Pub Date : 2024-01-01Epub Date: 2024-10-03DOI: 10.1080/20415990.2024.2406216
Mahshid Samadi, Mitra Jelvehgari, Sara Salatin
Aim: The main aim of this study was to formulate and optimize sustained release mini-tablets of guaifenesin.Materials & methods: Guaifenesin granules were successfully prepared using different blend ratios of carnauba wax to drug by melt granulation method. The properties of granules were further modified by combining them with ethyl cellulose. The obtained granules were then mixed and compressed into mini-tablets using a tablet press machine. The resulting mini-tablets were characterized in terms of weight, thickness, hardness, drug content and in vitro drug release.Results: Mini-tablets with 1:6 carnauba wax to drug ratio showed superior physicochemical characteristics, releasing about 100.03% of guaifenesin over 8 h. Ethyl cellulose offers a great potential to accurately control drug release from mini-tablets.Conclusion: The prepared mini-tablets seem to be a very promising alternative to guaifenesin conventional formulations and can be used in adults and elderly people.
{"title":"Development and optimization of guaifenesin sustained release mini-tablets for adult and geriatric patients.","authors":"Mahshid Samadi, Mitra Jelvehgari, Sara Salatin","doi":"10.1080/20415990.2024.2406216","DOIUrl":"10.1080/20415990.2024.2406216","url":null,"abstract":"<p><p><b>Aim:</b> The main aim of this study was to formulate and optimize sustained release mini-tablets of guaifenesin.<b>Materials & methods:</b> Guaifenesin granules were successfully prepared using different blend ratios of carnauba wax to drug by melt granulation method. The properties of granules were further modified by combining them with ethyl cellulose. The obtained granules were then mixed and compressed into mini-tablets using a tablet press machine. The resulting mini-tablets were characterized in terms of weight, thickness, hardness, drug content and <i>in vitro</i> drug release.<b>Results:</b> Mini-tablets with 1:6 carnauba wax to drug ratio showed superior physicochemical characteristics, releasing about 100.03% of guaifenesin over 8 h. Ethyl cellulose offers a great potential to accurately control drug release from mini-tablets.<b>Conclusion:</b> The prepared mini-tablets seem to be a very promising alternative to guaifenesin conventional formulations and can be used in adults and elderly people.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"859-869"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11497993/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142366629","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-01Epub Date: 2024-10-11DOI: 10.1080/20415990.2024.2408214
Mengistie Diress, Armin Mooranian, Hani Al-Salami
{"title":"Industry updates in the field of therapeutic delivery in June 2024.","authors":"Mengistie Diress, Armin Mooranian, Hani Al-Salami","doi":"10.1080/20415990.2024.2408214","DOIUrl":"https://doi.org/10.1080/20415990.2024.2408214","url":null,"abstract":"","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":"15 11","pages":"819-828"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142475370","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}
Acute myeloid leukemia (AML), a heterogeneous hematopoietic cancer prevalent in adults, has been a leading cause of leukemia-associated deaths for decades. Despite advancements in understanding its pathology and pharmacological targets, therapeutic strategies have seen minimal change. The standard treatment, combining cytarabine and anthracycline, has persisted, accompanied by challenges such as pharmacokinetic issues and non-specific drug delivery, leading to severe side effects. Nanotechnology offers a promising solution through combination drug delivery. FDA-approved CPX351 (VYXEOS™) a liposomal formulation delivering doxorubicin and cytarabine, exemplifies enhanced therapeutic efficacy. Ongoing research explores various nanocarriers for delivering multiple bioactives, addressing drug targeting, pharmacokinetics and chemoresistance. This review highlights nanotechnology-based combination therapies for the effective management of AML, presenting a potential breakthrough in leukemia.
