Diuretic effects of Hecogenin and Hecogenin acetate via aldosterone synthase inhibition.

Hecogenin (HEC) is a steroidal saponin found in many plant species and serves as a precursor for steroidal drugs. The diuretic effects of HEC and its derivative, hecogenin acetate (HA), remain largely unexplored. The present study aimed to explore the potential diuretic effects of HEC and HA compared to furosemide (FUR) and spironolactone (SPIR). Additionally, the study aimed to explore the underlying mechanism particularly focusing on aldosterone synthase gene expression. Fifty-four Sprague-Dawley rats were allocated into nine groups (Group 1-9). Group 1 (control) received the vehicle, Groups 2 received FUR 10 mg/kg, Group 3, 4, and 5 were given HEC, while Groups 6, 7 and 8 received HA i.p at doses of 5, 10, and 25 mg/kg, respectively. Group 9 received SPIR i.p at the dose of 25 mg/kg. Urine volume, diuretic index and diuretic activity were monitored at 1, 2, 3, 4, 5, 6, and 24 h post-administration. Treatment was given daily for seven days. After that, rats were sacrificed and blood was collected for serum electrolytes determination. Adrenal glands were dissected out for gene expression studies. The results revealed that HEC and HA at the administered doses significantly and dose-dependently increased urine and electrolyte excretion. These results were primarily observed at 25 mg/kg of each compound. Gene expression studies demonstrated a dose-dependent reduction in aldosterone synthase gene expression, suggesting aldosterone synthesis inhibition as a potential mechanism for their diuretic activity. Notably, HA exhibited more pronounced diuretic effects surpassing those of HEC. This enhanced diuretic activity of HA can be attributed to its stronger impact on aldosterone synthase inhibition. These findings offer valuable insights into the diuretic effects of both HEC and HA along with their underlying molecular mechanisms.

Synthesis, Characterization, and Investigation of Novel Ionic Liquid-Based Tooth Bleaching Gels: A Step towards Safer and Cost-Effective Cosmetic Dentistry.

The objective of this study was to synthesize a novel choline hydroxide ionic liquid-based tooth bleaching gel. Ionic liquid-based gels were synthesized and characterized using FTIR along with pH testing. Tooth sample preparation was carried out in line with ISO 28399:2020. The effects of synthesized gels on tooth samples were tested. Tooth samples were stained and grouped into three experimental groups: EAI (22% choline hydroxide gel), EAII (44% choline hydroxide gel), and EB (choline citrate gel) and two control groups: CA (commercial at-home 16% carbamide peroxide gel) and CB (deionized water). The tooth color analysis, which included shade matching with the Vitapan shade guide (n = 2), and digital colorimetric analysis (n = 2) were evaluated. The surface characteristics and hardness were analyzed with 3D optical profilometry, Scanning Electron Microscopy (SEM), Energy Dispersive X-ray Spectroscopy (EDX), and Microhardness testing (n = 3), respectively. The tooth color analysis (Vitapan shade guide) revealed that all the tooth samples treated with synthesized choline citrate gel (EB) showed an A1 shade as compared to the other four groups, giving a range of shades. An analysis of the ΔE values from digital colorimetry; EAI, EAII, CA, and CB showed ΔE values in a range that was clinically perceptible at a glance. However, EB showed the highest value of ΔE. The mean microhardness values for the five groups showed that the effects of three experimental gels i.e., 44% choline hydroxide, 22% choline hydroxide, and choline citrate, on the microhardness of the tooth samples were similar to that of the positive control, which comprised commercial at-home 16% carbamide peroxide gel. SEM with EDX of three tested subgroups was closely related in surface profile, elemental composition, and Ca/P ratio. The roughness average values from optical profilometry of four tested subgroups lie within approximately a similar range, showing a statistically insignificant difference (p > 0.05) between the tested subgroups. The synthesized novel experimental tooth bleaching gels displayed similar tooth bleaching actions without any deleterious effects on the surface characteristics and microhardness of the treated tooth samples when compared with the commercial at-home tooth bleaching gel.

Formulation design and evaluation of epalrestat mouth dissolving tablets comprising superdisintegrant from natural sources manufactured by direct compression method and stability studies of optimized formulation.

