Pub Date : 2024-01-15DOI: 10.2174/0115672018275954231220101637
Sijing Chen, Kana Wang, Qiao Wang
Mannose, an isomer of glucose, exhibits a distinct molecular structure with the same formula but a different atom arrangement, contributing to its specific biological functions. Widely distributed in body fluids and tissues, particularly in the nervous system, skin, testes, and retinas, mannose plays a crucial role as a direct precursor for glycoprotein synthesis. Glycoproteins, essential for immune regulation and glycosylation processes, underscore the significance of mannose in these physiological activities. The clinical and biomedical applications of mannose are diverse, encompassing its anti-inflammatory properties, potential to inhibit bacterial infections, role in metabolism regulation, and suggested involvement in alleviating diabetes and obesity. Additionally, mannose shows promise in antitumor effects, immune modulation, and the construction of drug carriers, indicating a broad spectrum of therapeutic potential. The article aims to present a comprehensive review of mannose, focusing on its molecular structure, metabolic pathways, and clinical and biomedical applications, and also to emphasize its status as a promising therapeutic agent.
{"title":"Mannose: A Promising Player in Clinical and Biomedical Applications.","authors":"Sijing Chen, Kana Wang, Qiao Wang","doi":"10.2174/0115672018275954231220101637","DOIUrl":"https://doi.org/10.2174/0115672018275954231220101637","url":null,"abstract":"<p><p>Mannose, an isomer of glucose, exhibits a distinct molecular structure with the same formula but a different atom arrangement, contributing to its specific biological functions. Widely distributed in body fluids and tissues, particularly in the nervous system, skin, testes, and retinas, mannose plays a crucial role as a direct precursor for glycoprotein synthesis. Glycoproteins, essential for immune regulation and glycosylation processes, underscore the significance of mannose in these physiological activities. The clinical and biomedical applications of mannose are diverse, encompassing its anti-inflammatory properties, potential to inhibit bacterial infections, role in metabolism regulation, and suggested involvement in alleviating diabetes and obesity. Additionally, mannose shows promise in antitumor effects, immune modulation, and the construction of drug carriers, indicating a broad spectrum of therapeutic potential. The article aims to present a comprehensive review of mannose, focusing on its molecular structure, metabolic pathways, and clinical and biomedical applications, and also to emphasize its status as a promising therapeutic agent.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139682292","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}
Respiratory disorders, such as tuberculosis, cystic fibrosis, chronic obstructive pulmonary disease, asthma, lung cancer, and pulmonary inflammation, are among the most prevalent ailments in today's world. Dextran, an exopolysaccharide formed by Leuconostoc mesenteroides (slimeproducing bacteria), and its derivatives are investigated for several therapeutic utilities. Dextranbased drug delivery system can become an innovative strategy in the treatment of several respiratory ailments as it offers numerous advantages, such as mucolytic action, airway hydration, antiinflammatory properties, and radioprotective effect as compared to other polysaccharides. Being biocompatible, flexible hydrophilic nature, biodegradable, tasteless, odourless, non-mutagenic, watersoluble and non-toxic edible polymer, dextran-based drug delivery systems have been explored for a wide range of therapeutic applications, especially in lungs and respiratory diseases. The present article comprehensively discusses various derivatives of dextran with their attributes to be considered for drug delivery and extensive therapeutic benefits, with a special emphasis on the armamentarium of dextran-based formulations for the treatment of respiratory disorders and associated pathological conditions. The information provided will act as a platform for formulation scientists as important considerations in designing therapeutic approaches for lung and respiratory diseases. With an emphasis on lung illnesses, this article will offer an in-depth understanding of dextran-based delivery systems in respiratory illnesses.