{"title":"Nanotechnology-assisted combination drug delivery: a progressive approach for the treatment of acute myeloid leukemia.","authors":"Neelam Poonia, Nikita Vijay Jadhav, Davuluri Mamatha, Manoj Garg, Atul Kabra, Amit Bhatia, Shreesh Ojha, Viney Lather, Deepti Pandita","doi":"10.1080/20415990.2024.2394012","DOIUrl":"10.1080/20415990.2024.2394012","url":null,"abstract":"<p><p>Acute myeloid leukemia (AML), a heterogeneous hematopoietic cancer prevalent in adults, has been a leading cause of leukemia-associated deaths for decades. Despite advancements in understanding its pathology and pharmacological targets, therapeutic strategies have seen minimal change. The standard treatment, combining cytarabine and anthracycline, has persisted, accompanied by challenges such as pharmacokinetic issues and non-specific drug delivery, leading to severe side effects. Nanotechnology offers a promising solution through combination drug delivery. FDA-approved CPX351 (VYXEOS™) a liposomal formulation delivering doxorubicin and cytarabine, exemplifies enhanced therapeutic efficacy. Ongoing research explores various nanocarriers for delivering multiple bioactives, addressing drug targeting, pharmacokinetics and chemoresistance. This review highlights nanotechnology-based combination therapies for the effective management of AML, presenting a potential breakthrough in leukemia.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"893-910"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11497954/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142296096","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Breast cancer is the leading cause of cancer-related deaths among women globally. The difficulties with anticancer medications, such as ineffective targeting, larger doses, toxicity to healthy cells and side effects, have prompted attention to alternate approaches to address these difficulties. RNA interference by small interfering RNA (siRNA) is one such tactic. When compared with chemotherapy, siRNA has several advantages, including the ability to quickly modify and suppress the expression of the target gene and display superior efficacy and safety. However, there are known challenges and hurdles that limits their clinical translation. Decomposition by endonucleases, renal clearance, hydrophilicity, negative surface charge, short half-life and off-target effects of naked siRNA are obstacles that hinder the desired biological activity of naked siRNA. Nanoparticulate systems such as polymeric, lipid, lipid-polymeric, metallic, mesoporous silica nanoparticles and several other nanocarriers were used for effective delivery of siRNA and to knock down genes involved in breast cancer and triple-negative breast cancer. The focus of this review is to provide a comprehensive picture of various strategies utilized for delivering siRNA, such as combinatorial delivery, development of modified nanoparticles, smart nanocarriers and nanocarriers that target angiogenesis, cancer stem cells and metastasis of breast cancer.
{"title":"Therapeutic delivery of siRNA for the management of breast cancer and triple-negative breast cancer.","authors":"Boya Manasa Sai, Yirivinti Hayagreeva Dinakar, Hitesh Kumar, Rupshee Jain, Sharyu Kesharwani, Siddharth S Kesharwani, Shyam Lal Mudavath, Ajmeer Ramkishan, Vikas Jain","doi":"10.1080/20415990.2024.2400044","DOIUrl":"10.1080/20415990.2024.2400044","url":null,"abstract":"<p><p>Breast cancer is the leading cause of cancer-related deaths among women globally. The difficulties with anticancer medications, such as ineffective targeting, larger doses, toxicity to healthy cells and side effects, have prompted attention to alternate approaches to address these difficulties. RNA interference by small interfering RNA (siRNA) is one such tactic. When compared with chemotherapy, siRNA has several advantages, including the ability to quickly modify and suppress the expression of the target gene and display superior efficacy and safety. However, there are known challenges and hurdles that limits their clinical translation. Decomposition by endonucleases, renal clearance, hydrophilicity, negative surface charge, short half-life and off-target effects of naked siRNA are obstacles that hinder the desired biological activity of naked siRNA. Nanoparticulate systems such as polymeric, lipid, lipid-polymeric, metallic, mesoporous silica nanoparticles and several other nanocarriers were used for effective delivery of siRNA and to knock down genes involved in breast cancer and triple-negative breast cancer. The focus of this review is to provide a comprehensive picture of various strategies utilized for delivering siRNA, such as combinatorial delivery, development of modified nanoparticles, smart nanocarriers and nanocarriers that target angiogenesis, cancer stem cells and metastasis of breast cancer.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"871-891"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11498026/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142354280","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-01Epub Date: 2024-04-30DOI: 10.4155/tde-2023-0107
Mohammad Soroosh Hajizade, Mohammad Javad Raee, Seyed Nooreddin Faraji, Fakhrossadat Farvadi, Maryam Kabiri, Sedigheh Eskandari, Ali Mohammad Tamaddon
Aim: Streptokinase has poor selectivity and provokes the immune response. In this study, we used in silico studies to design a fusion protein to achieve targeted delivery to the thrombus. Materials & methods: Streptokinase was analyzed computationally for mapping. The fusion protein modeling and quality assessment were carried out on several servers. The enzymatic activity and the stability of the fusion protein and its complex with plasminogen were assessed through molecular docking analysis and molecular dynamics simulation respectively. Results: Physicochemical properties analysis, protein quality assessments, protein-protein docking and molecular dynamics simulations predicted that the designed fusion protein is functionally active. Conclusion: Our results showed that this fusion protein might be a prospective candidate as a novel thrombolytic agent with better selectivity.
