applied topically over the excision and incision wounds. The change in healing process was observed till 20â days. The percentages of closure of excision wound area were 92.89 % and 93.43 %, when treated with topical herbal gels containing B. acutangula fruit extract of 5 % and 10 %, respectively. The tensile strengths of incision area in rats treated with topical herbal gels containing 5 % and 10 % methanol extract of B. acutangula fruits were found to be 25±5.12â g and 30±4.10â g, respectively. The wound healing activity of topical herbal gels containing B. acutangula fruit extract in rats was found to be significant when compared with that of the reference standard and untreated groups. In addition, in silico studies suggested about good skin permeability and binding to the proteins responsible for delaying wound healing. It can be concluded that this topical herbal gels containing B. acutangula fruit extract could be used clinically for the treatment of wounds.
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Frutas , Géis , Extratos Vegetais , Cicatrização , Animais , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/administração & dosagem , Cicatrização/efeitos dos fármacos , Frutas/química , Géis/química , Ratos , Administração Tópica , Ratos Wistar , Masculino , Pele/efeitos dos fármacos , Pele/metabolismo , Simulação por ComputadorRESUMO
Carboxylesterase enzymes convert a prodrug ramipril into the biologically active metabolite ramiprilat. It is prescribed for controlling ocular hypertension after oral administration. High concentrations of carboxylesterase enzymes in rectal and colon tissue can transform ramipril significantly to ramiprilat. Sustained rectal delivery of ramipril has been developed for intra-ocular pressure lowering effect using a normotensive rabbit model. Rectal suppositories have been formulated using a matrix base of HPMC K100-PEG 400-PEG 6000, incorporating varying amounts of Gelucire by the fusion moulding method. The presence of Gelucire in the suppository exhibited sustained structural relaxation-based release kinetics of RM compared to its absence. Intravenous and oral administration of ramipril has decreased IOP in the treated rabbit up to 90 and 360 min, respectively. Treated rabbits with suppositories have revealed decreased IOP for an extended period compared to the above. Formulation containing GEL 3% reduced intra-ocular pressure to 540 min, with the highest area under the decreased IOP curve. Compared to oral, the pharmacodynamic bioavailability of ramipril has been improved significantly using a sustained-release rectal suppository. A rectal suppository for sustained delivery of ramipril could be used to lower IOP significantly.
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Administração Retal , Preparações de Ação Retardada , Pressão Intraocular , Pró-Fármacos , Ramipril , Animais , Coelhos , Pressão Intraocular/efeitos dos fármacos , Pró-Fármacos/administração & dosagem , Pró-Fármacos/farmacocinética , Pró-Fármacos/farmacologia , Ramipril/administração & dosagem , Ramipril/farmacocinética , Ramipril/farmacologia , Supositórios , Masculino , Disponibilidade Biológica , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/farmacocinética , Anti-Hipertensivos/farmacologia , Lipídeos/química , Liberação Controlada de Fármacos , Administração Oral , PolietilenoglicóisRESUMO
Pharmaceutical grade sugars manufactured under Current Good Manufacturing Practice (cGMP) and complied with International Pharmaceutical Excipients Council (IPEC) quality standards, also contain a significant amount of nano-particulate impurities (NPIs). This review will focus on the origin of NPIs, the mechanism of their interference with Dynamic light scattering (DLS) and endotoxin tests, filtration technology to effectively reduce the NPIs, methodologies for analytical quantification of NPIs, guidance for setting the limits of threshold concentration and the overall impact of NPIs on the therapeutic activity, performance, stability of biopharmaceuticals and protein-based formulations. NPIs with an average particle size of 100 to 200 nm are present in sugars and are a combination of various chemicals such as dextrans (with the presence of ß-glucans), ash, inorganic metal salts, aromatic colorants, etc. These NPIs primarily originate from raw materials and cannot be removed during the sugar refinement process. While it is commonly believed that filtering the final formulation with a 0.22 µ sterilizing grade filter removes all microbes and particles, it is important to note that NPIs cannot be filtered using this standard sterile filtration technology. Exceeding the threshold limit of NPIs can have detrimental effects on formulations containing proteins, monoclonal Antibodies (mAbs), nucleic acids, and other biopharmaceuticals. NPIs and ß-glucans have a critical impact on the functionality and therapeutic activity of biomolecules and if present below the threshold limit of reaction, stability and shelf-life of biologics formulation will be greatly improved and the risk of immunogenic reactions must be significantly decreased.
