An insight into the role of experimental parameters in advanced oxidation process applied for pharmaceutical degradation.

The advanced oxidation process (AOP) is an efficient method to treat recalcitrance pollutants such as pharmaceutical compounds. The essential physicochemical factors in AOP experiments significantly influence the efficiency, speed, cost, and safety of byproducts of the treatment process. In this review, we collected recent articles that investigated the elimination of pharmaceutical compounds by various AOP systems in a water medium, and then we provide an overview of AOP systems, the formation mechanisms of active radicals or reactive oxygen species (ROS), and their detection methods. Then, we discussed the role of the main physicochemical parameters (pH, chemical interference, temperature, catalyst, pollutant concentration, and oxidant concentration) in a critical way. We gained insight into the most frequent scenarios for the proper and improper physicochemical parameters for the degradation of pharmaceutical compounds. Also, we mentioned the main factors that restrict the application of AOP systems in a commercial way. We demonstrated that a proper adjustment of AOP experimental parameters resulted in promoting the treatment performance, decreasing the treatment cost and the treatment operation time, increasing the safeness of the system products, and improving the reaction stoichiometric efficiency. The outcomes of this review will be beneficial for future AOP applicants to improve the pharmaceutical compound treatment by providing a deeper understanding of the role of the parameters. In addition, the proper application of physicochemical parameters in AOP systems acts to track the sustainable development goals (SDGs).

Deciphering Campylobacter jejuni DsbA1 protein dynamics in the presence of anti-virulent compounds: a multi-pronged computer-aided approach.

The current study aims to evaluate Asinex library compounds against Campylobacter jejuni DsbA1 protein, a thiol disulfide oxidoreductase enzyme that plays a major role in the oxidative folding of bacterial virulence proteins, making it a promising anti-viral drug target. By employing several techniques of computer-aided drug design, BDC25697459, BDD33601083, and BDC30129064 were identified with binding energy scores of -8.8 kcal/mol, -8.8 kcal/mol, and -8.3 kcal/mol, respectively. However, the control molecule, tetraethylene glycol, exhibited a binding energy score of -7.0 kcal/mol. The control, BDD33601083, and BDC30129064 were unveiled to bind the same co-crystallized binding site (pocket 1), while BDC25697459 interacted with a new binding pocket (pocket 2) adjacent to the control binding region. The molecular dynamics simulation showed that complexes exhibit stable dynamics without significant global or residue-level fluctuations. The average RMSD values were in the range of 2.07 Å-2.45 Å. Similarly, mean RMSF was recorded between 1.30 and 1.42 Å. The C. jejuni DsbA1 was also observed as compact in the presence of the compounds, showing a mean RoG value in the range of 16.42 Å-16.55 Å. In terms of MM/PBSA binding energy, the BDC30129064 complex was ranked top with -44.88 ± 4.14 kcal/mol, whereas the positive control molecule exhibited -22.22 ± 3.33 kcal/mol. From a pharmacokinetic perspective, the compounds are suitable candidates for clinical trial investigation. Preliminary computational analysis of these virtual hits indicates that these compounds have a low potential for ADME and toxicity-associated liabilities. In summary, the compounds displayed a high affinity for the C. jejuni DsbA1 protein, indicating potential efficacy that requires further investigation.Communicated by Ramaswamy H. Sarma.

Utilization of Waste Eggshell Powder as an Excipient for Vitamin D3 Tablet Preparation.

