Mariam Zewail, Haidy Abbas, HussamElDin Y Aboukilila, Mai F Ragab, Miranda F Kamal, Passent M E Gaafar
{"title":"l -肌肽负载硫酸软骨素功能化提案作为经皮类风湿性关节炎治疗的有效工具。","authors":"Mariam Zewail, Haidy Abbas, HussamElDin Y Aboukilila, Mai F Ragab, Miranda F Kamal, Passent M E Gaafar","doi":"10.1080/1061186X.2025.2557465","DOIUrl":null,"url":null,"abstract":"<p><p>Rheumatoid arthritis (RA) is a chronic autoimmune disease that causes joint inflammation, cartilage deterioration, and oxidative stress. The study developed transdermal RA treatment with L-carnosine (CAR)-loaded chondroitin sulphate (CHS) functionalised proposomes. CHS-functionalised proposomes measured 285 ± 0.89 nm, with PDI of 0.31 ± 0.05, zeta potential of -13.6 ± 0.67 mV, and entrapment efficiency of 73.96 ± 0.87. TEM confirmed their spherical shape and homogenous CHS coating. Biphasic drug release <i>in vitro</i> began with 13.2% burst release in 0.5 h and over 8 h, sustained release reached 83.79%. <i>Ex-vivo</i> permeation results revealed that the selected formulation increased CAR flux by 30.97 folds compared to CAR gel. <i>In vivo</i> testing in rats with AIA model showed that group treated with selected formulation demonstrated reduced joint inflammation and soft tissue swelling that was further confirmed by X-ray radiography. ELISA results showed significant reduction in TNF-α and IL-1β and elevation in NRF2 and SOD with levels comparable to the negative control group. Histopathological investigation showed cartilage integrity and proteoglycan content similar to the negative control. The CHS-functionalised CAR-loaded proposomes improved CAR permeation, targeted inflammatory joints, and reduced oxidative stress, making them a viable non-invasive RA treatment.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-16"},"PeriodicalIF":3.9000,"publicationDate":"2025-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"L-Carnosine loaded chondroitin sulphate functionalized proposomes as an effective tool for transdermal rheumatoid arthritis management.\",\"authors\":\"Mariam Zewail, Haidy Abbas, HussamElDin Y Aboukilila, Mai F Ragab, Miranda F Kamal, Passent M E Gaafar\",\"doi\":\"10.1080/1061186X.2025.2557465\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Rheumatoid arthritis (RA) is a chronic autoimmune disease that causes joint inflammation, cartilage deterioration, and oxidative stress. The study developed transdermal RA treatment with L-carnosine (CAR)-loaded chondroitin sulphate (CHS) functionalised proposomes. CHS-functionalised proposomes measured 285 ± 0.89 nm, with PDI of 0.31 ± 0.05, zeta potential of -13.6 ± 0.67 mV, and entrapment efficiency of 73.96 ± 0.87. TEM confirmed their spherical shape and homogenous CHS coating. Biphasic drug release <i>in vitro</i> began with 13.2% burst release in 0.5 h and over 8 h, sustained release reached 83.79%. <i>Ex-vivo</i> permeation results revealed that the selected formulation increased CAR flux by 30.97 folds compared to CAR gel. <i>In vivo</i> testing in rats with AIA model showed that group treated with selected formulation demonstrated reduced joint inflammation and soft tissue swelling that was further confirmed by X-ray radiography. ELISA results showed significant reduction in TNF-α and IL-1β and elevation in NRF2 and SOD with levels comparable to the negative control group. Histopathological investigation showed cartilage integrity and proteoglycan content similar to the negative control. The CHS-functionalised CAR-loaded proposomes improved CAR permeation, targeted inflammatory joints, and reduced oxidative stress, making them a viable non-invasive RA treatment.</p>\",\"PeriodicalId\":15573,\"journal\":{\"name\":\"Journal of Drug Targeting\",\"volume\":\" \",\"pages\":\"1-16\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2025-09-15\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Drug Targeting\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/1061186X.2025.2557465\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Drug Targeting","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/1061186X.2025.2557465","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
L-Carnosine loaded chondroitin sulphate functionalized proposomes as an effective tool for transdermal rheumatoid arthritis management.
Rheumatoid arthritis (RA) is a chronic autoimmune disease that causes joint inflammation, cartilage deterioration, and oxidative stress. The study developed transdermal RA treatment with L-carnosine (CAR)-loaded chondroitin sulphate (CHS) functionalised proposomes. CHS-functionalised proposomes measured 285 ± 0.89 nm, with PDI of 0.31 ± 0.05, zeta potential of -13.6 ± 0.67 mV, and entrapment efficiency of 73.96 ± 0.87. TEM confirmed their spherical shape and homogenous CHS coating. Biphasic drug release in vitro began with 13.2% burst release in 0.5 h and over 8 h, sustained release reached 83.79%. Ex-vivo permeation results revealed that the selected formulation increased CAR flux by 30.97 folds compared to CAR gel. In vivo testing in rats with AIA model showed that group treated with selected formulation demonstrated reduced joint inflammation and soft tissue swelling that was further confirmed by X-ray radiography. ELISA results showed significant reduction in TNF-α and IL-1β and elevation in NRF2 and SOD with levels comparable to the negative control group. Histopathological investigation showed cartilage integrity and proteoglycan content similar to the negative control. The CHS-functionalised CAR-loaded proposomes improved CAR permeation, targeted inflammatory joints, and reduced oxidative stress, making them a viable non-invasive RA treatment.
期刊介绍:
Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs.
Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.