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Bioelectronic medicine is a multidisciplinary field that combines molecular medicine, neurology, engineering, and computer science to design devices for diagnosing and treating diseases. The advancements in bioelectronic medicine can improve the precision and personalization of illness treatment. Bioelectronic medicine can produce, suppress, and measure electrical activity in excitable tissue. Bioelectronic devices modify specific neural circuits using electrons rather than pharmaceuticals and use bioelectronic processes to regulate the biological processes underlining various diseases. This promotes the potential to address the underlying causes of illnesses, reduce adverse effects, and lower costs compared to conventional medication. The current review presents different important aspects of bioelectronic medicines with recent advancements. The area of bioelectronic medicine has a lot of potential for treating diseases, enabling non-invasive therapeutic intervention by regulating brain impulses. Bioelectronic medicine uses electricity to control biological processes, treat illnesses, or regain lost capability. These new classes of medicines are designed by the technological developments in the detection and regulation of electrical signaling methods in the nervous system. Peripheral nervous system regulates a wide range of processes in chronic diseases; it involves implanting small devices onto specific peripheral nerves, which read and regulate the brain signaling patterns to achieve therapeutic effects specific to the signal capacity of a particular organ. The potential for bioelectronic medicine field is vast, as it investigates for treatment of various diseases, including rheumatoid arthritis, diabetes, hypertension, paralysis, chronic illnesses, blindness, etc.
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Background and Aim: Severe viral hemorrhagic fever (VHF) is caused by Marburg virus which is a member of the Filoviridae (filovirus) family. Many Marburg virus disease (MVD) outbreaks are reported in five decades. A major notable outbreak with substantial reported cases of infections and deaths was in 2022 in Uganda. The World Health Organisation (WHO) reported MVD outbreak in Ghana in July 2022 following the detection of two probable VHF patients there. Further, the virus was reported from two other African countries, the Equatorial Guinea (February 2023) and Tanzania (March 2023). There have been 35 deaths out of 40 reported cases in Equatorial Guinea, and six of the nine confirmed cases in Tanzania so far. Methods: Data particularly on the several MVD outbreaks as reported from the African countries were searched on various databases including the Pubmed, Scopus, and Web-of-science. Also, the primary data and reports from health agencies like the WHO and the Centers for Disease Control and Prevention CDC) were evaluated and the efficacy reviewed. Results: Chiroptera in general and bat species like Rousettus aegyptiacus and Hipposideros caffer in particular are natural reservoirs of the Marburg virus. MVD-infected nonhuman primate African fruit-bat and the MVD-infected humans pose significant risk in human infections. Cross-border viral transmission and its potential further international ramification concerns raise the risk of its rapid spread and a potential outbreak. Occurrence of MVD is becoming more frequent in Africa with higher case fatality rates. Effective prophylactic and therapeutic interventions to counter this deadly virus are suggested. Conclusion: In the face of the lack of effective therapeutics and preventives against MVD, supportive care is the only available option which contributes to the growing concern and disease severity. In view of the preventive approaches involving effective surveillance and monitoring system following the "One Health" model is extremely beneficial to ensure a healthy world for all, this article aims at emphasizing several MVD outbreaks, epidemiology, zoonosis of the virus, current treatment strategies, risk assessments, and the mitigation strategies against MVD.
