Preparation and in vivo evaluation of nano sized cubosomal dispersion loaded with Ruta graveolens extracts as a novel approach to reduce asthma-mediated lung inflammation.

Asthma is a chronic disease affecting people of all ages. Asthma medications are associated with adverse effects restricting their long-term usage, demanding newer alternative therapies. This study aimed to investigate the anti-asthmatic properties of Ruta graveolens extract and its prepared nano-cubosomal dispersion (Ruta-ND). Firstly, the R. graveolens methanolic extract exhibited higher anti-inflammatory activity on Lipopolysaccharide (LPS)-activated BEAS-2B cells. To ensure best bioavailability and hence best cellular uptake, R. graveolens extract was loaded in nano-cubosomal dispersion (ND). Then, the anti-asthmatic effects of Ruta extract and ND were simultaneously evaluated in rats' model with ovalbumin-induced allergic asthma. R. graveolens extract and Ruta-ND subsided asthma score and improved lung function by restoring FEV1/FVC ratio to the expected values in control rats. Also, it showed strong antioxidant and anti-inflammatory activities manifested by lowering levels of malondialdehyde (MDA), IL-4, IL-7, TGF-ß, and Ig-E, and increasing levels of superoxide dismutase (SOD) and INF-γ in bronchoalveolar lavage fluid. Our research findings also indicate autophagy induction and apoptosis inhibition by Ruta extract and Ruta-ND. Finally, the HPLC MS/MS phytochemical profiling of R. graveolens extract evident production of various alkaloids, flavonoids, coumarins, and other phenolics with reported pharmacological properties corresponding to/emphasize our study findings. In conclusion, R. graveolens exhibited promise in managing Ova-induced allergic asthma and could be developed as an alternative anti-allergic asthma drug.

Taste Masking of Promethazine Hydrochloride Using l-Arginine Polyamide-Based Nanocapsules.

Promethazine hydrochloride (PMZ), a potent H1-histamine blocker widely used to prevent motion sickness, dizziness, nausea, and vomiting, has a bitter taste. In the present study, taste masked PMZ nanocapsules (NCs) were prepared using an interfacial polycondensation technique. A one-step approach was used to expedite the synthesis of NCs made from a biocompatible and biodegradable polyamide based on l-arginine. The produced NCs had an average particle size of 193.63 ± 39.1 nm and a zeta potential of −31.7 ± 1.25 mV, indicating their stability. The NCs were characterized using differential scanning calorimetric analysis and X-ray diffraction, as well as transmission electron microscopy that demonstrated the formation of the NCs and the incorporation of PMZ within the polymer. The in vitro release study of the PMZ-loaded NCs displayed a 0.91 ± 0.02% release of PMZ after 10 min using artificial saliva as the dissolution media, indicating excellent taste masked particles. The in vivo study using mice revealed that the amount of fluid consumed by the PMZ-NCs group was significantly higher than that consumed by the free PMZ group (p < 0.05). This study confirmed that NCs using polyamides based on l-arginine and interfacial polycondensation can serve as a good platform for the effective taste masking of bitter actives.

Medication errors in Najran, Saudi Arabia: Reporting, responsibility, and characteristics: A cross-sectional study.

Background: Medication error is a preventable adverse effect of medical care, whether or not it is evident or harmful to the patient. Disclosure of medication errors and improvement of patient safety are inexorably related, and they provide one of the strongest reasons to report and disclose errors, including near misses in which no harm comes to the patient. This study aimed to identify medication errors at the southern province of Saudi Arabia. Methods: A cross-sectional retrospective study was conducted by reviewing all medical records in the King Khaled Hospital in Najran, Saudi Arabia. Medication errors related information were extracted from the electronic medical system for the duration between 2018 and 2020. Results: During the study period of 2018 to 2020, a total of 4860 medication errors were identified. More than half of the reported medication errors (66.9%) were linked to ordering, prescribing, or transcribing medications. The most commonly reported medication errors connected to ordering/prescribing/transcribing were inappropriate dosage, dosage units, and therapeutic duplication of medication. The most commonly reported medication errors linked to administration were missing documentation during administration, not performing independent double-checks during the administration of high alert medications, and the administration of look-alike sound-alike (LASA) medications. The intensive care unit (ICU), female medical ward, and male medical ward were the most commonly reported locations for medication errors. Pharmacists detected more than half of the reported medication errors. Physicians were found to be responsible for 66.0% of reported medication errors, followed by nurses. Conclusion: Medication errors are common in hospital settings in Saudi Arabia's southern provinces. Efforts should be made to improve drug ordering, prescribing, and transcription in hospital settings. To guarantee optimum practices, the entire medical team should take responsibility for the patient's optimal medication administration.