{"title":"Dextran-based Drug Delivery Approaches for Lung Diseases: A Review.","authors":"Manisha Kumari, Sanyam Sharma, Navjot Kanwar, Subh Naman, Ashish Baldi","doi":"10.2174/0115672018267737231116100812","DOIUrl":"https://doi.org/10.2174/0115672018267737231116100812","url":null,"abstract":"<p><p>Respiratory disorders, such as tuberculosis, cystic fibrosis, chronic obstructive pulmonary disease, asthma, lung cancer, and pulmonary inflammation, are among the most prevalent ailments in today's world. Dextran, an exopolysaccharide formed by Leuconostoc mesenteroides (slimeproducing bacteria), and its derivatives are investigated for several therapeutic utilities. Dextranbased drug delivery system can become an innovative strategy in the treatment of several respiratory ailments as it offers numerous advantages, such as mucolytic action, airway hydration, antiinflammatory properties, and radioprotective effect as compared to other polysaccharides. Being biocompatible, flexible hydrophilic nature, biodegradable, tasteless, odourless, non-mutagenic, watersoluble and non-toxic edible polymer, dextran-based drug delivery systems have been explored for a wide range of therapeutic applications, especially in lungs and respiratory diseases. The present article comprehensively discusses various derivatives of dextran with their attributes to be considered for drug delivery and extensive therapeutic benefits, with a special emphasis on the armamentarium of dextran-based formulations for the treatment of respiratory disorders and associated pathological conditions. The information provided will act as a platform for formulation scientists as important considerations in designing therapeutic approaches for lung and respiratory diseases. With an emphasis on lung illnesses, this article will offer an in-depth understanding of dextran-based delivery systems in respiratory illnesses.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139514472","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 : 2024-01-12DOI: 10.2174/0115672018279213240110045557
Majed M Masadeh, Noor M Bany-Ali, Mai S Khanfar, Karem H Alzoubi, Majd M Massadeh, Enaam M Almomani
Background: The misuse of antibiotics leads to a global increase in antibiotic resistance. Therefore, it is imperative to search for alternative compounds to conventional antibiotics. ZnO nanoparticles (Zn NP) are one of these alternatives because they are an effective option to overcome biofilm bacterial cells and a novel way to overcome multidrug resistance in bacteria. The current research study aims to characterize the efficacy of ZnO nanoparticles alone and in combination with other antibacterial drugs against bacterial biofilms.
Methods: ZnO NPs were prepared by co-precipitation method, and their anti-biofilm and antibacterial activities alone or combined with four types of broad-spectrum antibacterial (Norfloxacin, Colistin, Doxycycline, and Ampicillin) were evaluated against E. coli and S. aureus bacterial strains. Finally, the cytotoxicity and the hemolytic activity were evaluated.
Results: ZnO NPs were prepared, and results showed that their size was around 10 nm with a spherical shape and a zeta potential of -21.9. In addition, ZnO NPs were found to have a strong antibacterial effect against Gram-positive and Gram-negative microorganisms, with a minimum inhibitory concentration (MIC) of 62.5 and 125 μg/mL, respectively. Additionally, they could eradicate biofilmforming microorganisms at a concentration of 125 μg/m. ZnO NPs were found to be non-toxic to erythrocyte cells. Still, some toxicity was observed for Vero cells at effective concentration ranges needed to inhibit bacterial growth and eradicate biofilm-forming organisms. When combined with different antibacterial, ZnO NP demonstrated synergistic and additive effects with colistin, and the MIC and MBEC of the combination decreased significantly to 0.976 μg/mL against planktonic and biofilm strains of MDR Gram-positive bacteria, resulting in significantly reduced toxicity.
Conclusion: The findings of this study encourage the development of alternative therapies with high efficacy and low toxicity. ZnO nanoparticles have demonstrated promising results in overcoming multi-drug resistant bacteria and biofilms, and their combination with colistin has shown a significant reduction in toxicity. Further studies are needed to investigate the potential of ZnO nanoparticles as a viable alternative to conventional antibiotics.