Keeping in mind the health scenario in Kingdom of Saudi Arabia with respect to vitamin D3 (VD3) deficiency and its significant role in calcium homeostasis and human metabolism, this research is exploring the combination of eggshell (as a source of calcium) and VD3 as a very economical solution for this problem. Eggshells from local restaurant were collected, washed, ground, sieved, and characterized by Fourier transforms infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Brunauer-Emmett-Teller (BET) techniques. The results of FTIR, SEM, DSC, XRD, and BET indicate that eggshell powder (ESP) was properly processed. Directly compressed tablets containing 2.5 mg of VD3 (equivalent to 50,000 IU), that are based on the use of ESP as tablet filler, were manufactured based on mixing Avicel PH 101 with ESP in different ratios (9:1, 1:1, and 1:9) in addition to the use of both Avicel PH 101 and ESP alone as tablet filler. Tablets properties were evaluated according to USP30-NF25 pharmacopoeia tests in terms of weight variation test, drug content uniformity, tablet hardness, tablet friability, tablet disintegration, and in vitro dissolution profile. The VD3 contents were found to be 98.77-102.35% in all formulations. After 90 min of study, all formulations showed in vitro drug release content in the range of 99.29-101.05%. All of the tested parameters of ESP tablets were similar to those of commercial Avicel PH 101. All of the tested properties of tablets with ESP as a filler were found to be within the acceptable limits of the pharmacopeia recommendations. Therefore, ESP could be exploited for its use as a filler in direct compression tablets.

Eco-Friendly High-Performance Thin-Layer Chromatography Method for the Determination of Tenoxicam in Commercial Formulations.

There is a dearth of information in the literature regarding environmentally benign high-performance thin-layer chromatography (HPTLC) methods to determine tenoxicam (TNX). Therefore, designing and validating an HPTLC method to detect TNX in commercial tablets and capsules was the goal of this investigation. The green mobile phase utilized was the combination of ethanol/water/ammonia solution (50:45:5 v/v/v). The TNX was quantified at a wavelength of 375 nm. The proposed method's greenness profile was established using the Analytical GREEnness (AGREE) approach. The proposed methodology for determining TNX was linear in the range of 25-1400 ng/band. The proposed methodology for measuring TNX was accurate (% recoveries = 98.24-101.48), precise (% RSD = 0.87-1.02), robust (% RSD = 0.87-0.94), sensitive (LOD = 0.98 ng/band and LOQ = 2.94 ng/band), and environmentally friendly. The AGREE scale for the present methodology was derived to be 0.75, indicating an outstanding greenness profile. TNX was found to be highly stable under acidic, base, and thermal stress conditions. However, it completely decomposed under oxidative stress conditions. Commercial tablets and capsules were found to have 98.46 and 101.24% TNX, respectively. This finding supports the validity of the current methodology for measuring TNX in commercial formulations. The outcomes of this work showed that the proposed eco-friendly HPTLC methodology can be used for the routine analysis of TNX in commercial formulations.

Quantification of Suvorexant in Human Urine Using a Validated HPTLC Bioanalytical Method.

Suvorexant (SUV) is a new sedative/hypnotic medicine that is recommended to treat insomnia. It is an important medicine from a forensic point of view due to its sedative/hypnotic and depressant effects. To the best of our knowledge, high-performance thin-layer chromatography (HPTLC) bioanalytical methods have not been published to measure SUV in human urine and pharmaceutical samples. Accordingly, this study was designed and validated a sensitive and rapid bioanalytical HPTLC method to determine SUV in human urine samples for the very first time. The densitometric measurement of SUV and the internal standard (IS; sildenafil) was performed on glass-coated silica gel normal-phase-60F254S TLC plates using a mixture of chloroform and methanol (97.5:2.5 v/v) as the eluent system. Both the SUV and IS were detected at a wavelength of 254 nm. Both analytes were extracted using the protein precipitation technique utilizing methanol as the solvent. For the IS and SUV, the Rf values were 0.09 and 0.45, respectively. The proposed bioanalytical method for SUV was linear in the 50-1600 ng/band range. The current bioanalytical technique was linear, precise (% RSD = 3.28-4.20), accurate (% recovery = 97.58-103.80), robust (% recovery = 95.31-102.34 and % RSD = 2.81-3.15), rapid, and sensitive (LOD = 3.73 ng/band and LOQ = 11.20 ng/band). These findings suggested that the current bioanalytical method can be regularly used to determine SUV in wide varieties of urine samples.

Quantification of Pomalidomide Using Conventional and Eco-Friendly Stability-Indicating HPTLC Assays: A Contrast of Validation Parameters.

