Fabrication, evaluation, and enhanced penetration of vinyl and cellulose-engineered transdermal patch of nifedipine using essential oil as penetration enhancer.

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.

Green synthesis of copper nanoparticles by using pineapple peel waste: in vitro characterizations and antibacterial potential.

A considerable amount of fruit waste is being produced every day worldwide. The green synthesis of metal nanoparticles from fruit peel waste can be an innovative, cost-effective, and eco-friendly alternative to traditional methods. Copper nanoparticles (CuNPs) were synthesized by a green method using the pineapple peels extract (PLX) and copper sulfate pentahydrate. The formation of CuNPs was visually identified and detected by UV-Visible spectroscopy. The CuNPs were characterized by Fourier-transform infrared (FTIR) spectroscopy, particle size analyzer, scanning electron microscopy (SEM), and X-ray diffraction (XRD). The antioxidant and reducing power of CuNPs were conducted by %DPPH scavenging and electron transfer-based ferric reducing antioxidant power (FRAP) assay, respectively. The antibacterial properties of CuNPs were determined in gram-positive, and gram-negative bacteria. The results showed that the CuNPs were spherical in shape with mean particle size 290.5 nm. The zeta potential of the nanoparticles was found to be - 12.3 mV indicating the instability in the colloidal state. The FTIR study confirmed the peaks of phytochemicals present in the PLX and the nanoparticles supporting the use of pineapple peels as stabilizing, reducing and capping agents. Both the DPPH and reducing power assay depicted that the synthesized CuNPs had significant antioxidant activity. However, the synthesized CuNPs had strong inhibitory capacity against both gram-positive and gram-negative test organisms. Thus, the CuNPS could be used for its viable antibacterial potential to preserve fruits, flowers, and vegetables from bacterial contamination.

Formulation of silver nanoparticles using Duabanga grandiflora leaf extract and evaluation of their versatile therapeutic applications.

The current research focused on the green synthesis of silver nanoparticles (AgNPs) using Duabanga grandiflora leaf extract. The green synthesis of AgNPs was confirmed by the surface plasmon resonance band at 453 nm in a UV-Visible analysis. The formulated AgNPs had a diameter of around 99.72 nm with a spherical shape. Fourier transform infrared (FTIR) spectrum revealed the bio-reducing potential of phytochemicals present in D. grandiflora, which fundamentally influenced the synthesis of AgNPs. Zeta potential, dynamic light scattering (DLS), scanning electron microscopic (SEM), energy-dispersive X-ray spectroscopic (EDX), X-ray diffraction (XRD), and transmission electron microscopic (TEM) analyses were executed to reveal the physicochemical attributes of the AgNPs. The AgNPs were further investigated for their antioxidant, antidiabetic, anticancer, and antibacterial potential. The DPPH free radical assay revealed the potential radical scavenging capacity (IC50 = 76.73 µg/ml) of green synthesized AgNPs. α-Amylase inhibitory assay displayed significant inhibitory potential (IC50 = 162.11 µg/ml) of this starch-breaking enzyme by AgNPs, revealing the antidiabetic potential of AgNPs. AgNPs exhibited potential cytotoxic activity (IC50 = 244.57 µg/ml) against malignant human kidney cells. In addition, AgNPs showed outstanding antibacterial activity against both Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacterial strains. Interestingly, AgNPs showed cytotoxic and antimicrobial activities at much higher concentrations than radical scavenging and α-amylase inhibitory concentrations. Thus, our finding elaborated the scope of green synthesized AgNPs for diverse therapeutic applications (dose-dependent) for further clinical translation.

Papaya peel extract-mediated green synthesis of zinc oxide nanoparticles and determination of their antioxidant, antibacterial, and photocatalytic properties.

This study describes an effective and eco-friendly approach to the synthesis of zinc oxide nanoparticles (ZnONPs) utilizing papaya fruit peel extract (PPE). The structural evaluation and morphological features of synthesized ZnONPs were examined using various physicochemical analyses. The formulated ZnONPs were spherical to hexagonal in shape with ⁓ 170 nm in diameter. ZnONPs exhibited improved antioxidant potential in terms of DPPH radical scavenging activity (IC50 = 98.74 µg/ml) and ferric-reducing potential compared with PPE. The antibacterial activity of ZnONPs was measured against pathogenic strains of Salmonella typhi, Bacillus subtilis, Staphylococcus aureus, and Escherichia coli. The biosynthesized ZnONPs showed potential antibacterial efficacy against all microbes. In addition, ZnONPs exhibited potential photocatalytic activity in rhodamine B degradation in the presence of sunlight. The results indicated that papaya peels, which are these fruit wastes, could be helpful for the green synthesis of ZnONPs with good dose-responsive antioxidant, antibacterial, and photocatalytic activities.

