ABSTRACT
BACKGROUND: Estimation of the drug and development of the method is a critical aspect of formulation development and a critical factor for analytical scientists. Gefitinib is a poorly soluble anticancer drug. OBJECTIVE: The present research focuses on the topic of the development of innovative quality by design methods for the estimation of gefitinib (GF) from bulk, pharmaceutical tablet formulation, and complex nanoformulations. METHODS: To simplify the estimation of poorly soluble drugs such as GF, response surface methodology (RSM) was adopted with effective leverages to obtain precise computation design space using the Box-Behnken design (BBD) model. The major three mixed-effect independent factors (percentage of buffer, pH of buffer, and flow rate) were screened with three prominent dependent responses (viz., theoretical plate, retention time, and tailing factor) selected for optimal analysis. Furthermore, co-processed steps were employed for the estimation of the analyte from the complex formulation. RESULTS: The RP-HPLC method uses the quality by design (QbD) approach can effectively estimate the analyte concentration of less than 4.5 min. The developed method was economically robust and sensitive and shows a relative standard deviation (RSD, %) of less than 2% for all the selected validation parameters. The estimated design space suggests the highest desirability (R2-0.998) at 60% of buffer in the mobile phase, pH 4.25, and flow rate of 0.7 mL/min. CONCLUSIONS: The QbD approach was used to design and develop the method by understanding the interaction between dependent and independent variables to get the optimum values. The developed method was validated successfully and can be useful for formulation scientists to estimate drug concentration and drug release profiles from complex nanoformulations. HIGHLIGHTS: The analytical approach was designed and quantified using a quality-by-design approach to make the RP-HPLC method more robust and efficient for the estimation of analytes from complex nanoformulations. The method is also useful to eliminate the interfering molecule during estimation by employing co-processing steps. The developed method saves time and cost of solvent and employs QbD as a requirement of recent regulatory concern.
Subject(s)
Gefitinib , Tablets , Chromatography, High Pressure Liquid/methods , Gefitinib/analysis , Gefitinib/chemistry , Antineoplastic Agents/analysis , Antineoplastic Agents/chemistry , Nanoparticles/chemistry , Drug Compounding/methods , Hydrogen-Ion Concentration , Chromatography, Reverse-Phase/methodsABSTRACT
Nanotechnology is an emerging applied science delivering crucial human interventions. Biogenic nanoparticles produced from natural sources have received attraction in recent times due to their positive attributes in both health and the environment. It is possible to produce nanoparticles using various microorganisms, plants, and marine sources. The bioreduction mechanism is generally employed for intra/extracellular synthesis of biogenic nanoparticles. Various biogenic sources have tremendous bioreduction potential, and capping agents impart stability. The obtained nanoparticles are typically characterized by conventional physical and chemical analysis techniques. Various process parameters, such as sources, ions, and temperature incubation periods, affect the production process. Unit operations such as filtration, purification, and drying play a role in the scale-up setup. Biogenic nanoparticles have extensive biomedical and healthcare applications. In this review, we summarized various sources, synthetic processes, and biomedical applications of metal nanoparticles produced by biogenic synthesis. We highlighted some of the patented inventions and their applications. The applications range from drug delivery to biosensing in various therapeutics and diagnostics. Although biogenic nanoparticles appear to be superior to their counterparts, the molecular mechanism degradation pathways, kinetics, and biodistribution are often missing in the published literature, and scientists should focus more on these aspects to move them from the bench side to clinics.
ABSTRACT
The surface drying process is an important technology in the pharmaceutical, biomedical, and food industries. The final stage of formulation development (i.e., the drying process) faces several challenges, and overall mastering depends on the end step. The advent of new emerging technologies paved the way for commercialization. Thin film freezing (TFF) is a new emerging freeze-drying technique available for various treatment modalities in drug delivery. TFF has now been used for the commercialization of pharmaceuticals, food, and biopharmaceutical products. The present review highlights the fundamentals of TFF along with modulated techniques used for drying pharmaceuticals and biopharmaceuticals. Furthermore, we have covered various therapeutic applications of TFF technology in the development of nanoformulations, dry powder for inhalations and vaccines. TFF holds promise in delivering therapeutics for lung diseases such as fungal infection, bacterial infection, lung dysfunction, and pneumonia.
ABSTRACT
The research study reflects the development of novel voriconazole (VCZ) loaded nanoparticles (NPs) for prolonged delivery for the management of ocular diseases. The in situ ophthalmic gel was prepared by incorporating NPs into carboxymethyl chitosan (CMCh) and poloxamer. The central composite design was used to optimize the process for the preparation of nanoparticles by the o/w solvent evaporation method. The developed nanoparticles were evaluated for the encapsulation efficiency (89.6 ± 1.2%), particle size (219.3 ± 1.8 nm), polydispersity index (PDI, 0.1), zeta potential (- 21.1 ± 1.12 mV), saturation solubility, DSC study, and drug release. The etherification process grafts carboxyl surface functional groups, on chitosan, and was confirmed by FTIR and NMR studies. The developed CMCh-poloxamer based gelling system was found to be clear and transparent with gelation temperature varying from 33 to 40 °C. The nanoparticle-loaded gel containing CMCh demonstrated enhanced antifungal activity against Candida albicans. The optimized batch containing CMCh showed improved mucoadhesion by 2.86-fold compared to VCZ nanosuspension. The drug release was prolonged up to 8 h with an ex vivo study suggesting the enhanced permeation across goat cornea estimated via fluorescent microscope. The hen's egg chorioallantoic membrane study revealed that the formulation was non-irritant and tolerated by the chorioallantoic membrane. The present study concludes that the VCZ loaded nanoparticulate in situ ophthalmic gel using CMCh may act as a potential alternative for traditional eye drops.