{"title":"Synergistic Antibacterial Effect of ZnO Nanoparticles and Antibiotics against Multidrug-Resistant Biofilm Bacteria.","authors":"Majed M Masadeh, Noor M Bany-Ali, Mai S Khanfar, Karem H Alzoubi, Majd M Massadeh, Enaam M Almomani","doi":"10.2174/0115672018279213240110045557","DOIUrl":"https://doi.org/10.2174/0115672018279213240110045557","url":null,"abstract":"<p><strong>Background: </strong>The misuse of antibiotics leads to a global increase in antibiotic resistance. Therefore, it is imperative to search for alternative compounds to conventional antibiotics. ZnO nanoparticles (Zn NP) are one of these alternatives because they are an effective option to overcome biofilm bacterial cells and a novel way to overcome multidrug resistance in bacteria. The current research study aims to characterize the efficacy of ZnO nanoparticles alone and in combination with other antibacterial drugs against bacterial biofilms.</p><p><strong>Methods: </strong>ZnO NPs were prepared by co-precipitation method, and their anti-biofilm and antibacterial activities alone or combined with four types of broad-spectrum antibacterial (Norfloxacin, Colistin, Doxycycline, and Ampicillin) were evaluated against E. coli and S. aureus bacterial strains. Finally, the cytotoxicity and the hemolytic activity were evaluated.</p><p><strong>Results: </strong>ZnO NPs were prepared, and results showed that their size was around 10 nm with a spherical shape and a zeta potential of -21.9. In addition, ZnO NPs were found to have a strong antibacterial effect against Gram-positive and Gram-negative microorganisms, with a minimum inhibitory concentration (MIC) of 62.5 and 125 μg/mL, respectively. Additionally, they could eradicate biofilmforming microorganisms at a concentration of 125 μg/m. ZnO NPs were found to be non-toxic to erythrocyte cells. Still, some toxicity was observed for Vero cells at effective concentration ranges needed to inhibit bacterial growth and eradicate biofilm-forming organisms. When combined with different antibacterial, ZnO NP demonstrated synergistic and additive effects with colistin, and the MIC and MBEC of the combination decreased significantly to 0.976 μg/mL against planktonic and biofilm strains of MDR Gram-positive bacteria, resulting in significantly reduced toxicity.</p><p><strong>Conclusion: </strong>The findings of this study encourage the development of alternative therapies with high efficacy and low toxicity. ZnO nanoparticles have demonstrated promising results in overcoming multi-drug resistant bacteria and biofilms, and their combination with colistin has shown a significant reduction in toxicity. Further studies are needed to investigate the potential of ZnO nanoparticles as a viable alternative to conventional antibiotics.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139479370","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 : 2024-01-11DOI: 10.2174/0115672018279370240103062944
Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao, Mingguan Piao
Background: Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.
Objective: The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.
Methods: Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.
Results: The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.
Conclusion: These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.
{"title":"Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation.","authors":"Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao, Mingguan Piao","doi":"10.2174/0115672018279370240103062944","DOIUrl":"https://doi.org/10.2174/0115672018279370240103062944","url":null,"abstract":"<p><strong>Background: </strong>Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.</p><p><strong>Objective: </strong>The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.</p><p><strong>Methods: </strong>Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.</p><p><strong>Results: </strong>The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.</p><p><strong>Conclusion: </strong>These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139514473","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 : 2024-01-11DOI: 10.2174/0115672018270396231213074746
Ankush Saini, Mohit Sharma, Indu Singh, Rajan Swami
Contact lenses (CLs) have become an essential tool in ocular drug delivery, providing effective treatment options for specific eye conditions. In recent advancements, Therapeutic CLs (TCLs) have emerged as a promising approach for maintaining therapeutic drug concentrations on the eye surface. TCLs offer unique attributes, including prolonged wear and a remarkable ability to enhance the bioavailability of loaded medications by more than 50%, thus gaining widespread usage. They have proven beneficial in pain management, medication administration, corneal healing, and protection. To achieve sustained drug delivery from TCLs, researchers are exploring diverse systems, such as polymeric nanoparticulate systems, lipidic systems, and the incorporation of agents like vitamin E or rate-limiting polymers. However, despite breakthrough successes, certain challenges persist, including ensuring drug stability during processing and manufacturing, controlling release kinetics, and biomaterial interaction, reducing protein adhesion, and addressing drug release during packaging and storage etc. While TCLs have shown overall success in treating corneal and ocular surface disorders, careful consideration of potential issues and contraindications is vital. This review offers an insightful perspective on the critical aspects that need to be addressed regarding TCLs, with a specific emphasis on their advantages and limitations.
