{"title":"增强甲氨蝶呤在CFA性关节炎大鼠模型中的局部递送的NEs的配方和优化。","authors":"Amruta Parmar, Brijesh Sukumaran","doi":"10.1080/1061186X.2025.2565409","DOIUrl":null,"url":null,"abstract":"<p><p>Methotrexate (MTX) is widely used in treating cancers and inflammatory conditions like psoriasis and rheumatoid arthritis (RA), however is associated with side effects. Nanoemulsions (NEs) offer enhanced stability, protection and improved permeation <i>via</i> various delivery routes. MTX-loaded oil-in-water NEs (O/W NEs) were formulated to improve entrapment efficiency, permeation ability and efficacy in CFA-induced arthritis model. The area of NEs was identified by pseudoternary phase diagrams, optimisation of MTX-NEs was performed using I-optimal mixture design, and characterised for %entrapment efficiency, droplet size, polydispersity index, zeta potential, morphology and %transmittance. The MTX-NE gel was evaluated for rheology, <i>in vitro</i> drug release, <i>ex vivo</i> permeation and efficacy in a CFA-induced arthritic rats. The MTX-NEs were prepared using S<sub>mix</sub> ratio of 3:1 with 0.2 N sodium hydroxide as aqueous phase. It showed >90% entrapment efficiency, size of 161.4 ± 13.5 nm, and 94 ± 1.8% of %transmittance. MTX-NE gel showed sustained release of 86 ± 1.8% MTX, and cumulative permeation of 77.6 ± 1.4% with a flux of 0.184 µg/cm<sup>2</sup>·h. Efficacy studies in a CFA-induced rat model resulted in significant reduction of paw oedema, radiographic, histopathological and inflammatory biomarkers. The optimised MTX-NE gel showed enhanced delivery, sustained release and significant anti-arthritic effects, supporting its potential as an effective for RA therapy.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-17"},"PeriodicalIF":3.9000,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Formulation and optimisation of nanoemulsions for enhancing topical delivery of methotrexate in CFA induced arthritis rat model.\",\"authors\":\"Amruta Parmar, Brijesh Sukumaran\",\"doi\":\"10.1080/1061186X.2025.2565409\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Methotrexate (MTX) is widely used in treating cancers and inflammatory conditions like psoriasis and rheumatoid arthritis (RA), however is associated with side effects. Nanoemulsions (NEs) offer enhanced stability, protection and improved permeation <i>via</i> various delivery routes. MTX-loaded oil-in-water NEs (O/W NEs) were formulated to improve entrapment efficiency, permeation ability and efficacy in CFA-induced arthritis model. The area of NEs was identified by pseudoternary phase diagrams, optimisation of MTX-NEs was performed using I-optimal mixture design, and characterised for %entrapment efficiency, droplet size, polydispersity index, zeta potential, morphology and %transmittance. The MTX-NE gel was evaluated for rheology, <i>in vitro</i> drug release, <i>ex vivo</i> permeation and efficacy in a CFA-induced arthritic rats. The MTX-NEs were prepared using S<sub>mix</sub> ratio of 3:1 with 0.2 N sodium hydroxide as aqueous phase. It showed >90% entrapment efficiency, size of 161.4 ± 13.5 nm, and 94 ± 1.8% of %transmittance. MTX-NE gel showed sustained release of 86 ± 1.8% MTX, and cumulative permeation of 77.6 ± 1.4% with a flux of 0.184 µg/cm<sup>2</sup>·h. Efficacy studies in a CFA-induced rat model resulted in significant reduction of paw oedema, radiographic, histopathological and inflammatory biomarkers. The optimised MTX-NE gel showed enhanced delivery, sustained release and significant anti-arthritic effects, supporting its potential as an effective for RA therapy.</p>\",\"PeriodicalId\":15573,\"journal\":{\"name\":\"Journal of Drug Targeting\",\"volume\":\" \",\"pages\":\"1-17\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2025-09-29\",\"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.2025.2565409\",\"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.2025.2565409","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Formulation and optimisation of nanoemulsions for enhancing topical delivery of methotrexate in CFA induced arthritis rat model.
Methotrexate (MTX) is widely used in treating cancers and inflammatory conditions like psoriasis and rheumatoid arthritis (RA), however is associated with side effects. Nanoemulsions (NEs) offer enhanced stability, protection and improved permeation via various delivery routes. MTX-loaded oil-in-water NEs (O/W NEs) were formulated to improve entrapment efficiency, permeation ability and efficacy in CFA-induced arthritis model. The area of NEs was identified by pseudoternary phase diagrams, optimisation of MTX-NEs was performed using I-optimal mixture design, and characterised for %entrapment efficiency, droplet size, polydispersity index, zeta potential, morphology and %transmittance. The MTX-NE gel was evaluated for rheology, in vitro drug release, ex vivo permeation and efficacy in a CFA-induced arthritic rats. The MTX-NEs were prepared using Smix ratio of 3:1 with 0.2 N sodium hydroxide as aqueous phase. It showed >90% entrapment efficiency, size of 161.4 ± 13.5 nm, and 94 ± 1.8% of %transmittance. MTX-NE gel showed sustained release of 86 ± 1.8% MTX, and cumulative permeation of 77.6 ± 1.4% with a flux of 0.184 µg/cm2·h. Efficacy studies in a CFA-induced rat model resulted in significant reduction of paw oedema, radiographic, histopathological and inflammatory biomarkers. The optimised MTX-NE gel showed enhanced delivery, sustained release and significant anti-arthritic effects, supporting its potential as an effective for RA therapy.
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.
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