High-performance thin-layer chromatographic (HPTLC) assays for pomalidomide (PMD) measurement are lacking in the published database. Furthermore, eco-friendly stability-indicating analytical assays for PMD measurement are also lacking in the published database. In order to detect PMD in commercial products more accurately and sustainably than the conventional normal-phase HPTLC (NP-HPTLC) assay, an effort was made to design and verify a sensitive and eco-friendly reversed-phase HPTLC (RP-HPTLC) assay. The silica gel 60 NP-18F254S and 60 RP-18F254S plates were used as the stationary phases for NP-HPTLC and RP-HPTLC methods, respectively. The solvent system for NP-HPTLC was chloroform-methanol (90:10 v/v). However, the solvent system for RP-HPTLC was ethanol-water (75:25 v/v). The greenness scores for both assays were measured by AGREE approach. PMD measurement was performed for both assays at 372 nm. In the 50-600 and 20-1000 ng/band ranges, the NP-HPTLC and RP-HPTLC methods were linear for PMD measurement. The RP-HPTLC assay was superior to the NP-HPTLC method for measuring PMD in terms of sensitivity, accuracy, precision, and robustness. The ability of both methods to identify PMD in the presence of its degradation products suggests that both methods have stability-indicating features. When employing the NP-HPTLC and RP-HPTLC assays, respectively, the assay for PMD in commercial capsules was 88.68 and 98.83%. The AGREE scores for NP-HPTLC and RP-HPTLC assays were calculated to be 0.44 and 0.82, respectively, suggesting an outstanding greenness characteristic of the RP-HPTLC method than the NP-HPTLC method. The RP-HPTLC method was found to be superior to the NP-HPTLC method based on these findings. Therefore, the RP-HPTLC method could be successfully applied for the determination of PMD in pharmaceutical products.

Insight into Structure Activity Relationship of DPP-4 Inhibitors for Development of Antidiabetic Agents.

This article sheds light on the various scaffolds that can be used in the designing and development of novel synthetic compounds to create DPP-4 inhibitors for the treatment of type 2 diabetes mellitus (T2DM). This review highlights a variety of scaffolds with high DPP-4 inhibition activity, such as pyrazolopyrimidine, tetrahydro pyridopyrimidine, uracil-based benzoic acid and esters, triazole-based, fluorophenyl-based, glycinamide, glycolamide, ß-carbonyl 1,2,4-triazole, and quinazoline motifs. The article further explains that the potential of the compounds can be increased by substituting atoms such as fluorine, chlorine, and bromine. Docking of existing drugs like sitagliptin, saxagliptin, and vildagliptin was done using Maestro 12.5, and the interaction with specific residues was studied to gain a better understanding of the active sites of DPP-4. The structural activities of the various scaffolds against DPP-4 were further illustrated by their inhibitory concentration (IC50) values. Additionally, various synthesis schemes were developed to make several commercially available DPP4 inhibitors such as vildagliptin, sitagliptin and omarigliptin. In conclusion, the use of halogenated scaffolds for the development of DPP-4 inhibitors is likely to be an area of increasing interest in the future.

An immuno-informatics approach for annotation of hypothetical proteins and multi-epitope vaccine designed against the Mpox virus.

A worrying new outbreak of Monkeypox (Mpox) in humans is caused by the Mpox virus (MpoxV). The pathogen has roughly 28 hypothetical proteins of unknown structure, function, and pathogenicity. Using reliable bioinformatics tools, we attempted to analyze the MpoxV genome, identify the role of hypothetical proteins (HPs), and design a potential candidate vaccine. Out of 28, we identified seven hypothetical proteins using multi-server validation with high confidence for the occurrence of conserved domains. Their physical, chemical, and functional characterizations, including molecular weight, theoretical isoelectric point, 3D structures, GRAVY value, subcellular localization, functional motifs, antigenicity, and virulence factors, were performed. We predicted possible cytotoxic T cell (CTL), helper T cell (HTL) and linear and conformational B cell epitopes, which were combined in a 219 amino acid multiepitope vaccine with human ß defensin as a linker. This multi-epitopic vaccine was structurally modelled and docked with toll-like receptor-3 (TLR-3). The dynamical stability of the vaccine-TLR-3 docked complexes exhibited stable interactions based on RMSD and RMSF tests. Additionally, the modelled vaccine was cloned in-silico in an E. coli host to check the appropriate expression of the final vaccine built. Our results might conform to an immunogenic and safe vaccine, which would require further experimental validation.Communicated by Ramaswamy H. Sarma.