Depression and anxiety during the COVID-19 pandemic in Saudi Arabia: A cross-sectional study.

AIMS: The emergence of the COVID-19 global pandemic, with a high transmission and mortality rate, has created an extraordinary crisis worldwide. Such an unusual situation may have an undesirable impact on the mental health of individuals which, in turn, may influence their outcomes. This study aimed to explore the influence of the COVID-19 pandemic on the psychological disposition of residents of the Kingdom of Saudi Arabia. METHODS: A cross-sectional study using an online survey was conducted in Saudi Arabia between 27 March and 27 April 2020. The Patient Health Questionnaire (PHQ-9) and Generalised Anxiety Disorder-7 (GAD-7) were used to assess depression and anxiety. Logistic regression analysis was used to identify predictors of these. RESULTS: A total of 2081 individuals participated in the study. The prevalence of depression and anxiety among the study participants was 9.4% and 7.3% respectively. Non-Saudi residents, individuals aged 50 years and above, divorced people, retired people, university students and those with an income between 2000 and 10 000 SR were at higher risk of developing depression. Saudi individuals, married people, the unemployed and those with a high income (>10 000 RS) were at higher risk of developing anxiety. CONCLUSION: We found that there is a wide range of Saudi residents who are at higher risk of developing mental illness during the current COVID-19 pandemic. Policymakers and mental healthcare providers are advised to provide continuous monitoring of the psychological consequences during this pandemic and provide the required health support.

Effectiveness of an educational intervention in improving the patient medication reconciliation in the emergency department.

AIMS: This study aimed to evaluate the effectiveness of an educational intervention in improving the patient medication reconciliation process. METHOD: This was a cross-sectional study that was conducted at St. Jude hospital, California (CA), United States. An educational intervention was provided to the healthcare team working in the emergency department (ED) to explore its effectiveness in improving their patient medication reconciliation practices. A survey was administered to explore the healthcare staff's views on where responsibility lay in their team concerning the fulfilment of appropriate medication reconciliation procedures. Additionally, we identified the barriers facing the completion of appropriate medication reconciliation using open-ended question provided to healthcare staff at the hospital. RESULTS: In the pre-intervention phase, the percentage of patients who received medication reconciliation was statistically significantly higher during the day shift (71.0% compared with 51.3%). In the postintervention phase, the percentage of patients who received medication reconciliation was statistically significantly higher during the night shift (96.7% compared with 75.8%). Overall, the percentage of patients who received medication reconciliation was statistically significantly higher in the postintervention group (81.3%) compared with the pre-intervention group (64.7%) (P < .001). CONCLUSION: Educational intervention is an effective tool in improving medication reconciliation practices in inpatient settings. The process of medication reconciliation should be conducted based on shared responsibility between healthcare providers and aimed at reducing medication errors and improving patient safety.

The perspectives of physicians regarding antidiabetic therapy de-intensification and factors affecting their treatment choices-A cross-sectional study.

AIMS: Comprehensive diabetes management may include treatment intensification or the administration of antidiabetic combination therapy. However, this may be associated with an increased risk of adverse events and death. The aim of this study was to understand physicians' perspectives regarding treatment de-intensification, HbA1c goals individualisation, and factors affecting their treatment choice for patients with type 2 diabetes mellitus (T2DM). METHODS: A cross-sectional study was conducted in primary and secondary care units in Saudi Arabia using online questionnaire. Two previously validated questionnaires were used to understand physicians' awareness of, agreement with, and their practices of individualising HbA1c goals and antidiabetic treatment optimisation, and to assess factors affecting physicians' treatment choice when prescribing antidiabetic treatment for patients with type 2 diabetes mellitus. Study population were physicians who are treating patients with diabetes mellitus during the period between October 2017 and May 2018. RESULTS: A total of 205 physicians have participated in the study. Approximately 50% of physicians had family medicine speciality (n = 98, 47.8%). The majority of physicians (n = 183, 89.3%) were familiar with the concept of HbA1c goals individualisation. However, only 66.3% of them (n = 136) reported that they apply it either always or most of the time. 58.5% (n = 120) of physicians reported that they would not initiate conversations about de-intensifying antidiabetic therapy even if their patients had a stable HbA1c values for one year. Physicians showed higher consideration to objective patient clinical data and their assessment of patient's health status, with minor consideration to patient-related factors. CONCLUSIONS: Healthcare professionals should focus more on implementing contemporary practices and applying any necessary treatment de-intensification or dose adjustment. Subjective patient factors should be taken into account further, as these factors are associated with better disease management.