Among the oral route, mouth dissolving tablets (MDTs) offer a benefit for drugs with slow dissolution and having low oral bioavailability. Epalrestat is one of the best effective diabetic neuropathy medication used for treating nerve pain. The problem associated with this drug is high first pass metabolism and low solubility in acidic media as well in basic media leads to short half-life, delayed dissolution and side effects. Therefore, the goal of the current work is to developed an epalrestat MDTs tablet that will provide quick drug dissolution and a quick onset of action for the treatment of nerve pain. MDTs of epalrestat were formulated by direct compression using natural superdis integrants obtained from the various sources such as fenugreek, gum karaya and banana powder. All of the pre- and post-compression parameter results were shown to be in accordance with established specifications. In comparison to other formulations of MDTs, formulation F3 with 15 mg (7.5%) of banana powder displayed a higher rate of dissolution. It was determined that epalrestat MDTs containing natural superdisintegrant were successfully formulated with acceptable physical and chemical properties, quick oral cavity disintegration, a quick onset of action and improved patient compliance.

Novasomes as Nano-Vesicular Carriers to Enhance Topical Delivery of Fluconazole: A New Approach to Treat Fungal Infections.

The occurrence of fungal infections has increased over the past two decades. It is observed that superficial fungal infections are treated by conventional dosage forms, which are incapable of treating deep infections due to the barrier activity possessed by the stratum corneum of the skin. This is why the need for a topical preparation with advanced penetration techniques has arisen. This research aimed to encapsulate fluconazole (FLZ) in a novasome in order to improve the topical delivery. The novasomes were prepared using the ethanol injection technique and characterized for percent entrapment efficiency (EE), particle size (PS), zeta potential (ZP), drug release, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM) and antifungal activity. The FN7 formulation with 94.45% EE, 110 nm PS and -24 ZP proved to be the best formulation. The FN7 formulation showed a 96% release of FLZ in 8 h. FTIR showed the compatibility of FLZ with excipients and DSC studies confirmed the thermal stability of FLZ in the developed formulation. The FN7 formulation showed superior inhibition of the growth of Candida albicans compared to the FLZ suspension using a resazurin reduction assay, suggesting high efficacy in inhibiting fungal growth.

Optimization and fabrication of the nanosponge carriers of on dansetron using one-factor design.

The current studies were aimed to formulate ethyl cellulose (EC), beta-cyclodextrin (ß-CD facilitated EC based Ondansetron nanosponges (NS) using Response Surface Methodology (RSM) by employing One Factor Design. The NS were fabricated by Emulsion Solvent Diffusion method, followed by characterizations including, drug-polymer compatibility, entrapment efficiency, percentage yield, zeta size, zeta potential and in-vitro release of drug and Scanning Electron Microscopy (SEM) and X-Ray Diffractometry (XRD). The outcomes of Fourier Transformed Infra-Red Spectroscopy (FTIR) have confirmed the compatibility of the drug and excipients. It was found that NS have good entrapment efficiency along with their satisfactory percentage yield. Particle size analysis has confirmed the synthesis of nanosized NS (87.8nm to 108.2nm), having spongy surface, that was described by SEM results. Furthermore, the drug release studies have described a good sustained release of ondansetron for the period of 8 hours. The kinetic modeling has predicted that drug would follow the non fickian type of diffusion mechanism. The application of statistical approach was found helpful in designing and evaluating the NS, avoiding the laborious work, needs to be conducted while using hit and trial method.

Fast dissolving oral films: An approach to co-load and deliver the atorvastatin and ezetimibe for better therapeutic response.