Developing Nanosuspension Loaded with Azelastine for Potential Nasal Drug Delivery: Determination of Proinflammatory Interleukin IL-4 mRNA Expression and Industrial Scale-Up Strategy.

In order to increase bioavailability and intranasal absorbance, the current work set out to create azelastine nasal spray based on nanosuspension. Chondroitin was utilized as a polymer to prepare azelastine nanosuspension through the precipitation procedure. A size of 500 nm and a polydispersity index of 0.276 with a negative potential (-20 mV) were achieved. X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, thermal analysis including differential scanning calorimetry and thermogravimetric analysis, in vitro release, and diffusion studies were used to characterize the optimized nanosuspension. MTT assay was used to assess the viability of the cells, and hemolysis assay was used to assess the blood compatibility. Using RNA extraction and reverse transcription polymerase chain reaction, the levels of the anti-inflammatory cytokine IL-4, which is most closely related to cytokines in allergic rhinitis, were measured in mouse lungs. The drug dissolution and diffusion study indicated 2.0-fold increase compared to pure reference sample. Therefore, the azelastine nanosuspension could be suggested as a practical and simple nanosystem for intranasal delivery with improved permeability and bioavailability. The outcome obtained in this study indicated that azelastine nanosuspension has great potential to treat allergic rhinitis as intranasal treatment.

A Rapid and Sensitive Stability-Indicating Eco-Friendly HPTLC Assay for Fluorescence Detection of Ergotamine.

Eco-friendly liquid chromatographic methods for measuring ergotamine (EGT) are scant in the published database. Accordingly, the goal of the current study was to develop a high-performance thin-layer chromatography (HPTLC) method for fluorescence detection of EGT in commercially available tablets. This approach was based on the application of ethyl alcohol-water (80:20 v/v) as the eco-friendly eluent mixture. The fluorescence detection of EGT was carried out at 322 nm. The greenness score of the present approach was evaluated by "Analytical GREENness (AGREE)" technology. The present approach for measuring EGT in the 25-1000 ng band-1 range was linear. The present assay for fluorescence detection of EGT was validated successfully by ICH guidelines for various parameters. The method was found to be rapid, sensitive, eco-friendly, and stability-indicating. The computed AGREE index for the current strategy was 0.84, displaying outstanding greenness features. The present methodology successfully separated the EGT degradation products under forced-degradation circumstances, exhibiting its stability-indicating qualities and selectivity. An amount of 99.33% of EGT was found in commercial formulations, indicating the validity of the current method for pharmaceutical analysis of EGT in commercial products. The results showed that EGT in commercial products might be regularly measured by the existing method.

Optimisation of a Greener-Approach for the Synthesis of Cyclodextrin-Based Nanosponges for the Solubility Enhancement of Domperidone, a BCS Class II Drug.

BCS class II molecules suffer from low oral bioavailability because of their poor permeability and sub-optimal aqueous solubility. One of the approaches to enhance their bioavailability is using cyclodextrin-based nanosponges. This study aimed to optimise and evaluate the feasibility of a microwave-assisted approach to synthesise nanosponges and improve domperidone's solubility and drug delivery potential. In the production process, microwave power level, response speed, and stirring speed were optimised using the Box-Behnken approach. Ultimately, the batch with the smallest particle size and highest yield was chosen. The optimised method of synthesis of the nanosponges resulted in a product yield of 77.4% and a particle size of 195.68 ± 2.16 nm. The nanocarriers had a drug entrapment capacity of 84 ± 4.2% and a zeta potential of -9.17± 0.43 mV. The similarity and the difference factors demonstrated proof-of-concept, showing that the drug release from the loaded nanosponges is significantly greater than the plain drug. Additionally, spectral and thermal characterisations, such as FTIR, DSC, and XRD, confirmed the entrapment of the drug within the nanocarrier. SEM scans revealed the porous nature of the nanocarriers. Microwave-assisted synthesis could be used as a better and greener approach to synthesise these nanocarriers. It could then be utilised to load drugs and improve their solubility, as seen in the case of domperidone.

