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Lung cancer has become the leading cause of cancer‐related deaths, surpassing all other forms of cancer. Among lung cancers, non‐small cell lung cancer (NSCLC) accounts for approximately 85% of cases. The use of tobacco, genetic traits, and radiation exposure are amongst the major reasons of lung cancer. The ongoing research in the medical field has considered the efficacy of nanocarriers in targeting various cancer cells. Among several biomaterials, lipid‐based nanocarriers have gained special attention due to their excellent compatibility, improved targeting efficacy, and encapsulation ability of diverse therapeutic agents. Phospholipids are naturally occurring amphiphilic moieties found in all living creatures. The presence of phospholipids in biomembrane aids the permeability of phospholipid‐based drug carrier. It can also facilitate targeting of therapeutic agents to cancer microenvironment without degrading the encapsulated drug. Phospholipids can be employed to develop conjugated nanocarriers and vesicular nanoformulation that can result in prolonged circulatory half‐life and controlled release of drugs. Phospholipids are also suitable biomaterials to attach a ligand for tissue‐specific targeting. Recent researches have reported effective targeting of chemotherapeutic agents, genes, and vaccines through phospholipid‐based nanocarriers to lung cancer cells. This review focuses on the rationality and applications of phospholipid‐based nanocarriers in lung cancer therapy. [ABSTRACT FROM AUTHOR]

The aim of this study was to develop and evaluate the transdermal patch formulations of nifedipine. The patch formulations containing nifedipine were prepared and optimized with different ratios of vinyl and cellulose-derived polymers, drug contents, and permeation enhancers. Among the various formulations, the patch formulation containing a 1:5 ratio of ethyl cellulose and polyvinyl pyrrolidone was selected for ex vivo pharmacokinetic study based on in vitro permeation studies using stratum corneum of the pig's skin. The cumulative percentage release after the transdermal administration of the optimized patch formulation was 71.43%, and the plasma concentration of nifedipine was maintained for 16 hrs. The physicochemical evaluation study including flatness, thickness, moisture content and uptake, drug content in vitro release, and ex vivo permeation indicated satisfactory results. The formulation batch with clove oil as a penetration enhancer has shown better ex vivo permeation as compared to the formulations without enhancers and another synthetic enhancer. These results suggest that the optimized patch formulation Q3 could be further developed for clinical applications, providing the therapeutic plasma level of nifedipine over an extended period. Hence analyzing the results of the evaluation tests, in vitro and ex vivo data on the preparation and optimization of nifedipine-loaded transdermal patch, it can be concluded that the formulation shows its feasibility as an effective transdermal delivery system for nifedipine. [ABSTRACT FROM AUTHOR]

The present work was designed to investigate the effect of maceration, ultra-sound, and microwave-assisted extraction on free, esterified, and bound phenolics of Tulaipanji rice (Oryza sativa L.) flour. Antioxidant activity was measured by DPPH, ABTS, SOD, and reducing power assays. HPTLC analysis was performed for identification and quantification of phenolics in different extracts. Total phenolic (TPC) and total flavonoid contents (TFC) were found significantly high (p < 0.05) in microwave-assisted extraction of bound phenolics compared with other methods. Microwave-assisted extracts showed highest DPPH radicals, ABTS radicals, SOD, and reducing power activity. Further, Pearson's correlation study exhibited a significant positive correlation within % yield, TPC, and TFC. Significant negative correlation was found within % yield, TPC, TFC, and antioxidant activity. The study found that extractive value, antioxidant activity, and phenolic contents varied with the extraction methods. Microwave-assisted extraction technique showed the best performance for extraction as compared to other methods. [ABSTRACT FROM AUTHOR]

