Evaluation of Extended-release of Piroxicam-loaded Pectin-zein Hydrogel Microspheres: In vitro, Ex vivo, and In vivo Studies.

OBJECTIVE: This study evaluated drug delivery systems based on Pectin (P) and Zein (Z) hydrogel microspheres. Piroxicam (Px) loaded P/Z hydrogel microspheres (P/Z HM) were developed, and their extended-release pharmacokinetic properties were evaluated. METHODS: Experiments were executed under three different conditions: in vitro, ex vivo, and in vivo. Then, the in vitro-in vivo correlations (IVIVC) and ex vivo-in vivo correlations (EVIVC) were examined. RESULTS: Analysis of drug release mechanisms were evaluated by fitting the in vitro data into the Ritger- Peppas equation, showing the contribution of both polymers' relaxation and drug diffusion from the hydrogel microspheres. The fraction absorbed in vivo was determined by the deconvolution of plasma concentration data using the Loo-Riegelman method. After oral single-dose administration of the two formulations, their basic independent model parameters were calculated. CONCLUSION: P/Z HM had different drug release behaviors in in vitro and in vivo conditions. However, the ex vivo and in vivo characteristics were similar (R² = 0.99). It seemed reasonable to use the ex vivo method to predict the in vivo drug absorption behavior during the polymeric drug delivery system developmental studies. The P/Z HM formulation maintained the drug dose at the colon site for a long duration and could be applied for delivery of active pharmaceutical and food ingredients to the colon site.

The antibiotic knowledge, attitudes and behaviors of patients, doctors and pharmacists in the WHO Eastern European region - a qualitative, comparative analysis of the culture of antibiotic use in Armenia, Georgia, Kazakhstan, Moldova, Russia and Tajikistan.

BACKGROUND: To reduce antimicrobial resistance (AMR), initiatives such as surveillance activities and activities to increase knowledge about how and why antibiotics (ABs) are (mis)used are needed. More surveillance systems are in place in the WHO Western European region than in the Eastern region, and only sparse knowledge exists about the current culture of AB use in the Eastern European countries. OBJECTIVE: To investigate AB knowledge, attitudes and behaviors in countries in the WHO Eastern European region in order to identify overall similarities and differences across the region and how AB knowledge, attitudes and behavior patterns may be influenced by the national health care system. METHODS: Semi-structured interviews were conducted in Armenia, Georgia, Kazakhstan, Moldova, Russia and Tajikistan with patients, doctors and pharmacists. In total, 80 interviews were carried out. A directed content analysis was applied, followed by a comparative analysis, identifying the similarities and differences in AB attitudes, knowledge and behaviors between the countries and discussing how the national health care systems might influence these patterns. RESULTS: Cross-national patterns were identified regarding patients seeking ABs over-the-counter (OTC), patient variations in their requests for ABs when consulting doctors, and, finally, doctors and pharmacists appearing knowledgeable about ABs and their uses, with doctors displaying careful attitudes towards AMR. Indications of national differences between the countries included the ability of patients to afford ABs, prescribing practices of doctors and pharmacist attitudes towards selling ABs without prescriptions. Multiple aspects involved in patient and pharmacist AB decision making were detected, such as various rationales involved in buying/selling ABs OTC, implying that these processes are more complex than previously reported in the literature. CONCLUSIONS: Similarities across the Eastern European region could be seen in patient needs and uses of antibiotics obtained OTC at community pharmacies, whereas doctors appeared more influenced by specific structures of the national healthcare system.

Antimicrobial Medicines Consumption in Eastern Europeand Central Asia - An Updated Cross-National Study and Assessment of QuantitativeMetrics for Policy Action.

Introduction: Surveillance of antimicrobial medicines consumption is central to improving their use and reducing resistance rates. There are few published data on antibiotic consumption in Eastern Europe and Central Asia. To address this, 18 non-European Union (EU) countries and territories contribute to the WHO Regional Office for Europe (WHO Europe) Antimicrobial Medicines Consumption (AMC) Network. Objectives: (i) Analyze 2015 consumption of J01 class antibacterials for systemic use from 16 AMC Network members; (ii) compare results with 2011 data and 2015 ESAC-Net estimates; (iii) assess consumption against suggested indicators; (iv) evaluate the impact of planned changes to defined daily doses (DDDs) in 2019 for some commonly used antibiotics; and (v) consider the utility of quantitative metrics of consumption for policy action. Methods: Analysis methods are similar to ESAC-Net for EU countries. The Anatomical Therapeutic Chemical (ATC) classification and DDD methodology were used to calculate total consumption (DDD/1000 inhabitants/day [DID]), relative use measures (percentages), extent of use of WHO Watch and Reserve group antibiotics and impact of DDD changes. Findings: Total J01 consumption in 2015 ranged 8.0-41.5 DID (mean 21.2 DID), generally lower than in 2011 (6.4-42.3 DID, mean 23.6 DID). Beta-lactam penicillins, cephalosporins, and quinolones represented 16.2-56.6, 9.4-28.8, and 7.5-24.6% of total J01 consumption, respectively. Third-generation cephalosporins comprised up to 90% of total cephalosporin consumption in some countries. Consumption of WHO Reserve antibiotics was very low; Watch antibiotics comprised 17.3-49.5% of total consumption (mean 30.9%). Variability was similar to 2015 ESAC-Net data (11.7-38.3 DID; mean 22.6 DID). DDD changes in 2019 impact both total and relative consumption estimates: total DIDs reduced on average by 12.0% (7.3-35.5 DID), mostly due to reduced total DDDs for commonly used penicillins; impact on rankings and relative use estimates were modest. Discussion: Quantitative metrics of antibiotic consumption have value. Improvements over time reflect national activities, however, changes in total volumes may conceal shifts to less desirable choices. Relative use measures targeting antibiotics of concern may be more informative. Some, including WHO Watch and Reserve classifications, lend themselves to prescribing targets supported by guidelines and treatment protocols.

Cytotoxicity of the Essential Oil of Fennel (Foeniculum vulgare) from Tajikistan.

The essential oil of fennel (Foeniculum vulgare) is rich in lipophilic secondary metabolites, which can easily cross cell membranes by free diffusion. Several constituents of the oil carry reactive carbonyl groups in their ring structures. Carbonyl groups can react with amino groups of amino acid residues in proteins or in nucleotides of DNA to form Schiff's bases. Fennel essential oil is rich in anise aldehyde, which should interfere with molecular targets in cells. The aim of the present study was to investigate the chemical composition of the essential oil of fennel growing in Tajikistan. Gas chromatographic-mass spectrometric analysis revealed that the main components of F. vulgare oil were trans-anethole (36.8%); α-ethyl-p-methoxy-benzyl alcohol (9.1%); p-anisaldehyde (7.7%); carvone (4.9%); 1-phenyl-penta-2,4-diyne (4.8%) and fenchyl butanoate (4.2%). The oil exhibited moderate antioxidant activities. The potential cytotoxic activity was studied against HeLa (human cervical cancer), Caco-2 (human colorectal adenocarcinoma), MCF-7 (human breast adenocarcinoma), CCRF-CEM (human T lymphoblast leukaemia) and CEM/ADR5000 (adriamycin resistant leukaemia) cancer cell lines; IC50 values were between 30-210 mg L-1 and thus exhibited low cytotoxicity as compared to cytotoxic reference compounds.