Pub Date : 2023-11-01Epub Date: 2023-12-12DOI: 10.4155/tde-2023-0064
Yotomi Desia Eka Rani, Mahardian Rahmadi, Dewi Melani Hariyadi
Aim: Inhalable microspheres made of polymers as a targeted drug delivery system have been developed to overcome the limitation of current treatments in Tuberculosis. Materials & methods: Isoniazid inhalable microspheres were created using a gelation ionotropic method with sodium alginate, carrageenan and calcium chloride in four different formulations. Result: The particle morphology has smooth surfaces and round spherical shapes with sizes below 5 μm; good flowability. The drug loading and entrapment efficiency values ranged from 1.69 to 2.75% and 62.44 to 85.30%, respectively. The microspheres drug release followed the Korsmeyer-Peppas model, indicating Fickian diffusion. Conclusion: Isoniazid inhalable microspheres achieved as targeted lung delivery for tuberculosis treatment.
{"title":"Characteristics and release of isoniazid from inhalable alginate/carrageenan microspheres.","authors":"Yotomi Desia Eka Rani, Mahardian Rahmadi, Dewi Melani Hariyadi","doi":"10.4155/tde-2023-0064","DOIUrl":"10.4155/tde-2023-0064","url":null,"abstract":"<p><p><b>Aim:</b> Inhalable microspheres made of polymers as a targeted drug delivery system have been developed to overcome the limitation of current treatments in Tuberculosis. <b>Materials & methods:</b> Isoniazid inhalable microspheres were created using a gelation ionotropic method with sodium alginate, carrageenan and calcium chloride in four different formulations. <b>Result:</b> The particle morphology has smooth surfaces and round spherical shapes with sizes below 5 μm; good flowability. The drug loading and entrapment efficiency values ranged from 1.69 to 2.75% and 62.44 to 85.30%, respectively. The microspheres drug release followed the Korsmeyer-Peppas model, indicating Fickian diffusion. <b>Conclusion:</b> Isoniazid inhalable microspheres achieved as targeted lung delivery for tuberculosis treatment.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":"14 11","pages":"689-704"},"PeriodicalIF":4.2,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138797681","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}
Pub Date : 2023-11-01Epub Date: 2023-11-28DOI: 10.4155/tde-2023-0076
Annapurna Padaraju, Falguni Dwivedi, Gautam Kumar
According to estimates, up to 25% of the world's population has fungal skin diseases, making them the most prevalent infectious disease. Several chemical classes of antifungal drugs are available to treat fungal infections. However, the major challenges of conventional formulations of antifungal drugs include poor pharmacokinetic profiles like solubility, low permeability, side effects and decreased efficacy. Novel drug delivery is a promising approach for overcoming pharmacokinetic limitations and increasing the effectiveness of antibiotics. In this review, we have shed light on microemulsions, nanoemulsions, and emulgels as novel drug delivery approaches for the topical delivery of antifungal antibiotics. We believe these formulations have potential translational value and could be developed for treating fungal infections in humans.
{"title":"Microemulsions, nanoemulsions and emulgels as carriers for antifungal antibiotics.","authors":"Annapurna Padaraju, Falguni Dwivedi, Gautam Kumar","doi":"10.4155/tde-2023-0076","DOIUrl":"10.4155/tde-2023-0076","url":null,"abstract":"<p><p>According to estimates, up to 25% of the world's population has fungal skin diseases, making them the most prevalent infectious disease. Several chemical classes of antifungal drugs are available to treat fungal infections. However, the major challenges of conventional formulations of antifungal drugs include poor pharmacokinetic profiles like solubility, low permeability, side effects and decreased efficacy. Novel drug delivery is a promising approach for overcoming pharmacokinetic limitations and increasing the effectiveness of antibiotics. In this review, we have shed light on microemulsions, nanoemulsions, and emulgels as novel drug delivery approaches for the topical delivery of antifungal antibiotics. We believe these formulations have potential translational value and could be developed for treating fungal infections in humans.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"721-740"},"PeriodicalIF":4.2,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138446321","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}
Pub Date : 2023-11-01Epub Date: 2023-11-28DOI: 10.4155/tde-2023-0044
Vishal Kumar, Nethish Kumaar R, D Aswin, Sreeja C Nair
Aim: To develop a propranolol HCL-loaded liposomal nasal formulation for migraine prophylaxis. Materials & methods: Formulated the liposomes through thin layer hydration method and optimized via design of experiments (DOE). The prepared liposomes were characterized for particle size, zeta potential, PDI, drug entrapment and drug loading. Assessed for in vitro release kinetics, ex vivo permeability, histopathology and stability. Results: Optimized liposomes: 135.52 ± 5.87 nm, -19.9 ± 0.075 mV, 95.41 ± 0.05% entrapment, 43.37 ± 0.02% loading. Showed immediate (30.07 ± 2.09%) and sustained release (95.69 ± 4.58%) over 10 h. Enhanced permeation compared with controls; well-tolerated histopathologically. Conclusion: Liposomal formulation offers promise for intranasal propranolol HCL delivery in migraine prophylaxis, with stability under refrigeration.
