Pub Date : 2025-01-15DOI: 10.2174/0115672018346286241121052105
Rubhan Chandran, Eusni Rahayu Mohd Tohit, Johnson Stanslas, Norazlinaliza Salim, Tuan Mazlelaa Tuan Mahmood
Introduction: Poly(methyl vinyl ether co-maleic acid) (PMVE/MA) hydrogel microneedles (HMN) are investigated for transdermal delivery of macromolecular drugs owing to their biocompatibility and super-swelling properties. However, the drug delivery efficacy reduces with increasing molecular weight due to the entrapment within the HMN matrices. Furthermore, integrating external drug reservoirs extends the drug diffusion path and reduces the efficiency of drug permeation.
Methods: A direct drug loading approach in the HMN matrix was introduced in this work following a pH modification step. The effect of pH modification on the physicochemical properties of HMN was studied. Then, bovine serum albumin (BSA), a model protein, was loaded into the pH-modified HMN, and the morphological changes in HMN and protein stability were also assessed. Finally, the efficacy of BSA-loaded HMN in the transdermal delivery was evaluated ex vivo.
Results: A significant increase in swelling was recorded following the pH modification of HMN (p < 0.001). The structure of pH-modified hydrogel was highly porous, and ATR-FTIR spectra indicated a shift in the carboxylic peak. The secondary structure of BSA loaded in the pH-modified HMN was also preserved. The BSA-loaded HMN mediated a sustained ex-vivo drug release with a cumulative release of 64.70% (3.88 mg) in 24 h.
Conclusion: Hence, the model drug-incorporated PMVE/MA HMN system shows potential for sustainable transdermal delivery of proteins.
{"title":"Drug-Loaded Hydrogel Microneedles for Sustainable Transdermal Delivery of Macromolecular Proteins.","authors":"Rubhan Chandran, Eusni Rahayu Mohd Tohit, Johnson Stanslas, Norazlinaliza Salim, Tuan Mazlelaa Tuan Mahmood","doi":"10.2174/0115672018346286241121052105","DOIUrl":"https://doi.org/10.2174/0115672018346286241121052105","url":null,"abstract":"<p><strong>Introduction: </strong>Poly(methyl vinyl ether co-maleic acid) (PMVE/MA) hydrogel microneedles (HMN) are investigated for transdermal delivery of macromolecular drugs owing to their biocompatibility and super-swelling properties. However, the drug delivery efficacy reduces with increasing molecular weight due to the entrapment within the HMN matrices. Furthermore, integrating external drug reservoirs extends the drug diffusion path and reduces the efficiency of drug permeation.</p><p><strong>Methods: </strong>A direct drug loading approach in the HMN matrix was introduced in this work following a pH modification step. The effect of pH modification on the physicochemical properties of HMN was studied. Then, bovine serum albumin (BSA), a model protein, was loaded into the pH-modified HMN, and the morphological changes in HMN and protein stability were also assessed. Finally, the efficacy of BSA-loaded HMN in the transdermal delivery was evaluated ex vivo.</p><p><strong>Results: </strong>A significant increase in swelling was recorded following the pH modification of HMN (p < 0.001). The structure of pH-modified hydrogel was highly porous, and ATR-FTIR spectra indicated a shift in the carboxylic peak. The secondary structure of BSA loaded in the pH-modified HMN was also preserved. The BSA-loaded HMN mediated a sustained ex-vivo drug release with a cumulative release of 64.70% (3.88 mg) in 24 h.</p><p><strong>Conclusion: </strong>Hence, the model drug-incorporated PMVE/MA HMN system shows potential for sustainable transdermal delivery of proteins.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143019493","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 : 2025-01-13DOI: 10.2174/0115672018296163240910111938
Rameshwar Dass, Meenakshi Bhatia, Goutam Rath, Ashwani K Dhingra
Prokinetic agents are drugs used to enhance gastrointestinal motility and treat disorders such as Gastroesophageal Reflux Disease (GERD) and gastroparesis. pH-dependent release systems offer targeted drug delivery, allowing prokinetic agents to be released specifically in desired regions of the gastrointestinal tract. This optimizes drug efficacy and minimizes systemic side effects. Gastroretentive formulations enable sustained drug release, which is particularly beneficial in conditions requiring prolonged gastric residence time, such as gastroparesis. Nanoparticles have emerged as promising carriers for improving prokinetic agent delivery and enhancing drug stability, solubility, and absorption. These nano-systems protect drugs from degradation, leading to improved bioavailability and controlled drug release. Furthermore, incorporating mucoadhesive technologies promotes prolonged drug-mucosa interactions, facilitating enhanced drug absorption and reducing dosing frequency. These recent advancements have the potential to revolutionize the oral drug delivery of prokinetic agents, offering improved therapeutic outcomes, enhanced patient compliance, and reduced side effects. However, scalability, biocompatibility, and safety challenges warrant further investigation and validation through preclinical and clinical studies. This review highlights recent advances in oral drug delivery systems for prokinetic agents, focusing on innovative approaches such as pH-dependent release, gastroretentive formulations, nanoparticles, and mucoadhesive technologies. In conclusion, integrating advanced oral drug delivery systems for prokinetic agents presents a promising avenue for managing gastrointestinal disorders. Continued research and collaboration among academia, industry, and healthcare professionals are crucial to unlocking the full potential of these innovations and ultimately translating them into clinically effective treatments for patients.
