Journal of Drug Delivery Science and Technology最新文献

{"title":"Microneedles-based technology as an innovative strategy for alleviating neurological disorders – Current progress and future perspectives","authors":"Sathyaraj Weslen Vedakumari ,&nbsp;Lokesh Prabakaran ,&nbsp;Yovan Raja Pravin","doi":"10.1016/j.jddst.2025.106890","DOIUrl":"10.1016/j.jddst.2025.106890","url":null,"abstract":"<div><div>Neurological diseases serve as the second major cause of death among the global population. Complicated treatment procedures, specialized care with skilled technician, constant access to physician and numerous diagnostic practices are required to manage neurological diseases. Intradermal, intravenous and intramuscular modes of drug administration are the common routes of drug delivery. Administering drugs to central nervous system (CNS) is highly complicated due to different barriers such as blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB). Discovering innovative treatment strategies for alleviating neurological disorders serves as a major concern for clinical research. Currently, microneedles (MNs) have gained huge attention owing to their biocompatible, non-invasive and painless method of transdermal drug delivery. This review article highlights the potential use and recent progress in MNs-based technology for treating neurological diseases.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106890"},"PeriodicalIF":4.5,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143777300","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of poly (vinyl alcohol)/carboxymethyl chitosan hydrogels loaded with encapsulated tea tree oil for wound care application","authors":"Pairayaphak Ngamplang ,&nbsp;Chasuda Choipang ,&nbsp;Sonthaya Chaiarwut ,&nbsp;Piyachat Chuysinuan ,&nbsp;Pitt Supaphol","doi":"10.1016/j.jddst.2025.106867","DOIUrl":"10.1016/j.jddst.2025.106867","url":null,"abstract":"<div><div>In daily life, accidents and diseases are major causes of wounds. Wound management and wound dressing are significant functions of wound healing. A hydrocolloid film composed of a natural polymer such as carboxymethyl chitosan (CMCS) is a good candidate for use in the treatment of low exudate wounds such as superficial and black/grey necrotic wounds. The hydrocolloid film can be easily removed from a wound and promotes tissue granulation. In recent years, concerns have arisen regarding the existence of harmful chemical substances in products that come into direct contact with human skin. Therefore, natural substances are an exceptional choice. Due to their antibacterial properties, tea tree oil (TTO) and its active components have found uses in various applications, e.g. cosmetics, wound care, and food packaging. However, TTO has major drawbacks due to its high volatility and poor solubility in water as well as other polar solvents. Cyclodextrin is an ideal choice for enhancing its water solubility while preserving its antibacterial characteristics by utilizing the formation of an inclusion complex (IC) with certain TTO components. Various techniques have been utilized to examine the obtained ICs, i.e. GC-MS, UV–vis, 1H NMR, DSC, TG/DTG, FTIR, Zeta-sizer, and SEM. Moreover, molecular docking was employed to examine the preferred orientation of terpinene-4-ol within the cyclodextrin cavity. The hydrocolloid film loaded with a cyclodextrin/TTO IC exhibited enhanced antibacterial activity through observations of their Time-kill assay against model bacteria, e.g., <em>Staphylococcus aureus</em> (<em>S. aureus</em>) and Methicilin-Resistant <em>Staphylococcus aureus</em> (MRSA) (gram-positive bacteria) and <em>Escherichia coli</em> (<em>E. coli</em>) and Acinetobacter baumannii (A. baumannii) (gram-negative bacteria). A hydrocolloid film with a concentration of 3.5 % ICs demonstrated the highest efficacy in inhibiting bacterial activity. Finally, a hydrocolloid film loaded with a cyclodextrin/TTO IC exhibited improved physical properties and antibacterial activity.