{"title":"From Vision Correction to Drug Delivery: Unraveling the Potential of Therapeutic Contact Lens.","authors":"Ankush Saini, Mohit Sharma, Indu Singh, Rajan Swami","doi":"10.2174/0115672018270396231213074746","DOIUrl":"https://doi.org/10.2174/0115672018270396231213074746","url":null,"abstract":"<p><p>Contact lenses (CLs) have become an essential tool in ocular drug delivery, providing effective treatment options for specific eye conditions. In recent advancements, Therapeutic CLs (TCLs) have emerged as a promising approach for maintaining therapeutic drug concentrations on the eye surface. TCLs offer unique attributes, including prolonged wear and a remarkable ability to enhance the bioavailability of loaded medications by more than 50%, thus gaining widespread usage. They have proven beneficial in pain management, medication administration, corneal healing, and protection. To achieve sustained drug delivery from TCLs, researchers are exploring diverse systems, such as polymeric nanoparticulate systems, lipidic systems, and the incorporation of agents like vitamin E or rate-limiting polymers. However, despite breakthrough successes, certain challenges persist, including ensuring drug stability during processing and manufacturing, controlling release kinetics, and biomaterial interaction, reducing protein adhesion, and addressing drug release during packaging and storage etc. While TCLs have shown overall success in treating corneal and ocular surface disorders, careful consideration of potential issues and contraindications is vital. This review offers an insightful perspective on the critical aspects that need to be addressed regarding TCLs, with a specific emphasis on their advantages and limitations.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139428216","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}
Objective: Angiogenesis is the process of forming new blood vessels from pre-existing vessels and occurs during development, wound healing, and tumor growth. In this review, we aimed to present a comprehensive view of various factors contributing to angiogenesis during carcinogenesis. Anti-angiogenesis agents prevent or slow down cancer growth by interrupting the nutrients and blood supply to the tumor cells, and thus can prove beneficial for treatment.
Method: The discovery of several novel angiogenic inhibitors has helped to reduce both morbidity and mortality from several life-threatening diseases, such as carcinomas. There is an urgent need for a new comprehensive treatment strategy combining novel anti-angiogenic agents for the control of cancer. The article contains details of various angiogenic inhibitors that have been adopted by scientists to formulate and optimize such systems in order to make them suitable for cancer.
Results: The results of several researches have been summarized in the article and all of the data support the claim that anti-angiogenic agent is beneficial for cancer treatment.
Conclusion: This review focuses on novel antiangiogenic agents that play a crucial role in controlling carcinogenesis.
{"title":"Novel Products as Promising Therapeutic Agents for Angiogenesis Inhibition.","authors":"Shaheen Sultana, Shahnaz Sultana, Shehla Nasar Mir Najib Ullah, Ameeduzzafar Zafar","doi":"10.2174/0115672018277869231217165048","DOIUrl":"https://doi.org/10.2174/0115672018277869231217165048","url":null,"abstract":"<p><strong>Objective: </strong>Angiogenesis is the process of forming new blood vessels from pre-existing vessels and occurs during development, wound healing, and tumor growth. In this review, we aimed to present a comprehensive view of various factors contributing to angiogenesis during carcinogenesis. Anti-angiogenesis agents prevent or slow down cancer growth by interrupting the nutrients and blood supply to the tumor cells, and thus can prove beneficial for treatment.</p><p><strong>Method: </strong>The discovery of several novel angiogenic inhibitors has helped to reduce both morbidity and mortality from several life-threatening diseases, such as carcinomas. There is an urgent need for a new comprehensive treatment strategy combining novel anti-angiogenic agents for the control of cancer. The article contains details of various angiogenic inhibitors that have been adopted by scientists to formulate and optimize such systems in order to make them suitable for cancer.</p><p><strong>Results: </strong>The results of several researches have been summarized in the article and all of the data support the claim that anti-angiogenic agent is beneficial for cancer treatment.</p><p><strong>Conclusion: </strong>This review focuses on novel antiangiogenic agents that play a crucial role in controlling carcinogenesis.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139418908","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}
Background: Adding a suitable surfactant can enhance the transdermal permeability of transethosomes while also leveraging its functionality as a functional material. In this study, transethosomes were prepared using D-α-tocopherol acid polyethylene glycol succinate (TPGS) as edge activators for transdermal delivery of curcumin (Cur).
