Recent advances in anti-infective drug discovery最新文献

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Can the Therapeutic Spectrum of Probiotics be Extended: Exploring Potential of Gut Microbiome. 益生菌的治疗范围能否扩大:探索肠道微生物组的潜力。
Recent advances in anti-infective drug discovery Pub Date : 2023-01-01 DOI: 10.2174/2772434418666221124124317
Sonakshi Rastogi, Aditi Singh, Abhishek Nandy, Akanksha Gupta, Jyotsna Agarwal, Irena Kostova
{"title":"Can the Therapeutic Spectrum of Probiotics be Extended: Exploring Potential of Gut Microbiome.","authors":"Sonakshi Rastogi,&nbsp;Aditi Singh,&nbsp;Abhishek Nandy,&nbsp;Akanksha Gupta,&nbsp;Jyotsna Agarwal,&nbsp;Irena Kostova","doi":"10.2174/2772434418666221124124317","DOIUrl":"https://doi.org/10.2174/2772434418666221124124317","url":null,"abstract":"<p><p>Natural therapeutic microorganisms provide a potent alternative healthcare treatment nowadays, with the potential to prevent several human diseases. These health-boosting living organisms, probiotics mostly belong to Gram-positive bacteria such as Lactobacillus, Bifidobacterium, Streptococcus, Saccharomyces, Bacillus and Enterococcus. Initiated almost a century ago, the probiotic application has come a long way. The present review is focused on the potential therapeutic role of probiotics in ameliorating multiple infections, such as upper respiratory tract infections and viral respiratory infections, including COVID-19; liver diseases and hepatic encephalopathy; neurological and psychiatric disorders; autoimmune diseases, particularly rheumatoid arthritis, systemic lupus erythematosus and multiple sclerosis. Apart from these, the therapeutic exacerbations of probiotics in urinary tract infections have been extremely promising, and several approaches are reviewed and presented here. We also present upcoming and new thrust areas where probiotic therapeutic interventions are showing promising results, like faecal microbial transplant and vaginal microbial transplant.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"18 2","pages":"120-147"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9546586","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A Perspective into "TEL"-Tenofovir, Emtricitabine and Lamivudine Antileprotic Activities by Drug Repurposing and Exploring the Possibility of Combination Chemotherapy with Drug Rescued Molecules for a Leprosy Free Mankind. “TEL”-替诺福韦、恩曲他滨和拉米夫定药物再利用抗麻风活性及探索药物拯救分子联合化疗的可能性
Recent advances in anti-infective drug discovery Pub Date : 2023-01-01 DOI: 10.2174/2772434418666230220123217
Pugazhenthan Thangaraju, Sree Sudha Tanguturi Yella, Vijayakumar Arumugam Ramamurthy, Irfan Navabshan, Thameemul Ansari Lappathai Habeeb Mohamed
{"title":"A Perspective into \"TEL\"-Tenofovir, Emtricitabine and Lamivudine Antileprotic Activities by Drug Repurposing and Exploring the Possibility of Combination Chemotherapy with Drug Rescued Molecules for a Leprosy Free Mankind.","authors":"Pugazhenthan Thangaraju,&nbsp;Sree Sudha Tanguturi Yella,&nbsp;Vijayakumar Arumugam Ramamurthy,&nbsp;Irfan Navabshan,&nbsp;Thameemul Ansari Lappathai Habeeb Mohamed","doi":"10.2174/2772434418666230220123217","DOIUrl":"https://doi.org/10.2174/2772434418666230220123217","url":null,"abstract":"<p><strong>Background: </strong>Since leprosy bacilli cannot grow in vitro, testing for antimicrobial resistance against Mycobacterium leprae or assessing the anti-leprosy activity of new drugs remains hard. Furthermore, developing a new leprosy drug through the traditional drug development process is not economically captivating for pharmaceutical companies. As a result, repurposing existing drugs/approved medications or their derivatives to test their anti-leprotic potency is a promising alternative. It is an accelerated method to uncover different medicinal and therapeutic properties in approved drug molecules.</p><p><strong>Aims: </strong>The study aims to explore the binding potential of anti-viral drugs such as Tenofovir, Emtricitabine, and Lamivudine (TEL) against <i>Mycobacterium leprae</i> using molecular docking.