Silver nanoparticles (Ag NPs) via green synthesis using medicinal plants have been widely used in natural product research due to the economical and eco‐friendly properties of NPs. The plant‐derived Ag NPs biosynthesis comprises the interaction between silver nitrate (precursor) and bioactive components of plant extract (reducing agents). In this work, Ag NPs were biosynthesized using Osbeckia stellata leaves aqueous extract. Characterization of Ag NPs was done by using ultraviolet–visible absorption (UV–Vis) spectroscopy, dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), X‐ray powder diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and energy‐dispersive X‐ray analysis (EDX). Further, antioxidant, antidiabetic, cytotoxicity, and antimicrobial activities were evaluated to establish the pharmacological properties of Ag NPs. UV–Vis spectroscopy and FTIR showed an absorption peak of Ag NPs due to the surface plasmonic resonance. In contrast, the particle size in the nanometer range was analyzed by XRD and DLS. The size of the particle was confirmed by the SEM, TEM, and EDX in the nanometer range. This study showed the spherical shape and crystalline nature of NPs. Zeta potential was used to determine the stability of Ag NPs. Biosynthesized Ag NPs showed significantly potent antioxidant, antidiabetic, and cytotoxicity activity. Ag NPs also showed effectiveness against gram‐positive (Escherichia coli) and gram‐negative (Staphylococcus aureus) bacteria in the antimicrobial activity study. The result concluded that these Ag NPs might be used in biomedical and pharmacological fields. [ABSTRACT FROM AUTHOR]

Alongside oral delivery of therapeutics, transdermal delivery systems have gained increased patient acceptability over past few decades. With increasing popularity, novel techniques were employed for transdermal drug targeting which involves microneedle patches, transdermal films and hydrogel based formulations. Hydrogel forming ability along with other rheological behaviour makes natural polysaccharides an attractive option for transdermal use. Being a marine originated anionic polysaccharide, alginates are widely used in pharmaceutical, cosmetics and food industries. Alginate possesses excellent biodegradability, biocompatibility and mucoadhesive properties. Owing to many favourable properties required for transdermal drug delivery systems (TDDS), the application of alginates are increasing in recent times. This review summarizes the source and properties of alginate along with several transdermal delivery techniques including the application of alginate for respective transdermal systems. [ABSTRACT FROM AUTHOR]

Tea is the most popular daily drink consumed globally, with a high concentration of caffeine and polyphenols. In this study, the effects of ultrasonic‐assisted extraction and quantification of caffeine and polyphenols from green tea were investigated and optimized using 23‐full factorial design and high‐performance thin‐layer chromatography. Three parameters were optimized to maximize the concentration of caffeine and polyphenols extracted using ultrasound: crude drug‐to‐solvent ratio (1:10–1:5), temperature (20–40°C), and ultrasonication time (10–30 min). The optimal conditions achieved from the model for tea extraction were as follows: crude drug‐to‐solvent ratio, 0.199 g/ml; temperature, 39.9°C; and time, 29.9 min; the extractive value was found to be 16.8%. Images from scanning electron microscopy showed that the matrix underwent a physical alteration and cell wall disintegration, which intensified and accelerated the extraction. This process might be simplified using sonication, which results in a higher extractive yield and a significant concentration of caffeine and polyphenols than the traditional approach, with a smaller quantity of solvent and faster analytical times. The result of high‐performance thin‐layer chromatography analysis proves a significant positive correlation between extractive value and caffeine and polyphenol concentrations. [ABSTRACT FROM AUTHOR]

Potentiality of Synthetic Aperture Radar (SAR) based Radar Forest Degradation Index (RFDI) combined with field observations for monitoring spatio-temporal dynamics of intertidal mudflat vegetation was assessed in this study. Five vegetation zones were delineated in the Junput mudflat of eastern India with very high classification accuracy (Kappa coefficient ≥ 0.79). Fragmentation and coalescence patterns of different vegetation zones under two plantation initiatives were also analysed by different spatial metrics. Results reveal gradual degradation of tree dominated vegetation zones and growth of shrub dominated and herbaceous ones from 2007 to 2019. Plantation of exotic species like Eucalyptus globulus and Casuarina equisetifolia along the shoreline had been found to be less effective against storms and sea surges. Conversely, native mangrove plantations and associated herbs had demonstrated remarkable growth in the intertidal areas. Based on the findings, the study pointed out that a zone-wise cum site-specific plantation strategy is needed towards developing effective bio-shields. [ABSTRACT FROM AUTHOR]