{"title":"Recent Developments in Oral Drug Delivery of Prokinetic Agents: Nanoparticles and Beyond.","authors":"Rameshwar Dass, Meenakshi Bhatia, Goutam Rath, Ashwani K Dhingra","doi":"10.2174/0115672018296163240910111938","DOIUrl":"https://doi.org/10.2174/0115672018296163240910111938","url":null,"abstract":"<p><p>Prokinetic agents are drugs used to enhance gastrointestinal motility and treat disorders such as Gastroesophageal Reflux Disease (GERD) and gastroparesis. pH-dependent release systems offer targeted drug delivery, allowing prokinetic agents to be released specifically in desired regions of the gastrointestinal tract. This optimizes drug efficacy and minimizes systemic side effects. Gastroretentive formulations enable sustained drug release, which is particularly beneficial in conditions requiring prolonged gastric residence time, such as gastroparesis. Nanoparticles have emerged as promising carriers for improving prokinetic agent delivery and enhancing drug stability, solubility, and absorption. These nano-systems protect drugs from degradation, leading to improved bioavailability and controlled drug release. Furthermore, incorporating mucoadhesive technologies promotes prolonged drug-mucosa interactions, facilitating enhanced drug absorption and reducing dosing frequency. These recent advancements have the potential to revolutionize the oral drug delivery of prokinetic agents, offering improved therapeutic outcomes, enhanced patient compliance, and reduced side effects. However, scalability, biocompatibility, and safety challenges warrant further investigation and validation through preclinical and clinical studies. This review highlights recent advances in oral drug delivery systems for prokinetic agents, focusing on innovative approaches such as pH-dependent release, gastroretentive formulations, nanoparticles, and mucoadhesive technologies. In conclusion, integrating advanced oral drug delivery systems for prokinetic agents presents a promising avenue for managing gastrointestinal disorders. Continued research and collaboration among academia, industry, and healthcare professionals are crucial to unlocking the full potential of these innovations and ultimately translating them into clinically effective treatments for patients.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142985883","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 : 2025-01-10DOI: 10.2174/0115672018336704241128101556
Samin Hamidi, Ali Reza Shafiee-Kandjani, Sara Salatin
Due to the blood-brain barrier (BBB) and issues with oral and other traditional routes of administration, psychiatric disorders present significant challenges in getting therapeutics into the brain. The nose-to-brain pathway, also known as intranasal delivery, has shown promise in overcoming these barriers since it targets the brain directly and bypasses the BBB. This review explores nanocarriers' potential for intranasal delivery of therapeutics in the treatment of psychiatric disorders. Nanocarriers, such as polymeric nanoparticles, liposomes, and nanoemulsions, offer unique advantages for enhancing the delivery of various therapeutic agents to the brain via the intranasal route. The methodology involved conducting preliminary searches on databases such as PubMed, ScienceDirect, Web of Science, and Google Scholar using keywords related to "psychiatric disorders, intranasal delivery, nose-to-brain drug delivery, and nano formulations for intranasal delivery." This review highlights the advantages of the intranasal drug delivery pathway as a non-invasive, reliable, and efficient method for targeting the brain by bypassing the BBB. Furthermore, it discusses the application of various novel nanocarrier-based formulations, including nanoparticles, in-situ gels, nanoemulsions, hydrogels, and liposomes, for the effective intranasal delivery of therapeutics in the treatment of psychiatric conditions such as mood and anxiety disorders schizophrenia, and other illnesses.