Knowledge and awareness of the general population and healthcare providers about retinoblastoma: It is time to know the glow.

Retinoblastoma is the most frequent primary intraocular tumour in childhood. Early detection of retinoblastoma is the key to successful management with a higher chance of survival. This study aims to assess the knowledge of the general population and healthcare providers about retinoblastoma in term of presentation, risk factors, timing for diagnosis, and complications. A cross-sectional study using an online survey was conducted in three Arab countries (Jordan, Saudi Arabia, and Iraq) between 28 August and 16 September 2020. The questionnaire tool was constructed based on an extensive literature review to explore the study's aim and objectives. Logistic regression was used to identify predictors of better knowledge about retinoblastoma. A total of 3676 participants were involved in the study (Jordan = 2654, Saudi Arabia = 604, and Iraq = 418). The average retinoblastoma knowledge score for the whole study population was 6.25 (SD = 4.12) out of 21, representing 29.8% (out of the maximum possible total score). Participants aged above 50 years old, married individuals, those with a secondary education level, those who work as professionals in industry, those who have more than four children, and those who reported that they were not in direct contact with a large number of children were less likely to be knowledgeable about retinoblastoma presentation, risk factors, the timing for diagnosis, and complications (P < .05). Early detection is the cornerstone for decreasing morbidity and mortality among children with retinoblastoma. However, the awareness and knowledge about retinoblastoma are very limited in our study population. Efforts should be directed at increasing awareness of both the general population and healthcare providers regarding retinoblastoma. Policymakers are responsible for improving knowledge and awareness about retinoblastoma to facilitate early detection of the disease by conducting awareness campaigns in addition to improve screening skills of healthcare providers and providing them with proper screening and diagnostic tools.

Development of orally dissolving films for pediatric-centric administration of anti-epileptic drug topiramate - A design of experiments (DoE) study.

Children have often been treated as small adults in relation to drug formulation, but research has now shown this not to be the case. Therefore, there is a push from regulatory bodies to provide drug formulations specifically tailored towards the needs of this fragmented population. Orally dissolving films (ODFs) have been identified as an emerging opportunity, to bridge this gap. Therefore, the aim of this study was to prepare ODFs containing topiramate, an antiepileptic drug, using solvent casting method as a potential alternative to oral tablets/powders for paediatrics. For this purpose, a Design of Experiment (DoE) was employed to optimise formulation parameters. 24 formulations were prepared by changing the polymer type (HPMC, Guar-Gum or PEO), concentration (0.4%-1.2%w/v); plasticizer type (glycerol\sorbitol) and concentration (0.1-0.3%w/v). Disintegration time, content-uniformity, film quality and thickness uniformity were the responses. Surface and molecular profiling were conducted on the optimal formulation (N4). TGA and XRD results demonstrated the stability of materials upon production into films, while the SEM images showed smooth films that proved to be resilient due to good mechanical properties. HPMC-glycerine based ODFs are presented as an effective dosage form to enhance the ease of administration and patient compliance of topiramate, specifically for paediatric patients.

Formulation of sublingual promethazine hydrochloride tablets for rapid relief of motion sickness.