Methods: The TPGS-mediated curcumin-loaded transethosomes (Cur@TES) were prepared and formulated optimally, and the optimized formulations were characterized for their morphology, particle size, entrapment efficiency (EE) and drug loading (DL). The stability and deformability of Cur@TES were investigated, while the transdermal delivery of Cur@TES was investigated through in vitro transdermal assays and fluorescence imaging. A mouse ear swelling model was performed to determine the anti-inflammatory effect of Cur@TES.
Results: Cur@TES appeared round or elliptical in shape. The particle size, EE and DL for the optimized formulation were observed as 131.2 ± 7.2 nm, 97.68 ± 2.26%, and 6.58 ± 0.62%, respectively. X-ray diffraction analysis confirmed the formation of disordered structures in the inner core of the vesicles. Moreover, Cur@TES system demonstrated better stability and deformability compared to the curcumin-loaded ethosomes (Cur@ES). In-vitro transdermal experiments demonstrated that Cur@TES significantly increased the amount of drug retained in the skin (P<0.05). Fluorescence imaging confirmed that the skin distribution were distinctly enhanced with the delivery by TPGS mediated transethosomes. In addition, Cur@TES showed a significant inhibitory effect on Inflammatory swelling in the mouse ear-swelling model.
Conclusion: TPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.
{"title":"TPGS-mediated Transethosomes Enhance Transdermal Administration of Curcumin via Effects on Deformability and Stability.","authors":"Teng Guo, Chenming Zhang, Yuling Chen, Yihan Wu, Zhenda Liu, Yongtai Zhang, Nianping Feng","doi":"10.2174/0115672018279577231208055415","DOIUrl":"https://doi.org/10.2174/0115672018279577231208055415","url":null,"abstract":"<p><strong>Background: </strong>Adding a suitable surfactant can enhance the transdermal permeability of transethosomes while also leveraging its functionality as a functional material. In this study, transethosomes were prepared using D-α-tocopherol acid polyethylene glycol succinate (TPGS) as edge activators for transdermal delivery of curcumin (Cur).</p><p><strong>Methods: </strong>The TPGS-mediated curcumin-loaded transethosomes (Cur@TES) were prepared and formulated optimally, and the optimized formulations were characterized for their morphology, particle size, entrapment efficiency (EE) and drug loading (DL). The stability and deformability of Cur@TES were investigated, while the transdermal delivery of Cur@TES was investigated through in vitro transdermal assays and fluorescence imaging. A mouse ear swelling model was performed to determine the anti-inflammatory effect of Cur@TES.</p><p><strong>Results: </strong>Cur@TES appeared round or elliptical in shape. The particle size, EE and DL for the optimized formulation were observed as 131.2 ± 7.2 nm, 97.68 ± 2.26%, and 6.58 ± 0.62%, respectively. X-ray diffraction analysis confirmed the formation of disordered structures in the inner core of the vesicles. Moreover, Cur@TES system demonstrated better stability and deformability compared to the curcumin-loaded ethosomes (Cur@ES). In-vitro transdermal experiments demonstrated that Cur@TES significantly increased the amount of drug retained in the skin (P<0.05). Fluorescence imaging confirmed that the skin distribution were distinctly enhanced with the delivery by TPGS mediated transethosomes. In addition, Cur@TES showed a significant inhibitory effect on Inflammatory swelling in the mouse ear-swelling model.</p><p><strong>Conclusion: </strong>TPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139418909","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}
Background: Gefitinib (GFN) is an Epithelial Growth Factor Receptor (EGFR) inhibitor, and Food and Drug Administration (FDA) has approved medication to treat lung cancer. However, this investigation aimed to produce and characterize Gefitinib (GFN)-loaded chitosan and soy lecithin nanoparticles (NPs) modified with D-α-tocopheryl polyethylene glycol 1000 succinate mono ester (TPGS) and assess their therapeutic potential against HepG2 liver cell lines.
