Pharmacological Significance Research Articles

Therapeutic potential and industrial applications of Terminalia arjuna bark.

Terminalia arjuna (Roxb. ex DC.) Wight & Arnot (Combretaceae) is one of the most frequently used medicinal trees in Indian traditional medicinal systems. It is used for the treatment of a variety of diseases including cardiovascular disorders. The purpose of this review was to provide a comprehensive overview of the phytochemistry, medicinal uses, toxicity, and industrial applications of T. arjuna bark (BTA), as well as to identify gaps in research and applications of this important tree. It also aimed to analyze trends and future research paths to utilize the full potential of this tree. Extensive bibliographic research on the T. arjuna tree was carried out using scientific research engines and databases such as Google Scholar, PubMed, and Web of Science, covering all relevant English-language articles. The database "World Flora Online (WFO)" (http://www.worldfloraonline.org) was used to confirm plant taxonomy. To date, BTA has been traditionally employed for several disorders such as snakebites, scorpion stings, gleets, earaches, dysentery, sexual disorders, and urinary tract infections along with the cardioprotective activity. About 38 phytocompounds were identified from BTA and were classified as triterpenoids, tannins, flavonoids, and glycosides. A wide range of in vitro and in vivo pharmacological effects of BTA were reported such as anti-cancer, antimicrobial, antiviral, anti-inflammatory, antioxidant, hepatoprotective, anti-allergic, anti-diabetic, and wound healing activities. The oral administration of BTA (500mg/kg) per day did not result in any toxicity in humans. The in vivo acute and sub-acute toxicity analysis of the methanol extract of BTA and one of its major compounds, 7-methyl gallate, did not produce any adverse effects up to a dose of 1000mg/kg. This comprehensive review highlights various aspects of traditional knowledge, phytochemicals, and pharmacological significance of BTA. The review covered safety information on employing BTA in pharmaceutical dosage forms. Despite its long history of medicinal benefit, more studies are needed to understand the molecular mechanisms, structure-activity relationship, and potential synergistic and antagonistic effects of its phytocompounds, drug administration, drug-drug interactions, and toxicological effects.

Synthesis, Computational Analysis, Antimicrobial, Antioxidant, Trypan Blue Exclusion Assay, β-hematin Assay and Anti-inflammatory Studies of some Hydrazones (Part-I).

Hydrazone and its azomethine (-NHN=CH-) derivatives are widely reported for their immense pharmacological potential. They have also been reported to possess potent anti-tuberculosis, anti-malarial, anti-inflammatory, and anti-oxidant activities. Considering their pharmacological significance, we herein synthesized a set of 10 hydrazones (1S-10S) using green, biodegradable chitosan and HCl as catalyst. All synthesized compounds were characterized using modern spectroscopic techniques, including Nuclear magnetic resonance, 1H-/13C-NMR; Fourier transform infrared spectroscopy (FT-IR); Ultraviolet-visible spectroscopy; Mass spectrometry (m/z), etc. Synthesized compounds were in silico screened using molecular docking, dynamics, pharmacokinetics, theoretical properties, and common pharmacophore analysis. Moreover, we also subjected all compounds to DPPH radical scavenging assay, protein denaturation assay, Trypan Blue assay for cell viability assessments, β-hematin assay for hemozoin inhibition analysis and standard antimicrobial analysis. Our results suggested that the synthesized compound 2S had high potency against studied microbial strains (minimum MIC = 3.12 μg/mL). Our antioxidant analysis for 1S-10S revealed that our compounds had radical scavenging effects ranging from 25.1-80.3 %. Compounds 2S exhibited % cell viability of 68.92% (at 100 μg concentration of sample), while the same compound retained anti-inflammatory % inhibition at 62.16 %. Compound 2S was obtained as the best docked molecule, with a docking score of -5.32 Kcal/mol with target pdb id: 1d7u protein. Molecular dynamics simulation and normal mode analysis for 100 ns for 1d7u:2S retained good stability. Finally, in silico pharmacokinetics, theoretical properties and pharmacophoric features were assessed. In summary, synthesized hydrazone exhibited a good biological profile according to in silico and in vitro studies. However, further in vivo studies are required that may shed more insights on its potencies.