{"title":"Propranolol HCL-loaded liposomes for intranasal delivery: <i>in vitro</i> and <i>ex vivo</i> evaluation of optimized formulation using design of experiments.","authors":"Vishal Kumar, Nethish Kumaar R, D Aswin, Sreeja C Nair","doi":"10.4155/tde-2023-0044","DOIUrl":"10.4155/tde-2023-0044","url":null,"abstract":"<p><p><b>Aim:</b> To develop a propranolol HCL-loaded liposomal nasal formulation for migraine prophylaxis. <b>Materials & methods:</b> Formulated the liposomes through thin layer hydration method and optimized via design of experiments (DOE). The prepared liposomes were characterized for particle size, zeta potential, PDI, drug entrapment and drug loading. Assessed for <i>in vitro</i> release kinetics, <i>ex vivo</i> permeability, histopathology and stability. <b>Results:</b> Optimized liposomes: 135.52 ± 5.87 nm, -19.9 ± 0.075 mV, 95.41 ± 0.05% entrapment, 43.37 ± 0.02% loading. Showed immediate (30.07 ± 2.09%) and sustained release (95.69 ± 4.58%) over 10 h. Enhanced permeation compared with controls; well-tolerated histopathologically. <b>Conclusion:</b> Liposomal formulation offers promise for intranasal propranolol HCL delivery in migraine prophylaxis, with stability under refrigeration.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"705-720"},"PeriodicalIF":4.2,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138446322","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}
Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The in situ floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion:In situ floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.
目的:硫酸阿扎那韦属 BCS II 类药物,由于其快速的首过代谢和 P-gp 外流,其口服生物利用度有限。材料与方法:采用离子凝胶法制备了使用复方药物的原位浮动凝胶,并按照 32 全因子设计优化了配方。结果:胶凝聚合物的浓度会影响药物释放和浮滞时间,反之亦然。结论硫酸阿扎那韦原位浮动凝胶由于增加了胃停留时间而有望持续释放药物,从而提高了潜在治疗效果。
{"title":"<i>In situ</i> gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation.","authors":"Rajashree Masareddy, Pradnya Sandure, Archana Patil, Yadishma Gaude, Arpana Patil","doi":"10.4155/tde-2023-0037","DOIUrl":"10.4155/tde-2023-0037","url":null,"abstract":"<p><p><b>Aim:</b> Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. <b>Materials & methods:</b> The <i>in situ</i> floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 3<sup>2</sup> full factorial design. <b>Results:</b> Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and <i>vice versa</i>. <b>Conclusion:</b> <i>In situ</i> floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"619-633"},"PeriodicalIF":4.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138488487","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}
Pub Date : 2023-10-01Epub Date: 2023-12-05DOI: 10.4155/tde-2023-0059
Vinayak S Patil, Kishori P Sutar, Rachana D Pockle, Siddarth Usulkar, Vishwanath A Jadhav
Aim: To develop stable non-ionic surfactant vesicles containing amisulpride (AMS) to improve brain uptake via nose to brain mechanism. Methods: Niosomes were developed using a modified ethanol injection technique, optimized using 32 factorial design and evaluated for the vesicle size (VS), percent encapsulation efficiency (EE), zeta potential (ZP) and % cumulative drug release (%CDR). Results: Optimized niosomes (Span-60: cholesterol ratio 0:1) showed 191.4 nm VS, 84.25% EE, -38.2 ZP and 81.31% CDR. In situ gel with these niosomes displayed 78% CDR. TEM analysis revealed spherical niosomes. Pharmacokinetic and brain tissue distribution studies in rats showed enhanced plasma and brain concentrations, indicating successful brain targeting. Conclusion: This strategy demonstrates improved AMS permeation via the nasal cavity, enhancing bioavailability for treating schizophrenia.