Subject(s)
Chitosan , Nanoparticles , Animals , Female , Poloxamer/chemistry , Chitosan/chemistry , Voriconazole , Chickens , Nanoparticles/chemistry , Gels/chemistry , Particle Size , Colloids , Drug Carriers/chemistryABSTRACT
Lung cancer (LC) is heading up as a substantial cause of mortality worldwide. Despite enormous progress in cancer management, LC remains a crucial problem for oncologists due to the lack of early diagnosis and precise treatment. In this context, numerous early diagnosis and treatment approaches for LC at the cellular level have been developed using advanced nanomaterials in the last decades. Amongst this, graphene quantum dots (GQDs) as a novel fluorescent material overwhelmed the horizons of materials science and biomedical fields due to their multifunctional attributes. Considering the complex nature of LC, emerging diagnostic and therapeutic (Theranostics) strategies using GQDs proved to be an effective way for the current practice in LC. In this line, we have abridged various approaches used in the LC theranostics using GQDs and its surface-engineered motif. The admirable photophysical attributes of GQDs realised in photolytic therapy (PLT), hyperthermia therapy (HTT), and drug delivery have been discussed. Furthermore, we have engrossed the impasse and its effects on the use of GQDs in cancer treatments from cellular level (in vivo-in vitro) to clinical. Inclusively, this review will be an embodiment for the scientific fraternity to design and magnify their view for the theranostic application of GQDs in LC treatment.
Subject(s)
Graphite , Lung Neoplasms , Quantum Dots , Drug Delivery Systems , Humans , Lung Neoplasms/diagnosis , Lung Neoplasms/drug therapy , Precision MedicineABSTRACT
Graphene, graphene oxide (GO) and graphene quantum dots (GQDs) are expected to play a vital role in the diagnosis of severe ailments. Computer-based simulation approaches are helpful for understanding theoretical tools prior to experimental investigation. These theoretical tools still have a high computational requirement. Thus, more efficient algorithms are required to perform studies on even larger systems. The present review highlights the recent advancement in structural confinement using computer simulation approaches along with biosensory applications of graphene-based materials. The computer simulation approaches help to identify the interaction between interacting molecules and sensing elements like graphene sheets. The simulation approach reduces the wet-lab experiment time and helps to predict the interaction and interacting environment. The experimental investigation can be tuned at a molecular level easily to predict small changes in structural configuration. Here, the molecular simulation study could be useful as an alternative to actual wet experimental approaches. The sensing ability of graphene-based materials is a result of interactions like hydrogen bonding, base-base interaction, and base-to-pi interaction to name a few. These interactions help in designing and engineering a substrate for sensing of various biomolecules.
ABSTRACT
Graphene quantum dots (GQDs), impressive materials with enormous future potential, are reviewed from their inception, including different precursors. Considering the increasing burden of industrial and ecological bio-waste, there is an urgency to develop techniques which will convert biowaste into active moieties of interest. Amongst the various materials explored, we selectively highlight the use of potential carbon containing bioprecursors (e.g. plant-based, amino acids, carbohydrates), and industrial waste and its conversion into GQDs with negligible use of chemicals. This review focuses on the effects of different processing parameters that affect the properties of GQDs, including the surface functionalization, paradigmatic characterization, toxicity and biocompatibility issues of bioprecursor derived GQDs. This review also examines current challenges and s the ongoing exploration of potential bioprecursors for ecofriendly GQD synthesis for future applications. This review sheds further light on the electronic and optical properties of GQDs along with the effects of doping on the same. This review may aid in future design approaches and applications of GQDs in the biomedical and materials design fields.
ABSTRACT
The major objective of the present investigation was to assess the targeting potential of a designed system for breast cancer at metastatic phases with imaging ability. In a nutshell, we have developed surface-engineered graphene oxide (GO) nanosheets by covalent linking with amine-functionalized iron oxide nanoparticles (IONPs) (GOIOIs). Gefitinib (Gf) was selected as a model drug and entrapped in between exfoliated GO sheets (GOIGF) via π-π* stacking before functionalization with IONPs. Preliminary characterization of GO, IONPs, GOIOI, and GOIGF was performed using UV-visible and Fourier transform infrared spectroscopy. Scanning and transmission electron microscopy studies confirmed successful surface engineering of GO with IONPs. The in vitro drug release study demonstrated sustained release of Gf. The magnetic behavior of IONPs and GOIOI demonstrated a sigmoidal-shaped hysteresis loop with superparamagnetic properties. The in vitro cell cytotoxicity assay was carried out on MDA-MB-231 breast cancer adenocarcinoma cell lines. The cell cytotoxicity assay showed 61.18% inhibition of cell growth with 30 ppm concentration containing 64% of the drug, whereas 100% of the pure drug revealed only 56% of inhibition. In the near future, GOIOI could be tailored further for theranostic research, especially for metastatic cancers. Graphical abstract.