Evaluation of Cassia fistula seed galactomannan as tablet-binder in formulation of diclofenac sodium-loaded monolithic matrix tablet.

The present study aimed to evaluate Cassia fistula seed galactomannan (CFSG) as a tablet-binder in the formulation of a monolithic matrix tablet using diclofenac sodium as a model drug. Initially, CFSG was extracted and purified from the seeds of the Cassia fistula tree and then screened for phytochemicals. Native CFSG was characterized with polysaccharide content determination, monosaccharide composition analysis, elemental analysis, FTIR, solid-state 13C NMR, molecular weight, zeta potential, DSC, TGA-DTA, XRD, viscosity, pH and surface tension, rheology, SEM and acute oral toxicity study. Prior to formulation, the drug-CFSG compatibility was checked by FTIR, DSC, and XRD. Diclofenac sodium-loaded granules were prepared by the wet granulation method and evaluated for various granule properties. Finally, granules were compressed into tablets and evaluated for binding and other tablet properties. The granules showed to have optimum micromeritic properties. Tablet hardness and friability were found to be approximately 7 kg/m2 and 0.3 %, respectively, which substantiate the excellent binding capacity of CFSG. Other tablet properties were also found to be within the Pharmacopoeial compliance limit. The tablets with a minimum concentration of CFSG (2.5%w/w) as binder showed appreciable mechanical strength and faster drug release, which ratifies CFSG as an alternative tablet binder.

Evaluation of maceration, microwave, ultrasound-assisted extraction methods on free, esterified and bound phenolic profile and antioxidant activity of black rice.

Black rice (Oryza sativa L.) is a rich source of phenolics and anthocyanins. It was aimed to investigate the effect of different extraction methods such as conventional solvent extraction, ultrasound-assisted extraction (UAE), and microwave-assisted extraction (MAE) on antioxidant activity and phenolic profiling of black rice free, esterified, and bound phenolics fractions. Spectrophotometric methods were used to evaluate antioxidant activity and HPTLC was used for phenolics profiling. The highest content of % yield, total anthocyanin (TAC), total phenolic (TPC), and total flavonoid (TFC) contents were detected in MAE. It was also observed that antioxidant activity based on DPPH, ABTS, superoxide radical-scavenging and ferric reducing antioxidant power (FRAP) assays showed highest activity in MAE. Eight phenolic compounds were identified and quantified by a validated HPTLC method. MAE showed most abundant phenolic compounds. A significant positive correlation was established between % yield, total phenolic content, and total flavonoid content (p < 0.05) where a significant negative correlation was established between % yield, TPC, and TFC with IC50 of antioxidant activity (p < 0.05). Diverse phenolic contents and antioxidant activity were studied with different forms of phenolics with the different extraction methods. It designates that the extraction techniques had effects on the bioactive compounds as well biological properties.

Preparation of silver nanoparticles by Osbeckia stellata aqueous extract via green synthesis approach: Characterization and assessment of their antioxidant, antidiabetic, cytotoxicity, and antibacterial properties.

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.

Impact of ultrasound-assisted extraction of polyphenols and caffeine from green tea leaves using high-performance thin-layer chromatography.

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.

Recent update on alginate based promising transdermal drug delivery systems.

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.

Chitosan Derivatives as Carriers for Drug Delivery and Biomedical Applications.

Over the past few decades, chitosan (CS) has gained the attention of researchers investigating newer biomaterial-based carriers for drugs in pharmaceutical and biomedical research. Combined with its nontoxic behavior, biodegradability, and biocompatibility, chitosan has found widespread applications in the fields of drug delivery, tissue engineering, and cosmetics. As a novel drug carrier, chitosan is regarded as one of the promising biomaterials in the pharmaceutical industry. The extensive use of this cationic biopolysaccharide in the delivery of therapeutic agents has brought a few limitations of chitosan into the limelight. Various chemical modifications of chitosan can minimize these limitations and improve the efficacy of chitosan as a drug carrier. The effectiveness of several chemically modified chitosan derivatives, including trimethyl chitosan, thiolated chitosan, PEGylated chitosan, and other chitosan derivatives, has been investigated by many researchers for the controlled and target specific delivery of therapeutics. The chemically modified chitosan derivatives exhibited greater importance in the current scenario on drug delivery due to their solubility in wide range of media along with their interaction with pharmaceutically active ingredients. Chitosan derivatives have also attracted attention in several biomedical fields, including wound healing, hyperthermia therapy, tissue engineering, and bioadhesives. The present review narrates the sources and common physicochemical properties of chitosan, including several important synthetic modifications to obtain chemically modified chitosans and their applications in target-specific drug delivery, along with several biomedical applications.