Atherosclerotic patients suffering with acute coronary disease are lying at high risk. This life-threatening problem can be curtailed by using statins e.g., ezetimibe (EZT), atorvastatin calcium (ATC). In this study, co-loaded Fast Dissolving oral films (FDOFs), of ATC-EZT with HPMC E5 prepared by solvent evaporation method. Prepared FDOFs were evaluated for physicochemical, thermal and mechanical properties. In-vivo animal studies were performed on albino rats against diet induced hyperlipidemia. Prepared FDOFs have rapid DT; 27sec, TDT >2min and in-vitro drug release 97% in a min. In DSC, FTIR and XRD analysis, prepared films were chemically compatible and no chemical interaction of drugs and excipient was found. In kinetic modeling, it was observed their EZT exhibited lowest R2 value for zero order kinetic and best fit model was first order kinetic (n, 0.9823). The korsmeyer peppas model films (n, 0.016) indicate fickian type drug diffusion. The groups treated with marketed suspension of drug and FODPs were compared with normal group and high fats diet group. Study reviled that combination FDOPs of both ATC/EZT significantly reduce hyperlipemia as compared to high fat diet group. It can be concluded that ATC and EZT encapsulated in FODFs provide instant drug release and better therapeutic outcomes.

Phytochemical profiling, in vitro and in vivo anti-inflammatory, analgesic and antipyretic potential of Sesuvium sesuvioides (Fenzl) Verdc. (Aizoaceae).

Sesuvium sesuvioides (Fenzl) Verdc is traditionally used in the treatment of inflammatory diseases such as arthritis and gout The aim of present study was to assess the possible anti-inflammatory, analgesic and antipyretic potential of the methanol extract of Sesuvium sesuvioides (SsCr) to prove scientifically its folklore use in the inflammatory diseases and to screen its total antioxidant capacity by multiple methods and phytocompounds by GC-MS. The preliminary phytochemical studies showed the presence of phenols, flavonoids, glycosides, coumarin, terpenoids, saponins, fats and carbohydrates in crude extract. The total phenolic contents (27.31 ± 0.28 mg GAE/g) and total flavonoids (3.58 ± 0.12 mgRE/g) values were observed. The antioxidant capacity of SsCr showed significant DPPH, ABTS, CUPRAC, FRAP, PBD and metal chelating results. GC-MS analysis displayed the phytoconstituents with anti-inflammatory potentials such as 2-methoxy-4-vinylphenol, vanillin, umbelliferone, methyl ferulate, palmitoleic acid, methyl palmitate and phytol. SsCr presented noteworthy HRBC membrane stability with maximum inhibition of cell hemolysis (47.79%). In carrageenan-induced hind paw edema assay result showed dose-dependent anti-inflammatory action. SsCr presented significant (p < 0.05) analgesic activity in hot-plate and tail flicking tests similarly it also showed the noteworthy inhibition in pain latency against formalin induced analgesia at 1st and 2nd phases. SsCr reduced the acetic acid-induced writhes at different doses (250, 500 and 750 mg). Results of antipyretic activity of SsCr extract were significant at 500 and 750 mg. The results of in vitro and in vivo experimental studies verified the anti-inflammatory, analgesic and antipyretic potential of Sesuvium sesuvioides and supported the folklore uses of this plant.

Self-Assembling Topical Nanomicellar Formulation to Improve Curcumin Absorption Across Ocular Tissues.

The pathophysiological mechanisms for dry and wet age-related macular degeneration (AMD) involve oxidative stress and increased VEGF release and expression. An ideal drug candidate for both types of AMD is the one which offers significant protection to the retinal cells from oxidative stress and inhibit VEGF release. Curcumin is one such natural product which provides numerous beneficial effects including antioxidant, anti-inflammatory, and anti-VEGF activities and has the potential for the treatment of both types of AMD. The bioavailability of curcumin is negligible due to its poor aqueous solubility. The purpose of this work is to develop an aqueous nanomicellar drop formulation of curcumin (CUR-NMF) for back of the eye delivery utilizing hydrogenated castor oil (HCO-40) and octoxynol-40 (OC-40) to treat AMD. A full factorial design was performed with JMP software analysis to optimize the formulation size, polydispersity index (PDI), entrapment efficiency, loading, and precipitation. MTT and LDH assays on human retinal pigmented epithelial (D407) cells revealed that 5-10 µM CUR-NMF dose is safe for ophthalmic use. Furthermore, CUR-NMF exhibited significant protection of retinal (D407) cells against H2O2-induced oxidative stress. In vitro drug release kinetics suggested a sustained drug release profile indicating a long-term protection ability of CUR-NMF against oxidative stress to retinal cells. In addition, an ELISA suggested that CUR-NMF significantly reduces vascular endothelial growth factor (VEGF) release in D407 cell line, hence diminishes the risk of angiogenesis. Collectively, these results suggest that the proposed CUR-NMF can be tremendously effective in treating both types of AMD.

