Sesame lignans as promising anti-inflammatory agent: Exploring novel therapeutic avenues with in silico and computational approach

Innumerable health-beneficial properties of sesame lignans like sesamol, sesamolin, sesamin and sesaminol make them lucrative agents in the pharmaceutical industry. To specify the mode of action of these phytochemicals, detailed computational physicochemical properties evaluation, and toxicity assessment (using free web servers and databases), as well as binding interactions with physiological inflammatory effectors (such as COX-2, TNF-α, IL-1β, IL-6) by means of rigid ligand-receptor docking (using software), have been thoroughly investigated. Interestingly, sesame lignans are conformed to have drug-likeness, indicating their efficacy and suitability like established therapeutics. These bioactive lignans possess drug-like attributes and effectively act as ligands in the present in-silico study. The basic pharmacokinetic profile of these compounds has suggested non-polar solvents or delivery systems for them to enhance their bioavailability in physiological systems. However, all the sesame lignans are toxic to the liver cells with a50 % lethal dose in the range of 500-1500 mg/kg. Toxicity study indicated minimum toxicity of lignans to normal cellular milieu, but noticeable cytotoxic effects against several cancerous cell lines suggesting their anti-carcinogenic properties. Finally, the findings of the molecular docking study have depicted a high affinity of these ligands for target proteins, even better than traditional anti-inflammatory drugs- Indomethacin and Ibuprofen. The molecular interactions have represented sesaminol as the most effective and Sesamol as the least potent ligand for target receptor whereas COX-2 seems to be the most vulnerable target. The docking scores varied widely (-4.7 to -11.0 kcal/mol). The present in-silico approach is expected to provide valuable resources for optimizing bioactive molecules as future-generation therapeutics before pre-clinical and clinical studies

A REVIEW ON PRESENT AND FUTURE OUTLOOK OF 3D PRINTING IN TRANSDERMAL DRUG DELIVERY SYSTEMS

Objective The suitability of different printing processes for the direct or indirect printing of microneedle arrays, as well as the modification of their surface with drug-containing coatings, has been investigated. Methodology 3D printing refers to a group of technologies that use numerically controlled apparatus to create a physical object from a virtual representation. The transdermal route has been introduced as an alternative to the bolus system. The skin is also identified to pose a barrier to permit molecules. The loss that occurred is compensated by transdermal delivery. 3D printing has several advantages in terms of waste reduction, design flexibility, and lowering the high cost. The compatibility of 3D printing techniques with printed medicine products is a factor in their selection. The variety of printable materials that are presently being used or could be utilized for 3D printing of transdermal drug delivery (TDD) devices. 3D printing has the potential to change today's "one size fits all" production and be used across the medication development process. Conclusion The impact and limitations of using 3D printing as a production process for transdermal drug delivery devices are required to be evaluated. This review discusses the present and future overlook of 3D printing technology of transdermal drug delivery system and some advantages and disadvantages of 3D printing technology over conventional drug delivery approach

Sesame lignans as promising anti-inflammatory agent: Exploring novel therapeutic avenues with in silico and computational approach

547-559Innumerable health-beneficial properties of sesame lignans like sesamol, sesamolin, sesamin and sesaminol make them lucrative agents in the pharmaceutical industry. To specify the mode of action of these phytochemicals, detailed computational physicochemical properties evaluation, and toxicity assessment (using free web servers and databases), as well as binding interactions with physiological inflammatory effectors (such as COX-2, TNF-α, IL-1β, IL-6) by means of rigid ligand-receptor docking (using software), have been thoroughly investigated. Interestingly, sesame lignans are conformed to have drug-likeness, indicating their efficacy and suitability like established therapeutics. These bioactive lignans possess drug-like attributes and effectively act as ligands in the present in-silico study. The basic pharmacokinetic profile of these compounds has suggested non-polar solvents or delivery systems for them to enhance their bioavailability in physiological systems. However, all the sesame lignans are toxic to the liver cells with a50 % lethal dose in the range of 500-1500 mg/kg. Toxicity study indicated minimum toxicity of lignans to normal cellular milieu, but noticeable cytotoxic effects against several cancerous cell lines suggesting their anti-carcinogenic properties. Finally, the findings of the molecular docking study have depicted a high affinity of these ligands for target proteins, even better than traditional anti-inflammatory drugs- Indomethacin and Ibuprofen. The molecular interactions have represented sesaminol as the most effective and Sesamol as the least potent ligand for target receptor whereas COX-2 seems to be the most vulnerable target. The docking scores varied widely (-4.7 to -11.0 kcal/mol). The present in-silico approach is expected to provide valuable resources for optimizing bioactive molecules as future-generation therapeutics before pre-clinical and clinical studies