{"title":"Targeted drug delivery to the thrombus by fusing streptokinase with a fibrin-binding peptide (CREKA): an <i>in silico</i> study.","authors":"Mohammad Soroosh Hajizade, Mohammad Javad Raee, Seyed Nooreddin Faraji, Fakhrossadat Farvadi, Maryam Kabiri, Sedigheh Eskandari, Ali Mohammad Tamaddon","doi":"10.4155/tde-2023-0107","DOIUrl":"10.4155/tde-2023-0107","url":null,"abstract":"<p><p><b>Aim:</b> Streptokinase has poor selectivity and provokes the immune response. In this study, we used <i>in silico</i> studies to design a fusion protein to achieve targeted delivery to the thrombus. <b>Materials & methods:</b> Streptokinase was analyzed computationally for mapping. The fusion protein modeling and quality assessment were carried out on several servers. The enzymatic activity and the stability of the fusion protein and its complex with plasminogen were assessed through molecular docking analysis and molecular dynamics simulation respectively. <b>Results:</b> Physicochemical properties analysis, protein quality assessments, protein-protein docking and molecular dynamics simulations predicted that the designed fusion protein is functionally active. <b>Conclusion:</b> Our results showed that this fusion protein might be a prospective candidate as a novel thrombolytic agent with better selectivity.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"399-411"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11285244/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140872178","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Aim: The present study aimed to prepare and evaluate fexofenadine self-microemulsifying drug-delivery systems (SMEDDS) formulation and to determine and compare its intestinal permeability using in situ single-pass intestinal perfusion (SPIP) technique.Methods: Fexofenadine-loaded SMEDDS were prepared and optimized. Droplet size, polydispersity index, zeta potential, drug release and intestinal permeability were evaluated.Results: Optimized formulation consisted of 15% oil, 80% surfactant and 5% cosolvent. Droplet size and drug loading of optimized formulation was 13.77 nm and 60 mg/g and it has released 90% of its drug content. Intestinal permeability of fexofenadine was threefold enhanced in SMEDDS compared with free fexofenadine.Conclusion: The results of our study revealed that SMEDDS could be a promising tool for oral delivery of fexofenadine with enhanced dissolution rate and intestinal permeability.
{"title":"Development of fexofenadine self-microemulsifying delivery systems: an efficient way to improve intestinal permeability.","authors":"Ziba Islambulchilar, Ashkan Barfar, Shahla Mirzaeei","doi":"10.1080/20415990.2024.2363635","DOIUrl":"10.1080/20415990.2024.2363635","url":null,"abstract":"<p><p><b>Aim:</b> The present study aimed to prepare and evaluate fexofenadine self-microemulsifying drug-delivery systems (SMEDDS) formulation and to determine and compare its intestinal permeability using <i>in situ</i> single-pass intestinal perfusion (SPIP) technique.<b>Methods:</b> Fexofenadine-loaded SMEDDS were prepared and optimized. Droplet size, polydispersity index, zeta potential, drug release and intestinal permeability were evaluated.<b>Results:</b> Optimized formulation consisted of 15% oil, 80% surfactant and 5% cosolvent. Droplet size and drug loading of optimized formulation was 13.77 nm and 60 mg/g and it has released 90% of its drug content. Intestinal permeability of fexofenadine was threefold enhanced in SMEDDS compared with free fexofenadine.<b>Conclusion:</b> The results of our study revealed that SMEDDS could be a promising tool for oral delivery of fexofenadine with enhanced dissolution rate and intestinal permeability.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"593-604"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11412145/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141470884","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-01Epub Date: 2024-10-03DOI: 10.1080/20415990.2024.2406226
Abrahem Sayed, Pranesh Ravichandran, Cecilia Canizela, Rehan M Hussain
EYP-1901 (Duravyu) has demonstrated promising outcomes in Phases I and II clinical trials for the treatment of neovascular age-related macular degeneration (nAMD) and diabetic macular edema (DME)/diabetic retinopathy. This innovative treatment capitalizes on the potent anti-angiogenic properties of vorolanib, an inhibitor that targets all isoforms of VEGF, effectively mitigating the pathological neovascularization and vascular permeability that underpin these retinal conditions. EYP-1901 is integrated with the Durasert drug delivery system to administer a sustained release of vorolanib directly to the posterior segment of the eye. This delivery system ensures a consistent therapeutic effect over an extended period and significantly reduces the frequency of clinical interventions required, offering a more convenient treatment regimen while maintaining patient safety.