Green synthesis of silver nanoparticles using Eupatorium adenophorum leaf extract: characterizations, antioxidant, antibacterial and photocatalytic activities.

The green synthesis of metallic nanoparticles has tremendous impacts in various fields as found in recent years due to their low cost, easy and environmentally friendly synthesis. In this article, we report a simple and eco-friendly method for the synthesis of silver nanoparticles (AgNPs) using an aqueous Eupatorium adenophorum (E. adenophorum) leaf extract as a bioreductant. Interestingly, Fourier transform infrared (FTIR) spectroscopy analysis established that the E. adenophorum extract not only served as a bioreductant but also acted as a capping agent to stabilize the nanoparticles by functionalizing the surfaces. Various characterization techniques were adopted, such as X-ray powder diffraction (XRD), FTIR, ultraviolet-visible absorption (UV-Vis) spectroscopy, dynamic light scattering, scanning electron microscopy and energy-dispersive X-ray spectroscopy (EDX) to analyze the biosynthesized AgNPs. Biosynthesized nanoparticles were also explored for antioxidant, antibacterial and photocatalytic activities. The AgNPs showed improved free radical scavenging activity (IC50 48.96 ± 0.84 µg/mL) and bacterial inhibitory effects against both gram-positive (Staphylococcus aureus; 64.5 µg/mL) and gram-negative (Escherichia coli; 82.5 µg/mL) bacteria. Photocatalytic investigation showed AgNPs were effective at degrading rhodamine dye (78.69% in 90 min) when exposed to sunlight. These findings collectively suggest that E. adenophorum AgNPs were successfully prepared without the involvement of any hazardous chemical and it may be an effective antibacterial, antioxidant and promising agent for the removal of hazardous dye from waste water produced by industrial dyeing processes.

Tissue specific changes of phytochemicals, antioxidant, antidiabetic and anti-inflammatory activities of tea [Camellia sinensis (L.)] extracted with different solvents.

Different parts of Camellia sinensis (L.) were extracted with solvents according to polarity, and the extracts' phytochemical profiling and biological activities were examined. The total phenolic (TPC) and total flavonoid (TFC) contents increased with the increasing polarity of the solvent which met its maximum in polar solvents. The increasing antioxidant, anti-inflammatory and antidiabetic activities were recorded with increasing polarity of solvents which showed hydroalcoholic as best solvent. The strong and significant correlation was among the TPC, TFC, DPPH, anti-inflammatory and antidiabetic activities for different parts of tea. HPTLC study of individual phenolic acids, epigallocatechin gallate, gallocatechin and theaflavin met their maximum level of content with polar solvents like hydroalcohol, methanol and water mostly in mainly tea leaves. Our finding suggested that the polar solvents and young leaves of tea were beneficial for obtaining extracts. On the other hand, phenolics were found to be potent antioxidant, anti-inflammatory and antidiabetic agent.

High-performance thin-layer chromatography coupled attenuated total reflectance-Fourier-transform infrared and NMR spectroscopy-based identification of α-amylase inhibitor from the aerial part of Asparagus racemosus Willd.

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.

Current challenges in different approaches to control COVID-19: a comprehensive review.

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.

Pharmacological studies of rhizomes of extract of Cyperus tegetum, emphasized on anticancer, anti-inflammatory and analgesic activity.

ETHNOPHARMACOLOGICAL RELEVANCE: With over 950 species, Cyperus is one of the most promising health boosting genera in the Cyperaceae family. Traditional uses of Cyperus sp. have been described for gastrointestinal blood abnormalities, menstrual irregularities, and inflammatory diseases, among others. Cyperus tegetum Roxb belonging to Cyperaceae family, is used in traditional medicine to treat skin cancers. AIM OF THE STUDY: The present study was carried out to explore the potential effect of the extract of the plant Cyperus tegetum against different pharmacological activity namely inflammatory, analgesic activity as well as skin cancer activity in mice. MATERIALS AND METHODS: Cytotoxicity of the extract was measured by MTT and Live/death assay on HeLa cell line. Skin cancer was induced by 7,12-dimethylbenz(a) anthracene (DMBA) and 12-O-tetradecanoylphorbol-13-acetate (TPA) in mice to measure its effects. RESULT: Stigmasterol and some poly phenolic compounds are identified using HPTLC process from the methanol extract of the rhizome of the plant Cyperus tegetum (CT-II). After confirmation of the presence of different polyphenolic compound and triterpenoids in the extract, it was subject to MTT and Live/death assay on HeLa cell line. From the observation it could be concluded that the IC50 of the extract is 300 µg/ml. Thus, the CTII was evaluated further for its in vivo anticancer property. In the tumorigenesis study, the number of tumor growths, the area and weight of the tumor significantly decreases with increment in the dose of CT-II extract and some elevated enzyme release in renal (creatinine, urea) as well as hepatic (AST, ALT, ALP) enzymes are also controlled with the increased dose of the same extract. The elevated enzyme release may be due to cancer induced rupture of the plasma and cellular damage. This CT-II extract also exhibits some other pharmacological activity like anti-inflammatory and analgesic activity. CONCLUSION: As metabolic activation via carcinogens and inflammation response plays important role in development of cancer, antioxidant, anti-inflammatory and analgesic properties can be correlated with anti-cancer properties. Taken all the above studies, it was illustrated that the extract of Cyperus tegetum might be a promising compound to reduce skin cancer risk.

