{"title":"Triptolide Nanoemulsion Gel as a Transdermal Drug Delivery System: Preparation, Pharmacokinetics, and Rheumatoid Arthritis Evaluation.","authors":"Meng Yang, Dishun Yang, Lu Han, Zhimin Fan, Jiyong Liu, Yongfang Yuan","doi":"10.2174/1567201821666230808114519","DOIUrl":"10.2174/1567201821666230808114519","url":null,"abstract":"<p><strong>Introduction: </strong>This study aimed to develop and evaluate triptolide nanoemulsion gels (TP-NE gels) as a transdermal drug delivery system.</p><p><strong>Methods: </strong>TP-NE was prepared and optimized via emulsification and the central composite design response surface method. The optimized TP-NE gel was evaluated in vitro and in vivo. TP-NE gel microstructure, in vitro and in vivo pharmacokinetics, and anti-rheumatoid arthritis effects were studied to evaluate the feasibility of its percutaneous administration.</p><p><strong>Results: </strong>The Optimized TP-NE was observed using a Malvern Autosizer Nano ZS 90 inspection system and a transmission electron microscope (TEM). The nanoemulsion had an average size of 162.9 ± 0.281 nm, a polydispersity index of 0.272 ± 0.024, a zeta potential of -30.03 ± 2.01 mV, and mostly spherical and uniform morphology. In addition, the TP-NE gel pharmacokinetics, assessed via a skin-blood twosite synchronous microdialysis, revealed that TP was higher in the skin than in the blood. TP-NE gel is crucial in reducing knee edema, inhibiting inflammation, and treating rheumatoid arthritis by regulating tumor necrosis factor-alpha, interleukin-1β, and -6 levels.</p><p><strong>Conclusion: </strong>The TP-NE gel is a promising local delivery method for rheumatoid arthritis (RA)- associated edema and inflammation and can serve as a prospective platform for percutaneous TP administration.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"765-778"},"PeriodicalIF":3.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9964291","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mujie Ju, Jinhuan Liu, Ding Guan, Nannan Leng, Samah Attia Algharib, Ali Sobhy Dawood, Wanhe Luo
{"title":"Antibacterial Activity of a Novel Glycyrrhizic Acid-loaded Chitosan Composite Nanogel <i>In vitro</i> Against <i>Staphylococcus Aureus</i> Small Colony Variants.","authors":"Mujie Ju, Jinhuan Liu, Ding Guan, Nannan Leng, Samah Attia Algharib, Ali Sobhy Dawood, Wanhe Luo","doi":"10.2174/1567201820666230117150253","DOIUrl":"10.2174/1567201820666230117150253","url":null,"abstract":"<p><strong>Introduction: </strong>This study aimed to improve the sustained and controlled release of glycyrrhizic acid to the infected site of Staphylococcus aureus small colony variants (SCVs).</p><p><strong>Methods: </strong>The glycyrrhizic acid-loaded chitosan composite nanogel was prepared by inclusion action, Schiff's base formation, and electrostatic action. Furthermore, the formulation screening, characteristics, in vitro release, and antibacterial activity of the glycyrrhizic acid composite nanogel were explored.</p><p><strong>Results: </strong>The final optimal formula comprised 10 mg/mL (chitosan) and 50 μL (glutaraldehyde). The loading capacity, encapsulation efficiency, mean size, polydispersity index, and zeta potential were 8.8%±1.6%, 92.1%±2.8%, 478.3±2.8 nm, 0.37±0.10, and 25.3±3.6 mv, respectively. Scanning electron microscope images showed a spherical shape with a relatively uniform distribution. The in vitro release study showed that glycyrrhizic acid composite nanogel exhibited a biphasic pattern with a sustained release of 52.1%±2.0% at 48 h in the pH 5.5 PBS. The minimum inhibitory and minimum biofilm inhibitory concentrations of glycyrrhizic acid composite nanogel against SCVs were 0.625 μg/mL. The time-killing curves and live/dead bacterial staining showed that glycyrrhizic acid composite nanogel had a stronger curative effect against SCVs strain with concentration-dependent.</p><p><strong>Conclusion: </strong>This study provides promising glycyrrhizic acid composite nanogel to improve the treatment of SCV infection.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"600-609"},"PeriodicalIF":3.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10541090","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Wentao Xu, Xiaowen Qin, Yang Liu, Jun Chen, Yuguang Wang