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"107 ","pages":"Article 106867"},"PeriodicalIF":4.5,"publicationDate":"2025-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143760477","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanoemulsion for enhanced absorption and anti-tumor activity of dasatinib","authors":"Dina A. Eltahan,&nbsp;Rania K. Eid,&nbsp;Shimaa M. Ashmawy,&nbsp;Gamal M. El Maghraby","doi":"10.1016/j.jddst.2025.106870","DOIUrl":"10.1016/j.jddst.2025.106870","url":null,"abstract":"<div><div>Dasatinib showed encouraging activity on triple-negative breast cancer. However, its minute oral bioavailability (about 34 %) is problematic. This minimum bioavailability is related to poor dissolution, low intestinal permeation and pre-systemic metabolism. The aim was to develop and evaluate SEDD for dissolution and permeability enhancement. Cinnamon oil with Tween 80 were utilized as principal composition (F1) with ethanol (F2) or PEG 200 (F3). The developed SEDDS was in the nanoscale after reconstitution. SEDDS hastened dasatinib dissolution with superiority of F2. In-situ rabbit intestinal absorption from aqueous solution verified the incomplete absorption with input from P-gp efflux. This was shown from the length needed for 95 % absorption (L95 %) which was 305.76, 388.38 and 224.85 cm for duodenum, jejuno-ileum and colon, respectively. Delivering dasatinib as nanoemulsion resulting from reconstitution of F2, enhanced intestinal absorption to reduce L95 % to 104.54, 155.84 and 58.91 in the same segments, respectively. The <em>in vivo</em> antitumor activity proved the superiority of nanoemulsion resulting from F1 and F2 compared with aqueous dispersion with F2 being more promising. The research introduced cinnamon oil SEDDS for augmented dasatinib dissolution, intestinal permeation and subsequently <em>in vivo</em> efficacy.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"107 ","pages":"Article 106870"},"PeriodicalIF":4.5,"publicationDate":"2025-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143776551","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and evaluation of novel dual-target drugs encapsulated in liposome against visceral leishmaniasis","authors":"Kushal Bora ,&nbsp;Shiv Kumar ,&nbsp;Shankar Prasad Kanaujia ,&nbsp;Vikash Kumar Dubey","doi":"10.1016/j.jddst.2025.106883","DOIUrl":"10.1016/j.jddst.2025.106883","url":null,"abstract":"<div><div>Earlier we have reported two novel dual-target anti-leishmanial drug candidates, ZINC000008876351 and ZINC000253403245. These compounds were designed to target two crucial enzymes in the antioxidant defense system of <em>Leishmania donovani</em>: iron superoxide dismutase (FeSODA) and trypanothione reductase (TryR). The aim was to optimize these dual-target agents within liposomal formulations for the treatment of visceral leishmaniasis. Liposomal formulations were thoroughly characterized to confirm successful drug encapsulation. <em>In vitro</em> assays demonstrated that the liposome-encapsulated drugs, ZINC000253403245-liposome and ZINC000008876351-liposome, exhibited enhanced antiparasitic activity compared to their free drug counterparts. Both formulations showed significantly lower IC50 values, indicating stronger inhibition of <em>L. donovani</em> growth in both promastigote and amastigote stages at low micromolar concentrations. Mechanistic studies revealed that both free and encapsulated forms of the drugs induced apoptosis-like cell death in <em>L. donovani</em> promastigotes, as evidenced by mitochondrial membrane depolarization and phosphatidylserine externalization, assessed via flow cytometry. These results suggest that liposomal encapsulation enhances therapeutic efficacy by inducing mitochondrial dysfunction and promoting parasite death. The promising results of the ZINC000253403245-liposome and ZINC000008876351-liposome formulations highlight their potential as new, effective treatments for visceral leishmaniasis, offering a promising alternative to current therapies and representing a significant advancement in drug development for this neglected tropical disease.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"107 ","pages":"Article 106883"},"PeriodicalIF":4.5,"publicationDate":"2025-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143776552","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A smart therapeutic approach for improving thin endometrium in rodent models – A maiden intra uterine preclinical approach","authors":"Azeena Saleem ,&nbsp;Alan M. Punnoose ,&nbsp;K. Brindha ,&nbsp;Radha Vembu","doi":"10.1016/j.jddst.2025.106874","DOIUrl":"10.1016/j.jddst.2025.106874","url":null,"abstract":"&lt;div&gt;&lt;div&gt;Recurrent endometrial injuries, such as those caused by miscarriages, curettage, or infections, leading to thin endometrium, are one of the main causes of female infertility. The current treatments for endometrial injury offer limited clinical benefits and cannot improve endometrial receptivity and pregnancy outcomes. Stem cell therapies, or regenerative medicine, are considered potential solutions to address this concern and may offer effective treatment