Methods: Chitosan, a cationic polymer with biocompatible and biodegradable properties, was combined with soy lecithin to develop the NPs loaded with GFN using a self-organizing ionic interaction methodology.
Results: The entrapment efficiency and drug loading were found to be 59.04±4.63 to 87.37±3.82% and 33.46±3.76 to 49.50±4.35%, respectively, and results indicated the encapsulation of GEN in NPs. The pH of the formulations was observed between 4.48-4.62. Additionally, all the prepared NPs showed the size and PDI range of 89.2±15.9 nm to 799.2±35.8 nm and 0.179±0.065 to 0.455±0.097, respectively. The FTIR bands in optimized formulation (GFN-NP1) indicated that the drug might be contained within the NP's core. The SEM photograph revealed the spherical shape of NPs. The kinetic release model demonstrated the combination of diffusion and erosion mechanisms. The IC50 value of GFN and GFN-NP1 formulation against the HepG2 cell lines were determined and found to be 63.22±3.36 μg/ml and 45.80±2.53 μg/ml, respectively. DAPI and PI staining agents were used to detect nuclear morphology.
Conclusion: It was observed that the optimized GFN-NP1 formulation successfully internalized and inhibited the growth of HepG2 cells. Hence, it can be concluded that the prepared NPs can be a new therapeutic option for treating liver cancer.
{"title":"TPGS-modified Chitosan Nanoparticles of EGFR Inhibitor: Physicochemical and In vitro Evaluation against HepG2 Cell Lines.","authors":"Mahendra Singh, Alka, Prashant Shukla, Zhi-Hong Wen, Chou-Yuan Ko, Ramachandran Vinayagam","doi":"10.2174/0115672018268315231206045504","DOIUrl":"https://doi.org/10.2174/0115672018268315231206045504","url":null,"abstract":"<p><strong>Background: </strong>Gefitinib (GFN) is an Epithelial Growth Factor Receptor (EGFR) inhibitor, and Food and Drug Administration (FDA) has approved medication to treat lung cancer. However, this investigation aimed to produce and characterize Gefitinib (GFN)-loaded chitosan and soy lecithin nanoparticles (NPs) modified with D-α-tocopheryl polyethylene glycol 1000 succinate mono ester (TPGS) and assess their therapeutic potential against HepG2 liver cell lines.</p><p><strong>Methods: </strong>Chitosan, a cationic polymer with biocompatible and biodegradable properties, was combined with soy lecithin to develop the NPs loaded with GFN using a self-organizing ionic interaction methodology.</p><p><strong>Results: </strong>The entrapment efficiency and drug loading were found to be 59.04±4.63 to 87.37±3.82% and 33.46±3.76 to 49.50±4.35%, respectively, and results indicated the encapsulation of GEN in NPs. The pH of the formulations was observed between 4.48-4.62. Additionally, all the prepared NPs showed the size and PDI range of 89.2±15.9 nm to 799.2±35.8 nm and 0.179±0.065 to 0.455±0.097, respectively. The FTIR bands in optimized formulation (GFN-NP1) indicated that the drug might be contained within the NP's core. The SEM photograph revealed the spherical shape of NPs. The kinetic release model demonstrated the combination of diffusion and erosion mechanisms. The IC50 value of GFN and GFN-NP1 formulation against the HepG2 cell lines were determined and found to be 63.22±3.36 μg/ml and 45.80±2.53 μg/ml, respectively. DAPI and PI staining agents were used to detect nuclear morphology.</p><p><strong>Conclusion: </strong>It was observed that the optimized GFN-NP1 formulation successfully internalized and inhibited the growth of HepG2 cells. Hence, it can be concluded that the prepared NPs can be a new therapeutic option for treating liver cancer.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139418910","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}
Background: Transdermal drug delivery systems (TDDS) offer several advantages over traditional methods like injections and oral administration, including preventing first-pass metabolism, providing consistent and sustained activity, reducing side effects, enabling the use of short halflife drugs, improving physiological response, and enhancing patient convenience. However, the permeability of skin poses a challenge for TDDS, as it is impermeable to large molecules and hydrophilic drugs but permeable to small molecules and lipophilic medications. To overcome this barrier, researchers have investigated vesicular systems, such as transfersomes, liposomes, niosomes, and ethosomes. Among these vesicular systems, transfersomes