{"title":"Advances in Enzyme-responsive Supramolecular <i>In situ</i> Self-assembled Peptide for Drug Delivery.","authors":"Wentao Xu, Xiaowen Qin, Yang Liu, Jun Chen, Yuguang Wang","doi":"10.2174/1567201820666230726151607","DOIUrl":"10.2174/1567201820666230726151607","url":null,"abstract":"<p><p>Because of low immunogenicity, ease of modification, and inherent biosafety, peptides have been well recognized as vehicles to deliver therapeutic agents to targeted regions with improved pharmacokinetic characteristics. Enzyme-responsive self-assembled peptides (ERSAPs) show superiority over their naive forms due to their enhanced targeting efficacy and long-retention property. In this review, we have summarized recent advances in the therapeutic application of ERSAPs, mainly focusing on their self-therapeutic properties and potential as vehicles to deliver different drugs.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"374-386"},"PeriodicalIF":2.8,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9876281","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Brenda Regina de Araujo, Tatielle do Nascimento, Ana Paula Dos Santos Matos, Vanessa Brandao de Souza Belmiro, Mariana Sato de Souza de Bustamante Monteiro, Ralph Santos-Oliveira, Eduardo Ricci-Junior
{"title":"Nanocarriers for siRNA Delivery Aimed at the Treatment of Melanoma: Systematic Review.","authors":"Brenda Regina de Araujo, Tatielle do Nascimento, Ana Paula Dos Santos Matos, Vanessa Brandao de Souza Belmiro, Mariana Sato de Souza de Bustamante Monteiro, Ralph Santos-Oliveira, Eduardo Ricci-Junior","doi":"10.2174/1567201820666230425234700","DOIUrl":"10.2174/1567201820666230425234700","url":null,"abstract":"<p><p>Melanoma is a malignant skin cancer type with a high lethality rate due to active metastasis. Among the risk factors for its development is exposure to ultraviolet radiation (UV) and phenotypical characteristics such as clear skin and eyes. Given the difficulties of the conventional therapy, the high cost of the treatment and the low bioavailability of drugs, it is important to develop new therapeutic methods to circumvent this situation. Nanosystems such as micelles, liposomes and nanoparticles present advantages when compared to conventional treatments. The objective of this paper is to carry out a literature review based on articles that dealt with the use of siRNA-loaded nanosystems for the treatment of melanoma, with trials carried out <i>in vivo</i> to assess tumor size. The search was conducted in the Web of Science and PubMed databases considering the last 5 years, that is, the period between January 2017 to December 2021. The <i>\"SiRNA and Drug Delivery Systems and Melanoma\"</i> keywords were used in both databases, and the articles were analyzed using the inclusion and exclusion criteria established for this paper. The results obtained indicated that using siRNA transported <i>via</i> nanosystems was capable of silencing the BRAF tumor genes and of reducing tumor size and weight, not presenting <i>in vitro</i> and/or <i>in vivo</i> toxicity. Such being the case, the development of these systems becomes a non-invasive and promising option for the treatment of melanoma.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"431-449"},"PeriodicalIF":2.8,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9447012","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Biological Properties of Arginine-rich Peptides and their Application in Cargo Delivery to Cancer.","authors":"Minghai Ma, Ruizhao Zhao, Xing Li, Minxuan Jing, Rundong Song, Jinhai Fan","doi":"10.2174/1567201820666230417083350","DOIUrl":"10.2174/1567201820666230417083350","url":null,"abstract":"<p><p>Cell-penetrating peptides (CPPs) comprise short peptides of fewer than 30 amino acids, which are rich in arginine (Arg) or lysine (Lys). CPPs have attracted interest in the delivery of various cargos, such as drugs, nucleic acids, and other macromolecules over the last 30 years. Among all types of CPPs, arginine-rich CPPs exhibit higher transmembrane efficiency due to bidentate bonding between their guanidinium groups and negatively charged cellular components. Besides, endosome escape can be induced by arginine-rich CPPs to protect cargo from lysosome-dependent degradation. Here we summarize the function, design principles, and penetrating mechanisms of arginine-rich CPPs, and outline their biomedical applications in drug delivery and biosensing in tumors.