由于血脑屏障(BBB)以及口服和其他传统给药途径的问题,精神疾病在使治疗药物进入大脑方面面临重大挑战。鼻到脑途径,也被称为鼻内输送,已经显示出克服这些障碍的希望,因为它直接针对大脑,绕过血脑屏障。这篇综述探讨了纳米载体在鼻内给药治疗精神疾病方面的潜力。纳米载体,如聚合纳米颗粒、脂质体和纳米乳液,为通过鼻内途径增强各种治疗药物向大脑的输送提供了独特的优势。该方法包括在PubMed、ScienceDirect、Web of Science和b谷歌Scholar等数据库中进行初步搜索,使用与“精神疾病、鼻内给药、鼻至脑药物给药和鼻内给药纳米配方”相关的关键词。这篇综述强调了鼻内给药途径作为一种绕过血脑屏障靶向大脑的无创、可靠和有效的方法的优势。此外,它还讨论了各种新型纳米载体配方的应用,包括纳米颗粒、原位凝胶、纳米乳液、水凝胶和脂质体,用于治疗精神疾病(如情绪和焦虑症、精神分裂症和其他疾病)的有效鼻内递送疗法。
{"title":"Nanosystems for Intranasal Delivery of Therapeutics in Psychiatric Disorders.","authors":"Samin Hamidi, Ali Reza Shafiee-Kandjani, Sara Salatin","doi":"10.2174/0115672018336704241128101556","DOIUrl":"https://doi.org/10.2174/0115672018336704241128101556","url":null,"abstract":"<p><p>Due to the blood-brain barrier (BBB) and issues with oral and other traditional routes of administration, psychiatric disorders present significant challenges in getting therapeutics into the brain. The nose-to-brain pathway, also known as intranasal delivery, has shown promise in overcoming these barriers since it targets the brain directly and bypasses the BBB. This review explores nanocarriers' potential for intranasal delivery of therapeutics in the treatment of psychiatric disorders. Nanocarriers, such as polymeric nanoparticles, liposomes, and nanoemulsions, offer unique advantages for enhancing the delivery of various therapeutic agents to the brain via the intranasal route. The methodology involved conducting preliminary searches on databases such as PubMed, ScienceDirect, Web of Science, and Google Scholar using keywords related to \"psychiatric disorders, intranasal delivery, nose-to-brain drug delivery, and nano formulations for intranasal delivery.\" This review highlights the advantages of the intranasal drug delivery pathway as a non-invasive, reliable, and efficient method for targeting the brain by bypassing the BBB. Furthermore, it discusses the application of various novel nanocarrier-based formulations, including nanoparticles, in-situ gels, nanoemulsions, hydrogels, and liposomes, for the effective intranasal delivery of therapeutics in the treatment of psychiatric conditions such as mood and anxiety disorders schizophrenia, and other illnesses.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142985798","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}
Introduction: Assessing the cytotoxicity of gold nanoparticles (GNPs) has gained importance due to their development in the biomedical field.
Method: In this study, we systematically synthesized gold nanorods (GNRs), gold nanobipyramids (GNBPs), and gold nanocups (GNCs) using a seed-mediated method, with an average length of 32.53 ± 4.67 nm, 72.90 ± 7.54 nm and 118.01 ± 11.02 nm, respectively.
Results: Furthermore, using the cell counting kit-8 (CCK-8) assay, we assessed the cellular cytotoxicity of three different types of GNPs with various different surface coatings, such as organic cetyltrimethylammonium bromide (CTAB) and polyethylene glycol (PEG). The results showed that the cytotoxic behavior of GNPs was shape-dependent in the concentration range of 3.125 -100 μg/mL. The types of GNPs and their surface coating had a significant impact on how the GNPs behaved in cells. Compared to PEG-coated GNPs, which do not induce cell injury, CTAB-coated GNPs show more noticeable cytotoxicity.