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Effective treatment of vaginal infections with conventional antibiotics often faces challenges like unavoidable dose-related side effects with increased risk of bacterial resistance. The study aims to deliver linezolid through natural gum based mucoadhesive nano lipogel to improve therapeutic effectiveness against vaginal infections. The linezolid loaded nanoliposomes (LNLs) were developed by thin film hydration method and were characterized by FTIR, DSC, XRD, FESEM, particle size analysis, zeta potential, drug loading capacity, in vitro release study etc. Selected LNLs was loaded into suitable gel formulation containing Aegle marmelos gum (as the mucoadhesive agent) and evaluated for in vitro, in vivo potentiality. FTIR/DSC test confirmed absence of any major interaction between selected drug and excipients. XRD showed amorphization of the drug encapsulated in NLs. FESEM studies showed spherical LNLs having smooth surface. LNLs had nanosize (51.03 nm), negative surface charge (-25.7 mV), satisfied drug loading capacity (11.5 ± 0.7 %) with sustained drug release. The experimental LNLs loaded lipogel showed desired physico-chemical properties viz. viscosity (37000 cps), spreadability (6.5 gm.cmsec-1), mucoadhesion (21.9 gf) and 61.04 % release of drug across rabbit vaginal mucosal membrane. The nanolipo gel exhibited improved antimicrobial activity against E. coli and C. albicans with respect to the pure linezolid. A good correlation was observed in between in vitro drug release and ex vivo permeation. Improved pharmacokinetic parameters like AUC, AUMC, MRT, Vd was observed for experimental nanolipo gel Vs. marketed formulation. The experimental nanolipo gel could be explored further for futuristic clinical application.
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Aegle , Animais , Feminino , Coelhos , Linezolida , Aegle/química , Escherichia coli , Fenômenos Químicos , Administração CutâneaRESUMO
This study aimed to deliver a potential water-soluble antiviral drug (sofosbuvir) through optimized vesicular lipid nanocarriers (LNs) to the rat brain as a novel strategy against viral meningitis. A 23 factorial design approach was established to assess the effect of formulation composition and process variables on the physicochemical properties of the LNs. Sofosbuvir-loaded LNs (SLNs) were developed by lipid layer hydration method utilizing optimized parameters and evaluated for various in vitro characterizations like FTIR, DSC, XRD, FESEM, vesicle size, zeta potential, drug carrying capacity and drug release. Plasma and brain pharmacokinetic (PK) studies were conducted in Sprague-Dawley rats. FTIR data depicted the absence of any major interaction between the drug and the excipients. DSC revealed a sharp endothermic peak for the drug. XRD showed the amorphic nature of the SLNs. Optimized SLNs were spherical as depicted from FESEM with 42.43 nm size, -49.21 mV zeta potential, 8.31% drug loading and sustained drug release in vitro. Plasma/brain PK studies depicted significant improvement in key PK parameters, viz. AUC, AUMC, MRT, and Vd, compared to those for the free drug. A more than 3.5-fold increase in MRT was observed for optimized SLNs (11.2 h) in brain tissue compared to the free drug (3.7 h). Ex vivo hemolysis data confirmed the non-toxic nature of the SLNs to human red blood cells. In silico docking study further confirmed strong interaction between the drug and selected protein 4YXP (herpes simplex) with docking score of -7.5 and 7EWQ protein (mumps virus) with docking score of -7.3. The optimized SLNs may be taken for further in vivo studies to pave the way towards clinical translation.
