Nanotechnology has significantly improved drug delivery and targeting in central nervous system diseases and neurodegenerative diseases. Intranasal drug delivery has emerged as a promising approach for enhancing therapeutic outcomes by leveraging the unique anatomical and physiological characteristics of the nasal cavity. This route offers several advantages, including rapid absorption, bypassing the blood-brain barrier for central nervous system targeting, and improved patient compliance. The highly vascularized nasal mucosa facilitates efficient systemic drug absorption, making it an attractive option for both local and systemic treatments. This article explores the principles of intranasal drug delivery, the influence of nasal anatomy on drug bioavailability, and advancements in formulation strategies to optimize efficacy. Additionally, it addresses current challenges, including mucociliary clearance and enzymatic degradation, as well as innovative solutions designed to enhance drug stability and absorption. Understanding the interplay between nasal anatomy and drug delivery mechanisms can pave the way for novel therapeutic interventions and enhance the effectiveness of intranasal medications in various clinical applications. It also highlights challenges in the nasal delivery of therapeutics.
The research work presents the microwave-assisted transesterification process to transform the Karanja oil into biodiesel. The different optimization and modelling techniques were compared and parameters were optimized to obtain the highest yield. Adaptive neuro-fuzzy inference System (ANFIS), Artificial Neural Network (ANN) and Response Surface Methodology (RSM) are assessed in the transesterification of Karanja oil esterified with methanol in the appearance of NaOH as a catalyst with microwave power. The investigation was carried out by considering the time, methanol/oil mole ratio, volume and catalyst concentration parameters and using Box Behnken design for experimentation. Statistical performance gauge showed Root mean square error (RMSE), coefficient of determination (R 2 ) adjusted R 2 , Sum of square error (SSE) and mean square error (MSE). A modified Domestic Microwave used for experimentation, which is functioning at 2450 MHz, the topmost power output of 700W attached with DC motor having 100 rpm for stirring action. The highest yield of 87.34% was extracted with optimized parameters of rection.
Cubosomes are bicontinuous cubic phase nanoparticles with a size range from 10-500 nm. They offer various advantages with some limitations at the production level, e.g., cubosomes have the feature to encapsulate a large amount of the drug due to its large internal area owing to cuboidal shape but limited in large scale production due to its high viscosity which is associated with the problem in homogenization. This nanoparticulate formulation is compatible for administration by various routes like oral, transdermal, topical, buccal, etc. The drug release mechanism from cubosomes was reported to be dependent on the partition coefficient and diffusion process. Compared with liposomes, cubosomes show many differences in various aspects like shape, size, ingredients, and mode of action. The main ingredients for the preparation of cubosomes include lipids, stabilizers, aqueous phase and therapeutic agents. Several methods have been reported for cubosomes, including the top-down method, the bottom-up method and the adopted coarse method. For the optimization of cubosomes, the key factors to be considered, which will affect the cubosomes characteristics include the concentration of lipid, temperature and pH. At present, many research groups are exploring the potential of cubosomes as biosensors and nanocarriers. Based on the latest reports and research, this review illuminates the structure of the cubosomes, mechanism of the drug release, different methods of preparation with factors affecting the cubosomes, application of cubosomes in different sectors, differences from the liposomes, and their advantages.
Accidents are inevitable, and situations of emergency can happen anytime, we cannot really ensure total safety but we can definitely make certain steps towards better precaution and safety of us and our loved ones. There are operations that are performed in distant areas such as fishing, mining, there are times when we enter into an accident or theft-prone areas.This work focuses on a tracking system as well as a heart monitoring system that is solely intended to provide security to the elderly, women, children, and remote workers by monitoring their pulse rate and ensuring that they never feel helpless when confronted with social challenges or in the event of an emergency. The pulse sensor continuously monitors pulse measurements, and an advanced system is intended to detect the location using a GPS receiver. The microcontroller Arduino Nano receives the feedback and sends it through text SMS to the registered phone number.
Vesicular systems have many advantages like prolonging the existence of the drug in the systemic circulation, minimizing the undesirable side-effects and helping the active moieties to reach their target sites using the carriers. However, the main drawback related to transdermal delivery is to cross stratum corneum, which can be overcome by the utilization of novel carrier systems e.g., transfersomes, which are ultra-deformable carrier systems composed of phospholipid (phosphatidylcholine) and edge activators (surfactants). Edge activators are responsible for the flexibility of the bilayer membranes of transfersomes. Different edge activators used in transfersomes include tween, span, bile salts (sodium cholate and sodium deoxycholate) and dipotassium glycyrrhizinate. These activators decrease the interfacial tension, thereby, increasing the deformability of the carrier system. Transfersomes can encapsulate both hydrophilic and hydrophobic drugs into a vesicular structure, which consists of one or more concentric bilayers. Due to the elastic nature of transfersomes, they can easily cross the natural physiological barriers i.e., skin and deliver the drug to its active site. The main benefit of using transfersomes as a carrier is the delivery of macromolecules through the skin by non-invasive route thereby increasing the patient’s compliance. The transfersomal formulations can be used in the treatment of ocular diseases, alopecia, vulvovaginal candidiasis, osteoporosis, atopic dermatitis, tumor, leishmaniasis. It is also used in the delivery of growth hormones, anaesthesia, insulin, proteins, and herbal drugs. This review also focuses on the patents and clinical studies for various transfersomal products.