Conclusion: Furthermore, compared to GNCs, the toxicity of GNRs and GNBPs against GES-1 cells, RAW 264.7 cells and LX-2 cells was greater. Our research provides an important new understanding of the effects of surface modification on the biocompatibility and the shape of GNPs in the biomedical field.
{"title":"Facile Synthesis of Monodisperse Gold Nanorods, Gold Nanobipyramids and Gold Nanocups with Different Coatings and Evaluation of Their Cellular Cytotoxicity.","authors":"Fanjiao Zuo, Shuting Zhou, Xiwei Wu, Boyao Wang, Jun He, Xilong Qiu","doi":"10.2174/0115672018337291241118045126","DOIUrl":"https://doi.org/10.2174/0115672018337291241118045126","url":null,"abstract":"<p><strong>Introduction: </strong>Assessing the cytotoxicity of gold nanoparticles (GNPs) has gained importance due to their development in the biomedical field.</p><p><strong>Method: </strong>In this study, we systematically synthesized gold nanorods (GNRs), gold nanobipyramids (GNBPs), and gold nanocups (GNCs) using a seed-mediated method, with an average length of 32.53 ± 4.67 nm, 72.90 ± 7.54 nm and 118.01 ± 11.02 nm, respectively.</p><p><strong>Results: </strong>Furthermore, using the cell counting kit-8 (CCK-8) assay, we assessed the cellular cytotoxicity of three different types of GNPs with various different surface coatings, such as organic cetyltrimethylammonium bromide (CTAB) and polyethylene glycol (PEG). The results showed that the cytotoxic behavior of GNPs was shape-dependent in the concentration range of 3.125 -100 μg/mL. The types of GNPs and their surface coating had a significant impact on how the GNPs behaved in cells. Compared to PEG-coated GNPs, which do not induce cell injury, CTAB-coated GNPs show more noticeable cytotoxicity.</p><p><strong>Conclusion: </strong>Furthermore, compared to GNCs, the toxicity of GNRs and GNBPs against GES-1 cells, RAW 264.7 cells and LX-2 cells was greater. Our research provides an important new understanding of the effects of surface modification on the biocompatibility and the shape of GNPs in the biomedical field.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142980791","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: Eczema, an inflammatory skin disease causing intense itching, is a function of a range of internal and external factors, impacting individuals of all ages and leading to economic loss. Inflammation is the most important manifestation of eczema, and Matricaria recutita essential oil (MREO) extracted from Matricaria recutita possesses excellent antibacterial and anti-inflammatory properties.
Methods: In this study, Matricaria recutita microemulsions were prepared by the trans-phase emulsification method and their stability was determined by evaluating the relevant indexes. Establishment of 2,4-dinitro-chlorobenzene-induced AD model in mice. Detection of serum indexes of IL-6, IL-17, and TNF-α, and on pathological tissue sections, the HE staining, toluidine blue staining, immunohistochemistry, and observation were performed.
Results: The study obtained optimal conditions for the preparation of microemulsion formulations of Matricaria recutita. Through quality evaluation, it was found that the microemulsion increased stability, reduced irritation, and retained anti-inflammatory activity and therapeutic effects on eczema compared to Matricaria recutita essential oil (MREO). Studies have demonstrated that microemulsion formulations of Matricaria recutita and Matricaria recutita significantly down regulate the proinflammatory factors TNF-α, IL-17, and IL-6. It was shown by hematoxylin-eosin (HE) staining that both Matricaria recutita essential oil (MREO) and Matricaria recutita microemulsion (MRME) improved the inflammatory status of eczematous skin tissues in mice. The number of mast cells expressed in the tissues was decreased in the surface-treated group, as shown by toluidine blue staining. Additionally, the number of mast cells expressed in the tissues in the surface-treated group was reduced, as demonstrated by immunohistochemistry. Furthermore, immunohistochemistry revealed that MREO and MRME have immunomodulatory effects on the tissues.
Conclusion: The study showed that microemulsion formulations of Matricaria recutita may serve as a novel remedy for eczema.