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Background: Historically, a critical aetiological agent of health concern stays till eternity after its discovery, so shall it be with the COVID-19 outbreak. It has transformed human life to a 'new normal' with huge tolls on the social, psychological, intellectual and financial spheres. Aim: This perspective aimed to collate numerous reported COVID-19 vaccine-associated adverse events and the predisposing factors. It focussed on the efficacy of mix-n-match (cocktail) vaccines to effectively counter COVID-19 infection to facilitate future research and possible interventions. Material and Methods: Databases like Scopus, Pubmed and the Web-of-science were searched for published literature on 'adverse events associated with COVID-19 vaccine'. The reports and updates from health agencies like the WHO and CDC were also considered for the purpose. The details with respect to the adverse events associated with COVID-19 vaccination and the predisposing factors were compiled to obtain insights and suggest possible future directions in vaccine research. Results: India stood strong to manage its health resources in time and turned into a dominant global vaccine supplier at a time when healthcare infrastructure of many countries was still significantly challenged. Developing indigenous vaccines and the vaccination drive in India were its major achievements during the second and the subsequent COVID-19 waves. The fully indigenous Covaxin vaccine, primarily as an emergency intervention, was successfully rapidly launched. Similar such vaccines for emergency use were developed elsewhere as well. However, all of these reached the marketplace with a 'emergency use only' tag, without formal clinical trials and other associated formalities to validate and verify them as these would require much longer incubation time before they are available for human use. Discussion: Many adverse events associated with either the first or the second/booster vaccination doses were reported. Evidently, these associated adverse events were considered as 'usually rare' or were often underreported. Without the additional financial or ethical burden on the vaccine companies, fortunately, the Phase IV (human) clinical trials of their manufactured vaccines are occurring by default as the human population receives these under the tag 'emergency use'. Thus, focused and collaborative strategies to unveil the molecular mechanisms in vaccine-related adverse events in a time-bound manner are suggested. Conclusion: Reliable data particularly on the safety of children is lacking as majority of the current over-the-counter COVID-19 vaccines were for emergency use. Many of these were still in their Phase III and Phase IV trials. The need for a mutant-proof, next-gen COVID-19 vaccine in the face of vaccine-associated adverse events is opined.
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The world faces multiple public health emergencies simultaneously, such as COVID-19 and Monkeypox (mpox). mpox, from being a neglected disease, has emerged as a global threat that has spread to more than 100 nonendemic countries, even as COVID-19 has been spreading for more than 3 years now. The general mpox symptoms are similar to chickenpox and measles, thus leading to a possible misdiagnosis. This study aimed at facilitating a rapid and high-brevity mpox diagnosis. Reportedly, mpox circulates among particular groups, such as sexually promiscuous gay and bisexuals. Hence, selectively vaccinating, isolating, and treating them seems difficult due to the associated social stigma. Deep learning (DL) has great promise in image-based diagnosis and could help in error-free bulk diagnosis. The novelty proposed, the system adopted, and the methods and approaches are discussed in the article. The present work proposes the use of DL models for automated early mpox diagnosis. The performances of the proposed algorithms were evaluated using the data set available in public domain. The data set adopted for the study was meant for both training and testing, the details of which are elaborated. The performances of CNN, VGG19, ResNet 50, Inception v3, and Autoencoder algorithms were compared. It was concluded that CNN, VGG19, and Inception v3 could help in early detection of mpox skin lesions, and Inception v3 returned the best (96.56%) classification accuracy.
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Dental caries, periodontal disease, and endodontic disease are major public health concerns worldwide due to their impact on individuals' quality of life. The present problem of dental disorders is the removal of the infection caused by numerous microbes, particularly, bacteria (both aerobes and anaerobes). The most effective method for treating and managing dental diseases appears to be the use of antibiotics or other antimicrobials, which are incorporated in some drug delivery systems. However, due to their insufficient bioavailability, poor availability for gastrointestinal absorption, and pharmacokinetics after administration via the oral route, many pharmaceutical medicines or natural bioactive substances have limited efficacy. During past few decades, a range of polysaccharide-based systems have been widely investigated for dental dug delivery. The polysaccharide-based carrier materials made of chitosan, alginate, dextran, cellulose and other polysaccharides have recently been spotlighted on the recent advancements in preventing, treating and managing dental diseases. The objective of the current review article is to present a brief comprehensive overview of the recent advancements in polysaccharide-based dental drug delivery systems for the delivery of different antimicrobial drugs.