Biochemical assessment of extract from <em>Oxalis corniculata</em> L.: Its role in food preservation, antimicrobial and antioxidative paradigms using <em>in situ</em> and <em>in vitro</em> models

230-243Food poisoning, often due to microbial contamination and improper storage practice, is a matter of concern. Plants and plant based products are gaining interest in processed food in food industry as an alternative to synthetic antimicrobials. In this context, here, we analysed flavonoid rich methanolic extract from the creeping woodsorrel, Oxalis corniculata L. leaf for its biochemical assessments along with its bioactivity against some common pathogenic bacteria. The bioactivity of the extract as evaluated in both in vitro and in situ methods, verified that the Oxalis corniculata leafextract exert reduces power, hydroxyl radical scavenging activity, inhibition in liposome peroxidation, and DPPH free radical quenching activity. The extract also inhibited the formation of peroxide during subsequent storage in the oil-emulsion system as well as in heated oil. The greater reducing activity of the extract prevented hydroxyl radical induced pUC18 DNA strand breaks and there by retain its original conformation. The extract also prevented the oxidative damage of goat liver cells during Fenton reaction. In vitro antimicrobial experiments implied that extract has inhibitory effect against Staphylococcus aureus, Escherichia coli, Salmonella Typhi, S. Typhiimurium and Vibrio cholera. E. coli showed the highest and V. cholera the lowest sensitivities against the extract. Moreover, the extract can be utilized for preservation of fish meat as it prevented the growth of food poisoning bacteria S. aureus during storage at 10°C. HPLC chromatogram detected the predominance of three active principal components, i.e. flavonoids in the following order: rutin>p-hydroxybenzoic acid>ferulic acid

A brief review on recent advancement of tablet coating technology

A tablet can be defined as a solid unit dosage form. There are several reasons for coating of solid dosage form, the most important reason is to control the release profile &amp; also to control the bioavailability parameters of the APIs (Active Pharmaceutical Ingredients). Tablets containing active pharmaceutical ingredients (API) can be coated with thin polymer-based film for various advantages. Generally, horizontal rotating pans are used for coating purposes &amp; coating solution can be spread through the spraying systems over the surface of tablets. Bitter taste masking, odor masking, physical and chemical protection, and also environmental protection are all benefits of the tablet coating. Despite that, Tablet coating also plays an important role in controlling the action site. Sugar-coating, film coating, and enteric coating are some of the conventional tablet coating processes. The primary objective for creating tablet coating technologies is to eliminate the numerous disadvantages of solvent-based coating. Coating solution preferentially applied on the surface of solid dosage forms without the need for any solvent in these novel technologies. This review article provides information regarding the techniques of conventional tablet coating, the recent advancement of tablet coating procedures, and tablet coating components

Fabrication of rice bran oil nanoemulsion and conventional emulsion with Mustard Protein Isolate as a novel excipient: Focus on shelf-life stability, lipid digestibility and cellular bioavailability

Proteins are one of the many effective biomolecules found in oilseed meals. In order to formulate an oil-in-water nanoemulsion based lipophilic nutraceutical delivery vehicle for Rice Bran oil (RBO) rich in γ-oryzanol, we used mustard seed meal protein isolate (MPI) as a novel natural surfactant together with a small molecular weight co-surfactant Tween 20 in various ratios (3:1, 1:1, 1:3) to stabilize the heterogeneous system. The oxidative stability, physico-chemical characterization in response to pH and ionic strength, shelf-life, and storage of the nanoemulsions containing 1% surfactant in total, comprising different ratios of MPI and Tween 20 were optimised to form an efficient biphasic surfactant system. The oil-in-water nanoemulsions fabricated utilizing high energy approach, i.e. high pressure homogenisation method was found to reduce dispersed phase particles size in the range of 150–160 nm. Minimal non-significant variation in droplet size and surface charge over the 8 weeks storage periods proves their excellent shelf-life stability. The use of MPI as surfactant for the delivery system also increased the lipid fraction digestibility releasing 70% of the fatty acids from dispersed phase oil droplets in simulated intestinal phase of three step in vitro digestion of nanoemulsion as compared to its conventional counterpart. The γ-oryzanol rich nanoemulsions improved prophylactic effectiveness against ROS in terms of overall cell survival and cell membrane integrity. The results will pave new domains to use MPI as surface active agents for delivery system formulation enriched with nutraceuticals and phytochemicals possessing superior functional advantages, bioavailability and antioxidative potentials