Antiviral medicinal plants of India as a potential tool against COVID-19: A review with ethno scientific evidence

Indian traditional medicinal systems are one of the oldest therapeutic systems in the world. Medicinal and aromatic plants play a dominant role in Indian traditional medicinal systems. Traditionally, many medicinal plants are used in India for their therapeutic relevance so much so that they have acquired a significant role in Indian religion as well. Many of these plants have proven antiviral effects. This review documents up-to-date information about many such medicinal herbs used in India which have got pharmacological significance in fighting viral infections. These plants surely have the potential to provide protection against Covid-19. The review presents a list of such plants along with their chemical ingredients and possible modes of action against the respective viral diseases. All information has been obtained by consulting the databases of Scopus, PubMed, Science Direct, Elsevier, Springer and relevant research papers and reports on COVID-19. The cited medicinal plants are used extensively in India as herbal remedies. The use of these plants is validated in light of research papers citing their ethnobotanical uses, important active principles and modes of action of the of medicinally important natural products. The plants listed have great potential to fight COVID-19 and other viral infections. Many of these are immunity boosters providing strength to the body to control the onset of diseases.

Attenuation of Strychnine-Induced Epilepsy Employing Amaranthus viridis L. Leaves Extract in Experimental Rats.

Epilepsy is one of the most prevalent neurological illnesses defined by periodic seizures with or without loss of consciousness caused by aberrant neural activity. There are many allopathic medications available for the treatment of epilepsy such as phenytoin (PHY), but the side effects are a major concern. Therefore, the present study involved the evaluation of the pharmacological significance of Amaranthus viridis L. extract (EAV) in the management of strychnine (STR)-induced epilepsy. STR (3.5 mg/kg, i.p.) was injected into male rats 30 minutes after the pre-treatment of a standard drug (PHY: 20 mg/kg) and the two doses of EAV (EAV-200 and EAV-400 mg/kg, p.o.) to the respective groups to cause the convulsions. The anti-convulsant effect of EAV-200 and EAV-400 against STR-induced convulsion in rats was investigated in terms of convulsion onset, duration of convulsions, number of convulsions, and convulsion score. Furthermore, the mitochondrial function and integrity in the brain's prefrontal cortex (PFC) were also estimated. EAV-400 significantly increased the onset of convulsion from 61.67 ± 3.051 to 119.2 ± 2.738 and reduced the STR-induced duration of convulsions from 144.8 ± 3.582 to 69.17 ± 3.736, number of convulsions from 4.000 ± 0.1592 to 1.533 ± 0.1542, and convulsion score from 5.000 ± 0.3651 to 2.833 ± 0.3073 in rats. EAV-400 significantly attenuated the STR-induced decrease in the mitochondrial function and integrity of the rat PFC. In rats, EAV-400 significantly accelerated the onset of convulsions while decreasing the STR-induced duration, frequency, and score. Based on investigational findings, EAV-400 could be inferred to be a possible anti-epileptic option for the treatment of epilepsy of this plan in preclinical research.

Thiazolidinone-Heterocycle Frameworks: A Concise Review of Their Pharmacological Significance.

Molecular hybridization is deemed an optimistic approach in drug design and the discovery of novel biologically active molecules as it may advance their affinity and potency while concurrently decreasing associated resistance and side effects. Approximately 20 % of approved drugs were developed using this approach in the past few years. Thiazolidinone is one of the privileged pharmacophores in medicinal chemistry and is associated with various biological activities; it forms a functional unit in several FDA-approved drugs. Consequently, this pharmacophore has attracted the attention of many research groups to further explore its pharmacological relevance by coupling it with other pharmacophoric moieties. This review presents a concise account of scholarly research exploits directed at the biological activities of newly synthesized thiazolidinone-tagged molecular hybrids. Focused attention is given to the existing structural activity relationship in each compound library and the toxicity profile of potent compounds including in silico docking studies (where applicable). This work would provide a base on which new pharmaceuticals with improved potency can be modelled.

Preparation and optimization of surface stabilized cryptotanshinone nanocrystals with enhanced bioavailability.