{"title":"Studies on the Preparation of a Microemulsion Formulation of Matricaria Recutita Essential Oil and the Treatment of 2,4-Dinitro-Chlorobenzene-Induced Eczema in Mice by Inhibiting Inflammation.","authors":"Dongxu Wang, Wenfei Wang, Qibin Zhang, Chang Liu, Xuefei Li, Kangrui Zuo, Yundong Xie, Xiaofei Zhang","doi":"10.2174/0115672018315617240826133041","DOIUrl":"10.2174/0115672018315617240826133041","url":null,"abstract":"<p><strong>Background: </strong>Eczema, an inflammatory skin disease causing intense itching, is a function of a range of internal and external factors, impacting individuals of all ages and leading to economic loss. Inflammation is the most important manifestation of eczema, and Matricaria recutita essential oil (MREO) extracted from Matricaria recutita possesses excellent antibacterial and anti-inflammatory properties.</p><p><strong>Methods: </strong>In this study, Matricaria recutita microemulsions were prepared by the trans-phase emulsification method and their stability was determined by evaluating the relevant indexes. Establishment of 2,4-dinitro-chlorobenzene-induced AD model in mice. Detection of serum indexes of IL-6, IL-17, and TNF-α, and on pathological tissue sections, the HE staining, toluidine blue staining, immunohistochemistry, and observation were performed.</p><p><strong>Results: </strong>The study obtained optimal conditions for the preparation of microemulsion formulations of Matricaria recutita. Through quality evaluation, it was found that the microemulsion increased stability, reduced irritation, and retained anti-inflammatory activity and therapeutic effects on eczema compared to Matricaria recutita essential oil (MREO). Studies have demonstrated that microemulsion formulations of Matricaria recutita and Matricaria recutita significantly down regulate the proinflammatory factors TNF-α, IL-17, and IL-6. It was shown by hematoxylin-eosin (HE) staining that both Matricaria recutita essential oil (MREO) and Matricaria recutita microemulsion (MRME) improved the inflammatory status of eczematous skin tissues in mice. The number of mast cells expressed in the tissues was decreased in the surface-treated group, as shown by toluidine blue staining. Additionally, the number of mast cells expressed in the tissues in the surface-treated group was reduced, as demonstrated by immunohistochemistry. Furthermore, immunohistochemistry revealed that MREO and MRME have immunomodulatory effects on the tissues.</p><p><strong>Conclusion: </strong>The study showed that microemulsion formulations of Matricaria recutita may serve as a novel remedy for eczema.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1180-1200"},"PeriodicalIF":3.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142127804","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 : 2025-01-01DOI: 10.2174/0115672018340056240924183806
Sedigheh Ehsanimehr, Kimya Badr, Wim Dehaen, Vahid Shafiei Irannejad, Peyman Najafi Moghadam
Introduction: The last strategy in targeted drug delivery systems is to deliver the anticancer drug to the tumor tissue to increase its therapeutic effect and minimize its undesirable side effects. In line with this goal in this research, the redox/pH-responsive disulfide magnetic nanocarriers based on PF127-NH2/L-cysteine-CM-β-CD-FA were synthesized and evaluated in a doxorubicin delivery system.
Methods: We effectively surrounded Fe3O4 nanoparticles with SiO2 using the sol-gel method, and then confidently coated them with oleic acid on Fe3O4@SiO2 nanoparticles.. In another reaction, a PF127-NH2/L-cysteine-CM-β-CD-FA was synthesized. The process involved modifying pluronic F127 (PF 127) with maleic anhydride and aminating it to form PF127-NH2. The obtained PF127-NH2 was attached to L-cysteine, followed by condensing with carboxymethyl-β-cyclodextrin and then functionalized by folic acid. Finally, PF127-NH2/L-cysteine-CM-β-CD-FA was coated on the surface of magnetic nanoparticles, and the resulting PF127-NH2/L-cysteine-CM-β-CD-FA was disulfidated to form the final nanocarrier network, which was abbreviated as LCMNPs-SS. The doxorubicin was used as a model drug and loaded into the LCMNPs-SS nanocarrier.
Results: The LCMNPs-SS nanocarrier exhibited excellent properties for controlled release, with a well-defined release rate, a controllable level by an external magnet, and adjusting by DLdithiothreitol concentration. The LCMNPs-SS nanocarrier could also break apart when exposed to an oxidant or a change in pH. This meant that the drug release could be fine-tuned in response to temperature, pH, or more than one stimulus.
Conclusion: These drug-carrying systems are valuable in reducing the dose of doxorubicin. High internalization of the synthesized LCMNPs-SS caused sped cellular uptake.