The delivery of antihistaminic agents via the oral route is problematic, especially for elderly patients. This study aimed to develop a sublingual formulation of promethazine hydrochloride by direct compression, and to mask its intensely bitter taste. Promethazine hydrochloride (PMZ) sublingual tablets prepared by direct compression were optimized using Box-Behnken full factorial design. The effect of a taste-masking agent (Eudragit E 100, X1), superdisintegrant (crospovidone; CPV, X2) and lubricant (sodium stearyl fumarate; SSF, X3) on sublingual tablets' attributes (responses, Y) was optimized. The prepared sublingual tablets were characterized for hardness (Y1), disintegration time (Y2), initial dissolution rate (IDR; Y3) and dissolution efficiency after 30 min (Dissolution Efficiency (DE); Y4). The obtained results showed a significant positive effect of the three independent factors on tablet hardness (P < 0.05), and the interactive effect of Eudragit E 100 and CPV on tablet hardness was significant. Disintegration time was mainly affected by Eudragit E 100 and CPV concentrations. Moreover, IDR was employed to assess the taste masking effect, lower values were obtained at higher Eudragit E 100 concentration despite it was statistically insignificant (p > 0.05). Optimized formulation that was suggested by the software was composed of: Eudragit E 100 (X1) = 2.5% w/w, CPV (X2) = 4.13% w/w, and SSF (X3) = 1.0% w/w. The observed values of the optimized formula were found to be close to the predicted optimized values. The Differential Scanning Calorimetric (DSC) studies indicated no interaction between PMZ and tablet excipients.

Middle East Respiratory Syndrome (MERS) and novel coronavirus disease-2019 (COVID-19): From causes to preventions in Saudi Arabia.

Saudi Arabia is one of the countries that has been affected by COVID-19. At the beginning of March 2020, it revealed a steadily rising number of laboratory-confirmed cases. By 20th May 2020, 59,854 infected cases had been confirmed, with 329 deaths. To prevent a further outbreak of COVID-19, this article discusses the current understanding of COVID-19 and compares it with the outbreak of Middle East Respiratory Syndrome (MERS) in 2012 in Saudi Arabia. It also discusses the causes, transmission, symptoms, diagnosis, treatments and prevention measures to identify an applicable measure to control COVID-19.

Knowledge about COVID-19 and beliefs about and use of herbal products during the COVID-19 pandemic: A cross-sectional study in Saudi Arabia.

The lack of treatment options for COVID-19 has raised many concerns among populations worldwide, which has led to many attempts to find alternative options to prevent the transmission of the disease or to alleviate the progression of the infection, including focusing more on preventive measures (to prevent transmission to other individuals) and the use of natural products and herbal extracts to increase immunity and decrease the probability of getting infected. This study explored the knowledge of the population of the Kingdom of Saudi Arabia (KSA) about COVID-19 preventive measures and their belief about the consumption of herbal products for the prevention of COVID-19 infection. A total of 5,258 individuals participated in this study. Participants' knowledge about the appropriate COVID-19 preventive measures in terms of handwashing procedures, self-quarantine and social distancing was moderate, with a mean score of 5.5 (SD: 1.7) out of 10 (representing around 55.0% of the total score). About 22.1% (n = 1,161) of the participants reported that they have used herbal products or nutritional supplements during the pandemic period, to protect themselves from the disease. Social media and the Internet (39.4%, n = 372) were the main motivators for the participants to try herbal products. Vitamin C was the most commonly used food supplement to increase immunity and reduces the chance of contracting COVID-19. Our study demonstrated that the general population in Saudi Arabia has a moderate level of knowledge about COVID-19 transmission and preventive measures. A considerable proportion of the population reported the use of herbal products or food supplements in order to protect themselves from the disease. Policymakers are suggested to provide further educational campaigns that increase population knowledge about the disease transmission routes and preventive measures. In addition, the use of herbal products should be evidence-based to ensure patient safety.

24 Factorial Design Formulation Optimization and In vitro Characterization of Desloratadine Nanosuspension Prepared Using Antisolvent Precipitation.

INTRODUCTION: Desloratadine, a second-generation antihistaminic drug, is poorly watersoluble and requires amelioration of the dissolution rate to improve its pharmacokinetics properties. METHOD: This study investigated the impact of polymer, surfactant types, and concentration on the particle size, zeta potential, and dissolution efficiency of nanosuspensions formulated through the solvent antisolvent precipitation method. To optimize the delivery of Desloratadine nanosuspension, we used Minitab software and a 4-factor, 2-level full factorial design. Physicochemical properties and drug release studies were conducted to evaluate the suggested nanosuspension formulations. The optimization goals included minimizing particle size and zeta potential while maximizing dissolution efficiencies. RESULT: The selected optimal nanosuspension demonstrated favourable values, including a particle size of 478.63 ± 15.67 nm, a zeta potential of -36.24 ± 3.21 mV, and dissolution efficiencies in double distilled water and buffer of 90.29 ± 3.75 % and 93.70 ± 3.67 %, respectively. The optimized formulation was subjected to additional analysis using X-ray powder diffraction (XPRD), scanning and transmission electron microscopy (SEM and TEM), and Fourier-transform infrared spectroscopy (FTIR). CONCLUSION: The optimized nanosuspension formulation also underwent further studies under optimal lyophilization conditions, revealing the effectiveness of mannitol as a cryoprotectant at a concentration of 8%.

