Teixobactin is a highly potent cyclic depsipeptide which kills a broad range of multi-drug resistant, Gram-positive bacteria, such as Methicillin-resistant Staphylococcus aureus (MRSA) without detectable resistance. In this work, we describe the design and rapid synthesis of novel teixobactin analogues containing two cysteine moieties, and the corresponding disulfide-bridged cyclic analogues. These analogues differ from previously reported analogues, such as an Arg10-teixobactin, in terms of their macrocyclic ring size, and feature a disulfide bridge instead of an ester linkage. The new teixobactin analogues were screened against Methicillin-resistant Staphylococcus aureus and Methicillin-sensitive Staphylococcus aureus. Interestingly, one teixobactin analogue containing all l-amino acid building blocks showed antibacterial activity against MRSA for the first time. Our data indicates that macrocyclisation of teixobactin analogues with disulfide bridging is important for improved antibacterial activity. In our work, we have demonstrated the unprecedented use of a disulfide bridge in constructing the macrocyclic ring of teixobactin analogues.
Solid dispersions have achieved significant interest as an effective means of enhancing the dissolution rate and thus the bioavailability of a range of weakly water-soluble drugs. Solid dispersions of weakly water-soluble drugs with water-soluble carriers have lowered the frequency of these problems and improved dissolution. Solid dispersion is a solubilization technology emphasizing mainly on, drug-polymer two-component systems in which drug dispersion and its stabilization is the key to formulation development. Therefore, this technology is recognized as an exceptionally useful means of improving the dissolution properties of poorly water-soluble drugs and in the latest years, a big deal of understanding has been accumulated about solid dispersion, however, their commercial application is limited. In this review article, emphasis is placed on solubility, BCS classification, and carriers. Moreover, this article presents the diverse preparation techniques for solid dispersion and gathers some of the recent technological transfers. The different types of solid dispersions based on the carrier used and molecular arrangement were underlined. Additionally, it summarizes the mechanisms, the methods of preparing solid dispersions, and the marketed drugs that are available using solid dispersion approaches.
Inappropriate antibiotic usage is a critical issue in many countries, especially in low- and middle-income countries, where access to antibiotics may be easier but proper prescribing and use practices are often lacking. This can contribute to the development of antibiotic resistance, which poses a significant threat to global public health. The research on assessing the awareness, attitude, and knowledge of senior pharmacy students in Jordanian universities regarding antibiotic use and resistance can have several impacts. Firstly, it can shed light on the current level of knowledge and awareness among pharmacy students, who are future healthcare professionals, and identify any gaps or misconceptions that need to be addressed through education and training programs. Secondly, the research findings can be used to develop targeted interventions to improve appropriate antibiotic use and reduce the emergence and spread of antibiotic resistance in Jordan and potentially other countries with similar contexts. Finally, the study can contribute to the growing body of knowledge on antibiotic resistance and help inform global efforts to address this critical public health issue. This study aimed to assess the awareness, attitude, and knowledge of senior pharmacy students in Jordanian universities in relation to antibiotic use and antibiotic resistance (AR). A proportionate random sampling method was employed, and a questionnaire was administered to 400 final-year pharmacy students from three universities in the northern region of Jordan over a period of six months (6/3/2022- 11/3/2022). The data was distributed electronically using emails, and Excel was used for data analysis. The findings revealed that the pharmacy students displayed a high level of knowledge (mean score of 86.5%), positive attitude (mean score of 87.2%), and responsible behavior towards antibiotic use, indicative of their awareness and understanding of the risks of AR. The statistical methods used to analyze the data included descriptive statistics and inferential statistics such as t-tests and ANOVA. The study also identified some areas of potential improvement, such as enhancing knowledge about antibiotic resistance mechanisms and the importance of completing the full course of antibiotics. To address these gaps, targeted educational interventions can be developed to empower pharmacy students to promote appropriate antibiotic use and minimize the emergence of antibiotic resistance.
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