Cryptotanshinone (CTS) is a plant product extracted from Salvia miltiorrhiza Bunge with various pharmacological significances. In addition to its activities against coronary heart disease, hyperlipidemia, stroke, hepatitis and chronic renal failure, it demonstrates antimetastatic effects. However, its clinical use is limited due to its poor aqueous solubility and oral bioavailability. Herein, CTS nanocrystals were prepared with the precipitation method followed by high-pressure homogenization using Poloxamer 407 as the stabilizer. A stable product was further obtained by lyophilization. The particle size of the CTS nanocrystals was 315.67 ± 11.02 nm, and the zeta potential was near 0mV. The crystallinity was confirmed by DSC and PXRD. The saturation solubility was substantially increased from 0.97 ± 0.12μg/ml to 62.29 ± 1.91μg/ml, and the dissolution rate was also significantly accelerated. A pharmacokinetic study in rats revealed an improvement in oral bioavailability (2.87-fold) with CTS nanocrystals compared to the raw drug. In conclusion, the results of this study suggest a feasible formulation for the oral delivery of CTS.

A review on the pharmacological potential of Indian spices in polycystic ovarian syndrome

Pharmacological Significance: India has a distinct position in history for using spices from cooking to prevent and cure a variety of illnesses. Numerous studies have been conducted to evaluate the potential of these spices for a variety of conditions such as diabetes, metabolic syndrome, and polycystic ovarian syndrome (PCOS). PCOS is a condition in which women of reproductive age experience common health difficulties such as genetic, metabolic, and endocrine abnormalities. Notably, this may be distinguished by symptoms such as hirsutism, acne, and obesity. Aim: In this review, we looked at numerous Indian spices that may help to manage PCOS and its symptoms. Materials and Methods: All data were gathered from the literature using several databases such as PubMed and Europe PMC, publishers such as Springer, Wiley, Elsevier, and Taylor and Francis, and academic libraries such as Google scholar and Sci-Hub. Results: This study focuses on natural spices and their chemical constituents that have varied therapeutic effects such as anti-inflammatory, anti-oxidant, anti-androgenic, anti-estrogenic, anti-thrombolytic, and anti-diabetic for the treatment of PCOS in women. Conclusion: In this review, we looked at the effects of several Indian spices on the management of PCOS.

Antioxidant prodigiosin-producing cold-adapted Janthinobacterium sp. ERMR3:09 from a glacier moraine: Genomic elucidation of cold adaptation and pigment biosynthesis

Janthinobacterium from cold niches has been studied broadly for bioactive violacein production. However, reports on the atypical red-pigmented Janthinobacterium strains are shallow. The bioactive red prodigiosin pigment has immense pharmacological significance, including antioxidant, antimicrobial and anticancer potential. Here, we report the first complete genome of a prodigiosin-producing Janthinobacterium sp. ERMR3:09 from Sikkim Himalaya in an attempt to elucidate its cold adaptation and prodigiosin biosynthesis. Nanopore sequencing and Flye assembly of the ERMR3:09 genome resulted in a single contig of 6,262,330 bp size and 62.26% GC content. Phylogenomic analysis and genome indices indicate that ERMR3:09 is a potentially novel species of the genus Janthinobacterium. The multicopy cold-responsive genes and gene upregulation under cold stress denoted its cold adaptation mechanisms. Genome analysis identified the unique genes, gene cluster and pathway for prodigiosin biosynthesis in ERMR3:09. Considering the notable antioxidant activity, it can be the next powerhouse of bioactive prodigiosin production.

Trace level identifications of fentanyl and eutylone in equine plasma, pharmacological significance and probable origins – a case report and analysis

Trace level identifications of fentanyl and eutylone in equine plasma, pharmacological significance and probable origins – a case report and analysis

QSAR Studies on Some Sulfonamides as Antidiabetic Agents

The need for antidiabetic agents is growing day by day in pharmaceutical industry to find novel, potent and more specialized class of medicine. To address the need we have evaluated a set of sulphonamide drugs for their potential to fight against diabetes. In the present study antidiabetic activity of 47 sulfonamide derivatives have been modeled using topological descriptors. The activity in terms of pKi have been modeled using descriptors calculated from Dragon software. The best model having R2 value 0.9897 have been reported after deleting two outliers. The model was tested using Cross validated method. The R2cv value for the reported five-parametric model comes out to be 0.9896. The model has also been tested for collinearity or defect of Chance. It has been established that the model is free from any defect. The author suggests the testing of these compound for in vivo studies to specify the other pharmacological significance and therapeutic potential for future use.