Capecitabine-loaded NLC for Breast Cancer Treatment: Preparation, Characterization, and In vitro Evaluation.

BACKGROUND: Cancer treatment often involves the use of potent antineoplastic drugs like Capecitabine [CAP], which can lead to serious toxicities. There is a need for dosage forms to manage these toxicities that can deliver the medication effectively to the target site while maintaining therapeutic efficacy at lower doses. To achieve the aforesaid objective, NLC containing capecitabine [NANOBIN] was prepared and evaluated. Different formulations of NANOBIN, denoted as CaTS, CaT1S, CaT2S, CaTS1, and CaTS2, were designed and evaluated to improve drug delivery and therapeutic outcomes. METHODS: The NANOBIN formulations were prepared using the hot homogenization method. The characterization of these formulations was conducted based on various parameters such as particle size, Polydispersity Index [PDI], Zeta Potential [ZP], Transmission Electron Microscopy [TEM] imaging, and Encapsulation Efficiency [EE]. In vitro evaluations included stability testing, release studies to assess drug release kinetics, and a cytotoxicity assay [MTT assay] to evaluate the efficacy of these formulations against human breast cancer cells [MCF-7]. RESULTS: The characterization results revealed that all NANOBIN formulations exhibited particle sizes ranging from 65 to 193 nm, PDI values within the range of 0.26-0.37, ZP values between 46.47 to 61.87 mV [-ve], and high EE percentages ranging from 94.121% to 96.64%. Furthermore, all NANOBIN formulations demonstrated sustained and slow-release profiles of CAP. The MTT assay showed that the NANOBINs exhibited significantly enhanced cytotoxic efficacy, approximately 10 times greater than free CAP when tested on MCF-7 cells. These findings indicate the potential of NANOBINs to deliver CAP effectively to the target site, enabling prolonged drug availability and enhanced therapeutic effects at lower doses. CONCLUSION: The study demonstrates that NANOBINs can effectively deliver CAP to target sites, prolonging drug exposure and enhancing therapeutic efficacy while reducing the required dose. Further studies are necessary to validate these findings and establish NANOBINs as a preferred treatment option for cancer therapy.

Prevalence and Knowledge of Respiratory Symptoms Among the General Public in the Southern Area of Najran, Saudi Arabia: A Cross-Sectional Health Survey Study.

Objective: To investigate the knowledge, prevalence of chronic respiratory disorders, and utilization of their medications among the adults at Najran region, Saudi Arabia. Methods: An online cross-sectional survey was carried out in Najran region, Saudi Arabia. A self-administered questionnaire was distributed among a random sample of the general population, aged 18 or above between March and December 2022. The survey instrument included questions regarding history and exposure, physician diagnosed-disorders, respiratory symptoms, allergy, use of medications and possible risk-related factors. Results: This research had a total of 712 individuals. Nearly one-third of the participants in the survey (n = 218; 30.6%) said that they or a member of their family suffer from respiratory ailments. The majority of research participants (n = 167; 76.8%) identified asthma as their primary respiratory condition. A total of 32.0% of participants (n = 70) reported dealing with dust or chemicals such as paints, fertilizers, and cleaning products on a daily basis at work or at home. Around 62.0% of the participants (n = 134) said that exposure to gases, fragrances, and other such substances negatively impacts their health. Almost 78.0% (n = 169) of them indicated that summer weather affects their health, whereas 63.0% (n = 138) reported that winter cold affects their health. Participants aged 41-50 years were 38.0% less likely to have CRDs compared to others (p < 0.05). Conclusion: This study is among the first few studies that explored the knowledge, prevalence of chronic respiratory disorders, and utilization of their medications among the adults at Najran region, Saudi Arabia. In the southern area of Najran, respiratory symptoms are frequent among the inhabitants of Saudi Arabia. More research is required to discover avoidable risk factors and create countermeasures for them. It is recommended that healthcare personnel increase their efforts to educate their patients about respiratory illness prevention methods.

Knowledge and Attitudes toward Autism Spectrum Disorder in Saudi Arabia.