methods for the regeneration of thin endometrium. This study spots light on a combined therapeutic approach conjoining vasculogenesis, angiogenesis, proliferation, and remodelling of cells of the uterine endometrium studied in Wistar albino rat models. The ultimate objective of this research was to regenerate the thin endometrium using commercially obtained bone marrow derived rat mesenchymal stem cells with hormone 17-beta estradiol incorporated into a thermosensitive injectable hydrogel PluronicF127 by a novel minimally invasive intrauterine approach, ensuring a controlled release of hormone estradiol from the hydrogel invitro and the delivery of stem cells to regenerate the thin endometrium. Combining the proven ability of the hydrogel PF127, oestradiol, and rat mesenchymal stem cells to regenerate the endometrial basalis layer and Functionalis layers by inducing vascularization &amp; angiogenesis, subsequently triggering the endometrial stem cells residing in the basalis layer. The injectable hydrogel (PluronicF127) showed satisfactory biocompatibility when loaded with oestradiol and rat mesenchymal stem cells. A thin endometrial rat model was established using 1 % Lugol's iodine rather than the traditional ethanol-induced method with the concept to preserve the endometrial basalis layer. The treatment with rat mesenchymal stem cells and oestradiol-loaded injectable hydrogel significantly enhanced the thickness of the endometrium and increased the abundance of blood vessels and glands in the injured endometrium compared to the control group. The rat mesenchymal stem cells and oestradiol-loaded injectable hydrogel treatment significantly reduced endometrial fibrosis; collagen deposits and increased the presence of endometrial glands. Endometrial thickness, angiogenesis, and molecular markers were assessed at 14- and 21-days post-treatment. Histological analysis revealed that PF127/E2/rMSCs significantly improved endometrial thickness, gland density, and vascularization compared to other groups. The PF127/E2/rMSCs group showed a significant decrease in collagen deposits, which Masson's trichrome staining confirmed. Angiogenesis markers (VEGFA, EGF) and genes linked to stem cells (SOX9, AXIN1, SSEA1) were found to be upregulated in molecular analysis, indicating increased vascularization and stem cell activation in the endometrial basalis layers. Oestradiol was released continuously by the encapsulated delivery system, which also promoted cellular integration and decreased inflammator","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"107 ","pages":"Article 106874"},"PeriodicalIF":4.5,"publicationDate":"2025-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143747298","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Curcumin delivered by ROS-responsive ibuprofen prodrug based on hyaluronic acid effectively suppressed the rheumatoid arthritis","authors":"Ping-fu Huang ,&nbsp;Miaomiao Ma ,&nbsp;Hao Wu ,&nbsp;Wen-min Niu ,&nbsp;Lu-lu Liu ,&nbsp;Jia-bing Tong","doi":"10.1016/j.jddst.2025.106868","DOIUrl":"10.1016/j.jddst.2025.106868","url":null,"abstract":"<div><h3>Purpose</h3><div>Rheumatoid arthritis (RA) is an autoimmune disease with systemic inflammatory. Ibuprofen (IBF) and curcumin (CUR) were the commonly therapeutic ingredients for RA treatment and the combination administration possessed the ideal efficacy, however, the low solubility and lack of targeting produced the significant obstacles for the treatment.</div></div><div><h3>Methods</h3><div>In this study, the IBF prodrug decorated with the CD44 receptors and ROS-sensitive was prepared and encapsulated with the CUR named CUR@HA-TK-IBF were designed, the characterization of CUR@HA-TK-IBF were performed <em>in vitro</em> and the efficacity effect were evaluated using collagen induced arthritis (CIA) model.</div></div><div><h3>Results</h3><div>The obtained product CUR@HA-TK-IBF exhibited the diameter of 137.3 ± 4.5 nm, and the morphology of the nanoparticles showed the sphericity via the TEM. In vitro release results indicated that the IBF and CUR could slowly release in the normal environment and quickly release at the H₂O₂ environment. Furthermore, the combination of CUR and IBF could significantly decrease the expression of the proinflammatory factors and the concentration of ROS and COX-2 <em>in vitro</em>. The animal experiment indicated that the CUR@HA-TK-IBF could alleviate the foot tumefaction and decrease the expression of proinflammatory factors in the RA model mice.