Cancer a leading cause of human mortality worldwide is characterised by the unseemly growth of cellular mass and signalled through the enlargement of stress. Management of cancer treatment is still buried and has been recently alerting the need to discover a drug molecule with lesser side effects. The objective of the present study is to explore the anticancer activity and docking studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazole derivatives. The compounds were evaluated for in-vitro anticancer activity under the drug discovery program of National Cancer Institute (NCI), USA. Only seven compounds were selected and screened for anticancer activity at a single high dose (10-5 M) using NCI 60 cancer cell lines. Among all the selected compounds, 4b and 4i exhibited significant anticancer activity against Leukemia cell lines. Molecular docking studies for the 5-phenyl-1-(5-substituted phenylisoxazol-3-yl)-1H-tetrazole analogues was done by Schrodinger software. Docking results stated that the compounds 4b and 4i has good dock score among the other derivatives which shows good binding efficiency towards receptor.
Currently the pharmaceutical scientists has exploring the possibilities of intranasal delivery as an alternative to other routes in the view of increasing number of reports related to problems associated with oral, parenteral and rectal routes for therapeutic delivery of different drugs.The present attemptwasfocused on nasal drug delivery systems fordifferent therapeutic potentials i.e. local, systemic, CNS delivery and vaccine delivery. The factors which affect the absorption of drugs or biomolecules through the nasal mucosa including biological, device-related and formulation factors are also discussed.This review may provide a complete and deep insight in relation to the nanotechnology based delivery systems for intranasal administration. A comparative study of conventional and novel delivery systems with respect to their advantages and shortcoming allows the in-depth information over the advancement of nasal delivery systems for different therapeutic purposes. The emphasis on current challenges and the possible solutions against them makes this attempt valuable for the researchers working on this platform.
Context: The selection of excipients and preformulation strategy plays a vital role for the development of nanoemulsion, due to anatomical and physiological challenges posed by nasal cavity. Objective: This attempt is focused on the selection and optimization of excipients for the development of a nanoemulsion system for intranasal delivery. Materials and methods: Excipients were selected on the basis of solubility of active drug, compatibility interactions and nasal irritancy. Surfactant and co-surfactant combination and their ratio were finalized on the basis of nanoemulsion region obtained from constructed phase diagrams with Capmul MCM as oil phase. A validated cut and weigh method was employed for the optimization of different phase diagrams with respect to nanoemulsion region. Results and discussion: The solubility of drug in Capmul MCM, Labrasol, and Transcutol-P was found to be superior with numeric values of 79.50 +/- 1.68 mg/ml, 51.10 +/- 1.39 mg/ml, and 36.60 +/- 0.85 mg/ml, respectively. On the basis of phase diagram analysis, Labrasol and Transcutol-P in 3: 1 ratio provides greater nanoemulsion region of 65.28 +/- 0.18%. The validation of cut and weigh method revealed that there was no significant statistical difference (P > 0.05) with a % RSD value of 2.38 for intersheet variation. Conclusion: The results of validation studies for cut and weigh method suggests that it can be effectively used as an optimization method for the selection of nanoemulsion composition.
Objective A novel multiparticulate system for the gastro-mucoadhesive delivery of ciprofloxacin HCl (CFN) was developed with the help of ion-exchange resin to deal with urinary tract (UT) infections effectively. Materials and methods An optimized complex (resinate) of CFN with sodium polystyrene sulfonate USP resin was prepared and entrapped within microbeads of sodium alginate and pectin. The developed systems were evaluated for drug entrapment efficiency, percentage of mucoadhesion and in vitro release patterns in simulated gastric fluid (pH 1.2). Results and discussion The interaction of the resin complex and polycation via alginate was consequently supported the formation of polyelectrolyte complex membrane. The in vitro drug release studies demonstrate that formulation without drug-resin complex (NRB) released the drug more swiftly than formulation containing drug-resin complex (DRC). This controlled release pattern of drug, resin complex containing microbeads was owed to complexation between drug and resin. Conclusion Preliminary results from the study suggested that this drug-resin complex-entrapped microbeads can be used to incorporate other antibiotic drugs and could be effective against UT infection. Such developed formulation could be subjected to in vivo studies in future in order to prove their efficacy for such type of infections.