AIMS: The diagnosis of autism spectrum disorder (ASD) is not easy as there is no direct test that exists to establish such a diagnosis. Increasing community and healthcare professional knowledge of the ASD spectrum is crucial because it will encourage parents of ASD children to seek screening and diagnosis from a specialist, allowing for better early detection and treatment. This study explored the knowledge of the general population in Saudi Arabia regarding ASD and assessed variables associated with an accurate understanding of ASD. METHODS: A total of 769 participants were involved in this cross-sectional study, which was conducted in Saudi Arabia between November 2021 and February 2022 using an online survey tool to explore the knowledge of the general population in Saudi Arabia regarding typical child development and ASD. A binary logistic regression analysis was used to determine factors affecting participants' knowledge of autism. RESULTS: Overall, the study participants showed a weak level of knowledge about autism with a mean score of 5.9 (SD: 3.1), comprising 34.7% of the total maximum obtainable score. Participants with a middle income category of 5000-7500 SR are less likely to be knowledgeable about autism compared to others (OR: 0.60 (95% CI: 0.39-0.92)) (p-value = 0.020). CONCLUSION: The participants in our study showed limited knowledge about autism. Government funds should be made available to facilitate educational services for ASD children. More funding and resources should be allocated by the government to provide assistance for children with special needs, and changes in public facilities are required to meet the demands of ASD patients. Through an informed educational effort, various media platforms should assist in improving the community's understanding of ASD and their attitude toward ASD patients. Educational campaigns should focus on enhancing the public's knowledge about ASD treatment and etiology.

Tamoxifen Citrate Containing Topical Nanoemulgel Prepared by Ultrasonication Technique: Formulation Design and In Vitro Evaluation.

The present study aims to design and develop a nanoemulgel formulation of Tamoxifen citrate (TAM), a water-insoluble, potent anticancer drug, using the spontaneous emulsification method to improve topical delivery, achieve high accumulation at the tumour site, and spare the healthy tissues. The oil-based selection was related to the TAM solubility, while the surfactant and co-surfactant were chosen based on the droplets' thermodynamic stability and size. Afterwards, a pseudo-ternary phase diagram was built for the most promising formulation using two oils, olive and sesame, with a varied mix of Tween 40 as the surfactant and Trascutol HP as the co-surfactant (Smix), by the optimisation of experiments. The nanoemulsion (NE) formulations that were prepared were found to have an average droplet size of 41.77 ± 1.23 nm and 188.37 ± 3.53 nm, with suitable thermodynamic stability and physicochemical properties. Both olive and sesame oils are natural food additives due to their associated antioxidant effects; therefore, they showed no toxicity profile on breast cell lines (MCF-7, ATCC number HTB-22). The TAM-NE preparations revealed a prolonged and doublings superior cumulative percentage of in vitro release of TAM compared to TAM plain gel suspension over 24 h. The release data suggested that the Higuchi model was the best fitting kinetical model for the developed formulations of NE1, NE9, and NE18. The extended release of the drug as well as an acceptable amount of the drug permeated TAM via nanogel preparations suggested that nanoemulgel (NEG) is suitable for the topical delivery of TAM in breast cancer management. Thus, this work suggests that a nanogel of TAM can improve anticancer properties and reduce systemic adverse effects compared to a suspension preparation of TAM when applied in the treatment of breast cancer.

Novel Thymoquinone Nanoparticles Using Poly(ester amide) Based on L-Arginine-Targeting Pulmonary Drug Delivery.

Thymoquinone (TQ), the main active constituent of Nigella sativa, has demonstrated broad-spectrum antimicrobial, antioxidant, and anti-inflammatory effects, which suggest its potential use in secondary infections caused by COVID-19. However, clinical deployment has been hindered due to its limited aqueous solubility and poor bioavailability. Therefore, a targeted delivery system to the lungs using nanotechnology is needed to overcome limitations encountered with TQ. In this project, a novel TQ-loaded poly(ester amide) based on L-arginine nanoparticles was prepared using the interfacial polycondensation method for a dry powder inhaler targeting delivery of TQ to the lungs. The nanoparticles were characterized by FTIR and NMR to confirm the structure. Transmission electron microscopy and Zetasizer results confirmed the particle diameter of 52 nm. The high-dose formulation showed the entrapment efficiency and loading capacity values of TQ to be 99.77% and 35.56%, respectively. An XRD study proved that TQ did not change its crystallinity, which was further confirmed by the DSC study. Optimized nanoparticles were evaluated for their in vitro aerodynamic performance, which demonstrated an effective delivery of 22.7-23.7% of the nominal dose into the lower parts of the lungs. The high drug-targeting potential and efficiency demonstrates the significant role of the TQ nanoparticles for potential application in COVID-19 and other respiratory conditions.