Correction: Shakir et al. Exorbitant Drug Loading of Metformin and Sitagliptin in Mucoadhesive Buccal Tablet: In Vitro and In Vivo Characterization in Healthy Volunteers. Pharmaceuticals 2022, 15, 686.

In the original publication, a mistake was observed in Figure 5 as published [...].

Recent Trends in Active and Passive Immunotherapies of Alzheimer's Disease.

In the elderly, a debilitating condition known as dementia, which is a major health concern, is caused by Alzheimer's disease (AD). Despite promising advances by researchers, there is currently no way to completely cure this devastating disease. It is illustrated by the deposition of amyloid ß-peptide (Aß) plaques that are followed by neural dysfunction and cognitive decline. Responses against AD activate an immune system that contributes to and accelerates AD pathogenesis. Potential efforts in the field of pathogenesis have prompted researchers to explore novel therapies such as active and passive vaccines against Aß proteins (Aß immunotherapy), intravenous immunoglobulin, and tau immunotherapy, as well as targets that include microglia and several cytokines for the treatment of AD. Aims are now underway by experts to begin immunotherapies before the clinical manifestation, which is made possible by improving the sensitivity of biomarkers used for the diagnosis of AD to have better outcome measures. This review provides an overview of approved immunotherapeutic strategies for AD and those currently being investigated in clinical trials. We examine their mechanisms of action and discuss the potential perspectives and challenges associated with immunotherapies for AD.

Assessing the status of Ichkeul Lake and its catchment through identifying potentially toxic cyanobacteria, simultaneously extracted metals and use of acid-volatile-sulfide model.

Lake Ichkeul is considered one of the most significant wetlands in the Mediterranean basin. It serves as a crucial wintering area for numerous western Palearctic birds. A notable decline in species diversity has been observed in the past decade, attributed to excessive water usage for irrigation and the effects of climate change. This study aimed to assess the status of Ichkeul Lake and its catchment through identifying potentially toxic cyanobacteria, and sediment quality. Our first striking finding was that Lyngbya majuscula the dominant potentially toxic cyanobacterium in the lake originated from the Tinja channel. Trace element concentrations in lake sediments exceeded SQG standards which is indicative of rare detrimental effects to biological life. However, the sediment in front of the Tinja channel exhibited high contamination levels of Zn and Cd. These findings call for an urgent need to ensure the ongoing management and conservation of this world heritage site.

Production, Characterization, and In Vitro and In Vivo Studies of Nanoemulsions Containing St. John's Wort Plant Constituents and Their Potential for the Treatment of Depression.

The current project was designed to prepare an oil-in-water (oil/water) hypericin nanoemulsion using eucalyptus oil for the preparation of an oil phase with chitosan as an emulsion stabilizer. The study might be a novelty in the field of pharmaceutical sciences, especially in the area of formulation development. Tween® 80 (Polysorbate) was used as the nonionic surfactant. The nanoemulsion was prepared by using the homogenization technique, followed by its physicochemical evaluation. The surface morphological studies showed the globular structure has a nano-sized diameter, as confirmed by zeta size analysis. The zeta potential analysis confirmed a positive surface charge that might be caused by the presence of chitosan in the formulation. The pH was in the range of 5.14 to 6.11, which could also be compatible with the range of nasal pH. The viscosity of the formulations was found to be affected by the concentration of chitosan (F1-11.61 to F4-49.28). The drug release studies showed that the presence of chitosan greatly influenced the drug release, as it was noticed that formulations having an elevated concentration of chitosan release lesser amounts of the drug. The persistent stress in the mouse model caused a variety of depressive- and anxiety-like behaviors that can be counteracted by chemicals isolated from plants, such as sulforaphane and tea polyphenols. In the behavioral test and source performance test, hypericin exhibited antidepressant-like effects. The results show that the mice treated for chronic mild stress had a considerably higher preference for sucrose after receiving continuous hypericin for 4 days (p = 0.0001) compared to the animals administered with normal saline (p ≤ 0.0001) as well as the naïve group (p ≤ 0.0001). In conclusion, prepared formulations were found to be stable and can be used as a potential candidate for the treatment of depression.