Introduction: α‐Amylase inhibitors from natural sources are of interest for new drug development for the treatment of diabetes mellitus (DM). High‐performance thin‐layer chromatography (HPTLC) coupled bioassay guided isolation of bioactive compounds has been improved within last few years. Objective: A microchemical derivatised HPTLC‐coupled attenuated total reflectance‐Fourier‐transform infrared (ATR‐FTIR) and nuclear magnetic resonance (NMR) spectroscopy was employed for profiling α‐amylase inhibitor from the aerial part of Asparagus racemosus Willd. Methodology: Asparagus racemosus Willd. aerial part extracted with different solvents (n‐hexane, chloroform, ethyl acetate, and methanol) and assayed to detect free radical scavengers and α‐amylase inhibitor by 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) assay and starch‐iodine assay method, respectively. HPTLC‐coupled ATR‐FTIR and NMR spectroscopy was used to identify the α‐amylase inhibitor. Results: Methanolic extract of A. racemosus showed highest antioxidant activity (21.99 μg GAE/μL) where n‐hexane extract showed lowest antioxidant activity (5.87 μg GAE/μL). The α‐amylase inhibition was recorded as highest and lowest in ethyl acetate extract (13.13 AE/μL) and n‐hexane extract (3.92 AE/μL), respectively. The deep blue zone of α‐amylase sprayed TLC plate of extracts with hRF = 72 analysed for ATR‐FTIR and NMR spectroscopy which revealed the presence of stigmasterol is responsible for α‐amylase inhibition. Conclusion: The present work establishes the α‐amylase inhibiting properties of A. racemosus maintaining its use for the treatment of DM as a traditional medicine. Bioassay guided isolation through HPTLC‐coupled ATR‐FTIR and NMR spectroscopy offers an effective method for the exploration of bioactive compounds such as α‐amylase inhibitor from complex plant extracts. A. racemosus is an important medicinal plant that is extensively used as hyperlipidaemia, hypertension, angina, dysmenorrhoea, anxiety disorders, benign prostatic hyperplasia (BPH), leucorrhoea, and urinary tract infections. Here, HPTLC‐based effect‐directed assay (EDA) approach was used to show the antioxidant activity and to identify the responsible α‐amylase inhibitor from the aerial parts of A. racemosus. [ABSTRACT FROM AUTHOR]

Background: The World Health Organization declared the outbreak of the novel coronavirus (COVID-19) as a global health emergency on January 30, 2020, and as a pandemic disease on March 11, 2020. This review highlights the international situation, risk factors, and related protections to be taken as prerequisite measures and probable treatment options for the COVID-19-infected population in the current scenario. Main text: The SARS-CoV-2 viruses and their variants caused mild-to-severe respiratory tract infection and used airborne pathways as a way of contagion. Human-to-human transmission led to an exponential growth in the rise in the number of cases making it a real burden to immobilize the rapid spread of the virus while asymptomatic patients created ambiguity for confirmation in the community. It was clear from the case studies of patients that most of them were asymptomatic but still vulnerable to the people around, and hence, in a flash, many countries around the globe went into a complete lockdown, influencing the economy and thrashing industrial outputs. On the other hand, numerous researches were made to counteract the spread through studies in antiviral therapy, immune-based therapy, vaccination development, and natural remedies. Conclusion: Although exploration for a specific drug required for the COVID-19 treatment is under extensive research worldwide and some of them are in clinical trial now. Virtual drug library screening is one of the current techniques for repurposing accessible compounds. This review could provide beneficial information about the potential current and future treatment strategies to treat the pandemic COVID-19 infection. [ABSTRACT FROM AUTHOR]

Asparagus racemosus Willd. is widely used to combat various diseases owing to its medicinal properties. In this study, arial parts of A. racemosus were investigated for their total phenolic content, total flavonoid content and antioxidative potential. A high‐performance thin‐layer chromatography (HPTLC) method combined with effect‐directed‐analysis was also developed to screen the antioxidant effects of A. racemosus and quantify biologically active compounds on chromatograms from A. racemosus. Total phenolics (154 mg gallic acid equivalent/g), flavonoid contents (497 mg quercetin/g) and IC50 (15.25 μg/ml) were found to be higher in methanolic extract of A. racemosus than in n‐hexane, chloroform and ethyl acetate extracts. HPTLC hyphenated with chemical derivatizations (DPPH•, p‐anisaldehyde/sulfuric acid, and ferric chloride) was used to evaluate antioxidant activity and the presence of phytosterols, terpenoids and polyphenolic contents. The same compounds at 100*retention factor = 58, 68, 74 and 65 in extracts were responsible for antioxidant activity. Hyphenated HPTLC allowed a rapid characterization of the active compound with a combination of effect‐directed‐analysis and attenuated total reflectance–Fourier transform infrared spectroscopy. Spectral analysis of the band from attenuated total reflectance identified myricetin, quercetin, p‐coumaric acid and caffeic acid as responsible for the antioxidant activity. [ABSTRACT FROM AUTHOR]

