{"title":"“探索阿魏酸负载纳米结构脂质载体的潜力:通过对接、配方、药代动力学和药效学研究抑制血管紧张素”。","authors":"Preeti Rajabhau Meshram, Nisharani Sudhakar Ranpise","doi":"10.1080/1061186X.2025.2453743","DOIUrl":null,"url":null,"abstract":"<p><p>Ferulic acid (FA) is a natural phenolic compound that has been documented for its antioxidant properties and potential in managing hypertension. However, its use is limited due to poor solubility and permeability (BCS Class IV classification). To overcome this, nanostructured lipid carriers (NLCs) of FA were developed using the emulsification probe sonication technique, with formulation optimized through Box-Behnken design. The optimized FA-NLCs (F12) demonstrated a particle size of 103.4 nm, zeta potential of -43.6 mV, polydispersity index of 0.531, and entrapment efficiency of 88.9%. Key Findings of the research manifested, that during <i>in-vitro</i> release studies, FA-NLCs showed sustained release action (40.34% over 24 h) compared to plain FA (103.13% in 4 h). Pharmacokinetics of FA-NLC suggested that increased C<sub>max</sub> by 2.6-fold, AUC by 1.9-fold, and half-life significantly (p < .001), also Pharmacodynamics revealed that FA-NLCs reduced blood pressure more effectively (39.9 mmHg vs. 30.8 mmHg for plain FA; p < .001). Furthermore, FA-NLC was showing successful intestinal uptake through lymphatic absorption via clathrin-mediated endocytosis, bypassing first-pass metabolism, hence showed enhancement in bioavailability, Thus the study concluded that FA-NLCs significantly improve therapeutic efficacy and sustained blood pressure reduction compared to plain FA.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-23"},"PeriodicalIF":4.3000,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Exploring the potential of ferulic acid-loaded nanostructured lipid carriers: angiotensin inhibition via docking, formulation and pharmacokinetic and pharmacodynamics studies.\",\"authors\":\"Preeti Rajabhau Meshram, Nisharani Sudhakar Ranpise\",\"doi\":\"10.1080/1061186X.2025.2453743\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Ferulic acid (FA) is a natural phenolic compound that has been documented for its antioxidant properties and potential in managing hypertension. However, its use is limited due to poor solubility and permeability (BCS Class IV classification). To overcome this, nanostructured lipid carriers (NLCs) of FA were developed using the emulsification probe sonication technique, with formulation optimized through Box-Behnken design. The optimized FA-NLCs (F12) demonstrated a particle size of 103.4 nm, zeta potential of -43.6 mV, polydispersity index of 0.531, and entrapment efficiency of 88.9%. Key Findings of the research manifested, that during <i>in-vitro</i> release studies, FA-NLCs showed sustained release action (40.34% over 24 h) compared to plain FA (103.13% in 4 h). Pharmacokinetics of FA-NLC suggested that increased C<sub>max</sub> by 2.6-fold, AUC by 1.9-fold, and half-life significantly (p < .001), also Pharmacodynamics revealed that FA-NLCs reduced blood pressure more effectively (39.9 mmHg vs. 30.8 mmHg for plain FA; p < .001). Furthermore, FA-NLC was showing successful intestinal uptake through lymphatic absorption via clathrin-mediated endocytosis, bypassing first-pass metabolism, hence showed enhancement in bioavailability, Thus the study concluded that FA-NLCs significantly improve therapeutic efficacy and sustained blood pressure reduction compared to plain FA.</p>\",\"PeriodicalId\":15573,\"journal\":{\"name\":\"Journal of Drug Targeting\",\"volume\":\" \",\"pages\":\"1-23\"},\"PeriodicalIF\":4.3000,\"publicationDate\":\"2025-01-29\",\"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.2025.2453743\",\"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.2025.2453743","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Exploring the potential of ferulic acid-loaded nanostructured lipid carriers: angiotensin inhibition via docking, formulation and pharmacokinetic and pharmacodynamics studies.
Ferulic acid (FA) is a natural phenolic compound that has been documented for its antioxidant properties and potential in managing hypertension. However, its use is limited due to poor solubility and permeability (BCS Class IV classification). To overcome this, nanostructured lipid carriers (NLCs) of FA were developed using the emulsification probe sonication technique, with formulation optimized through Box-Behnken design. The optimized FA-NLCs (F12) demonstrated a particle size of 103.4 nm, zeta potential of -43.6 mV, polydispersity index of 0.531, and entrapment efficiency of 88.9%. Key Findings of the research manifested, that during in-vitro release studies, FA-NLCs showed sustained release action (40.34% over 24 h) compared to plain FA (103.13% in 4 h). Pharmacokinetics of FA-NLC suggested that increased Cmax by 2.6-fold, AUC by 1.9-fold, and half-life significantly (p < .001), also Pharmacodynamics revealed that FA-NLCs reduced blood pressure more effectively (39.9 mmHg vs. 30.8 mmHg for plain FA; p < .001). Furthermore, FA-NLC was showing successful intestinal uptake through lymphatic absorption via clathrin-mediated endocytosis, bypassing first-pass metabolism, hence showed enhancement in bioavailability, Thus the study concluded that FA-NLCs significantly improve therapeutic efficacy and sustained blood pressure reduction compared to plain FA.
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.