Oral acute, sub-acute toxicity and phytochemical profile of Brassica carinata A. Braun microgreens ethanolic extract in Wistar rats

Ethnopharmacological relevanceCurrently, there is a remarkable increase in the consumption of microgreens, (young edible vegetables or herbs), as potential nutraceuticals for the management of diseases. Brassica carinata A. Braun is one of the traditional leafy vegetables cultivated in various parts of Sub- Saharan Africa. The plant is revered for its efficacy in the treatment of wounds and gastrointestinal disorders among other medicinal benefits. It is therefore crucial to characterize Brassica carinata microgreens for their phytoconstituents and ascertain their safety for use. Aim of the studyThe study evaluated the oral acute and subacute toxicity of Brassica carinata microgreens ethanol extract (BMEE) in Wistar rats and identification of its chemical composition and profile. Materials and methodsFor acute toxicity (14 days), rats were grouped into four and received a single oral dose, the control group received distilled water, while others received 500 mg/kg, 1000 mg/kg, and 2000 mg/kg of BMEE. For the subacute toxicity (28 days), rats in four groups received daily doses of 250 mg/kg, 500 mg/kg or 1000 mg/kg and distilled water. Daily clinical observations like lethargy and mortality were conducted. Hematological, biochemical, and histopathological evaluations were performed at the end of each experiment. Phytochemical profile was determined using a UV-VIS spectrophotometer and Gas Chromatography coupled to Mass Spectrometry (GC-MS) analysis determined the potential bioactive components in the microgreens extract. ResultsIn both acute and sub-acute toxicity studies, no mortalities, indications of abnormality, or any treatment related adverse effects were observed at doses of 2000 mg/kg, 1000 mg/kg, 500 mg/kg, and 250 mg/kg. The LD50 of BMEE was above 2000 mg/kg. No significant (p > 0.05) changes in the hematological and biochemical parameters of the treated groups compared to the control groups in both studies. Histopathological examination of the liver, kidney, lungs, and heart revealed a normal architecture of the tissues in all the treated animals. Phytochemical analyses revealed the presence of flavonoids (most abundant), phenols and alkaloids. Phytol, linoleic acid, and 9,12,15-octadecatrienoic acid, among other compounds, were identified by GC-MS analysis. ConclusionThe results showed that B. carinata microgreens ethanol extract is nontoxic and found to have several compounds with reported pharmacological significance suggesting safety for use.

Arctigenin: A Potential Component with Multifaceted Therapeutic Properties

Medicinal plants are an excellent source of new therapeutic drugs because of their phytochemical constituents. Arctium lappa L. (common name-burdock) is a perennial medicinal herb commonly found in China, Japan, Korea traditionally used as promising health supplement. promising health supplement. Major active constituent of A. lappa L. seeds are arctigenin which exhibits pharmacological potential such as anti-inflammatory, anticancer, antimicrobial and hepatoprotective properties. The purpose of this study is to provide an up-to-date evaluation of the literature on the pharmacological activities of Arctigenin from Articum lappa L. Literature is collected from Google scholar, Science Direct, Research Gate, PubMed, Google, and SciFinder databases published between 2012 and 2021 (Jan). Keywords used to retrieve the data are pharmacological profile, arctigenin, and Arctium lappa L. The antioxidant, anti-inflammatory, anti-tumor, hepatoprotective, renoprotective, neuroprotective, and CNS depressant properties of arctigenin demonstrated its pharmacological significance among traditional science According to different research, arctigenin is effective in the treatment of a variety of chronic disorders, including cancer (stomach, lungs, liver, and colon) and inflammatory diseases (rashes, and other skin conditions.). Future experiments based on the mechanism pathway responsible for the protective role of arctigenin's will help the scientist to uncover its health benefits.

The Synergistic Hepatoprotective Activity of Rosemary Essential Oil and Curcumin: The Role of the MEK/ERK Pathway.