A simple and sensitive UV-spectrophotometric method was developed and validated for the determination of hydrochloride salt of fluoxetine in bulk form. The validation of method as a stability indicating method was based on the forced degradation reactions in acidic, basic, oxidative, thermal and photolytic conditions. A linear relationship with a correlation coefficient (R2) value of 0.999 was found between the absorbance values and related concentrations in the range of 2–24 μg/ml. The detection limit and quantitation limit were found to be 0.53 μg/ml and 1.59 μg/ml, respectively. The % recoveries were found to be 99.77–99.92 with corresponding low % RSD values which indicates the high accuracy level of developed analytical method. Under stressed acidic and basic conditions, the extent of degradation was found to be 28.46±0.425% and 22.73±0.507%, respectively. Under stressed oxidative conditions, the extent of degradation was reduced to 17.84±0.276% whereas the thermal degradation was further lowered to an extent of 9.0±0.699%. In case of photolytic stressed conditions, negligible degradation (0.71±0.157%) was observed. The overall results of forced degradation studies suggest that the developed method could be successfully adopted as a stability indicating method for the estimation of fluoxetine hydrochloride.
Helicobacter pylori infection remains challenging as it mainly colonized beneath the deep gastric mucosa and adheres to epithelial cells of the stomach. Concanavalin-A (Con-A)-conjugated gastro-retentive poly (lactic-co-glycolic acid) (PLGA) nanoparticles of acetohydroxamic acid (AHA) and clarithromycin (CLR) were prepared and evaluated under in vitro conditions. Solvent evaporation method was employed for preparation of nanoparticles and characterized for particle size distribution, surface morphology, percent drug entrapment, and in vitro drug release in simulated gastric fluid. Optimized nanoparticles were conjugated with Con-A and further characterized for Con-A conjugation efficiency and mucoadhesion and tested for in vitro anti-H. pylori activity. The conjugation with Con-A further sustained the drug release over a period of 8 h when compared to non-conjugated nanoparticles of AHA and CLR. In vitro anti H. pylori study confirmed that Con-A-conjugated nanoparticles containing both drugs, i.e., CLR and AHA, had shown maximum zone of inhibition compared to other formulations. In a nut shell, results suggest that the developed systems could be used for better therapeutic activity against H. pylori infection.
This study is investigate the response of conventional steel reinforced concrete, artificial fiber reinforced concrete(FRP POLYPROPYLENE) and natural fiber(COCONUT FIBER) reinforced engineered cementitious composites members on their flexural loaddeformation behavior, compressive strength and behavior of concrete. The behavior of flexural loaddeformation and compressive strength of conventional reinforced concrete member are briefly reviewed and compared with fiber reinforced engineered cementitious composites .Compatible deformations of reinforcement and matrix leads to low interfacial bond stress and prevent the composite disintegration by bond splitting and lower spalling. Furthermore flexural strength as well as crack deformation and widths in fiber reinforced engineered cementitious composites members are found effectively independent of interfacial bond properties due to the tensile deformation characteristics of the compendious matrix. We can study the basic mechanical properties and behavior of different materials under embedded concrete. And find out that artificial made fiber are more capable of bearing both flexural and compression. By using this higher bond matrix we can use as an highly engineer made material to resist deformation and crack formation and propagation under high load such as load caused by heavy machineries such as milling, shaping machine and reciprocating compressors.
Context: Herpes viruses cause threatening infections in humans and stand second as causative agents for most human viral diseases, after influenza and cold viruses. Objective: A novel multiparticulate delivery system for acyclovir (ACV), based on ion-exchange resin, was developed to achieve a gastro-mucoadhesive effect in order to effectively combat the herpes simplex virus. Materials and methods: A combination of ACV and cholestyramine resin was optimized and further entrapped within sodium alginate and Carbopol microbeads. The developed systems were evaluated for drug entrapment efficiency (DEE), percentage of mucoadhesion, and in vitro release characteristics in simulated gastric fluid (SGF, pH 1.2). Results: With the aid of scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR), the interaction of the resinate and polycations with alginate has been revealed, which consequently supports the formation of the membrane by the polyelectrolyte complex. The in vitro drug release studies demonstrate that formulations without the drug-resin complex (DRC) released the drug more rapidly than formulations containing DRC, which released the drug in a controlled manner, due the formation of a complex between drug and resin. Discussion and conclusion: Preliminary results from this study suggest that these DRC-entrapped microbeads may be used to incorporate other antiviral drugs and could be effective against infections caused by herpes viruses. Such formulations developed could be subjected to in vivo studies in future, in order to prove complete clearance of herpes infections.