are particularly promising for non-invasive drug administration due to their deformability and flexible membrane. They have been extensively studied for delivering anticancer drugs, insulin, corticosteroids, herbal medicines, and NSAIDs through the skin. Transfersomes have demonstrated efficacy in treating skin cancer, improving insulin delivery, enhancing site-specific corticosteroid delivery, and increasing the permeation and therapeutic effects of herbal medicines. They have also been effective in delivering pain relief with minimal side effects using NSAIDs and opioids. Transfersomes have been used for transdermal immunization and targeted drug delivery, offering site-specific release and minimizing adverse effects. Overall, transfersomes are a promising approach for transdermal drug delivery in various therapeutic applications.
Objectives: The aim of the present review is to discuss the various advantages and limitations of transfersomes and their mechanism to penetration across the skin, as well as their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.
Methods: Data we searched from PubMed, Google Scholar, and ScienceDirect.
Results: In this review, we have explored the various methods of preparation of transferosomes and their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.
Conclusion: In comparison to other vesicular systems, transfersomes are more flexible, have greater skin penetration capability, can transport systemic medicines, and are more stable. Transfersomes are capable of delivering both hydrophilic and hydrophobic drugs, making them suitable for transdermal drug delivery. The developed transfersomal gel could be used to improve medicine delivery through the skin.
{"title":"Overcoming Skin Barrier with Transfersomes: Opportunities, Challenges, and Applications.","authors":"Bhupendra Dixena, Rashmi Madhariya, Anupama Panday, Alpana Ram, Akhlesh K Jain","doi":"10.2174/0115672018272012231213100535","DOIUrl":"https://doi.org/10.2174/0115672018272012231213100535","url":null,"abstract":"<p><strong>Background: </strong>Transdermal drug delivery systems (TDDS) offer several advantages over traditional methods like injections and oral administration, including preventing first-pass metabolism, providing consistent and sustained activity, reducing side effects, enabling the use of short halflife drugs, improving physiological response, and enhancing patient convenience. However, the permeability of skin poses a challenge for TDDS, as it is impermeable to large molecules and hydrophilic drugs but permeable to small molecules and lipophilic medications. To overcome this barrier, researchers have investigated vesicular systems, such as transfersomes, liposomes, niosomes, and ethosomes. Among these vesicular systems, transfersomes are particularly promising for non-invasive drug administration due to their deformability and flexible membrane. They have been extensively studied for delivering anticancer drugs, insulin, corticosteroids, herbal medicines, and NSAIDs through the skin. Transfersomes have demonstrated efficacy in treating skin cancer, improving insulin delivery, enhancing site-specific corticosteroid delivery, and increasing the permeation and therapeutic effects of herbal medicines. They have also been effective in delivering pain relief with minimal side effects using NSAIDs and opioids. Transfersomes have been used for transdermal immunization and targeted drug delivery, offering site-specific release and minimizing adverse effects. Overall, transfersomes are a promising approach for transdermal drug delivery in various therapeutic applications.</p><p><strong>Objectives: </strong>The aim of the present review is to discuss the various advantages and limitations of transfersomes and their mechanism to penetration across the skin, as well as their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.</p><p><strong>Methods: </strong>Data we searched from PubMed, Google Scholar, and ScienceDirect.</p><p><strong>Results: </strong>In this review, we have explored the various methods of preparation of transferosomes and their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.</p><p><strong>Conclusion: </strong>In comparison to other vesicular systems, transfersomes are more flexible, have greater skin penetration capability, can transport systemic medicines, and are more stable. Transfersomes are capable of delivering both hydrophilic and hydrophobic drugs, making them suitable for transdermal drug delivery. The developed transfersomal gel could be used to improve medicine delivery through the skin.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139099457","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 : 2024-01-03DOI: 10.2174/0115672018286832231218112557