{"title":"Multi-Stimuli-Responsive Biocompatible Magnetic Nanocarrier as Drug Delivery System to MCF-7 Breast Cancer Cells.","authors":"Sedigheh Ehsanimehr, Kimya Badr, Wim Dehaen, Vahid Shafiei Irannejad, Peyman Najafi Moghadam","doi":"10.2174/0115672018340056240924183806","DOIUrl":"10.2174/0115672018340056240924183806","url":null,"abstract":"<p><strong>Introduction: </strong>The last strategy in targeted drug delivery systems is to deliver the anticancer drug to the tumor tissue to increase its therapeutic effect and minimize its undesirable side effects. In line with this goal in this research, the redox/pH-responsive disulfide magnetic nanocarriers based on PF127-NH<sub>2</sub>/L-cysteine-CM-β-CD-FA were synthesized and evaluated in a doxorubicin delivery system.</p><p><strong>Methods: </strong>We effectively surrounded Fe<sub>3</sub>O<sub>4</sub> nanoparticles with SiO<sub>2</sub> using the sol-gel method, and then confidently coated them with oleic acid on Fe<sub>3</sub>O<sub>4</sub>@SiO<sub>2</sub> nanoparticles.. In another reaction, a PF127-NH<sub>2</sub>/L-cysteine-CM-β-CD-FA was synthesized. The process involved modifying pluronic F127 (PF 127) with maleic anhydride and aminating it to form PF127-NH<sub>2</sub>. The obtained PF127-NH<sub>2</sub> was attached to L-cysteine, followed by condensing with carboxymethyl-β-cyclodextrin and then functionalized by folic acid. Finally, PF127-NH<sub>2</sub>/L-cysteine-CM-β-CD-FA was coated on the surface of magnetic nanoparticles, and the resulting PF127-NH<sub>2</sub>/L-cysteine-CM-β-CD-FA was disulfidated to form the final nanocarrier network, which was abbreviated as LCMNPs-SS. The doxorubicin was used as a model drug and loaded into the LCMNPs-SS nanocarrier.</p><p><strong>Results: </strong>The LCMNPs-SS nanocarrier exhibited excellent properties for controlled release, with a well-defined release rate, a controllable level by an external magnet, and adjusting by DLdithiothreitol concentration. The LCMNPs-SS nanocarrier could also break apart when exposed to an oxidant or a change in pH. This meant that the drug release could be fine-tuned in response to temperature, pH, or more than one stimulus.</p><p><strong>Conclusion: </strong>These drug-carrying systems are valuable in reducing the dose of doxorubicin. High internalization of the synthesized LCMNPs-SS caused sped cellular uptake.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1201-1216"},"PeriodicalIF":3.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142396542","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 : 2025-01-01DOI: 10.2174/0115672018339596241120191113
Jiayi Yang, Shuo Yin, Tan Wu, Yangyang Zhang, Chunyun Zhu, Nianping Feng, Teng Guo
Background: Hot-melt Pressure-sensitive Adhesives (HMPSA) are eco-friendly pressuresensitive adhesives, with the potential of being used as substrates for transdermal patches. However, due to the low hydrophilicity of HMPSA, the application is limited in the field of Traditional Chinese Medicine (TCM) plasters.
Methods: Three modified HMPSA were prepared with acrylic resin EPO, acrylic resin RL100, and Polyvinylpyrrolidone (PVP) as the modifying materials. The physical compatibility between HMPSA and the modifying materials was investigated through in vitro release performance, viscosity, softening point, cohesion, and fluidity, so as to determine the most effective modifying material. The impact of the modified HMPSA on the release properties of different TCM ingredients was elucidated by the performance of water absorption and contact angle behavior.
Results: With the addition of the modifying materials, both the viscosity and the softening point of HMPSA were improved, with the flowability reduced and the cohesion maintained. The morphological and structural changes reflected the physical compatibility between HMPSA and the three modifying materials. According to the results of in vitro release experiments, PVP effectively improved the release performance of paeoniflorin, ephedrine hydrochloride, and cinnamaldehyde in HMPSA, with no significant impact on the release performance of eugenol. The changes in the drug release performance of HMPSA may be attributed to the improved hydrophilicity of HMPSA after physical modification.