</div></div><div><h3>Conclusion</h3><div>The CUR@HA-TK-IBF developed the new approach for co-deliver the IBF and CUR, which provided a new therapeutic strategy for the treatment of RA.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106868"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143746824","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An arginine-rich motif of the HIV-1 TAT protein promotes E. coli cellular entry and DNA delivery","authors":"Rasaq Olajide Akinsola ,&nbsp;Andrew Osahor ,&nbsp;Lena Vollmer ,&nbsp;Oluwafemi Adebayo Oyewole ,&nbsp;Choon Weng Lee ,&nbsp;Edmund Ui Hang Sim ,&nbsp;Kumaran Narayanan","doi":"10.1016/j.jddst.2025.106864","DOIUrl":"10.1016/j.jddst.2025.106864","url":null,"abstract":"<div><div><em>E. coli</em> is an attractive non-viral gene delivery vector due to its low immunogenicity and large gene-carrying capacity. However, its inherently low efficiency has been a significant obstacle that has limited its adoption for gene delivery. We tested a trimer of (HIV-1) Transactivator Transcription protein (TAT) 47–57 with cell-penetrating ability and nuclear localization sequences to enhance the efficiency of the <em>E. coli</em> vectors gene delivery into cancer cells, a strategy not explored before. Fourier-transformed Infrared (FTIR) and Raman spectroscopy (RAMAN) were used to study the interaction between the <em>E. coli</em> vector and TAT3 peptide, and this result was validated with atomic force microscopy (AFM) and Scanning electron microscopy (SEM). We demonstrate for the first time that a hybrid vector can be formed between the <em>E. coli</em> vector and TAT3. This hybrid vector formation is likely due to the electrostatic interaction between the negatively charged outer membrane of <em>E. coli</em> and the highly positively charged TAT3 peptides. Our result suggested that the TAT3 is internalized into <em>E. coli</em> and coated its surface to improve cellular uptake and gene delivery efficiency. TAT3 peptide enhances <em>E. coli</em> gene transfer efficiency by over 2.5 fold in HeLa, HT1080, HEK-293, and 1.3 fold in MCF-7, but not in A549. Additionally, internalization of <em>E. coli</em> increased by 1.2 fold in HeLa with no significant uptake by A549, demonstrating that cellular entry is a prerequisite to higher gene expression. This TAT-based complexing method may be applied to other bacterial-based vectors to enhance DNA and protein delivery into cells for DNA vaccination and cancer gene therapy.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106864"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143746818","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of liposome-loaded macrophages as tumor-targeted drug delivery carriers: Impact of macrophage phenotypes on their liposome-loading capacity and tumor-homing potential","authors":"Yusuke Kono,&nbsp;Kae Onishi,&nbsp;Himari Kitamura,&nbsp;Ken-ichi Ogawara","doi":"10.1016/j.jddst.2025.106866","DOIUrl":"10.1016/j.jddst.2025.106866","url":null,"abstract":"<div><div>Macrophages have not only a high phagocytic capacity, but also a tumor-homing ability, and, thus, nanoparticle-loaded macrophages are regarded as an active drug delivery carrier targeting tumors. Macrophages exhibit several phenotypes, such as proinflammatory M1 and anti-inflammatory M2; however, it remains unclear which phenotype possesses superior characteristics as a drug delivery carrier. Therefore, we herein comparatively examined the cellular uptake of doxorubicin (DOX)-encapsulated liposomes (DOX-Lip) and associated cytotoxicity in RAW264.7 murine macrophage-like cells with three different phenotypes: the naïve M0, M1, and tumor-associated macrophage (TAM)-like phenotypes, the latter of which shows similar characteristics to the M2 phenotype. The highest uptake of liposomes was by TAM-like RAW264.7 cells, whereas a significant reduction in cell viability associated with liposome uptake also occurred. M0-type and M1-type RAW264.7 cells showed high cell viability after liposome uptake. M0-type cells exhibited higher tolerance to DOX-Lip uptake than M1-type cells. An <em>in vitro</em> migration assay demonstrated that DOX-Lip-loaded M0-type cells preferentially migrated towards the tumor microenvironment, whereas DOX-Lip-loaded M1-type cells did not. DOX-Lip-loaded M0-type cells also efficiently accumulated in tumor tissue and exhibited significant anti-tumor efficacy in B16/BL6 tumor-bearing mice. These results provide valuable information for the development of a macrophage-based tumor-targeted active drug delivery system.