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Drug-Loaded Hydrogel Microneedles for Sustainable Transdermal Delivery of Macromolecular Proteins. 可持续经皮递送大分子蛋白的载药水凝胶微针。
Pub Date : 2025-01-15 DOI: 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.

简介:聚甲基乙烯醚共马来酸(PMVE/MA)水凝胶微针(HMN)由于其生物相容性和超溶胀特性,被研究用于大分子药物的透皮给药。然而,药物递送效率随着分子量的增加而降低,这是由于在HMN基质内的包裹。此外,整合外部药物储存库扩展了药物扩散路径,降低了药物渗透效率。方法:采用pH修饰后的HMN基质直接载药方法。研究了pH改性对HMN理化性能的影响。然后,将模型蛋白牛血清白蛋白(BSA)加载到ph修饰的HMN中,并评估HMN的形态变化和蛋白稳定性。最后,体外评估bsa负载HMN的透皮给药效果。结果:HMN pH改变后肿胀明显增加(p < 0.001)。ph修饰后的水凝胶结构多孔,ATR-FTIR光谱显示羧基峰移位。负载在ph修饰的HMN中的BSA的二级结构也被保留。bsa负载的HMN介导了持续的体外药物释放,24 h内累积释放量为64.70% (3.88 mg)。结论:因此,模型药物掺入PMVE/MA HMN系统具有持续透皮递送蛋白质的潜力。
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引用次数: 0
Recent Developments in Oral Drug Delivery of Prokinetic Agents: Nanoparticles and Beyond. 促动力学药物口服给药的最新进展:纳米颗粒及其他。
Pub Date : 2025-01-13 DOI: 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.

促动力剂是用于增强胃肠运动和治疗胃食管反流病(GERD)和胃轻瘫等疾病的药物。ph依赖性释放系统提供靶向药物递送,允许促动力学药物在胃肠道所需区域特异性释放。这可以优化药物疗效,并最大限度地减少全身副作用。胃保留制剂能够持续释放药物,这在需要延长胃停留时间的条件下特别有益,例如胃轻瘫。纳米颗粒已成为改善促动力学药物递送和增强药物稳定性、溶解度和吸收的有前途的载体。这些纳米系统保护药物免受降解,从而提高生物利用度和控制药物释放。此外,结合粘膜粘附技术可延长药物-粘膜相互作用,促进药物吸收并减少给药频率。这些最近的进展有可能彻底改变促动力学药物的口服给药方式,提供更好的治疗结果,增强患者的依从性,减少副作用。然而,可扩展性、生物相容性和安全性挑战需要通过临床前和临床研究进一步调查和验证。本文综述了促动力学药物口服给药系统的最新进展,重点介绍了ph依赖性释放、胃保留制剂、纳米颗粒和黏附技术等创新方法。综上所述,整合先进的口服药物给药系统为胃肠疾病的治疗提供了一条有希望的途径。学术界、工业界和医疗保健专业人员之间的持续研究和合作对于释放这些创新的全部潜力并最终将其转化为对患者有效的临床治疗至关重要。
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引用次数: 0
Nanosystems for Intranasal Delivery of Therapeutics in Psychiatric Disorders. 鼻内递送治疗精神疾病的纳米系统。
Pub Date : 2025-01-10 DOI: 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。
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引用次数: 0
Facile Synthesis of Monodisperse Gold Nanorods, Gold Nanobipyramids and Gold Nanocups with Different Coatings and Evaluation of Their Cellular Cytotoxicity. 不同涂层单分散金纳米棒、金纳米金字塔和金纳米杯的简易合成及其细胞毒性评价。
Pub Date : 2025-01-09 DOI: 10.2174/0115672018337291241118045126
Fanjiao Zuo, Shuting Zhou, Xiwei Wu, Boyao Wang, Jun He, Xilong Qiu

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.

导言:评估金纳米颗粒(GNPs)的细胞毒性由于其在生物医学领域的发展而变得重要。方法:采用种子介导法系统合成了金纳米棒(GNRs)、金纳米金字塔(gnbp)和金纳米棒(GNCs),其平均长度分别为32.53±4.67 nm、72.90±7.54 nm和118.01±11.02 nm。结果:此外,使用细胞计数试剂盒-8 (CCK-8)检测,我们评估了三种不同类型的GNPs的细胞毒性,这些GNPs具有不同的表面涂层,如有机十六烷基三甲基溴化铵(CTAB)和聚乙二醇(PEG)。结果表明,GNPs在3.125 ~ 100 μg/mL浓度范围内呈形状依赖性;GNPs的类型及其表面涂层对GNPs在细胞中的表现有显著影响。与不诱导细胞损伤的peg包被GNPs相比,ctab包被GNPs表现出更明显的细胞毒性。结论:与GNCs相比,GNRs和gnbp对GES-1细胞、RAW 264.7细胞和LX-2细胞的毒性更大。我们的研究为生物医学领域表面修饰对GNPs生物相容性和形状的影响提供了重要的新认识。
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引用次数: 0
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. 母菊精油微乳液制剂的制备及通过抑制炎症治疗 2,4-二硝基氯苯诱发的小鼠湿疹的研究。
IF 3 Pub Date : 2025-01-01 DOI: 10.2174/0115672018315617240826133041
Dongxu Wang, Wenfei Wang, Qibin Zhang, Chang Liu, Xuefei Li, Kangrui Zuo, Yundong Xie, Xiaofei Zhang

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.