Sudipta Das, Baishali Ghosh, Rudra Narayan Sahoo, Amit Kumar Nayak
Bioelectronic medicine is a multidisciplinary field that combines molecular medicine, neurology, engineering, and computer science to design devices for diagnosing and treating diseases. The advancements in bioelectronic medicine can improve the precision and personalization of illness treatment. Bioelectronic medicine can produce, suppress, and measure electrical activity in excitable tissue. Bioelectronic devices modify specific neural circuits using electrons rather than pharmaceuticals and use bioelectronic processes to regulate the biological processes underlining various diseases. This promotes the potential to address the underlying causes of illnesses, reduce adverse effects, and lower costs compared to conventional medication. The current review presents different important aspects of bioelectronic medicines with recent advancements. The area of bioelectronic medicine has a lot of potential for treating diseases, enabling non-invasive therapeutic intervention by regulating brain impulses. Bioelectronic medicine uses electricity to control biological processes, treat illnesses, or regain lost capability. These new classes of medicines are designed by the technological developments in the detection and regulation of electrical signaling methods in the nervous system. Peripheral nervous system regulates a wide range of processes in chronic diseases; it involves implanting small devices onto specific peripheral nerves, which read and regulate the brain signaling patterns to achieve therapeutic effects specific to the signal capacity of a particular organ. The potential for bioelectronic medicine field is vast, as it investigates for treatment of various diseases, including rheumatoid arthritis, diabetes, hypertension, paralysis, chronic illnesses, blindness, etc.
{"title":"Recent Advancements in Bioelectronic Medicine: A Review.","authors":"Sudipta Das, Baishali Ghosh, Rudra Narayan Sahoo, Amit Kumar Nayak","doi":"10.2174/0115672018286832231218112557","DOIUrl":"https://doi.org/10.2174/0115672018286832231218112557","url":null,"abstract":"<p><p>Bioelectronic medicine is a multidisciplinary field that combines molecular medicine, neurology, engineering, and computer science to design devices for diagnosing and treating diseases. The advancements in bioelectronic medicine can improve the precision and personalization of illness treatment. Bioelectronic medicine can produce, suppress, and measure electrical activity in excitable tissue. Bioelectronic devices modify specific neural circuits using electrons rather than pharmaceuticals and use bioelectronic processes to regulate the biological processes underlining various diseases. This promotes the potential to address the underlying causes of illnesses, reduce adverse effects, and lower costs compared to conventional medication. The current review presents different important aspects of bioelectronic medicines with recent advancements. The area of bioelectronic medicine has a lot of potential for treating diseases, enabling non-invasive therapeutic intervention by regulating brain impulses. Bioelectronic medicine uses electricity to control biological processes, treat illnesses, or regain lost capability. These new classes of medicines are designed by the technological developments in the detection and regulation of electrical signaling methods in the nervous system. Peripheral nervous system regulates a wide range of processes in chronic diseases; it involves implanting small devices onto specific peripheral nerves, which read and regulate the brain signaling patterns to achieve therapeutic effects specific to the signal capacity of a particular organ. The potential for bioelectronic medicine field is vast, as it investigates for treatment of various diseases, including rheumatoid arthritis, diabetes, hypertension, paralysis, chronic illnesses, blindness, etc.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139089844","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}