Development of tamarind seed gum (TSG)-hydrolyzed polymethacrylamide- g -gellan (h-Pmaa-g-GG) composite beads for extended release of diclofenac sodium using 3 2 full factorial design is the main purpose of this study. The ratio of h-Pmaa-g-GG and TSG and concentration of cross-linker CaCl 2 were taken as independent factors with three different levels of each. Effects of polymer ratio and CaCl 2 on drug entrapment efficiency (DEE), drug release, bead size and swelling were investigated. Responses such as DEE and different drug release parameters were statistically analyzed by 3 2 full factorial design using Design-Expert software and finally the formulation factors were optimized to obtain USP-reference release profile. Drug release rate was found to decrease with decrease in the ratio of h-Pmaa-g-GG:TSG and increase in the concentration of Ca 2+ ions in cross-linking medium. The optimized formulation showed DEE of 93.25% and an extended drug release profile over a period of 10 h with f 2 = 80.13. Kinetic modeling unveiled case-I-Fickian diffusion based drug release mechanism. [ABSTRACT FROM AUTHOR]

Development of a gastroretentive sustained release tablet of metformin based on poly (acrylic acid)-grafted-gellan (PAAc- g -GG) is the main purpose of this study. At first, PAAc- g -GG was synthesized by microwave-promoted free radical initiation method using cerric (IV) ammonium nitrate (CAN) as redox initiator and characterized by elemental analysis, FTIR, DSC-TGA, 13 C NMR, biodegradation and viscosity study. The synthetic parameters were optimized by 2 3 full factorial design using Design Expert software. Acute oral toxicity and histological studies were also performed as per OECD guideline. Tablets were then prepared employing wet granulation method using PAAc-g-GG and evaluated for various physical characters, in vitro drug release, ex-vivo mucoadhesion and swelling. Compatibility between drug and excipients was checked by DSC and FTIR analysis. The F3 batch showed excellent mucoadhesion and sustained drug release over a period of 10 h with dissolution similarity factor, f 2 = 77.43. Kinetic modeling unveiled Case-1 Fickian diffusion based drug release mechanism. [ABSTRACT FROM AUTHOR]

Formulation of a gastroretentive extended release tablet of metformin based on polymethacrylamide-g-gellan (Pmaa-g-GG)-tamarind seed gum (TSG) composite matrix is the main purpose of this study. Tablets were prepared employing wet granulation method taking amount of Pmaa-g-GG, TSG and NaHCO 3 (SBC, buoyancy contributor) as independent formulation variables. The tablets were then evaluated for in vitro drug release, buoyancy, ex vivo mucoadhesion, swelling and surface morphology. Compatibility between drug and excipients was checked by DSC, FTIR and XRD analysis. Buoyancy-lag-time, mucoadhesive strength, % drug release and release-rate constant were statistically analyzed using Design-Expert software (version 9.0.4.1) and the formulation was then numerically optimized to obtain USP-reference release profile. The optimized formulation showed excellent buoyancy over a 10 h period with buoyancy lag time of 2.76 min, significant mucoadhesion and drug release over a period of 10 h with f 2 = 71.58. Kinetic modeling unveiled anomalous non-Fickian transport based drug release mechanism. [ABSTRACT FROM AUTHOR]

In the present study, the microwave induced synthesis of polymethacrylamide-grafted-gellan gum (PMaa-g-GG) was carried out by free radical initiation using cerric (IV) ammonium nitrate (CAN) as redox initiator. Concentrations of methacrylamide (Maa), CAN and microwave irradiation time were taken as variable synthetic parameters. The modified polysaccharide obtained from different synthetic conditions was then characterized by FTIR, CHN analysis, DSC and powder X-ray diffraction. The yield and extent of grafting were assessed by determining percentage grafting, percentage grafting efficiency, percentage conversion and these were correlated with elemental analysis. The acute oral toxicity study of modified polysaccharide was performed as per OECD guideline. Histological comparison of different organs between control and test animal showed no significant difference. Sustained release tablets of diclofenac sodium (DS) were prepared with modified gellan. In vitro dissolution study showed the tablets were capable of releasing the drug over a period of 8 h. [ABSTRACT FROM AUTHOR]