Novel Fluticasone Propionate and Salmeterol Fixed-Dose Combination Nano-Encapsulated Particles Using Polyamide Based on L-Lysine.

One of the key challenges in developing a dry powder inhaler (DPI) of an inhalable potent fixed-dose combination (FDC) is the ability of the formulation to generate an effective and reproducible aerosol able to reach the lower parts of the lungs. Herein, a one-step approach is presented to expedite the synthesis of nanoaggregates made from a biocompatible and biodegradable polyamide based on L-lysine amino acid employing market-leading active pharmaceutical ingredients (fluticasone propionate (FP) and salmeterol xinafoate (SAL)) for the management of asthma. The nanoaggregates were synthesized using interfacial polycondensation that produced nanocapsules with an average particle size of 226.7 ± 35.3 nm and zeta potential of -30.6 ± 4.2 mV. Differential scanning calorimetric analysis and x-ray diffraction, as well as scanning electron microscopy of the produced FDC, revealed the ability of the produced nanocapsules to encapsulate the two actives and display the best aerodynamic performance. The FDC nanocapsules displayed 88.5% and 98.5% of the emitted dose for FP and SAL, respectively. The fine particle fraction of the nominated dose was superior to the marketed product (Seretide Diskus®, Brentford, United Kingdom). The in-vitro release study showed an extended drug release profile. Our findings suggest that nanoaggregates using polyamides based on L-lysine and interfacial polycondensation can serve as a good platform for pulmonary drug delivery of FDC systems.

Ellagitannins and simple phenolics from the halophytic plant Tamarix nilotica.

Three new [nilotinins M8‒M10 (1‒3)] and two known [tamarixinin A (4) and gemin D (5)] ellagitannins and seven simple phenolics [gallic acid (6), methyl gallate (7), 3,4-di-O-methylgallic acid (8), ellagic acid (9), 3-O-methylellagic acid (10), methyl ferulate 3-O-sulphate (11), and 7,4'-di-O-methylkaempferol (12)] were isolated from the halophytic plant Tamarix nilotica (Ehrenb.) Bunge (Tamaricaceae). Their structures were determined based on intensive spectroscopic studies and comparisons with reported data. Compounds 4, and 6-8 were evaluated for their cytotoxicity against lung adenocarcinoma cell line (A549) and anti-leishmanial activity against Leishmania major. Compounds 4, 6 and 7 showed promising cytotoxic properties against A549 (IC50 29 ± 2.3, 10.5 ± 0.7, and 20.7 ± 1.9 µg/mL), while compounds 4 and 7 showed higher growth-inhibitory effects against L. major promastigotes (IC50 40.5 ± 2.7 and 38.4 ± 2.5 µg/mL), as compared with the standards doxorubicin (IC50 0.42 µg/mL) and miltefosine (IC50 9.43 µg/mL), respectively.

Antileishmanial and lung adenocarcinoma cell toxicity of Withania somnifera (Linn.) dunal root and fruit extracts.

This study aims to evaluate the anti-Leishmania major and the lung adenocarcinoma (A549) cytotoxicity of Withania somnifera root and fruit. The total extracts were obtained by homogenisation in aqueous MeOH, and the sub-extracts [n-hexane, ethyl acetate (EtOAc), n-butanol (n-BuOH), and methanol (MeOH)] were obtained by flash chromatography. The activity evaluation showed that n-BuOH sub-extracts from root and fruit exhibited noticeable antileishmanial promastigote properties. The n-hexane and EtOAc sub-extracts from both organs, and the MeOH sub-extract from the fruit exerted mild to moderate effects on the promastigotes. In-vitro growth-inhibitory test results on axenic amastigote and cytotoxicity testing on macrophages (RAW264.7), the parasite-host at the amastigote stage, revealed that the activity was mainly concentrated in the root EtOAc and n-BuOH sub-extracts and to a lesser extent the fruit MeOH and EtOAc, and the root n-hexane sub-extracts. Only the roots' EtOAc and n-BuOH sub-extracts demonstrated low cytotoxicity on the A549 cell line.