Journal of Drug Delivery Science and Technology最新文献

筛选
英文 中文
Development and evaluation of novel dual-target drugs encapsulated in liposome against visceral leishmaniasis
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-31 DOI: 10.1016/j.jddst.2025.106883
Kushal Bora , Shiv Kumar , Shankar Prasad Kanaujia , Vikash Kumar Dubey
{"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}
引用次数: 0
A smart therapeutic approach for improving thin endometrium in rodent models – A maiden intra uterine preclinical approach
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-30 DOI: 10.1016/j.jddst.2025.106874
Azeena Saleem , Alan M. Punnoose , K. Brindha , Radha Vembu
{"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}
引用次数: 0
Curcumin delivered by ROS-responsive ibuprofen prodrug based on hyaluronic acid effectively suppressed the rheumatoid arthritis
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106868
Ping-fu Huang , Miaomiao Ma , Hao Wu , Wen-min Niu , Lu-lu Liu , Jia-bing Tong
{"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 H<sub>2</sub>O<sub>2</sub> 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}
引用次数: 0
An arginine-rich motif of the HIV-1 TAT protein promotes E. coli cellular entry and DNA delivery
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106864
Rasaq Olajide Akinsola , Andrew Osahor , Lena Vollmer , Oluwafemi Adebayo Oyewole , Choon Weng Lee , Edmund Ui Hang Sim , Kumaran Narayanan
{"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}
引用次数: 0
Development of liposome-loaded macrophages as tumor-targeted drug delivery carriers: Impact of macrophage phenotypes on their liposome-loading capacity and tumor-homing potential
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106866
Yusuke Kono, Kae Onishi, Himari Kitamura, Ken-ichi Ogawara
{"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}
引用次数: 0
Optimization of Linagliptin-loaded polymersomes via response surface methodology: A repurposed therapeutic strategy for hepatic encephalopathy prevention
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106855
Nabila M. Sweed , Heba T. Elbalkiny , Eslam Magdy , Mahitab Ramadan , Shahin Mahmoud , Toka Mohamed , Islam S. Mannaa , Mai A. Zaafan
{"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 (X<sub>1</sub>) and polymer type, whether Poly (D, L-lactic-co-glycolide) or polycaprolactone (X<sub>2</sub>) were studied. Fifteen formulae were prepared and evaluated for entrapment efficiency % (Y<sub>1</sub>), particle size (Y<sub>2</sub>), and zeta potential (Y<sub>3</sub>). 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}
引用次数: 0
An effective approach in osteoarthritis: Diacerein-loaded solid lipid nanoparticles, preparation and evaluation for targeted therapy
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106856
Badarqa Tul Ayesha , Alia Erum , Nariman Shahid , Ume Ruqia Tulain , Uzma Saleem
{"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}
引用次数: 0
Development of β-carotene-loaded casein nanoparticles with enhanced stability, permeability, and antioxidant activity that mitigates dexamethasone-induced muscle atrophy
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106865
Wan-Yi Liu , Yung-Yi Cheng , Yih-Fung Chen , Yu-Tse Wu
{"title":"Development of β-carotene-loaded casein nanoparticles with enhanced stability, permeability, and antioxidant activity that mitigates dexamethasone-induced muscle atrophy","authors":"Wan-Yi Liu ,&nbsp;Yung-Yi Cheng ,&nbsp;Yih-Fung Chen ,&nbsp;Yu-Tse Wu","doi":"10.1016/j.jddst.2025.106865","DOIUrl":"10.1016/j.jddst.2025.106865","url":null,"abstract":"<div><div>β-carotene (BC)-loaded casein nanoparticles (BC-CNPs) were developed to enhance the oral absorption and intestinal permeability of β-carotene and evaluated their antioxidant activity in the present study. The nanoparticles were fabricated using a simple coacervation method, which yielded particles with an average size of 217.4 nm, polydispersity index of 0.149, zeta potential of −18.49 mV, and encapsulation efficiency of 88 %, indicating uniformity and stability. Physicochemical evaluation revealed that the BC-CNPs were spherical with β-carotene in an amorphous form. The stability of BC-CNPs under heat and lyophilization was also confirmed, and they exhibited 1.6-fold enhancement in the permeability assay compared with BC, indicating an improvement in oral absorption. <em>In vitro</em> antioxidant tests demonstrated improved 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid free radical scavenging ability and ferric reducing antioxidant power. Fluorescence assay confirmed that the k<sub>q</sub> value of the BC-CNPs was higher than the maximum scatter collision quenching value, revealing the formation of a ground-state acceptor–ligand complex. Molecular docking results revealed that BC and sodium caseinate are combined via van der Waals and hydrophobic interactions. Furthermore, <em>in vivo</em> studies using a mouse model showed that BC-CNPs could prevent dexamethasone-induced muscle atrophy, increase glutathione peroxidase and catalase levels by 1370.0 % and 11.8 %, respectively, and reduce malondialdehyde levels and advanced oxidation protein products by 27.0 % and 30.1 %, respectively, in the plasma. These findings suggest that casein nanoparticles can effectively enhance BC oral absorption and mitigate muscle atrophy and oxidative stress. Overall, BC-CNPs can improve muscle atrophy by reducing oxidative stress.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"107 ","pages":"Article 106865"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143768647","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}