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"387-400"},"PeriodicalIF":2.8,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9736850","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The Blood-prostate Barrier: An Obstacle to Drug Delivery into the Prostate.","authors":"Yixuan Mou, Min Cao, Dahong Zhang","doi":"10.2174/1567201821666230807152520","DOIUrl":"10.2174/1567201821666230807152520","url":null,"abstract":"<p><p>The blood-prostate barrier (BPB), a non-static physical barrier, stands as an obstacle between the prostate stroma and the lumen of the prostate gland tube. The barrier has the ability to dynamically regulate and strictly control the mass exchange between the blood and the prostate, thereby limiting drug penetration into the prostate. The basement membrane, fibrous stromal layer, capillary endothelial cell, prostatic ductal epithelial cell, lipid layer, etc., have been confirmed to be involved in the composition of the barrier structure and altered membrane permeability mainly by regulating the size of paracellular ion pores. Various studies have been conducted to improve the efficiency of drug therapy for prostate diseases by changing the administration approaches, improving barrier permeability and increasing drug penetration. To gain a full understanding of BPB, the composition of BPB, the methodology for evaluating the permeability of BPB and alterations in barrier function under pathological conditions are summarized in this review. To find a shortcut for drug delivery across BPB, the biodistribution of drugs in the prostate and different methods of improving drug penetration across BPB are outlined. This review offers an applied perspective on recent advances in drug delivery across BPB.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"401-412"},"PeriodicalIF":2.8,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10008296","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Enhanced Therapeutic Potential of Liposome-Coated Bushen Jianpi Recipe for Hepatocellular Carcinoma","authors":"Siqi Feng, Yi Zhong, Yabin Li, Shiying Li, Yun Li, Zhangjie Zhou, Zhonghua Wu, Tingting Wu","doi":"10.2174/0115672018318595240902095514","DOIUrl":"https://doi.org/10.2174/0115672018318595240902095514","url":null,"abstract":"Objective: Hepatocellular carcinoma (HCC) poses a major healthcare burden globally. Traditional Chinese medicine formula Bushen Jianpi (BSJP) recipe shows inhibitory effects on HCC but suffers from low bioavailability. This study aims to develop a BSJP-loaded liposome (BSJP@Lip) for targeted HCC treatment. Methods: BSJP@Lip was prepared using a microfluidic device. Particle characterization included size, morphology, drug loading, encapsulation efficiency, and release kinetics analysis. In vitro cytotoxicity, cellular uptake, apoptosis, and protein expression were evaluated in hepG2, Smmc-7721, and hepa 1-6 hepatic cancer cell lines treated with BSJP@Lip. Results: BSJP@Lip nanoparticles showed a uniform spherical shape with an average size of 50 nm and zeta potential at around -2.24 mV. They significantly inhibited cell viability and induced apoptosis in a dose-dependent manner compared with traditional decoction formulations. Enhanced cellular uptake of BSJP@Lip increased the expression of proinflammatory factors IL-18 and NLRP3. Conclusion: BSJP@Lip nanoparticles were found to be efficiently internalized by hepatic cancer cell lines, resulting in a dose-dependent inhibition of cell viability and induction of apoptosis. This effect was accompanied by the upregulation of IL-18 and NLRP3.","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":"3 1","pages":""},"PeriodicalIF":2.4,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142255722","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tahmidul Islam Aquib, Sheikh Manjura Hoque, Mohammad Helal Uddin
{"title":"Lignin Nanoparticles as pH-responsive Nanocarriers for Gastric-Irritant Oral Drug Aspirin","authors":"Tahmidul Islam Aquib, Sheikh Manjura Hoque, Mohammad Helal Uddin","doi":"10.2174/0115672018318035240910050003","DOIUrl":"https://doi.org/10.2174/0115672018318035240910050003","url":null,"abstract":"Introduction: Although lignin is one of the most naturally abundant biopolymers, the overall status of its utilization has long been subpar. The ability of Lignin to readily self-assemble into nanoparticles, along with its good biocompatibility and minimal toxicity, makes it a perfect agent for nanocarriers and drug delivery. Method: Hence, in this study, we have attempted to examine lignin nanoparticles (LNPs) as an efficient pH-responsive nanocarrier for gastric-irritant oral NSAID, aspirin. Alkali lignin (AL) was extracted from rice straw via alkaline treatment, and the lignin nanoparticles were synthesized from lignin using the acid precipitation method. The average particle size was 201.37 ± 1.20 nm, and the synthesized LNPs exhibited a spherical shape and smooth outer surface along with high polydispersity (PDI= 0.284 ± 0.012). The LNPs showed moderate hemocompatibility during in vitro hemolysis studies. The nanoparticles presented nearly similar chemical structures to the AL from which they were developed, and the FT-IR absorption spectra confirmed the similarity of this chemical structure to the LNPs and AL. Aspirin was successfully loaded into the LNPs with a satisfactory drug loading value of 39.12 ± 1.50 and an excellent encapsulation