Combination of Cellulose Derivatives and Chitosan-Based Polymers to Investigate the Effect of Permeation Enhancers Added to In Situ Nasal Gels for the Controlled Release of Loratadine and Chlorpheniramine.

The purpose of the study is to develop and assess mucoadhesive in situ nasal gel formulations of loratadine and chlorpheniramine maleate to advance the bioavailability of the drug as compared to its conventional dosage forms. The influence of various permeation enhancers, such as EDTA (0.2% w/v), sodium taurocholate (0.5% w/v), oleic acid (5% w/v), and Pluronic F 127 (10% w/v), on the nasal absorption of loratadine and chlorpheniramine from in situ nasal gels containing different polymeric combinations, such as hydroxypropyl methylcellulose, Carbopol 934, sodium carboxymethylcellulose, and chitosan, is studied. Among these permeation enhancers, sodium taurocholate, Pluronic F127 and oleic acid produced a noticeable increase in the loratadine in situ nasal gel flux compared with in situ nasal gels without permeation enhancer. However, EDTA increased the flux slightly, and in most cases, the increase was insignificant. However, in the case of chlorpheniramine maleate in situ nasal gels, the permeation enhancer oleic acid only showed a noticeable increase in flux. Sodium taurocholate and oleic acid seems to be a better and efficient enhancer, enhancing the flux > 5-fold compared with in situ nasal gels without permeation enhancer in loratadine in situ nasal gels. Pluronic F127 also showed a better permeation, increasing the effect by >2-fold in loratadine in situ nasal gels. In chlorpheniramine maleate in situ nasal gels with EDTA, sodium taurocholate and Pluronic F127 were equally effective, enhancing chlorpheniramine maleate permeation. Oleic acid has a better effect as permeation enhancer in chlorpheniramine maleate in situ nasal gels and showed a maximum permeation enhancement of >2-fold.

Nanomaterials-Based Novel Immune Strategies in Clinical Translation for Cancer Therapy.

Immunotherapy shows a lot of promise for addressing the problems with traditional cancer treatments. Researchers and clinicians are working to create innovative immunological techniques for cancer detection and treatment that are more selective and have lower toxicity. An emerging field in cancer therapy, immunomodulation offers patients an alternate approach to treating cancer. These therapies use the host's natural defensive systems to identify and remove malignant cells in a targeted manner. Cancer treatment is now undergoing somewhat of a revolution due to recent developments in nanotechnology. Diverse nanomaterials (NMs) have been employed to overcome the limits of conventional anti-cancer treatments such as cytotoxic, surgery, radiation, and chemotherapy. Aside from that, NMs could interact with live cells and influence immune responses. In contrast, unexpected adverse effects such as necrosis, hypersensitivity, and inflammation might result from the immune system (IS)'s interaction with NMs. Therefore, to ensure the efficacy of immunomodulatory nanomaterials, it is essential to have a comprehensive understanding of the intricate interplay that exists between the IS and NMs. This review intends to present an overview of the current achievements, challenges, and improvements in using immunomodulatory nanomaterials (iNMs) for cancer therapy, with an emphasis on elucidating the mechanisms involved in the interaction between NMs and the immune system of the host.

Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation.

Luliconazole is a broad-spectrum topical antifungal agent that acts by altering the synthesis of fungi cell membranes. Literature suggests that the recurrence of fungal infection can be avoided by altering the pH of the site of infection. Studies have also suggested that fungi thrive by altering skin pH to be slightly acidic, i.e., pH 3-5. The current study is aimed to design, develop, characterize, and evaluate an alkaline pH-based antifungal spray solution for antifungal effects. Luliconazole was used as an antifungal agent and an alkaline spray was formulated for topical application by using Eudragit RS 100, propylene glycol (PG), water, sodium bicarbonate, and ethanol via solubilization method. Herein, sodium bicarbonate was used as an alkalizing agent. Based on DSC, FTIR, PXRD, scanning electron microscopy (SEM), and rheological analysis outcomes, the drug (luliconazole) and polymer were found to be compatible. F-14 formulation containing 22% Eudragit RS 100 (ERS), 1.5% PG, and 0.25% sodium bicarbonate was optimized by adopting the quality by design approach by using design of experiment software. The viscosity, pH, drying time, volume of solution post spraying, and spray angle were, 14.99 ± 0.21 cp, 8 pH, 60 s, 0.25 mL ± 0.05 mL, and 80 ± 2, respectively. In vitro drug diffusion studies and in vitro antifungal trials against Candida albicans revealed 98.0 ± 0.2% drug diffusion with a zone of inhibition of 9 ± 0.12 mm. The findings of the optimized luliconazole topical film-forming solution were satisfactory, it was compatible with human skin, and depicted sustained drug release that suggests promising applicability in facilitated topical antifungal treatments.