Curcumin is a natural product obtained from the rhizome of Curcuma longa. Rosemary (Rosmarinus officinalis) is a medicinal and aromatic plant that is widely spread in the Mediterranean region. Both Curcumin and rosemary essential oil are natural products of high medicinal and pharmacological significance. The hepatoprotective effect of both natural products is well-established; however, the mechanism of such action is not fully understood. Thus, this study is an attempt to explore the hepatoprotective mechanism of action of these remedies through their effect on MEK and ERK proteins. Furthermore, the effect of rosemary essential oil on the plasma concentration of curcumin has been scrutinized. The major constituents of REO were qualitatively and quantitatively determined by GC/MS and GC/FID, respectively. Curcumin and rosemary essential oil were given to mice in a pre-treatment model, followed by induction of liver injury through a high dose of paracetamol. Serum liver enzymes, lipid peroxidation, antioxidant activities, the inflammatory and apoptotic biomarkers, as well as the MEK and ERK portions, were verified. The plasma levels of curcumin were determined in the presence and absence of rosemary essential oil. The major constituents of REO were 1,8-cineole (51.52%), camphor (10.52%), and α-pinene (8.41%). The results revealed a superior hepatoprotective activity of the combination when compared to each natural product alone, as demonstrated by the lowered liver enzymes, lipid peroxidation, mitigated inflammatory and apoptotic biomarkers, and enhanced antioxidant activities. Furthermore, the combination induced the overexpression of MEK and ERK proteins, providing evidence for the involvement of this cascade in the hepatoprotective activity of such natural products. The administration of rosemary essential oil with curcumin enhanced the curcuminoid plasma level. The co-administration of both curcumin and rosemary essential oil together enhanced both their hepatoprotective activity and the level of curcumin in plasma, indicating a synergistic activity between both natural products.

Exploring the nutritional profiling and health benefits of Palmyra palm haustorium

The Palmyra tree has its own cultural, nutritional, and medicinal values from ancient times. Every part of the tree is useful either in its native form or a modified form, though the seeds is generally neglected by people as a waste and are not utilized. The current study is conducted with the germinated seed embryo of Asian Palmyra palm ( Borassus flabellifer ) termed as Palmyra haustorium (PH). The nutritional, phytochemical, and nutraceutical aspects were evaluated to explore the pharmacological significance of three different samples prepared from Palmyra haustorium (PH) i.e., Palmyra haustorium powder (PHP), Palmyra haustorium milk (PHM) and Palmyra haustorium milk extracted cake powder (PHMCP). The PHP is found to be superior in all nutritional aspects compared to other samples analyzed in the study. Proximate analysis of PH samples has shown that it is rich in carbohydrates, protein, and fiber but negligible in fat while PHMCP is a greater source of fiber content. Mineral analysis has shown that PHP is rich in Potassium and Phosphorus, moderate in Calcium and Sodium levels, whereas PHMCP is rich in Iron. High-performance liquid chromatography (HPLC) and Gas Chromatography-Mass Spectrometry (GCMS) analysis showed the presence of different phenolic compounds like Gallic acid and chlorogenic acid in all PH samples; similarly various phytochemicals such as Clindamycin, Sucrose, Hexadecanoic acid, Myristic acid were present in these samples. Functional groups present in samples were identified as aldehydes, primary amines, alkanes were carried out by Fourier transform infrared (FTIR) spectroscopy. The results depict that the germinated seed embryo of Palmyra palm is rich in macro and micronutrients that act as nutraceuticals in enhancing the human health and well-being. Also these products may help in mitigating the effects of malnutrition, prevalent among the vulnerable population and PHM can be an alternate nutrient for individuals susceptible to digest lactose. • The Palmyra seed embryo powder (PHP) is nutritionally superior especially rich in carbohydrates, proteins and minerals like potassium and phosphorus. • The presence of phenolic compounds like gallic acid, chlorogenic acid, rutin, caffeic acid improves the health condition by its property to scavenge free radicals. • The phytochemical like oleic acid, an unsaturated fatty acid is good to consume as it possesses cardio-protective effect. • The current study highlights the potent nutritional quality and explores the phytochemicals in Borassus flabellifer seed embryo samples.

Evaluation of antioxidant activity and total phenolics of selected mangrove plants in Sabah