efficiency value of 91.44 ± 0.59. Results: Finally, the LNPs were capable of protecting the loaded drug at the acidic pH of the stomach (1.2) with just 29.20% release of the loaded aspirin after 10 h of observation in vitro. Contrarily, the LNPs were capable of rapidly releasing the aspirin at the basic pH of the intestine (7.4) with nearly 90% release of the loaded drug after 10 h observation in vitro. The basic pH of the intestine might lead to gradual dissociation of the LNPs followed by swift release of the loaded cargo. Conclusion: These findings substantiate that the LNPs carry the potential to be an apt and safe nanocarrier for oral drugs like aspirin as well as parenteral drugs, and LNPs can be utilized as an efficient alternative to enteric coating.","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":"12 1","pages":""},"PeriodicalIF":2.4,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142255725","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Exploring the Insights on Exosomes and their Utility in Treating Ophthalmic Disease: Delving into the Clinical Approval and Present Trials","authors":"Ashish Ranjan Dwivedi, Yogesh Murti, Pramod Rawat, Shriya Mahajan, Harsimrat Kandhari, Gaurav Joshi, Bhupinder Kumar","doi":"10.2174/0115672018324046240905134931","DOIUrl":"https://doi.org/10.2174/0115672018324046240905134931","url":null,"abstract":": Ophthalmic diseases include a wide array of conditions, each requiring individualized treatment approaches. In ophthalmic research and as therapeutics against potential pharmacological indications, several subtypes of exosomes (EVs) have been reconnoitered, mainly for their regenerative, neuroprotective, and anti-inflammatory characteristics. EVs are recently gaining wider attention as promising vehicles for therapies because of their natural participation in communication between cells and targeted delivery. These small vesicles, derived from cells, transport numerous molecules between cells, thus contributing advantages like low immunogenicity, stability, and the ability to target cells specifically. These inherent advantages of carrying the therapeutic cargo and enabling intercellular signaling make them a captivating avenue for progressing ophthalmic disease treatment options. While research is ongoing, and clinical applications are still emerging, several EV subtypes have shown promise for possible applications in addressing several ophthalmic diseases, such as glaucoma, age-related macular degenerative disorders, retinal degenerative disorders, and ocular inflammatory conditions.","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":"211 1","pages":""},"PeriodicalIF":2.4,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142255723","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Gaidaa Dogheim, Sampath Chinnam, Mohamed T. Amralla
{"title":"Lipid Nanoparticles as a Platform for miRNA and siRNA Delivery in Hepatocellular Carcinoma","authors":"Gaidaa Dogheim, Sampath Chinnam, Mohamed T. Amralla","doi":"10.2174/0115672018292331240404070236","DOIUrl":"https://doi.org/10.2174/0115672018292331240404070236","url":null,"abstract":": Liver cancer is the sixth most common cancer and the fourth leading cause of death worldwide. Hepatocellular carcinoma (HCC) comprises 75-80% of liver cancer cases. Therapeutic strategies for HCC are available and have been shown to prolong survival but not treat HCC. Gene expression and regulation are responsible for the pathogenesis and progression of HCC. Altering these genetic networks can impact cellular behaviors and in turn cure HCC. Single-stranded and double-stranded non-coding ribonucleic acid known as microRNA and small interfering RNA, respectively have been investigated as possible therapeutic options. Currently, efficient delivery systems that ensure cell-specific targeting and efficient transfection into tumor cells are still under investigation. Viral vectors have been studied extensively, but immunogenicity hinders their use as delivery systems. Non-viral vectors which include inorganic, lipid, or polymeric nanoparticles are promising delivery systems. However, there are a lot of challenges during the formulation of such systems to ensure efficient and specific delivery. In vitro and in vivo studies have investigated different LNPs to deliver miRNA or siRNA. In this review, we highlight the role of LNPs as a delivery system for miRNA and siRNA in HCC in addition to the latest results achieved using this approach.","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":"67 1","pages":""},"PeriodicalIF":2.4,"publicationDate":"2024-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140840465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}