EYP-1901(Duravyu)在治疗新生血管性老年性黄斑变性(nAMD)和糖尿病性黄斑水肿(DME)/糖尿病视网膜病变的 I 期和 II 期临床试验中取得了良好的疗效。Vorolanib 是一种针对血管内皮生长因子所有异构体的抑制剂,这种创新疗法利用了 Vorolanib 的强效抗血管生成特性,有效缓解了支撑这些视网膜病变的病理性新生血管和血管通透性。EYP-1901 与 Durasert 给药系统集成,可直接向眼球后段持续释放沃罗来尼。这种给药系统可确保长期持续的治疗效果,并大大减少所需的临床干预频率,在保证患者安全的同时提供更方便的治疗方案。
{"title":"Role of EYP-1901 in neovascular age-related macular degeneration and diabetic eye diseases: review of Phase I/II trials.","authors":"Abrahem Sayed, Pranesh Ravichandran, Cecilia Canizela, Rehan M Hussain","doi":"10.1080/20415990.2024.2406226","DOIUrl":"10.1080/20415990.2024.2406226","url":null,"abstract":"<p><p>EYP-1901 (Duravyu) has demonstrated promising outcomes in Phases I and II clinical trials for the treatment of neovascular age-related macular degeneration (nAMD) and diabetic macular edema (DME)/diabetic retinopathy. This innovative treatment capitalizes on the potent anti-angiogenic properties of vorolanib, an inhibitor that targets all isoforms of VEGF, effectively mitigating the pathological neovascularization and vascular permeability that underpin these retinal conditions. EYP-1901 is integrated with the Durasert drug delivery system to administer a sustained release of vorolanib directly to the posterior segment of the eye. This delivery system ensures a consistent therapeutic effect over an extended period and significantly reduces the frequency of clinical interventions required, offering a more convenient treatment regimen while maintaining patient safety.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"829-843"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11497975/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142366630","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Aim: This study was conducted to investigate the effect of fibrin glue-CM11 antibacterial peptide mixture (FG-P) on the healing of infected wounds in vivo.Materials & methods: We formulated a mixture of FG-P and evaluated its antimicrobial activity in vitro against multidrug-resistant (MDR) bacteria involved in wound infection as well as its healing effect on wound infected by methicillin-resistant S. aureus (MRSA) in vivo.Results: The peptide had an MIC of 8 μg/ml against all bacteria isolates. Growth inhibition zones were evident for FG-P compared with FG. The in vivo study showed that the FG-P could be significantly effective in healing the MRSA-infected wound.Conclusion: The use of FG-P mixture is a very suitable option for treating infected wounds.
{"title":"Antimicrobial peptide-fibrin glue mixture for treatment of methicillin-resistant <i>Staphylococcus aureus</i>-infected wounds.","authors":"Mehran Bahreini, Mehrdad Moosazadeh Moghaddam, Masoud Ghorbani, Mohammad Reza Nourani, Reza Mirnejad","doi":"10.1080/20415990.2024.2369497","DOIUrl":"10.1080/20415990.2024.2369497","url":null,"abstract":"<p><p><b>Aim:</b> This study was conducted to investigate the effect of fibrin glue-CM11 antibacterial peptide mixture (FG-P) on the healing of infected wounds <i>in vivo</i>.<b>Materials & methods:</b> We formulated a mixture of FG-P and evaluated its antimicrobial activity <i>in vitro</i> against multidrug-resistant (MDR) bacteria involved in wound infection as well as its healing effect on wound infected by methicillin-resistant <i>S. aureus</i> (MRSA) <i>in vivo</i>.<b>Results:</b> The peptide had an MIC of 8 μg/ml against all bacteria isolates. Growth inhibition zones were evident for FG-P compared with FG. The <i>in vivo</i> study showed that the FG-P could be significantly effective in healing the MRSA-infected wound.<b>Conclusion:</b> The use of FG-P mixture is a very suitable option for treating infected wounds.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"577-591"},"PeriodicalIF":3.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11412140/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141620973","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}