A Cross-Sectional Study Using STROBE Platform to Examine Sleep Characteristics, Mental Health and Academic Performance of Female Applied Medical Sciences Students in the Southwest of Saudi Arabia.

Background: Medical students are expected to excel in their academics. Hence exposing them to a certain amount of strain may sometimes cause sleep disruptions. The purpose of this study was to determine the sleep quality among Saudi Applied Medical Sciences students and its potential connections with their academic performance and mental health. Methods: This online cross-sectional questionnaire-based study was conducted at Jazan University's College of Applied Medical Sciences in Saudi Arabia. The Pittsburgh Sleep Quality Index (PSQI), a known indicator of sleep quality, a validated mental health measure; Depression Anxiety Stress Scales-21 (DASS-21), and Academic Performance Scale (APS) with 89 internal consistencies were included in the questionnaire. The cumulative grade point average (GPA) was also used as a covariate to evaluate students' academic success. Results: 112 people responded (response rate = 93%), and 105 of them presented comprehensive information about their backgrounds, way of life, academic standing, sleep patterns, and mental health. Participants' average GPA and APS scores were 4.23 ± 0.52 and 33.16 ± 5.63, respectively. The mean global PSQI score was 6.47 with 2.34 of standard deviation (SD). The majority of individuals (60%) had poor sleep quality particularly due to abnormal sleep latency and lesser sleep duration, as determined by their PSQI score. The prevalence rates for depression, anxiety, and stress were higher; 53%, 54% and 40%, respectively. Both depression and anxiety were substantially correlated with poor sleep quality (p-value = 0.008, p-value = 0.01, respectively). Sleep quality had no significant effect on GPA while global PSQI and depression were significantly negatively correlated with an APS score of participants (p-value = 0.007 and 0.015, respectively). Conclusions: Higher rates of poor sleep quality and psychologically negative emotions were prevalent. Unhealthy sleep patterns were linked to increased levels of anxiety and depression. Self-perceived academic performance was negatively impacted by inadequate sleep and negative emotions, despite the fact that the GPA results were unaffected.

Knowledge, attitudes, and practices (KAP) during the malaria elimination phase: A household-based cross-sectional survey.

Malaria is a major health problem in Southwestern Saudi Arabia. This study aimed to measure the level of community understanding of malaria transmission, protection, and treatment. A questionnaire-based cross-sectional study enrolled 1070 participants from 2 districts with different malaria prevalence rates in Jazan Province. The response rate was 97.27%. Of the 1070 total; 754 (70.5%) had heard about malaria. Sixty-seven percentage know that fever was the main symptom. Approximately 59.8% did not know that stagnant water is one of the most important locations for mosquito breeding. Nevertheless, we found that 50% of the participants knew that mosquitoes bite at night and 96.9% confirmed that mosquitoes did not bite during the day. The most effective sources of information were distributed leaflets (41.8%) and video awareness (31.9%). The most significant factors affecting participants knowledge were gender, residence, family members, income, and education (P < .05). Knowledge levels were satisfactory in this study, and the majority of participants exhibited adequate attitudes and practices related to malaria prevention. However, knowledge differences were observed with regard to the place of residence. Greater emphasis should be directed towards education programs in malaria-endemic areas to ensure complete eradication of malaria.

Prevalence and Associated Risk Factors of Urinary Tract Infection among Diabetic Patients: A Cross-Sectional Study.