</p><p><strong>Methods: </strong>The current study evaluated and confirmed the possibility of repurposing antiviral drugs such as TEL (Tenofovir, Emtricitabine, and Lamivudine) by transferring the graphical window of the BIOVIA DS2017 with the Crystal Structure of a phosphoglycerate mutase gpm1 from <i>Mycobacterium leprae</i> (PDB ID: 4EO9). Utilizing the smart minimizer algorithm, the protein's energy was reduced in order to achieve a stable local minima conformation.</p><p><strong>Results: </strong>The protein and molecule energy minimization protocol generated stable configuration energy molecules. The protein 4EO9 energy was reduced from 14264.5 kcal/mol to -17588.1 kcal/mol.</p><p><strong>Conclusion: </strong>The CHARMm algorithm-based CDOCKER run docked all three molecules (TEL) inside the 4EO9 protein binding pocket (<i>Mycobacterium leprae</i>). The interaction analysis revealed that tenofovir had a better binding molecule with a score of - 37.7297 kcal/mol than the other molecules.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"18 3","pages":"170-177"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9573889","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
SARS-CoV-2 Pandemic-Therapeutics in Warp Speed. SARS-CoV-2大流行的治疗方法。
Recent advances in anti-infective drug discovery Pub Date : 2023-01-01 DOI: 10.2174/2772434418666230119101350
Sourav Sen, Nitin Kumar
{"title":"SARS-CoV-2 Pandemic-Therapeutics in Warp Speed.","authors":"Sourav Sen,&nbsp;Nitin Kumar","doi":"10.2174/2772434418666230119101350","DOIUrl":"https://doi.org/10.2174/2772434418666230119101350","url":null,"abstract":"<p><p>Ever since the coronavirus disease 2019 (COVID-19) pandemic struck, the challenges posed to the scientific community by its causative agent, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) have been countless, and still continue to emerge. Even though a host of repurposed and new therapeutic agents as well as vaccines have been, and are being assessed at a breakneck speed, this contagion continues to create havoc, returning back in waves, with appearance of newer viral variants which are associated with numerous challenges, which include greater transmissibility, increased virulence, immune escape, etc. In this study, we discuss the current status of various therapeutic agents which are being used, or in the various stages of preclinical/clinical trials for managing COVID-19.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"18 2","pages":"110-119"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9864347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Isoniazid Loaded PCL-PEG Copolymer Nanoparticles for Sustained Release Application. 异烟肼负载聚氯联苯-聚乙二醇共聚物纳米颗粒缓释应用。
Recent advances in anti-infective drug discovery Pub Date : 2023-01-01 DOI: 10.2174/2772434418666230228121730
Alpana Kulkarni, Priya Betai
{"title":"Isoniazid Loaded PCL-PEG Copolymer Nanoparticles for Sustained Release Application.","authors":"Alpana Kulkarni,&nbsp;Priya Betai","doi":"10.2174/2772434418666230228121730","DOIUrl":"https://doi.org/10.2174/2772434418666230228121730","url":null,"abstract":"<p><strong>Background: </strong>Tuberculosis (TB) is still a major cause of death worldwide, despite possibly curable therapies. Neurotoxicity, optic neuritis, and severe liver damage are side effects of isoniazid, a powerful first-line anti-TB drug.</p><p><strong>Objective: </strong>We investigated the use of PCL-PEG copolymer to sustain the release of isoniazid to reduce its adverse effects.</p><p><strong>Methods: </strong>In the present work, PCL-PEG copolymer was synthesized and characterized. Isoniazid-loaded nanoparticles (Inp) were prepared using a PCL-PEG copolymer. Furthermore, a 2<sup>3</sup> half factorial design was employed for the optimization of drug and emulsifier concentration in Inp. Full characterization of the nanoparticles was performed in terms of drug loading, entrapment efficiency, particle size, zeta potential, and in vitro drug release. The morphology, FTIR, DSC, and PXRD evaluation of the optimized Batch Inp F13 were studied. Stability was evaluated by storing the freeze-dried Inp F13 at various temperatures.