In recent years, research on medicinal plants has attracted much attention due to their wide range of pharmacological significance. Mangroves are biochemically unique, producing a wide array of natural products with unique bioactivity due to their abilityto survive in stressful conditions of high salinity, and low air humidity as well as strong variations therein. Six species of mangrove (Avicennia marina, Bruguiera gymnorrhiza, Ceriops tagal, Rhizohora apiculata, Rhizophora mucronata and Xylocarpus granatum)from different parts of the leaves, stem and roots were extracted successively with ethanol and water. This study aims to measure quantitatively the total phenolic content and assess the radical scavenging activity of the 26 mangrove extracts. All the extractswere subjected to the Follin-Ciocalteu assay for their phenolic content and the DPPH scavenging assay for the antioxidant activity respectively. Based on the results, the highest phenolic content was observed in ethanol extracts of C. tagal leaves (471.78 ± 0.056 mgGAE/g) while the lowest amount of phenolic was observed in water extract of A. marina root (20.40 ± 0.001 mgGAE/g). Interestingly, the ethanolic extract of C. tagal leaves also exhibited the strongest antioxidant activity with an IC50 value of 9.37 ppm. Among the six species investigated, C. tagal leaves extracts showed high total phenolic content and strong antioxidant activities and may be used as a potential source of natural antioxidants against free radical-associated diseases.

Phylogenomics, plastome structure and species identification in Mahonia (Berberidaceae)

BackgroundElucidating the phylogenetic relationships within species-rich genera is essential but challenging, especially when lineages are assumed to have been going through radiation events. Mahonia Nutt. (Berberidaceae) is a genus with cosmopolitan distribution, comprising approximately 100 species, two of which are known as Caulis Mahoniae (M. bealei and M. fortunei) with crucial pharmacological significance in Chinese herbal medicine. Mahonia is a taxonomically challenging genus, and intrageneric phylogenetic relationships still need to be explored using genome data. Universal DNA barcodes and floral morphological attributes have limited discriminatory power in Mahonia.ResultsWe sequenced 17 representative plastomes and integrated three published plastome data together to conduct comparative and phylogenetic analyses. We found that Mahonia and Berberis share a large IR expansion (~ 12 kb), which is recognized as a typical character of Berberideae. Repeated sequences are revealed in the species of Mahonia, which are valuable for further population genetic studies. Using a comparative plastome analysis, we determined eight hypervariable regions whose discriminative power is comparable to that of the whole plastid genomes. The incongruence of the ITS and the plastome tree topologies may be ascribed to ancestral hybridization events and/or to incomplete lineage sorting. In addition, we suggest that leaf epidermal characters could help to distinguish closely related species in Mahonia.ConclusionsWe propose an integrative approach combining special barcodes and micromorphological traits to circumscribe Mahonia species. The results cast a new light on the development of an integrative method for accurate species circumscription and provide abundant genetic resources for further research on Mahonia.

An Updated Review on Preparation and Characterization of Solid Lipid Nanoparticles

Drug delivery technology has a wide spectrum, which is continuously being upgraded at a stupendous speed. Different fabricated nanoparticles and drugs possessing low solubility and poor pharmacokinetic profiles are the two major substances extensively delivered to target sites. Among the colloidal carriers, nanolipid dispersions (liposomes, deformable liposomes, virosomes, ethosomes, and solid lipid nanoparticles) are ideal delivery systems with the advantages of biodegradation and nontoxicity. Among them, nano-structured lipid carriers and solid lipid nanoparticles (SLNs) are dominant, which can be modified to exhibit various advantages, compared to liposomes and polymeric nanoparticles. Nano-structured lipid carriers and SLNs are non-biotoxic since they are biodegradable. Besides, they are highly stable. Their (nano-structured lipid carriers and SLNs) morphology, structural characteristics, ingredients used for preparation, techniques for their production, and characterization using various methods are discussed in this review. Also, although nano-structured lipid carriers and SLNs are based on lipids and surfactants, the effect of these two matrixes to build excipients is also discussed together with their pharmacological significance with novel theranostic approaches, stability and storage. Solid lipid nanoparticles (SLN) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery and research. Due to their unique size dependent properties, lipid nanoparticles offer possibility to develop new therapeutics. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could use for drug targeting. Hence solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery and hence attracted wide attention of researchers. This review presents a broad treatment of solid lipid nanoparticles discussing their aims, production procedures, advantages, limitations and their possible remedies. Appropriate analytical techniques for the characterization of SLN like photon correlation spectroscopy, scanning electron microscopy, differential scanning calorimetry are highlighted. Aspects of SLN route of administration and the in vivo fate of the carriers are also discussed.