The objective of the present study was to modify okra gum (Abelmoschus esculentus) by carboxymethylation and subsequent graft-copolymerization, characterize and fabricate into sustained-release tablet matrix. Firstly, okra gum was carboxymethylated using sodium hydroxide and monochloroacetic acid followed by grafting with polymethacrylamide employing synergistic combination of free-radical-initiator and microwave-irradiation. The FTIR, NMR, elemental analysis and viscosity study corroborate the formation of sodium-carboxymethyl-okra gum–grafted-polymethacrylamide copolymer (SCMOG-g-PMA). The maximum degree of carboxymethyl-substitution (DCS) and % grafting (%G) were found to be 0.604 ± 0.011 and 644.1, respectively. Water-uptake-capacity was found to increase by 3.5 fold. The tablet formulation of diclofenac sodium with SCMOG-g-PMA (DCS 0.604 and 423.4% G) showed to exhibit excellent sustained-release capacity with 90% drug-release at 11.7 h and similarity-factor of 72.0. The toxicity and biodegradability study also exhibited the bio-compatible and biodegradable nature of the copolymer, which might make the copolymer suitable for sustained-release drug delivery systems as smart semi-synthetic biopolymer. • The study demonstrates synthesis of carboxymethyl okra gum-g-polymethacrylamide • The maximum degree of carboxymethyl substitution (DCS) was 0.604 ± 0.011 • The maximum % grafting was 644.1% • The modified gum was found to be biodegradable and non-toxic • The grade with DCS of 0.604 and 423.4%G exhibits T 90% of 11.7 h and f 2 = 72.0 [ABSTRACT FROM AUTHOR]

The main objective of the present study was to develop a sustained release multiple-unit beads of lamotrigine based on ionotropically cross-linked natural polysaccharides such as pectin (PTN) and okra mucilage (OM) and optimize the polymer-concentration, polymer ratio and cross-linker concentration by 23 full factorial design. Two different levels of three independent variables (total polymer concentration, polymer ratio and [CaCl 2) were considered for the experimental design. Drug-polymers compatibility was examined by FTIR, DSC, TGA and powder-XRD. The surface morphology of the bead before and after dissolution test was examined by SEM. Effects of the independent variables on bead-size, drug-encapsulation-efficiency (DEE), drug-release along with release similarity and difference factors were examined. The independent variables were then numerically optimized using Design-Expert software (Version 12) with the targets to meet USP-reference release profile after the analysis of variance of all the response parameters such as DEE, percent drug release at 2 h, 5 h, 12 h, Korsmeyer-Peppas rate constant, release similarity and difference factors. The optimized formulation showed excellent DEE of 89.2 ± 4.4% and a sustained release profile with release similarity factor of 94.9. Kinetic modeling of drug release data demonstrated a release mechanism combined of hydration, diffusion and erosion. • The study utilizes natural edible polysaccharides for formulation sustained release beads. • A nonhazardous green process was employed. • Quality-by-design was adopted to optimize the formulation with minimum experimentation. • Optimized formula exhibited 89.2 ± 4.4% drug encapsulation efficiency and drug release over 12 h. • An excellent of release similarity factor (94.9) was obtained from optimized formula. [ABSTRACT FROM AUTHOR]

The purpose of the present study was to develop buoyant beads for the intragastric delivery of furosemide in order to evaluate the effect of incorporated sunflower oil on physiochemical properties of alginate beads. Sunflower oil entrapped buoyant alginate beads of furosemide were prepared by the emulsion-gelation technique. During the preparation of various batches of beads, the ratio of sunflower oil to water (v/v), the ratio of drug to polymer (w/w), were kept as variables at two levels; either high or low. Smooth, spherical beads with nominal weight variation were obtained. All batches of beads floated for 24 hours with a lag time of 5-10 min. The release of drug followed for 5 hours. Higuchi and first order kinetic modeling indicated a diffusion-controlled release of drug from the beads. The study also demonstrated the influence of sunflower oil on drug entrapment (81-95%) and in vitro release. A higher level of oil increased drug entrapment efficiency but retarded drug release rate as compared to a lower level of oil containing beads. [ABSTRACT FROM AUTHOR]