Conclusion: The compatibility and the drug release performance of HMPSA were effectively enhanced after the addition of the modifying materials by the physical blending technique. Among the three modifying materials, PVP has been found to be an ideal modifying material for HMPSA in the field of TCM plasters due to its effects on drug release performance.
{"title":"Improvement in Compatibility and Drug Release Performance of Hot-Melt Pressure-Sensitive Adhesives by Physical Blending Technique.","authors":"Jiayi Yang, Shuo Yin, Tan Wu, Yangyang Zhang, Chunyun Zhu, Nianping Feng, Teng Guo","doi":"10.2174/0115672018339596241120191113","DOIUrl":"10.2174/0115672018339596241120191113","url":null,"abstract":"<p><strong>Background: </strong>Hot-melt Pressure-sensitive Adhesives (HMPSA) are eco-friendly pressuresensitive adhesives, with the potential of being used as substrates for transdermal patches. However, due to the low hydrophilicity of HMPSA, the application is limited in the field of Traditional Chinese Medicine (TCM) plasters.</p><p><strong>Methods: </strong>Three modified HMPSA were prepared with acrylic resin EPO, acrylic resin RL100, and Polyvinylpyrrolidone (PVP) as the modifying materials. The physical compatibility between HMPSA and the modifying materials was investigated through in vitro release performance, viscosity, softening point, cohesion, and fluidity, so as to determine the most effective modifying material. The impact of the modified HMPSA on the release properties of different TCM ingredients was elucidated by the performance of water absorption and contact angle behavior.</p><p><strong>Results: </strong>With the addition of the modifying materials, both the viscosity and the softening point of HMPSA were improved, with the flowability reduced and the cohesion maintained. The morphological and structural changes reflected the physical compatibility between HMPSA and the three modifying materials. According to the results of in vitro release experiments, PVP effectively improved the release performance of paeoniflorin, ephedrine hydrochloride, and cinnamaldehyde in HMPSA, with no significant impact on the release performance of eugenol. The changes in the drug release performance of HMPSA may be attributed to the improved hydrophilicity of HMPSA after physical modification.</p><p><strong>Conclusion: </strong>The compatibility and the drug release performance of HMPSA were effectively enhanced after the addition of the modifying materials by the physical blending technique. Among the three modifying materials, PVP has been found to be an ideal modifying material for HMPSA in the field of TCM plasters due to its effects on drug release performance.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1459-1468"},"PeriodicalIF":3.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143018620","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 : 2025-01-01DOI: 10.2174/0115672018349688241008220007
Vignesh Natarajan
Introduction/objective: The spread of tumors (48% in men and 51% in women), as well as the protection of malignant tumors by stromal cells and complex blood vessels, pose significant challenges to drug delivery to tumors. Modern chemotherapy, on the other hand, addresses tumor growth suppression by at least 60% through versatile formulation systems and numerous modifications to drug delivery systems. The renewable and naturally occurring polymers present invariably in all living cells form the fundamental foundation for most anticancer drug development. The review aims to discuss in detail the preparations of polysaccharide, lipid, and protein-based drug-loading vehicles for the targeted delivery of prominent anticancer drugs. It also provides an explanation of drug distribution in blood (cumulative releases of nearly 80% drug) and drug accumulation at tumor sites (1-5 mg/kg) due to enhanced permeability and retention (EPR).
Methods: Specific delivery examples for treating colorectal and breast carcinomas have been presented to distinguish the varied drug administration, bioavailability, and tumor internalization mechanisms between sugar, fatty acid, and amino acid polymers. Current therapy possibilities based on cutting-edge literature are provided, along with drug delivery systems tailored to tumor location and invasive properties.
Results: The unique combinations of the three natural polymers provide unparalleled solutions to minimize the toxicity (<20% drug release) of the chemotherapeutic drugs on normal tissues. Moreover, the development of a consolidated drug delivery system has contributed to a substantial reduction (dose reduction from 10.43 μM to 1.9 μM) in the undesirable consequences of higher dosages of chemotherapeutic drugs.
Conclusion: The review extensively covers safe chemotherapeutic systems with significant advantages (tumor volume shrinkage of 4T1 cells from 1000 mm3 to 200 mm3) in clinical applications of carcinoma treatments using natural polymers.