The main aim of this work is to develop and thoroughly evaluate resin-based multiparticles of repaglinide for effective management of type-2 diabetes mellitus. Repaglinide was complexed with cholestyramine resin; later the resin complexed drug was encapsulated in ethylcellulose microspheres. The microspheres were characterized for micromeritic properties, SEM analysis, entrapment efficiency, percentage yield, IR spectroscopy, buoyancy behaviour and in vitro drug release in simulated gastric fluid. Microparticles showed regular shape and spherical morphology with entrapment efficiency in the range 51-69%. Differential scanning calorimetry confirmed that there was no chemical interaction between the polymer and the drug. Resin-based microspheres showed good buoyancy behaviour (P < 0.05) due to the presence of bicarbonate ions and sustained release compared to plain drug microspheres (P < 0.05). Finally, the effectiveness of the formulations was evaluated in vivo for blood glucose lowering effect in both normal and streptozotocin-induced diabetic rats. Blood glucose lowering effect induced in diabetic rats by the repaglinide- loaded microspheres was significantly greater (P < 0.05) and prolonged (∼8 h) compared to plain drug microspheres. In a nutshell, floating microspheres containing drug resin complex were able to sustain the drug release in an effective manner for prolonged periods of time and proven in vivo effectiveness by reducing blood glucose level for a longer duration.
Context: In recent years, nanotechnology-based delivery systems have gained interest to overcome the problems of restricted absorption of therapeutic agents from the nasal cavity, depending upon the physicochemical properties of the drug and physiological properties of the human nose.Objective: The well-tolerated and non-invasive nasal drug delivery when combined with the nanotechnology-based novel formulations and carriers, opens the way for the effective systemic and brain targeting delivery of various therapeutic agents. To accomplish competent drug delivery, it is imperative to recognize the interactions among the nanomaterials and the nasal biological environment, targeting cell-surface receptors, drug release, multiple drug administration, stability of therapeutic agents and molecular mechanisms of cell signaling involved in patho-biology of the disease under consideration.Methods: Quite a few systems have been successfully formulated using nanomaterials for intranasal (IN) delivery. Carbon nanotubes (CNTs), chitosan, polylactic-co-glycolic acid (PLGA) and PLGA-based nanosystems have also been studied in vitro and in vivo for the delivery of several therapeutic agents which shown promising concentrations in the brain after nasal administration.Results and conclusion: The use of nanomaterials including peptide-based nanotubes and nanogels (NGs) for vaccine delivery via nasal route is a new approach to control the disease progression. In this review, the recent developments in nanotechnology utilized for nasal drug delivery have been discussed.
Cyclodextrins are capable to configure as a host-guest complexes in the company of hydrophobic molecules due to their emblematic nature imparted by their structural arrangement. The aim of present study is based on the application of in-silico tool for the selection of NSAID to develop novel drug delivery systems using beta-Cyclodextrin. An understanding of the structural and binding properties of cyclodextrin with NSAIDs reveals the suitability of the combination for drug delivery purpose. Among various NSAIDs, Zomepirac containing -OH and -CO group demonstrated maximum moldock score accompanied by highest re-ranks score. Naproxen showed lowest score with no H-bond interactions with the cyclodextrin. The binding information obtained from the present studies can be mapped which will be helpful in the selection of polymers for the formulation of appropriate NSAID. The results of the present study may provide a new approach to select the polymers for the formulation of different therapeutic agents to achieve better pharmacological activity with minimal consequences of toxicity.
Nasal cavity has used as alternative route for the drugs with poor water solubility, susceptible to acidic or enzymatic degradation and hepatic metabolism. The objective of the present study was to improve solubility of sertraline hydrochloride (STH), formulate microemulsions containing STH to accomplish rapid onset of action and to bypass the first-pass metabolism. A microemulsion system with Capmul MCM as oil phase, Labrasol as surfactant and Transcutol P as cosurfactant was developed for intranasal delivery of STH. Phase behaviour and solubilization capacity of the developed microemulsion system were characterized and STH microemulsions (SME) were prepared by titration method and evaluated for globule size, drug content, nasal ciliotoxicity, percentage transmittance, pH and viscosity. invitro studies for nasal absorption were carried out on goat nasal mucosa. The drug shows a high solubility of 117 mg/ml in a microemulsion containing 22.2% Capmul MCM, 44.5% (w/w) surfactant/cosurfactant (Labrasol: Transcutol P at 2:1) and 33.3% H2O. In invitro studies the nasal absorption was found to be 66.07±0.78% from SME2. These results indicate that intranasal microemulsion of STH may be beneficial for the treatment of depression.