</p><p><strong>Results: </strong>The entrapment efficiency and drug loading of nanoparticles prepared by double emulsion solvent evaporation were found to be the highest. The release study revealed that all batches of nanoparticles exhibited sustained drug release (60.26 - 88.59%) for 5 days. The cytotoxicity study conducted on <i>Mycobacterium tuberculosis </i>revealed a gradual release of isoniazid from Inp, reaching the maximum (on the 15<sup>th</sup> day) compared to plain isoniazid (on the 4<sup>th</sup> day). At 0.8 μg/mL concentration, the inhibitory activity of Inp F13 was maintained for 15 days, indicating sustained release of isoniazid.</p><p><strong>Conclusion: </strong>The nanoparticles having PCL:PEG in a 95:5 ratio, with 0.5% PVA and initial drug loading of 3 mg, produced the optimum batch. Isoniazid-loaded PCL-PEG nanoparticles allowed controlled (sustained) release of isoniazid.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"18 3","pages":"221-238"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9947808","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Whether Early Steroid dose is Associated with Lower Mortality in COVID-19 Critically Ill Patients-An Exploratory Chart Review. 早期类固醇剂量是否与COVID-19危重患者的低死亡率相关——一项探索性图表回顾
Recent advances in anti-infective drug discovery Pub Date : 2023-01-01 DOI: 10.2174/2772434417666220817121439
Abhishek Goyal, Ankur Joshi, Saurabh Saigal, Dodda Brahmam, Yogesh Niwariya, Alkesh Khurana, Sagar Khadanga, Arun Mitra
{"title":"Whether Early Steroid dose is Associated with Lower Mortality in COVID-19 Critically Ill Patients-An Exploratory Chart Review.","authors":"Abhishek Goyal,&nbsp;Ankur Joshi,&nbsp;Saurabh Saigal,&nbsp;Dodda Brahmam,&nbsp;Yogesh Niwariya,&nbsp;Alkesh Khurana,&nbsp;Sagar Khadanga,&nbsp;Arun Mitra","doi":"10.2174/2772434417666220817121439","DOIUrl":"https://doi.org/10.2174/2772434417666220817121439","url":null,"abstract":"<p><strong>Introduction: </strong>Steroids have shown its usefulness in critically ill COVID-19 patients. However, the time of starting steroid and dose tailored to severity remain a matter of inquiry due to still emerging evidences and wide-ranging concerns of benefits and harms. We did a retrospective record analysis in an apex teaching hospital ICU setting to explore optimal doses and duration of steroid therapy which can decrease mortality.</p><p><strong>Methods: </strong>114 adults with COVID-19-ARDS admitted to ICU between 20th March-15th August 2020 were included in chart review. We did preliminary exploratory analysis (rooted in steroid therapy matrix categorized by dose and duration) to understand the effect of several covariates on survival. This was followed by univariate and multivariate Cox proportion hazard regression analysis and model diagnostics.</p><p><strong>Results: </strong>Exploratory analysis and visualization indicated age, optimal steroid, severity (measured in P/F) of disease and infection status as potential covariates for survival. Univariate cox regression analysis showed significant positive association of age > 60 years {2.6 (1.5-4.7)} and protective effect of optimum steroid {0.38(0.2-0.72)} on death (hazard) in critically ill patients. Multivariate cox regression analysis after adjusting effect of age showed protective effect of optimum steroid on hazard defined as death {0.46(0.23-0.87), LR = 17.04, (p = 2e-04)}. The concordance was 0.70 and model diagnostics fulfilled the assumption criteria for proportional hazard model.</p><p><strong>Conclusion: </strong>Optimal dose steroid as per defined 'optimum' (<24 hours and doses tailored to P/F at presentation) criteria can offer protective effect from mortality which persists after adjusting for age. This protective effect was not found to be negatively influenced by the risk of infection.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"18 1","pages":"42-53"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9111169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Meet the Regional Editor 见见地区编辑
Recent advances in anti-infective drug discovery Pub Date : 2022-11-01 DOI: 10.2174/277243441703221110095800
A. Tsakris