{"title":"Alleviation of Tumor Invasion by the Development of Natural Polymer-based Low-risk Chemotherapeutic Systems - review on the Malignant Carcinoma Treatments.","authors":"Vignesh Natarajan","doi":"10.2174/0115672018349688241008220007","DOIUrl":"10.2174/0115672018349688241008220007","url":null,"abstract":"<p><strong>Introduction/objective: </strong>The spread of tumors (48% in men and 51% in women), as well as the protection of malignant tumors by stromal cells and complex blood vessels, pose significant challenges to drug delivery to tumors. Modern chemotherapy, on the other hand, addresses tumor growth suppression by at least 60% through versatile formulation systems and numerous modifications to drug delivery systems. The renewable and naturally occurring polymers present invariably in all living cells form the fundamental foundation for most anticancer drug development. The review aims to discuss in detail the preparations of polysaccharide, lipid, and protein-based drug-loading vehicles for the targeted delivery of prominent anticancer drugs. It also provides an explanation of drug distribution in blood (cumulative releases of nearly 80% drug) and drug accumulation at tumor sites (1-5 mg/kg) due to enhanced permeability and retention (EPR).</p><p><strong>Methods: </strong>Specific delivery examples for treating colorectal and breast carcinomas have been presented to distinguish the varied drug administration, bioavailability, and tumor internalization mechanisms between sugar, fatty acid, and amino acid polymers. Current therapy possibilities based on cutting-edge literature are provided, along with drug delivery systems tailored to tumor location and invasive properties.</p><p><strong>Results: </strong>The unique combinations of the three natural polymers provide unparalleled solutions to minimize the toxicity (<20% drug release) of the chemotherapeutic drugs on normal tissues. Moreover, the development of a consolidated drug delivery system has contributed to a substantial reduction (dose reduction from 10.43 μM to 1.9 μM) in the undesirable consequences of higher dosages of chemotherapeutic drugs.</p><p><strong>Conclusion: </strong>The review extensively covers safe chemotherapeutic systems with significant advantages (tumor volume shrinkage of 4T1 cells from 1000 mm3 to 200 mm<sup>3</sup>) in clinical applications of carcinoma treatments using natural polymers.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1240-1264"},"PeriodicalIF":3.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12715397/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142484985","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 : 2025-01-01DOI: 10.2174/0115672018325362240811164655
Jeneesha George, Asit Ranjan Ghosh
Conjugated Linoleic Acid (CLA) is a polyunsaturated dietary fatty acid. Probiotics can biohydrogenate CLA with multiple health benefits, especially in cancer treatment. In vitro, in vivo, and clinical studies have confirmed CLA isomers to possess anti-cancer activity. CLA has demonstrated its potential as an alternative treatment for cancer and also used as an adjuvant to reduce the side effects of existing treatment methods. The mechanism of the anticancer activity of CLA is still not clear; however, it may involve intervention with the cell cycle and modulation of gene expression. A greater potential of CLA for cancer treatment has been supported by more and more clinical trials to evaluate its potential. Some advanced technologies are in progress to overcome the flaws of current methods and enhance the microbial production of CLA. In conclusion, nutritional enrichment as a functional food and direct consumption of CLA may contribute to cancer management.
{"title":"Conjugated Linoleic Acid in Cancer Therapy.","authors":"Jeneesha George, Asit Ranjan Ghosh","doi":"10.2174/0115672018325362240811164655","DOIUrl":"10.2174/0115672018325362240811164655","url":null,"abstract":"<p><p>Conjugated Linoleic Acid (CLA) is a polyunsaturated dietary fatty acid. Probiotics can biohydrogenate CLA with multiple health benefits, especially in cancer treatment. <i>In vitro, in vivo</i>, and clinical studies have confirmed CLA isomers to possess anti-cancer activity. CLA has demonstrated its potential as an alternative treatment for cancer and also used as an adjuvant to reduce the side effects of existing treatment methods. The mechanism of the anticancer activity of CLA is still not clear; however, it may involve intervention with the cell cycle and modulation of gene expression. A greater potential of CLA for cancer treatment has been supported by more and more clinical trials to evaluate its potential. Some advanced technologies are in progress to overcome the flaws of current methods and enhance the microbial production of CLA. In conclusion, nutritional enrichment as a functional food and direct consumption of CLA may contribute to cancer management.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"450-464"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141989875","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":"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":" ","pages":"181-194"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","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}