Subject(s)
Amines , Antineoplastic Agents , Ferric Compounds , Gefitinib , Graphite , Methylamines , Nanoparticles , Amines/administration & dosage , Amines/chemistry , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Survival/drug effects , Drug Liberation , Erythrocytes/drug effects , Ferric Compounds/administration & dosage , Ferric Compounds/chemistry , Gefitinib/administration & dosage , Gefitinib/chemistry , Graphite/administration & dosage , Graphite/chemistry , Hemolysis/drug effects , Humans , Magnetic Phenomena , Methylamines/administration & dosage , Methylamines/chemistry , Nanoparticles/administration & dosage , Nanoparticles/chemistry , Neoplasms/drug therapy , Neoplasms/pathologyABSTRACT
Surface plasmon resonance (SPR) offers exceptional advantages such as label-free, in-situ and real-time measurement ability that facilitates the study of molecular or chemical binding events. Besides, SPR lacks in the detection of various binding events, particularly involving low molecular weight molecules. This drawback ultimately resulted in the development of several sensitivity enhancement methodologies and their application in the various area. Among graphene materials, graphene-based nanocomposites stands out owing to its significant properties such as strong adsorption of molecules, signal amplification by optical, high carrier mobility, electronic bridging, ease of fabrication and therefore, have established as an important sensitivity enhancement substrate for SPR. Also, graphene-based nanocomposites could amplify the signal generated by plasmon material and increase the sensitivity of molecular detection up to femto to atto molar level. This review focuses on the current important developments made in the potential research avenue of SPR and fiber optics based SPR for chemical and biological sensing. Latest trends and challenges in engineering and applications of graphene-based nanocomposites enhanced sensors for detecting minute and low concentration biological and chemical analytes are reviewed comprehensively. This review may aid in futuristic designing approaches and application of grapheneous sensor platforms for sensitive plasmonic nano-sensors.
Subject(s)
Biosensing Techniques , Graphite/chemistry , Nanocomposites/chemistry , Surface Plasmon Resonance , Adsorption , Fiber Optic TechnologyABSTRACT
Present investigation deals with, tacrolimus eluting, self-expandable, biodegradable stent fabricated by solvent casting method. The design was based on shape memory polymers, which possess the ability to memorize temporary shape that can substantially differ from their initial permanent shape. A set of biodegradable polymers blend was used such as poly-lactic acid (PLA) and poly-l-glycolic acid (PLGA) to study the shape memory effect of polymer. The prepared stent was assessed for various parameters like Scanning Electron Microscopy (SEM), In-vitro and Ex vivo expansion, Drug content, In-vitro drug release, Haemocompatibility, Differential Scanning Calorimetry (DSC), Fourier Transform Infrared spectroscopy (FTIR), and Textural Characterization.
Subject(s)
Absorption, Physicochemical , Drug-Eluting Stents , Polymers/chemistry , Animals , Cell Survival/drug effects , Goats , Human Umbilical Vein Endothelial Cells/cytology , Human Umbilical Vein Endothelial Cells/drug effects , Humans , Mechanical Phenomena , Platelet Adhesiveness/drug effectsABSTRACT
The present work deals with the design and process optimization for preparation of lactoferrin nanoparticles as carrier for delivery of curcumin (CLf-NPs) using quality by design (QbD) approach. Desolvation technique was selected for preparation of Lf-NPs. The concept of QbD was followed in stepwise manner including risk analysis FMEA methodology. Plackett-Burman screening design employing eight factors and two levels was selected for screening study and custom design was selected for further analysis. Curcumin was used as model polyphenol for assessing the encapsulating efficiency of Lf-NPs.
Subject(s)
Curcumin , Drug Delivery Systems , Lactoferrin , Nanoparticles/chemistry , Curcumin/chemistry , Curcumin/pharmacology , HeLa Cells , Humans , Lactoferrin/chemistry , Lactoferrin/pharmacologyABSTRACT
The present investigation deals with synthesis of graphene oxide (GO) and fabrication of GO-based hybrid nanocomposites (Ncs). Synthesized GO and Ncs were primarily confirmed by UV visible and Fourier transform infrared (FT-IR) spectroscopy. Fabricated Ncs showed potential antimicrobial activity against Gram-positive and Gram-negative bacterial strains. Surface morphology, Elemental analysis, and FTIR imaging analysis were carried out to confirm Ncs formation. The Ncs were impregnated into the pullulan polymeric layer-by-layer (LbL) ultrathin film by using novel spin-coating approach. Mechanical properties were determined using Brookfield texture analyzer, and percentage moisture content confirmed the physicochemical stability of LbL film.