引用次数: 0
Film-forming solutions for cutaneous application: current challenges and future directions in formulation design and characterization framework
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106863
Sandra Milinković , Ljiljana Đekić
{"title":"Film-forming solutions for cutaneous application: current challenges and future directions in formulation design and characterization framework","authors":"Sandra Milinković ,&nbsp;Ljiljana Đekić","doi":"10.1016/j.jddst.2025.106863","DOIUrl":"10.1016/j.jddst.2025.106863","url":null,"abstract":"<div><div>Film-forming solution (FFS) implies a novel formulation strategy for liquid preparations for cutaneous application with numerous advantages in comparison with compendial dosage forms, including flexibility of composition (active pharmaceutical ingredient (API) solution in volatile and non-volatile solvents, with film-forming polymers, plasticizers and chemical permeation agents) and the method of administration (rubbing or spraying). Research over the past two decades indicates the potential of FFS for comparable or improved dermal, regional and transdermal delivery of small-molecule drugs due to improved passive diffusion through: volatile solvents evaporation and API (super)saturation, and potential increase in stratum corneum (SC) permeability caused by excipients. Current commercial exploitation of FFS is limited due to demanding pharmaceutical development, the backbone of which is formulation design and product characterization. This comprehensive review gives insight into the complex relationship between the formulation composition, quality attributes (physicochemical properties, microstructure) and <em>in vitro</em> performance (drug release and permeation) of FFS. A characterization framework is proposed, taking into account published studies, relevant pharmacopoeial standards and announced guidelines of the European Medicines Agency (EMA) and The United States Food and Drug Administration (FDA). The importance of specific tests for evaluating the transformation of FFS at the site of application and the quality attributes of the <em>in situ</em> formed film, was pointed out. Directions for pharmaceutical development improvement are given, including the favoring of environmentally acceptable and biocompatible excipients, introduction of <em>in silico</em> formulation optimization techniques and development of standardized methodology for reliable and comparable assessment of quality, efficiency and safety of FFS.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106863"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143768497","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}
引用次数: 0
Curcumin loaded hyaluronan modified niosomes: Preparation, characterization and anti-cancer activity on triple-negative breast cancer cells
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-03-28 DOI: 10.1016/j.jddst.2025.106869
Mozhgan Abasi , Zaynab Sadeghi Ghadi , Younes Pilehvar , Pedram Ebrahimnejad
{"title":"Curcumin loaded hyaluronan modified niosomes: Preparation, characterization and anti-cancer activity on triple-negative breast cancer cells","authors":"Mozhgan Abasi ,&nbsp;Zaynab Sadeghi Ghadi ,&nbsp;Younes Pilehvar ,&nbsp;Pedram Ebrahimnejad","doi":"10.1016/j.jddst.2025.106869","DOIUrl":"10.1016/j.jddst.2025.106869","url":null,"abstract":"<div><div>Curcumin is a herbal polyphenolic compound with anti-cancer properties, but its low solubility, stability and bioavailability limit its therapeutic potential. In this study, we developed niosomes, nanosized vesicles composed of tween 80, Sorbitan monostearate, cholesterol and hyaluronan, as a novel delivery system for curcumin. The curcumin-loaded hyaluronan modified niosomes (cur-nio) were prepared by thin-film hydration method and characterized for their morphology, zeta potential, particle size and <em>in vitro</em> drug release. The anti-cancer activity and apoptotic effect of cur-nio were evaluated on MDA-MB-231 cell line by MTT assay, Real time PCR and Annexin V-FITC/PI staining. Moreover, migration and invasion phenotypes of cells were determined by transwell assays and wound healing assays. We were also interested in determining cur-nio effects on tumorigenicity of MDA-MB-231 cells by mammosphere formation assay. The results showed that the cur-nio had a spherical shape, a negative charge, a mean diameter of about 251 ± 7.14 nm and a high encapsulation efficiency of about 97.96 ± 0.55. The cur-nio exhibited a sustained release profile of curcumin. The cur-nio showed significant inhibition of cell viability and induction the expression of essential apoptotic genes compared to free curcumin and blank niosomes. The IC50 value of cur-nio was about 30 μM, which was approximately 2 times lower than that of free curcumin. Also, our results showed that cur-nio significantly inhibits cell migration, invasion, mammosphere formation and proliferation rate <em>in vitro</em>.These findings suggest that niosomes are a promising carrier for enhancing the delivery and efficacy of curcumin in cancer therapy.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"108 ","pages":"Article 106869"},"PeriodicalIF":4.5,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143760234","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}
引用次数: 0
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信