{"title":"Formulation, optimization and evaluation of amisulpride-loaded niosomal intranasal gel for brain targeting.","authors":"Vinayak S Patil, Kishori P Sutar, Rachana D Pockle, Siddarth Usulkar, Vishwanath A Jadhav","doi":"10.4155/tde-2023-0059","DOIUrl":"10.4155/tde-2023-0059","url":null,"abstract":"<p><p><b>Aim:</b> To develop stable non-ionic surfactant vesicles containing amisulpride (AMS) to improve brain uptake via nose to brain mechanism. <b>Methods:</b> Niosomes were developed using a modified ethanol injection technique, optimized using 3<sup>2</sup> factorial design and evaluated for the vesicle size (VS), percent encapsulation efficiency (EE), zeta potential (ZP) and % cumulative drug release (%CDR). <b>Results:</b> Optimized niosomes (Span-60: cholesterol ratio 0:1) showed 191.4 nm VS, 84.25% EE, -38.2 ZP and 81.31% CDR. <i>In situ</i> gel with these niosomes displayed 78% CDR. TEM analysis revealed spherical niosomes. Pharmacokinetic and brain tissue distribution studies in rats showed enhanced plasma and brain concentrations, indicating successful brain targeting. <b>Conclusion:</b> This strategy demonstrates improved AMS permeation via the nasal cavity, enhancing bioavailability for treating schizophrenia.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"635-647"},"PeriodicalIF":4.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138488511","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}
Pub Date : 2023-10-01Epub Date: 2023-11-28DOI: 10.4155/tde-2023-0036
M C Linju, M R Rekha
Recently, the role of inorganic ions has been explored for its wound-healing applications. Ions do play key role in the normal functioning of the skin, including the epidermal barrier property, maintaining redox balance, enzymatic activities, tissue remodeling, etc. The care of chronic wounds is a concern and new cost-effective therapeutic strategies that modulate the wound microenvironment and cell behaviour are needed. First, this review illustrates the ions that play a role in wound healing and their molecular mechanisms that are accountable for modifying the wound. Further, the emerging strategies using metal ions to modulate the healing will be discussed. In this direction, localized delivery of inorganic ions of importance using advanced wound care biomaterials for wound healing applications is discussed.
{"title":"Role of inorganic ions in wound healing: an insight into the various approaches for localized delivery.","authors":"M C Linju, M R Rekha","doi":"10.4155/tde-2023-0036","DOIUrl":"10.4155/tde-2023-0036","url":null,"abstract":"<p><p>Recently, the role of inorganic ions has been explored for its wound-healing applications. Ions do play key role in the normal functioning of the skin, including the epidermal barrier property, maintaining redox balance, enzymatic activities, tissue remodeling, etc. The care of chronic wounds is a concern and new cost-effective therapeutic strategies that modulate the wound microenvironment and cell behaviour are needed. First, this review illustrates the ions that play a role in wound healing and their molecular mechanisms that are accountable for modifying the wound. Further, the emerging strategies using metal ions to modulate the healing will be discussed. In this direction, localized delivery of inorganic ions of importance using advanced wound care biomaterials for wound healing applications is discussed.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"649-667"},"PeriodicalIF":4.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138446323","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}
Pub Date : 2023-10-01Epub Date: 2023-11-28DOI: 10.4155/tde-2023-0060
Igor L Medintz, Divita Mathur
{"title":"The potential of DNA nanotechnology to advance multiple therapeutic systems.","authors":"Igor L Medintz, Divita Mathur","doi":"10.4155/tde-2023-0060","DOIUrl":"10.4155/tde-2023-0060","url":null,"abstract":"","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"615-618"},"PeriodicalIF":4.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138446324","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}
Bozica Kovacevic, Melissa Jones, Susbin Raj Wagle, Corina Mihaela Ionescu, Thomas Foster, Maja Đanić, Momir Mikov, Armin Mooranian, Hani Al-Salami
Aim: Cellular bioactivity and pathophysiological changes associated with chronic disorders are considered pivotal detrimental factors when developing novel formulations for biomedical applications. Methods: This paper investigates the use of bile acids and synthetic polypeptide poly-L-ornithine (PLO) in formulations and their impacts on a variety of cell lines, with a particular focus on their cellular bioactivity. Results: The hepatic cell line was the most negatively affected by the presence of PLO, while the muscle and beta-pancreatic cell lines did not show as profound of a negative impact of PLO on cellular viability. PLO was the least disruptive regarding mitochondrial function for muscle and beta cells. Conclusion: The addition of bile acids generally decreased mitochondrial respiration and altered bioenergetic parameters in all cell lines.