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106866"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143746825","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimization of Linagliptin-loaded polymersomes via response surface methodology: A repurposed therapeutic strategy for hepatic encephalopathy prevention","authors":"Nabila M. Sweed ,&nbsp;Heba T. Elbalkiny ,&nbsp;Eslam Magdy ,&nbsp;Mahitab Ramadan ,&nbsp;Shahin Mahmoud ,&nbsp;Toka Mohamed ,&nbsp;Islam S. Mannaa ,&nbsp;Mai A. Zaafan","doi":"10.1016/j.jddst.2025.106855","DOIUrl":"10.1016/j.jddst.2025.106855","url":null,"abstract":"<div><div>This study aims to prepare linagliptin-loaded polymersomes in order to enhance its stability, bioavailability, and to investigate its potential in the prophylaxis against hepatic encephalopathy (HE). Polymersomes were formulated using solvent injection technique and optimized using D-optimal design, where the effect of drug to polymer ratio (X₁) and polymer type, whether Poly (D, L-lactic-co-glycolide) or polycaprolactone (X₂) were studied. Fifteen formulae were prepared and evaluated for entrapment efficiency % (Y₁), particle size (Y₂), and zeta potential (Y₃). The optimized formula was prepared using polycaprolactone polymer with a drug to polymer ratio of 1:8.9. The optimized formula showed an entrapment efficiency % of 73 ± 1.04 %, a particle size of 184.1 ± 1.45 nm, and a zeta potential of −21.2 ± 0.97 mV. In-vitro drug release showed remarkable sustained release profile for linagliptin-loaded polymersomes as compared to the standard linagliptin. In-vivo pharmacokinetic studies in rats showed a 262 % increase in bioavailability of linagliptin-loaded polymersomes. Moreover, linagliptin-loaded polymersomes showed promising results in a rat model of hepatic encephalopathy, with marked improvement in markers such as alanine transaminase (ALT), aspartate aminotransferase (AST), ammonia levels, and hippocampus brain-derived neurotrophic factor levels (BDNF). Our results showed that the optimized linagliptin-loaded polymersomes formula is a promising drug delivery system for enhancing linagliptin bioavailability, offering potential therapeutic benefits for managing HE and other diseases requiring sustained release and enhanced bioavailability.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106855"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143799518","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An effective approach in osteoarthritis: Diacerein-loaded solid lipid nanoparticles, preparation and evaluation for targeted therapy","authors":"Badarqa Tul Ayesha ,&nbsp;Alia Erum ,&nbsp;Nariman Shahid ,&nbsp;Ume Ruqia Tulain ,&nbsp;Uzma Saleem","doi":"10.1016/j.jddst.2025.106856","DOIUrl":"10.1016/j.jddst.2025.106856","url":null,"abstract":"<div><div>Diacerein (DC) is primarily used for the treatment of degenerative diseases, such as osteoarthritis (OA). The purpose of this study is to develop a stable targeted preparation of DC for intra-articular delivery with prolonged effect. The Response Surface methodology approach was applied to optimize DC-loaded solid lipid nanoparticles (DC-SLNs). For optimization of SLNs, the DC-SLNs were fabricated with different ratios of stearic acid and glyceryl monostearate. SLNs of DC were prepared by a hot homogenization process and were characterized for particle size, zeta potential, polydispersity index, entrapment efficiency, and drug loading. FTIR, DSC, PXRD, and SEM analysis were also performed. <em>In-vitro</em> dissolution studies were also performed for 24 h. <em>In-vivo</em> studies were executed by utilizing papain-induced osteoarthritis rat model including plain DC and DC-SLNs administered orally and intra-articularly. The knee diameter was measured and behavioral studies were done which include the gait analysis, locomotor activity, and forced swim test. The results of these studies revealed that DC-SLNs administered intra-articularly have anti-inflammatory effects in the osteoarthritic rat model. Biochemical analysis displayed a positive effect on the osteoarthritic animal model. The inflammatory marker mediators like; TNF-α, IL-6, and NF-κB, were evaluated and indicated that intra-articular administration of DC-SLNs IA inhibited the inflammation and was also found effective in protecting against cartilage degradation. Thus, the study concluded that DC-SLNs IA can be used as an efficient anti-inflammatory delivery system with minimal side effects.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106856"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143791682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}