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Anti-Infecciosos , Quitosana , Cárie Dentária , Humanos , Alginatos , Celulose , Dextranos , Qualidade de Vida , Polissacarídeos/uso terapêutico , Sistemas de Liberação de MedicamentosRESUMO
Microbial fuel cells (MFCs) have attracted widespread interest due to their capability to generate power while treating wastewater. In the present investigation, rice mill wastewater (RMW) was treated in a dual-chamber MFC with a biological cathode (MFCB), in which anaerobic treatment was provided in the anode compartment, and aerobic treatment was enployed in the cathode compartment. The performance was compared with an identical MFC with an abiotic cathode (MFCA). During continuous operation, the hydraulic retention time (HRT) of the anode compartments of both MFCs was kept at 12â h. The maximum volumetric power density obtained in MFCB (379.53â mW/m3) was lower than MFCA (791.72â mW/m3). Similarly, the maximum open-circuit voltage (OCV) and operating voltages were 0.519 V and 0.170â V for MFCB, while for the MFCA, they were 0.774â V and 0.251â V, respectively. The internal resistance of MFCA was 372.34 Ω while the MFCB showed a higher internal resistance of 533.89 Ω. The linear sweep voltammetry and cyclic voltammetry also demonstrated high electrochemical activity in MFCA compared to MFCB. However, MFCB has shown a higher chemical oxygen demand (COD) removal efficiency (96.8%) than MFCA (88.4%) under steady-state conditions. Both anaerobic and aerobic degradation of organic substrates significantly reduced the COD of RMW. Furthermore, the absence of an expensive catalyst in the cathode substantially reduces the cost of the system. The electrical performance of the system can be enhanced by employing novel cathode material with surface modification.
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Fontes de Energia Bioelétrica , Oryza , Águas Residuárias , Anaerobiose , EletricidadeAssuntos
COVID-19 , Pandemias , Humanos , COVID-19/epidemiologia , Probabilidade , Estudos Longitudinais , Atenção à SaúdeRESUMO
The microbial fuel cell (MFC) is one of the sustainable technologies, which alongside treating wastewater, can generate electricity. However, its performance is limited by factors like methanogenesis where methanogens compete with the anode respiring bacteria for substrate, reducing the power output. Thus, sodium nitrate, which has been previously reported to target the hydrogenotrophic methanogens, was used as a methanogenic suppressor in this study. The performance of MFC with and without sodium nitrate was studied during the treatment of rice mill wastewater. A significantly higher power density and coulombic efficiency (CE) were noted in the MFC with sodium nitrate (MFCT) (271.26 mW/m3) as compared to the control MFC (MFCC) (107.95 mW/m3). Polarization studies showed lower internal resistance for the MFCT (330 Ω) as compared to MFCC (390 Ω). Linear sweep voltammetry and cyclic voltammetry indicated a higher electron discharge on the anode surface due to enhancement of electrogenic activity. Considerable reduction (76.8%) in specific methanogenic activity was also observed in anaerobic sewage sludge mixed with sodium nitrate compared to the activity of anaerobic sewage sludge without any treatment. Due to the inhibition of methanogens, a lower chemical oxygen demand (COD) and phenol removal efficiency were observed in MFCT as compared to MFCC. The COD balance study showed an increase in substrate conversion to electricity despite the increase in nitrate concentration. Therefore, selective inhibition of methanogenesis had been achieved with the addition of sodium nitrate, thus enhancing the power generation by MFCs.
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Fontes de Energia Bioelétrica , Oryza , Fontes de Energia Bioelétrica/microbiologia , Eletricidade , Eletrodos , Nitratos , Esgotos/microbiologia , Águas ResiduáriasRESUMO
Ceramic separators have recently been investigated as low-cost, robust, and sustainable separators for application in microbial fuel cells (MFC). In the present study, an attempt was made to develop a low-cost MFC employing a clayware ceramic separator modified with silica. The properties of separators with varying silica content (10%-40% w/w) were evaluated in terms of oxygen and proton diffusion. The membrane containing 30% silica exhibited improved performance compared to the unmodified membrane. Two identical MFCs, fabricated using ceramic separators with 30% silica content (MFCS-30) and without silica (MFCC), were operated at hydraulic retention time of 12 h with real rice mill wastewater with a chemical oxygen demand (COD) of 3,200 ± 50 mg/L. The maximum volumetric power density of 791.72 mW/m3 and coulombic efficiency of 35.77% was obtained in MFCS-30, which was 60.4% and 48.5%, respectively, higher than that of MFCC. The maximum COD and phenol removal efficiency of 76.2% and 58.2%, respectively, were obtained in MFCS-30. MFC fabricated with modified ceramic separator demonstrated higher power generation and pollutant removal. The presence of hygroscopic silica in the ceramic separator improved its performance in terms of hydration properties and proton transport.
