Formulation, optimisation, and evaluation of Lornoxicam-loaded Novasomes for targeted ulcerative colitis therapy: in vitro and in vivo investigations.

IF 4.3 4区 医学 Q1 PHARMACOLOGY & PHARMACY Journal of Drug Targeting Pub Date : 2025-01-25 DOI:10.1080/1061186X.2025.2456929
Asmaa Badawy Darwish, Abeer Salama, Inas Essam Ibrahim Al-Samadi
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Abstract

The purpose of this work was to create and assess Lornoxicam (LOR) loaded Novasomes (Novas) for the efficient treatment of ulcerative colitis. The study was performed using a 23 factorial design to investigate the impact of several formulation variables. Three separate parameters were investigated: Surface Active agent (SAA) type (X1), LOR concentration (X2), and SAA: Oleic acid ratio (X3). The dependent responses included encapsulation efficiency (Y1: EE %), particle size (Y2: PS), zeta potential (Y3: ZP), and polydispersity index (Y4: PDI). The vesicles demonstrated remarkable LOR encapsulation efficiency, ranging from 81.32 ± 3.24 to 98.64 ± 0.99%. The vesicle sizes ranged from 329 ± 9.88 to 583.4 ± 9.04 nm with high negative zeta potential values. The release pattern for Novas' LOR was biphasic and adhered to Higuchi's model. An in-vivo study assessed how LOR-Novas affected rats' acetic acid-induced ulcerative colitis (UC). The optimised LOR-Novas effectively reduced colonic ulceration (p < 0.05) and reduced the inflammatory pathway via inhibiting Toll-like receptor 4 (TLR4), Nuclear factor kappa β (NF-κβ) and inducible nitric oxide (iNO). At the same time, it elevated Silent information regulator-1(SIRT-1) and reduced glutathione (GSH) colon contents. Thus, the current study suggested that the formulation of LOR-Novas may be a viable treatment for ulcerative colitis.

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含氯诺昔康的novasome靶向治疗溃疡性结肠炎的处方、优化和评价:体外和体内研究。
这项工作的目的是创建和评估氯诺昔康(LOR)负载novasome (Novas)有效治疗溃疡性结肠炎。该研究采用23因子设计来调查几个配方变量的影响。考察了3个单独的参数:表面活性剂(SAA)类型(X1)、LOR浓度(X2)和SAA:油酸比(X3)。相关响应包括包封效率(Y1: EE %)、粒径(Y2: PS)、zeta电位(Y3: ZP)和多分散性指数(Y4: PDI)。包封率为81.32±3.24 ~ 98.64±0.99%。微泡大小在329±9.88 ~ 583.4±9.04 nm之间,具有较高的zeta负电位值。Novas的LOR释放模式为双相,符合Higuchi模型。一项体内研究评估了loro - novas如何影响大鼠醋酸诱导的溃疡性结肠炎(UC)。优化后的LOR-Novas通过抑制toll样受体4 (TLR4)、核因子κβ (NF-κβ)和诱导型一氧化氮(iNO),有效减少结肠溃疡(P < 0.05),降低炎症通路。同时,提高沉默信息调节因子-1(SIRT-1)和降低谷胱甘肽(GSH)结肠含量。因此,目前的研究表明,LOR- Novas制剂可能是治疗溃疡性结肠炎的可行方法。
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来源期刊
CiteScore
9.10
自引率
0.00%
发文量
165
审稿时长
2 months
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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