{"title":"Meet the Regional Editor","authors":"A. Tsakris","doi":"10.2174/277243441703221110095800","DOIUrl":"https://doi.org/10.2174/277243441703221110095800","url":null,"abstract":"","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77855522","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Meet the Regional Editor 认识地区编辑
Recent advances in anti-infective drug discovery Pub Date : 2022-08-01 DOI: 10.2174/277243441702221007104933
Michael R. Hamblin
{"title":"Meet the Regional Editor","authors":"Michael R. Hamblin","doi":"10.2174/277243441702221007104933","DOIUrl":"https://doi.org/10.2174/277243441702221007104933","url":null,"abstract":"<jats:sec>\u0000<jats:title />\u0000<jats:p />\u0000</jats:sec>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81935839","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
A study on the bio-responses of a freshwater snail (Biomphalaria alexandrina) to fungal derived compounds. 淡水蜗牛(Biomphalaria alexandrina)对真菌衍生化合物的生物反应研究。
Recent advances in anti-infective drug discovery Pub Date : 2022-06-10 DOI: 10.2174/2772434417666220610110226
A. Mekawey, Salah A R, Mohammed Yosri
{"title":"A study on the bio-responses of a freshwater snail (Biomphalaria alexandrina) to fungal derived compounds.","authors":"A. Mekawey, Salah A R, Mohammed Yosri","doi":"10.2174/2772434417666220610110226","DOIUrl":"https://doi.org/10.2174/2772434417666220610110226","url":null,"abstract":"BACKGROUND\u0000Biomphalaria alexandrina snails, as transitional hosts of schistosomiasis, plays an essential part in spread of the illness. Control of these snails by the substance molluscicides antagonistically influences the oceanic climate, causing poisonous and cancer-causing consequences for non-target life forms.\u0000\u0000\u0000OBJECTIVE\u0000Looking for new naturally safe substances can be used for treatment of schistosomiasis disease with minimal side effects on environment and plants, fish wealth and did not affect on human vital functions.\u0000\u0000\u0000METHODS\u0000Fifty fungal species were used to evaluate their activity against Biomphalaria alexandrina. Study the effect of fungal extract on vital functions of Biomphalaria alexandrina and fish wealth. Purification of active substances and identification of their chemical structures. Results Cladosporium nigrellum and Penicillium aurantiogresium metabolites were effective against B. alexandrina snails, the effects of promising fungal extracts sub-lethal concentrations (IC10 & IC25) on the levels of steroid sex hormones, liver enzymes, total protein, lipids, albumin and glucose were determined. Chemical analyses of this filtrate resulted in the separation of a compound effective against snails; it was identified. Protein electrophoresis showed that fungal filtrate affects the protein pattern of snails' haemolymph. Little or no mortality of Daphnia pulex individuals was observed after their exposure to sub lethal concentrations of each treatment.\u0000\u0000\u0000CONCLUSION\u0000Certain compounds from fungal cultures could be safely used for biological control of Biomphalaria alexandrina snails.","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82306242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, Synthesis, Anti-microbial and Molecular Docking Studies of Novel 5-Pyrazyl-2-Sulfanyl-1, 3, 4-Oxadiazole Derivatives. 新型5-吡唑-2-磺胺基- 1,3,4 -恶二唑衍生物的设计、合成、抗菌及分子对接研究。
Recent advances in anti-infective drug discovery Pub Date : 2022-06-09 DOI: 10.2174/2772434417666220609105755
R. Das, D. Mehta, Sumeet Gupta, Meenakshi Dhanawat
{"title":"Design, Synthesis, Anti-microbial and Molecular Docking Studies of Novel 5-Pyrazyl-2-Sulfanyl-1, 3, 4-Oxadiazole Derivatives.","authors":"R. Das, D. Mehta, Sumeet Gupta, Meenakshi Dhanawat","doi":"10.2174/2772434417666220609105755","DOIUrl":"https://doi.org/10.2174/2772434417666220609105755","url":null,"abstract":"BACKGROUND\u0000Chemical modification of Oxadiazole may lead to a potent therapeutic agent. A series of novel 5-pyrazyl-2-sulfanyl-1, 3, 4-oxadiazole derivatives (5a-g) have been synthesised utilising pyrazinoic acid as a precursor. The new oxadiazole compounds were docked against potential targets and evaluated for antibacterial and antitubercular activity.