背景:湿疹是一种引起剧烈瘙痒的炎症性皮肤病,由一系列内部和外部因素引起,影响着各个年龄段的人,并导致经济损失。炎症是湿疹最重要的表现,而从母菊中提取的母菊精油(MREO)具有很好的抗菌和消炎作用:本研究采用反相乳化法制备了洋甘菊微乳液,并通过评估相关指标确定了其稳定性。建立2,4-二硝基氯苯诱导的小鼠AD模型。检测血清中IL-6、IL-17和TNF-α的指标,并对病理组织切片进行HE染色、甲苯胺蓝染色、免疫组化和观察:研究获得了制备洋甘菊微乳剂的最佳条件。通过质量评估发现,与洋甘菊精油(MREO)相比,微乳剂提高了稳定性,减少了刺激性,并保留了抗炎活性和对湿疹的治疗效果。研究表明,洋甘菊和母菊花的微乳液配方能显著降低促炎因子 TNF-α、IL-17 和 IL-6。苏木精-伊红(HE)染色表明,洋甘菊精油(MREO)和洋甘菊微乳液(MRME)都能改善小鼠湿疹皮肤组织的炎症状况。甲苯胺蓝染色显示,表面处理组组织中表达的肥大细胞数量减少。此外,免疫组化显示,表面处理组组织中表达的肥大细胞数量减少。此外,免疫组化显示,MREO 和 MRME 对组织有免疫调节作用:研究表明,洋甘菊微乳液制剂可作为治疗湿疹的一种新型疗法。
{"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}
引用次数: 0
Multi-Stimuli-Responsive Biocompatible Magnetic Nanocarrier as Drug Delivery System to MCF-7 Breast Cancer Cells. 多刺激响应性生物相容性磁性纳米载体作为 MCF-7 乳腺癌细胞的药物输送系统
IF 3 Pub Date : 2025-01-01 DOI: 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.

导言:靶向给药系统的最后一个策略是将抗癌药物输送到肿瘤组织,以提高其治疗效果并减少其不良副作用。根据这一目标,本研究合成了基于 PF127-NH2/L-cysteine-CM-β-CD-FA 的氧化还原/pH 响应二硫化物磁性纳米载体,并在多柔比星给药系统中进行了评估:方法:采用溶胶-凝胶法将Fe3O4纳米粒子与SiO2有效包覆在一起,然后用油酸将其包覆在Fe3O4@SiO2纳米粒子上。在另一个反应中,合成了 PF127-NH2/L-半胱氨酸-CM-β-CD-FA。该过程包括用马来酸酐对 Pluronic F127(PF 127)进行改性,然后将其胺化,形成 PF127-NH2。得到的 PF127-NH2 与 L-半胱氨酸连接,然后与羧甲基-β-环糊精缩合,再与叶酸官能化。最后,PF127-NH2/L-半胱氨酸-CM-β-CD-FA 被包覆在磁性纳米粒子的表面,所得的 PF127-NH2/L- 半胱氨酸-CM-β-CD-FA 被二硫化,形成最终的纳米载体网络,简称为 LCMNPs-SS。以多柔比星为模型药物,将其装载到 LCMNPs-SS 纳米载体中:结果:LCMNPs-SS 纳米载体具有良好的控释性能,释放速率明确,可通过外部磁铁控制释放水平,并可通过 DLdithiothreitol 浓度进行调节。LCMNPs-SS 纳米载体在遇到氧化剂或 pH 值变化时也会破裂。这意味着可以根据温度、pH 值或多种刺激因素对药物释放进行微调:结论:这些载药系统对减少多柔比星的剂量很有价值。合成的 LCMNPs-SS 的高内化率加快了细胞吸收。
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引用次数: 0
Improvement in Compatibility and Drug Release Performance of Hot-Melt Pressure-Sensitive Adhesives by Physical Blending Technique. 物理共混技术改善热熔压敏胶的相容性和释药性能。
IF 3 Pub Date : 2025-01-01 DOI: 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.