High-performance thin-layer chromatography based approach for bioassay and ATR-FTIR spectroscopy for the evaluation of antioxidant compounds from Asparagus racemosus Willd. aerial parts.

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.

Synthesis, characterization and fabrication of sodium carboxymethyl-okra-gum-grafted-polymethacrylamide into sustained release tablet matrix.

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.

Quality-by-design approach for development of sustained-release multiple-unit beads of lamotrigine based on ion-cross-linked composite of pectin and okra mucilage: An in vitro appraisal.

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 [CaCl2]) 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.

Formulation of Extended-Release Beads of Lamotrigine Based on Alginate and Cassia fistula Seed Gum by QbD Approach.

AIM: This study was focused on the formulation of the multi-unit extended-release peroral delivery device of lamotrigine for better management of epilepsy. BACKGROUND: The single-unit extended-release peroral preparations often suffer from all-or-none effect. A significant number of multi-unit delivery systems have been reported as a solution to this problem. But most of them are found to be composed of synthetic, semi-synthetic or their combination having physiological toxicity as well as negative environmental impact. Therefore, fabrication and formulation of multi-unit extended-release peroral preparations with natural, non-toxic, biodegradable polymers employing green manufacturing processes are being appreciated worldwide. OBJECTIVE: Lamotrigine-loaded extended-release multi-unit beads have been fabricated with the incorporation of a natural polysaccharide Cassia fistula seed gum in calcium-cross-linked alginate matrix employing a simple green process and 23 full factorial design. METHODS: The total polymer concentration, polymer ratio and [CaCl2] were considered as independent formulation variables with two different levels of each for the experiment-design. The extended-release beads were then prepared by the ionotropic gelation method using calcium chloride as the crosslinkerions provider. The beads were then evaluated for drug encapsulation efficiency and drug release. ANOVA of all the dependent variables such as DEE, cumulative % drug release at 2h, 5h, 12h, rate constant and dissolution similarity factor (f2) was done by 23 full factorial design using Design-Expert software along with numerical optimization of the independent variables in order to meet USP-reference release profile. RESULTS: The optimized batch showed excellent outcomes with DEE of 84.7 ± 2.7 (%), CPR2h of 8.41± 2.96 (%), CPR5h of 36.8± 4.7 (%), CPR12h of 87.3 ± 3.64 (%) and f2 of 65.9. CONCLUSION: This approach of the development of multi-unit oral devices utilizing natural polysaccharides might be inspiring towards the world-wide effort for green manufacturing of sustained-release drug products by the QbD route.

Graft-copolymer of polyacrylamide-tamarind seed gum: Synthesis, characterization and evaluation of flocculating potential in peroral paracetamol suspension.

In the present study, polyacrylamide-grafted-tamarind seed gum (PAAm-g-TSG) was synthesised employing free radical method assisted with microwave where cerric (IV) ammonium nitrate (CAN) was used as free radical initiator. Effects of monomer, CAN and microwave irradiation time (MW) on grafting were studied. Various grafting indicators such as % grafting (%G), % grafting efficiency (%GE) and % conversion (%Cn) were calculated. MW and CAN exhibited major contribution in the synthesis. Highest % grafting (890.3%) was shown in the batch with 10 g acrylamide, 400 mg CAN and 1 min MW. Grafted TSG was then characterized by elemental analysis, FTIR, solid state 13C NMR, DSC, TGA, XRD, viscosity, SEM, acute oral toxicity and biodegradability study. Nontoxic and biodegradable natures of PAAm-g-TSG were revealed in the study. Finally, flocculating property of the grafted gum was evaluated in paracetamol suspension. The flocculation study demonstrates that all batches of graft copolymer showed to have good flocculating efficiency in paracetamol suspension and the capacity increases with increase in both concentration and grafting. S11 batch (highest %G = 890.3) exhibited highest degree of flocculation (ß = 5.14 ± 0.26) among others.