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Fontes de Energia Bioelétrica , Oryza , Purificação da Água , Cerâmica , Eletricidade , Eletrodos , Dióxido de Silício , Águas ResiduáriasRESUMO
The crystallization technique has been established as a cost-effective and simple approach to improve the dissolution rate and oral bioavailability of poorly soluble drugs. This study was carried out to study the effect of some selected hydrophilic polymers such as methyl cellulose, hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol, and carboxymethyl cellulose on the crystal behavior and dissolution properties of celecoxib (CLX), a common nonsteroidal anti-inflammatory drug. Structural and spectral characteristics of crystallized CLX have been studied by Fourier transform infrared (FTIR) spectroscopy, diffraction scanning calorimetry (DSC), and X-ray diffraction (XRD) analysis. From FTIR and DSC analysis, no significant shifting of peaks or appearance of any new peaks (for polymers) were observed, which indicated the absence of any major interaction between drug and polymers as well as the absence of polymers in the final crystallized product of CLX. The XRD analysis showed a change in crystalline morphology to some extent. The dissolution rate of crystallized CLX in the presence of polymers (particularly with HPMC) was significantly improved compared with plain CLX. The improved dissolution profile of the experimental CLX crystal products could be an indication of improved bioavailability of CLX for better clinical outcome.
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Celecoxib/química , Inibidores de Ciclo-Oxigenase 2/química , Disponibilidade Biológica , Varredura Diferencial de Calorimetria , Cristalização , Cristalografia por Raios X , Portadores de Fármacos , Tamanho da Partícula , Polímeros/química , Solubilidade , Soluções , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Hydration behavior of hydrogel-based polymeric film possesses great importance in mucosal drug delivery. Modified Lag phase sigmoid model was used for the investigation of hydration of the film. Kaolin incorporated HPMC K100LVCR (HL) and K100M (HH) films containing dexamethasone as a model drug have been prepared for studying swelling kinetics. Swelling of HL and HH films was decreased with the gradual increase of kaolin content and HH of higher viscosity has shown higher value than HL matrix. Kaolin also inhibited the film erosion process. Mathematically modified lag phase sigmoid model demonstrated similarity of the predicted swelling content with the observed value. High R2 and small RMSE value confirmed the successful fitting of the modified lag phase sigmoid model to the experimental data of swelling content. τ value similar to the observed one was obtained. This modified model could be reliable enough for estimating hydration process in food grains, food packaging films etc.
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The immune system plays an important role in the prevention of infection and forms the first line of defense against pathogen attack. Delivering of antigen through mucosal route may elicit mucosal immune system as the mucosal surface is the most common site of pathogen entry. Mucosal immune system will be capable to counter pathogen at mucosal surface. Oral mucosal immunization opens the ways to deliver antigens at gut-associated lymphoid tissue. This can elicit both local and systemic immune response. Mucosal vaccines are economical, highly accessible, non parenteral delivery and capacity to produce mass immunization at the time of pandemics. To deliver antigens on the mucosal surface of the gastrointestinal tract, the immune system relies on specialized epithelial cell i.e. Microfold (M)-cell. An approach to exploit the targeting specific receptors on M-cell for entry of antigens has made a breakthrough in vaccine development. In this review, various strategies have been discussed for the possible entry of antigens through M-cells and an approach to increase the uptake and efficacy of vaccines for oral mucosal immunization.