背景:热熔压敏胶粘剂(HMPSA)是一种环保的压敏胶粘剂,具有作为透皮贴剂底物的潜力。然而,由于HMPSA的亲水性较低,在中药膏药领域的应用受到限制。方法:以丙烯酸树脂EPO、丙烯酸树脂RL100和聚乙烯吡咯烷酮(PVP)为改性材料制备3种改性HMPSA。通过体外释放性能、粘度、软化点、黏聚力、流动性等指标考察HMPSA与改性材料的物理相容性,确定最有效的改性材料。通过吸附性能和接触角行为研究改性后的HMPSA对不同中药成分释放性能的影响。结果:改性材料的加入提高了HMPSA的粘度和软化点,降低了其流动性,保持了其粘聚性。形态和结构的变化反映了HMPSA与三种改性材料之间的物理相容性。体外释放实验结果显示,PVP有效提高了HMPSA中芍药苷、盐酸麻黄碱、肉桂醛的释放性能,对丁香酚的释放性能无显著影响。HMPSA释药性能的变化可能与物理修饰后HMPSA的亲水性得到改善有关。结论:采用物理共混技术添加改性材料后,HMPSA的相容性和释药性能得到了有效提高。在这三种改性材料中,PVP因其对药物释放性能的影响而被认为是中药膏药领域中较为理想的HMPSA改性材料。
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引用次数: 0
Alleviation of Tumor Invasion by the Development of Natural Polymer-based Low-risk Chemotherapeutic Systems - review on the Malignant Carcinoma Treatments. 通过开发基于天然聚合物的低风险化疗系统减轻肿瘤侵袭--恶性肿瘤治疗综述。
IF 3 Pub Date : 2025-01-01 DOI: 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.

导言/目的:肿瘤的扩散(男性为 48%,女性为 51%)以及基质细胞和复杂血管对恶性肿瘤的保护,给肿瘤给药带来了巨大挑战。另一方面,现代化疗通过多功能制剂系统和对给药系统的大量改良,可将肿瘤生长抑制至少 60%。存在于所有活细胞中的可再生天然聚合物是大多数抗癌药物开发的基础。本综述旨在详细讨论基于多糖、脂质和蛋白质的载药载体的制备方法,以实现主要抗癌药物的靶向给药。它还解释了药物在血液中的分布(累积释放近 80% 的药物)以及由于渗透性和滞留性(EPR)增强而导致的药物在肿瘤部位的蓄积(1-5 mg/kg):方法:介绍治疗结直肠癌和乳腺癌的具体给药实例,以区分糖、脂肪酸和氨基酸聚合物的不同给药、生物利用度和肿瘤内化机制。根据前沿文献提供了当前治疗的可能性,以及根据肿瘤位置和侵袭特性定制的给药系统:结果:三种天然聚合物的独特组合提供了无与伦比的解决方案,将毒性降至最低:该综述广泛涵盖了使用天然聚合物治疗癌症的临床应用中具有显著优势(4T1 细胞的肿瘤体积从 1000 立方毫米缩小到 200 立方毫米)的安全化疗系统。
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引用次数: 0
Conjugated Linoleic Acid in Cancer Therapy. 癌症治疗中的共轭亚油酸
Pub Date : 2025-01-01 DOI: 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.

共轭亚油酸(CLA)是一种多不饱和膳食脂肪酸。益生菌可以生物氢化 CLA,对健康有多种益处,尤其是在癌症治疗方面。体外、体内和临床研究证实,CLA 异构体具有抗癌活性。CLA 已被证明具有作为癌症替代疗法的潜力,还可用作辅助剂,减少现有治疗方法的副作用。CLA 的抗癌机制尚不清楚,但可能涉及干预细胞周期和调节基因表达。越来越多的临床试验对 CLA 治疗癌症的潜力进行了评估。目前正在开发一些先进技术,以克服现有方法的缺陷,提高微生物生产 CLA 的能力。总之,作为一种功能性食品,CLA 的营养强化和直接食用可能有助于癌症的治疗。
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引用次数: 0
Novel Products as Promising Therapeutic Agents for Angiogenesis Inhibition. 抑制血管生成的新型治疗药物。
Pub Date : 2025-01-01 DOI: 10.2174/0115672018277869231217165048
Shaheen Sultana, Shahnaz Sultana, Shehla Nasar Mir Najib Ullah, Ameeduzzafar Zafar

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.

目的:血管生成是由原有血管形成新血管的过程,发生在发育、伤口愈合和肿瘤生长过程中。在这篇综述中,我们旨在全面介绍癌变过程中导致血管生成的各种因素。抗血管生成药物通过阻断肿瘤细胞的营养和血液供应,防止或减缓癌症的生长,从而有利于治疗:方法:几种新型血管生成抑制剂的发现有助于降低几种危及生命的疾病(如癌症)的发病率和死亡率。目前迫切需要一种新的综合治疗策略,将新型抗血管生成药物结合起来,以控制癌症。本文详细介绍了科学家们采用的各种血管生成抑制剂,以配制和优化此类系统,使其适用于癌症:结果:文章总结了多项研究成果,所有数据都支持抗血管生成剂有利于癌症治疗的说法:本综述重点介绍了在控制癌变方面发挥关键作用的新型抗血管生成剂。
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引用次数: 0
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Current drug delivery
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