{"title":"Influence of poly-L-ornithine-bile acid nano hydrogels on cellular bioactivity and potential pharmacological applications.","authors":"Bozica Kovacevic, Melissa Jones, Susbin Raj Wagle, Corina Mihaela Ionescu, Thomas Foster, Maja Đanić, Momir Mikov, Armin Mooranian, Hani Al-Salami","doi":"10.4155/tde-2023-0034","DOIUrl":"https://doi.org/10.4155/tde-2023-0034","url":null,"abstract":"<p><p><b>Aim:</b> Cellular bioactivity and pathophysiological changes associated with chronic disorders are considered pivotal detrimental factors when developing novel formulations for biomedical applications. <b>Methods:</b> This paper investigates the use of bile acids and synthetic polypeptide poly-L-ornithine (PLO) in formulations and their impacts on a variety of cell lines, with a particular focus on their cellular bioactivity. <b>Results:</b> The hepatic cell line was the most negatively affected by the presence of PLO, while the muscle and beta-pancreatic cell lines did not show as profound of a negative impact of PLO on cellular viability. PLO was the least disruptive regarding mitochondrial function for muscle and beta cells. <b>Conclusion:</b> The addition of bile acids generally decreased mitochondrial respiration and altered bioenergetic parameters in all cell lines.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":""},"PeriodicalIF":4.2,"publicationDate":"2023-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10508281","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}
Atopic dermatitis is a prevalent chronic skin inflammation affecting 2.1 to 4.1% of adults globally. The complexity of its pathogenesis and the relapsing nature make it challenging to treat. Current treatments follow European Academy of Dermatology and Venerology guidelines, but advanced cases with recurring lesions lack effective therapies. To address this gap, researchers are exploring nanotechnology for targeted drug delivery. Nanoparticles offer benefits such as improved drug retention, stability, controlled release and targeted delivery through the disrupted epidermal barrier. This integrated review evaluates the current state of AD treatment and highlights the potential of novel nano-formulations as a promising approach to address the disease.
{"title":"Emerging nanotechnology backed formulations for the management of atopic dermatitis.","authors":"Ranjit Kumar Mahato, Mohini Singh, Hemanta Pathak, Niva Rani Gogoi, Rikynjai Kharbithai, Pinky Chowrasia, Pankaj Lochan Bora, Tumpa Sarkar, Bani Kumar Jana, Bhaskar Mazumder","doi":"10.4155/tde-2023-0033","DOIUrl":"10.4155/tde-2023-0033","url":null,"abstract":"<p><p>Atopic dermatitis is a prevalent chronic skin inflammation affecting 2.1 to 4.1% of adults globally. The complexity of its pathogenesis and the relapsing nature make it challenging to treat. Current treatments follow European Academy of Dermatology and Venerology guidelines, but advanced cases with recurring lesions lack effective therapies. To address this gap, researchers are exploring nanotechnology for targeted drug delivery. Nanoparticles offer benefits such as improved drug retention, stability, controlled release and targeted delivery through the disrupted epidermal barrier. This integrated review evaluates the current state of AD treatment and highlights the potential of novel nano-formulations as a promising approach to address the disease.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"543-569"},"PeriodicalIF":4.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10162612","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}