\u0000\u0000\u0000METHODS\u0000The 5-pyrazyl-2-substituted sulfanyl-1,3,4-oxadiazole derivatives (5a-g) were synthesized from the crucial intermediate 2-sulfanyl-5-pyrazyl-1,3,4-oxadiazole (4), which was prepared by treating the 2-pyrazyl hydrazide with CS2 and pyridine. IR, 1HNMR, 13C, MS and elemental analyses were used to confirm the chemical structures.\u0000\u0000\u0000RESULTS\u0000Antimicrobial activity was determined for each synthesized compound. Additionally, compounds were evaluated for antitubercular activity against the Mycobacterium Tuberculosis H37Rv strain. Compounds 5c, 5g, and 5a had a favourable antibacterial profile, while 5c and 5g (MIC = 25 g/ml) demonstrated potential antitubercular activity when compared to the other produced compounds. Molecular docking experiments using V-Life Science MDS 4.6 supplemented the biological data.\u0000\u0000\u0000CONCLUSION\u0000Each compound has been tested for antibacterial and antitubercular action against a variety of microorganism strains and exhibits considerable activity. Additionally, molecular docking analysis confirmed the experimental results by describing improved interaction patterns.","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"103 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74371927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Assessment of the anti-malarial properties of dihydroartemisinin-piperaquine phosphate solid lipid-based tablets. 磷酸二氢青蒿素-哌喹固体脂基片抗疟疾性能评价。
Recent advances in anti-infective drug discovery Pub Date : 2022-06-06 DOI: 10.2174/2772434417666220606105822
Chime Salome A, A. A., Onunkwo Godswill C
{"title":"Assessment of the anti-malarial properties of dihydroartemisinin-piperaquine phosphate solid lipid-based tablets.","authors":"Chime Salome A, A. A., Onunkwo Godswill C","doi":"10.2174/2772434417666220606105822","DOIUrl":"https://doi.org/10.2174/2772434417666220606105822","url":null,"abstract":"BACKGROUND\u0000Artemisinin based combination therapies (ACTs) typified by dihydroartemisinin-piperaquine phosphate is one of the first line drugs used in the treatment of Plasmodium falciparum malaria. However, the emergence of drug resistance to ACTs show the necessity to develop novel sustained release treatment in order to ensure maximum bioavailability.\u0000\u0000\u0000OBJECTIVES\u0000To formulate dihydroartemisinin (DHA)-piperaquine phosphate (PQ) sustained release tablets based on solidified reverse micellar solutions (SRMS).\u0000\u0000\u0000METHODS\u0000The SRMS was prepared by fusion using varying ratios of Phospholipon® 90H and Softisan® 154 and characterised. The tablets were prepared by using an in-house made and validated mould. The formulations were tested for uniformity of weight, hardness, friability, softening time, erosion time and in vitro-in vivo dissolution rate. Anti malarial properties were studied by modified Peter's 4-days suppressive test in mice. One-way analysis of variance (ANOVA) was used in analysis of results.\u0000\u0000\u0000RESULTS\u0000Smooth caplets, with average weight of 1300 ± 0.06 to 1312 ± 0.11 mg, drug content of 61 mg for DHA and t 450 mg for PQ. Tablets hardness ranged from 7.1 to 9.0 Kgf and softening time of 29.50 ± 1.90 min. Erosion time of 62.00 ± 2.58 to 152.00 ± 1.89 min were obtained for tablets formulated with Poloxamer 188 (Batches R2, S2 and T2) which significantly reduced the softening and erosion time (p < 0.05). In vitro release showed that optimized formulation had maximum release at 12 h. Formulations exhibited significantly higher parasitaemia clearance and in vivo absorption compared to marketed formulations at day 7 (p < 0.05).\u0000\u0000\u0000CONCLUSION\u0000DHA-PQ tablets based on SRMS is much easier and relatively cheaper to produce than compressed tablets. They also showed exceptionally better treatment of malaria owing to their sustained release properties and improved bioavailability and is recommended to Pharmaceutical companies for further studies.","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88173535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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