Urinary tract infections (UTIs) are one of the most common long-term complications of diabetes mellitus (DM). Additionally, various factors, such as socio-demographics, type of DM, fasting blood glucose, regular diabetes monitoring, comorbid chronic diseases, HbA1c, body mass index (BMI), and duration of DM, are also thought to predispose individuals to developing UTIs more frequently when they have DM. This research aims to evaluate the risk factors for UTIs and their prevalence among people with DM in Saudi Arabia (KSA). This cross-sectional study was conducted among 440 adults with type 1, type 2, and gestational DM. The participants had to be at least 18 years old, of both genders, and had been suffering from DM for any period of time. A self-administered questionnaire was utilized to collect data on demographic characteristics, such as sex, age, height, weight, material state, education level, income, and clinical profiles of DM and UTI. The crude (COR) and adjusted odds ratios (AOR) were calculated using logistic regression in the IBM SPSS software. The incidence of types 1 and 2 DM and gestational diabetes reached 34.1, 60.9, and 5%, respectively. Most of the participants had first-degree relatives with DM (65.9%). UTI was common in 39.3% of participants. A chi-squared statistical analysis revealed that the frequency of UTI varied depending (χ2 = 5.176, P = 0.023) on the type of DM. Burning urination and abdominal pain were the most common symptoms. The CORs for sex, marital status, hypertension, and BMI were significant (P < 0.05) and had values of 2.68 (95% CI = 1.78-4.02), 0.57 (95% CI = 0.36-0.92), 1.97 (95% CI = 1.14-3.43), and 2.83 (95% CI = 1.19-2.99), respectively. According to the adjusted model, only sex influenced the occurrence of UTIs. The AOR for sex was 3.45 (95% CI = 2.08-5.69). Based on this study, the authorities related to the health of DM patients can use its findings to guide awareness programs and clinical preparedness.

Broad-Spectrum Theranostics and Biomedical Application of Functionalized Nanomaterials.

Nanotechnology is an important branch of science in therapies known as "nanomedicine" and is the junction of various fields such as material science, chemistry, biology, physics, and optics. Nanomaterials are in the range between 1 and 100 nm in size and provide a large surface area to volume ratio; thus, they can be used for various diseases, including cardiovascular diseases, cancer, bacterial infections, and diabetes. Nanoparticles play a crucial role in therapy as they can enhance the accumulation and release of pharmacological agents, improve targeted delivery and ultimately decrease the intensity of drug side effects. In this review, we discussthe types of nanomaterials that have various biomedical applications. Biomolecules that are often conjugated with nanoparticles are proteins, peptides, DNA, and lipids, which can enhance biocompatibility, stability, and solubility. In this review, we focus on bioconjugation and nanoparticles and also discuss different types of nanoparticles including micelles, liposomes, carbon nanotubes, nanospheres, dendrimers, quantum dots, and metallic nanoparticles and their crucial role in various diseases and clinical applications. Additionally, we review the use of nanomaterials for bio-imaging, drug delivery, biosensing tissue engineering, medical devices, and immunoassays. Understandingthe characteristics and properties of nanoparticles and their interactions with the biological system can help us to develop novel strategies for the treatment, prevention, and diagnosis of many diseases including cancer, pulmonary diseases, etc. In this present review, the importance of various kinds of nanoparticles and their biomedical applications are discussed in much detail.

Self-Assembled Nanomicellar Formulation of Docetaxel as a Potential Breast Cancer Chemotherapeutic System.

Docetaxel (DTX) is classified as a class IV drug that exhibits poor aqueous solubility (6-7 µg/mL in water) and permeability (P-glycoprotein substrate). The main objective of this study was to construct, characterize, and evaluate docetaxel loaded nanomicellar formulation in vitro for oral delivery to enhance the absorption and bioavailability of DTX, as well as to circumvent P-gp efflux inhibition. Formulations were prepared with two polymeric surfactants, hydrogenated castor oil-40 (HCO-40) and D-α-Tocopherol polyethylene glycol 1000 succinate (VIT E TPGS) with solvent evaporation technique, and the resulting DTX nanomicellar formulations were characterized by proton nuclear magnetic resonance spectroscopy (1H NMR), Fourier Transform Infrared Spectroscopy (FT-IR), X-ray powder diffraction (XRD), and transmission electron microscopy (TEM). Proton NMR, FT-IR, and XRD data indicated that DTX was completely encapsulated within the hydrophobic core of the nanomicelles in its amorphous state. TEM data revealed a smooth spherical shape of the nanomicellar formulation. The optimized formulation (F-2) possessed a mean diameter of 13.42 nm, a zeta potential of -0.19 mV, with a 99.3% entrapment efficiency. Dilution stability study indicated that nanomicelles were stable up to 100-fold dilution with minimal change in size, poly dispersity index (PDI), and zeta potential. In vitro cytotoxicity study revealed higher anticancer activity of DTX nanomicelles at 5 µM compared to the native drug against breast cancer cell line (MCF-7) cells. The LC-MS data confirmed the chemical stability of DTX within the nanomicelles. In vitro drug release study demonstrated faster dissolution of DTX from the nanomicelles compared to the naked drug. Our experimental results exhibit that nanomicelles could be a drug delivery system of choice to encapsulate drugs with low aqueous solubility and permeability that can preserve the stability of the active constituents to provide anticancer activity.