Formulation, In Vitro and In Silico Evaluations of Anise (Pimpinella anisum L.) Essential Oil Emulgel with Improved Antimicrobial Effects.

Over the past decade, researchers have made several efforts to develop gel-based formulations that provide an alternative to traditional hydrogels and emulgel. Due to its excellent antibacterial properties, anise, the main constituent of Pimpinella anisum L., widely used in pharmaceuticals, was selected as the active ingredient in this study. Since many bacteria have developed considerable antibiotic resistance, this research aimed to develop an herbal emulgel for treating skin infections caused by bacteria. Given these obstacles, we developed and evaluated a new, cost-effective topical emulgel solution containing anise essential oil against Escherichia coli (E. coli). Anise-based emulgels, potential drug delivery platforms, have been evaluated for various parameters, including physical properties, viscosity, pH, rheology, encapsulation efficiency, and in vitro release research. The AEOs emulgel demonstrated remarkable colloidal stability, with a zeta potential of 29 mV, a size of 149.05 nm, and considerable polydispersity. The efficacy of anise-loaded emulgels as antibacterial formulations was evaluated in vitro. E. coli was used as a model microbial organism for the antibacterial study. Human keratinocytes (HaCaT) were used to examine the biocompatibility of the emulgel. Molecular docking revealed that the essential oil components of Pimpinella anisum L. possess a high affinity for the bacterial adhesin protein FimH of E. coli. These findings indicate that the developed AEOs have the potential to be analyzed using E. coli as a model organism.

Pyrazoline scaffold: hit identification to lead synthesis and biological evaluation as antidiabetic agents.

Background: Mining of novel scaffolds as potential DPP-IV inhibitors for future development of potential candidates as antidiabetic agents to address global issues. Methodology: The identified hit KB-10 from a previously reported study was taken as a lead for designing a library of analogues and screened initially based on in silico parameters and docking score. A series of selected (2[4-(1-acetyl-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenoxy]-1-phenylethanone derivatives were synthesized and evaluated through in vitro studies. Compounds KB-23, KB-22 and KB-06 were found to be as potent, with IC50 values of 0.10 µM, 0.12 µM and 0.35 µM, respectively. They also showed promising antihyperglycemic potential in in vivo studies (oral glucose tolerance tests) in Wistar rats. Conclusion: This work establishes pyrazoline analogues KB-23, KB-22 and KB-06 as promising starting points for the development of potential antidiabetic agents.

Molecular insight into the modulation of ovalbumin fibrillation by allura red dye at acidic pH.

The synthetic food additive dye induces amyloid fibrillation has many implications in the laboratory and industries. The effect of Allura red (AR), on the fibrillation of ovalbumin (Ova) at pH 2.0 was investigated. The influence of salt and pH was also seen on AR-induced Ova aggregation. We have used several spectroscopic and microscopy techniques to characterize the changes. The turbidity data suggest that concentrations above 0.05 mM of AR induce aggregation, and the size of aggregates increased in response to AR concentration. The kinetics data showed that the AR induces Ova aggregation quickly without lag time. The aggregates induced by AR have amyloid-like aggregates confirmed by far-UV CD and TEM. NaCl has very marginal effects in AR-induced aggregation. The turbidity results clearly state that Ova is not forming aggregates with pH above 4.0 due to electrostatic repulsion. However, Ova forms bigger aggregates in the presence of 0.5 mM AR at a pH below 4.0. These spectroscopic data suggest that the amyloid fibrillation that occurs in Ova is due to electrostatic and hydrophobic interaction. The amyloid fibrillation induced by AR dye in protein should be taken seriously for food safety purposes.