Release kinetics of 3D printed oral solid dosage forms: An overview

Three-dimensional printing (3DP) is one of the most extensively researched methods for producing nano/micro scale biomaterials. This method is typically applied layer by layer. The 3DP method has many advantages over traditional manufacturing methods and ensures that personalized drug design is feasible. Individual dose adjustment provides significant benefits, particularly in some disadvantaged patient groups. Individual release characteristics may be required in these patient groups in addition to dose adjustment. 3DP technology also allows for the adjustment of release kinetics. All of these factors were also increasing interest in 3DP technology in the pharmaceutical industry. The goal of this review is to understand the pharmacological significance of 3DP technology as well as the parameters influencing the release profiles in tablets produced by using technique, and to establish a correlation between them. Within the scope of this review, 79 literature research studies were examined, and it was determined that there is limited data to determine whether there is a correlation between release kinetics and 3DP techniques. When the release profiles obtained by considering the polymer type used in these techniques are evaluated, immediate and rapid release was obtained in studies using PVA + PLA polymers and studies using PVP polymer, immediate release in studies using Kollidon® and Kollicoat® derivatives, and controlled, extended and sustained release was observed in studies using PCL polymer.

The Atypical Antipsychotic Lurasidone Affects Brain but Not Liver Cytochrome P450 2D (CYP2D) Activity. A Comparison with Other Novel Neuroleptics and Significance for Drug Treatment of Schizophrenia.

The aim of this work was to study the effect of prolonged lurasidone administration on the cytochrome 2D (CYP2D) expression and activity in the rat liver and selected brain structures involved in the therapeutic or side effects of this neuroleptic. Male Wistar rats received lurasidone (1 mg/kg ip.) for two weeks. The activity of CYP2D was measured in brain and liver microsomes as the rate of bufuralol 1'-hydroxylation. The CYP2D protein level was determined in microsomes by Western blot analysis. The CYP2D gene expression was estimated in liver tissue by a qRT-PCR method. Lurasidone decreased the activity and protein level of CYP2D in the frontal cortex but increased them in the striatum, nucleus accumbens, brain stem, substantia nigra, and the remainder of the brain. The neuroleptic did not affect CYP2D in the hippocampus, hypothalamus, and cerebellum. In the liver, lurasidone did not affect the CYP2D activity and protein level, though it enhanced the mRNA of CYP2D1 without affecting that of CYP2D2, CYP2D3, CYP2D4, and CYP2D5. In conclusion, lurasidone regulates brain (but not liver) CYP2D activity/protein level in a region-dependent manner, which is similar to that of other atypical neuroleptics (iloperidone and asenapine) as concerns the frontal cortex (down-regulation) and nigrostriatal pathway (up-regulation) and may be of pharmacological significance. However, further molecular studies with selective receptor agonists are necessary to find out which individual monoaminergic receptors/signaling pathways are involved in the regulation of the rat CYP2D4 and human CYP2D6 enzyme in particular brain structures.

Ethnopharmaceutical importance of under-explored plant species Hyptissuaveolens (L.)

Plants store a variety of important secondary metabolites with pharmacognostic and pharmacological implications, some of which have the potential to become super medicines in the future. In-vivo generation of these metabolites is influenced bya number of biotic and abiotic factors resulting in a constant accumulation of various phytochemicals and their derivatives that could be relevant in future medication research and development. There are over 70,000 plant species are employed ethnomedicinally in various ancient medical systems such as Ayurveda, Siddha, and Unani, as well as in Allopathy. The goal of this study is to look into the therapeutic potential of secondary metabolites as well as the probable pharmacological and pharmacognostic significance of the under-explored/underutilized plant Hyptissuaveolens (L.) Poit.Almost all parts of this plant are being employed in conventional drug to treat various diseases. It has been reported that it shows protection against peptic ulcer diseases and has anti-cancerous properties. The leaves of Hyptissuaveolenssecreted essential oil by hydrodistillation have been linked to the genus Hyptis' broad range of biological activity. It contains phytochemicals like alkaloids, tannins, saponins, flavonoids, terpenoids, minerals (like calcium, magnesium, sodium) and metals (like zinc and iron). The ursolic acid found in H. suaveolens can be used as a COVID-19 virus treatment agent. In addition, the ethnobotanical study claims that the beneficial plant has neuroprotective, antioxidant, antibacterial, antidiarrhoeal, anthelmintic, anti-inflammatory, wound healing, insecticidal, antimitotic, anti-proliferative, antisecretory, hepatoprotective, and acaricidal properties. The phytochemicals and extracts obtained from the plant have a great deal of therapeutic promise. As a result, we can use this plant for a variety of purposes.