Technologies for Solubility, Dissolution and Permeation Enhancement of Natural Compounds.

The current review is based on the advancements in the field of natural therapeutic agents which could be utilized for a variety of biomedical applications and against various diseases and ailments. In addition, several obstacles have to be circumvented to achieve the desired therapeutic effectiveness, among which limited dissolution and/or solubility and permeability are included. To counteract these issues, several advancements in the field of natural therapeutic substances needed to be addressed. Therefore, in this review, the possible techniques for the dissolution/solubility and permeability improvements have been addressed which could enhance the dissolution and permeability up to several times. In addition, the conventional and modern isolation and purification techniques have been emphasized to achieve the isolation and purification of single or multiple therapeutic constituents with convenience and smarter approaches. Moreover, a brief overview of advanced natural compounds with multiple therapeutic effectiveness have also been anticipated. In brief, enough advancements have been carried out to achieve safe, effective and economic use of natural medicinal agents with improved stability, handling and storage.

Development of Statistically Optimized Chemically Cross-Linked Hydrogel for the Sustained-Release Delivery of Favipiravir.

Nowadays, the use of statistical approaches, i.e., Box-Bhenken designs, are becoming very effective for developing and optimizing pharmaceutical drug formulations. In the current work, a Box-Bhenken design was employed using Design Expert version 11 to develop, evaluate, and optimize a hydrogel-based formulation for sustained release of an antiviral drug, i.e., favipiravir. The hydrogels were prepared using the free radical polymerization technique. ß-Cyclodextrin (ß-CD), N,N'-methylenebisacrylamide (MBA), acrylic acid (AA), and potassium per sulfate (KPS) were used as oligomer, crosslinker, monomer, and initiator, respectively. Three variables, including ß-CD (X1), MBA (X2), and AA (X3) were used at various concentrations for the preparation of hydrogels, followed by evaluation of a sol-gel fraction, swelling, porosity, chemical compatibilities, in vitro drug release, and entrapment efficiency. The results of the studies revealed that the degree of swelling was pH dependent, the best swelling being at pH 7.2 (1976%). On the other hand, for the low sol fraction of 0.2%, the reasonable porosity made the hydrogel capable of loading 99% favipiravir, despite its hydrophobic nature. The maximum entrapment efficiency (99%) was observed in optimized hydrogel formulation (F15). Similarly, in vitro drug release studies showed that the prepared hydrogels exhibited a good, sustained release effect till the 24th hour. The kinetic modelling of drug release data revealed that the Korsmeyer-Peppas model was best fit model, describing a diffusion type of drug release from the prepared hydrogels. Conclusively, the outcomes predict that the hydrogel-based system could be a good choice for developing a sustained-release, once-daily dosage form of favipiravir for improved patient compliance.

Medicinal Importance and Chemosensing Applications of Pyridine Derivatives: A Review.

Pyridine derivatives are the most common and significant heterocyclic compounds, which play an important role in various fields ranging from medicinal to chemosensing applications. Pyridine derivatives possess different biological activities such as antifungal, antibacterial, antioxidant, antiglycation, analgesic, antiparkinsonian, anticonvulsant, anti-inflammatory, ulcerogenic, antiviral, and anticancer activity. Furthermore, these derivatives have a high affinity for various ions and neutral species and can be used as a highly effective chemosensor for the determination of different species. In this review article, generally used synthetic routes of pyridine, structural characterization, medicinal applications, and potential of pyridine derivatives in analytical chemistry as chemosensors have been discussed. We hope this study will support the new thoughts to design biological active compounds and highly selective and effective chemosensors for the detection of various species (anions, cations, and neutral species) in various samples (environmental, agricultural, and biological).