Tween 80-Based Self-Assembled Mixed Micelles Boost Valsartan Transdermal Delivery.

Valsartan (Val) is an important antihypertensive medication with poor absorption and low oral bioavailability. These constraints are due to its poor solubility and dissolution rate. The purpose of this study was to optimize a mixed micelle system for the transdermal delivery of Val in order to improve its therapeutic performance by providing prolonged uniform drug levels while minimizing drug side effects. Thin-film hydration and micro-phase separation were used to produce Val-loaded mixed micelle systems. A variety of factors, including the surfactant type and drug-to-surfactant ratio, were optimized to produce micelles with a low size and high Val entrapment efficiency (EE). The size, polydispersity index (PDI), zeta potential, and drug EE of the prepared micelles were all measured. The in vitro drug release profiles were assessed using dialysis bags, and the permeation through abdominal rat skin was assessed using a Franz diffusion cell. All formulations had high EE levels exceeding 90% and low particle charges. The micellar sizes ranged from 107.6 to 191.7 nm, with average PDI values of 0.3. The in vitro release demonstrated a uniform slow rate that lasted one week with varying extents. F7 demonstrated a significant (p < 0.01) transdermal efflux of 68.84 ± 3.96 µg/cm2/h through rat skin when compared to the control. As a result, the enhancement factor was 16.57. In summary, Val-loaded mixed micelles were successfully prepared using two simple methods with high reproducibility, and extensive transdermal delivery was demonstrated in the absence of any aggressive skin-modifying enhancers.

Promising Role of Silk-Based Biomaterials for Ocular-Based Drug Delivery and Tissue Engineering.

Silk is a wonderful biopolymer that has a long history of medical applications. Surgical cords and medically authorised human analogues made of silk have a long history of use in management. We describe the use of silk in the treatment of eye diseases in this review by looking at the usage of silk fibroin for eye-related drug delivery applications and medication transfer to the eyes. During this ancient art endeavour, a reduced engineering project that employed silk as a platform for medicine delivery or a cell-filled matrix helped reignite interest. With considerable attention, this study explores the present usage of silk in ocular-based drug delivery. This paper also examines emerging developments with the use of silk as a biopolymer for the treatment of eye ailments. As treatment options for glaucoma, diabetic retinopathy, retinitis pigmentosa, and other retinal diseases and degenerations are developed, the trans-scleral route of drug delivery holds great promise for the selective, sustained-release delivery of these novel therapeutic compounds. We should expect a swarm of silk-inspired materials to enter clinical testing and use on the surface as the secrets of silk are unveiled. This article finishes with a discussion on potential silk power, which adds to better ideas and enhanced ocular medicine delivery.

Recent Advancement in Drug Design and Discovery of Pyrazole Biomolecules as Cancer and Inflammation Therapeutics.

Pyrazole, an important pharmacophore and a privileged scaffold of immense significance, is a five-membered heterocyclic moiety with an extensive therapeutic profile, viz., anti-inflammatory, anti-microbial, anti-anxiety, anticancer, analgesic, antipyretic, etc. Due to the expansion of pyrazolecent red pharmacological molecules at a quicker pace, there is an urgent need to put emphasis on recent literature with hitherto available information to recognize the status of this scaffold for pharmaceutical research. The reported potential pyrazole-containing compounds are highlighted in the manuscript for the treatment of cancer and inflammation, and the results are mentioned in % inhibition of inflammation, % growth inhibition, IC50, etc. Pyrazole is an important heterocyclic moiety with a strong pharmacological profile, which may act as an important pharmacophore for the drug discovery process. In the struggle to cultivate suitable anti-inflammatory and anticancer agents, chemists have now focused on pyrazole biomolecules. This review conceals the recent expansion of pyrazole biomolecules as anti-inflammatory and anticancer agents with an aim to provide better correlation among different research going around the world.