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Evaluation of chloramphenicol derivative N-phenyl 2, 2 dichloroacetamide anticancer and antibacterial properties. 氯霉素衍生物n -苯基2,2二氯乙酰胺的抗癌和抗菌性能评价。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-03-10 DOI: 10.1080/20415990.2025.2476928
Arwa Al Khatib, Anas Abed, Hamdi Nsairat, Mohamed El-Tanani, Muhammad Yaqoob, Hisham Al-Obaidi

Aims: This study aimed to develop microparticles of N-phenyl-2,2-dichloroacetamide (PDA), a chloramphenicol derivative with potential antibacterial and anticancer properties, to improve drug release and selectivity while reducing toxicity.

Materials & methods: PDA microparticles were prepared via spray-drying using L-leucine, Trehalose, and Mannitol. The particles were characterized for size, drug release, antibacterial activity, and cytotoxicity against A549 cancer cells and fibroblasts.

Results: PDA formulations exhibited controlled release and enhanced selectivity for cancer cells. S1 showed antibacterial activity against S. aureus. L-leucine formulations had reduced toxicity to normal fibroblasts.

Conclusions: PDA microparticles offer potential as safer, targeted antibacterial and anticancer therapies, providing controlled release and reduced side effects.

目的:制备具有潜在抗菌和抗癌特性的氯霉素衍生物n -苯基-2,2-二氯乙酰胺(PDA)微颗粒,以改善药物释放和选择性,同时降低毒性。材料与方法:采用l -亮氨酸、海藻糖、甘露醇喷雾干燥法制备PDA微颗粒。颗粒的大小、药物释放、抗菌活性以及对A549癌细胞和成纤维细胞的细胞毒性进行了表征。结果:PDA制剂对肿瘤细胞具有控释和增强的选择性。S1对金黄色葡萄球菌具有抗菌活性。l -亮氨酸制剂降低了对正常成纤维细胞的毒性。结论:PDA微颗粒具有控释和减少副作用的特点,具有更安全、靶向抗菌和抗癌治疗的潜力。
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引用次数: 0
Next-gen ferulic acid-stabilized gold nanoparticles: exploring their sensing capabilities and therapeutic efficacy. 新一代阿魏酸稳定金纳米颗粒:探索其传感能力和治疗效果。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-03-20 DOI: 10.1080/20415990.2025.2472733
Atiya Kaleem, Aisha Sana, Rafia Usman Khan, Safila Naveed, Fatima Qamar, Syeda Zainab, Javed Iqbal, Brijesh Sathian

Aim: This study focuses on the synthesis and evaluation of innovative gold nanoparticles (AuNps) stabilized by short-chain ferulic acid (FA), specifically 4-hydroxy-3-methoxy-cinnamic acid.

Methods: We analyzed the size and distribution of FA-TSC-AuNps and FA-NaBH4-AuNps, with the reduction kinetics of Au3 + to Au0. The electronic and optical properties of these AuNps were scrutinized using UV-visible, AFM, and FT-IR.

Results: AFM distinctly showcased spherical particles, average diameters of 4 ± 1 nm for FA-TSC-AuNps and 11 ± 1 nm for FA-NaBH4-AuNps systems. In the DPPH assay, the anti-scavenging activity recorded values of: FA at 15.4% ± 0.32, FA-TSC-AuNps at an impressive 86.8% ± 0.32, and FA-NaBH4-AuNps at 61.5% ± 0.22. The ABTS assay yielded results of: FA at 13%, FA-TSC-AuNps at 70.14%, and FA-NaBH4-AuNps at a remarkable 92.8%. Catalytic investigations revealed that both facilitated the swift conversion of p-nitrophenol to p-aminophenol. Additionally successful chemo sensing capabilities were assessed, particularly in relation to ciprofloxacin antibiotic by distinct shift in color signifies the effective detection capability of both sensory systems for the drug. Moreover, with FA-TSC-AuNps exhibiting significant sensitivity toward aluminum.

Conclusion: These nanoparticles suggest promising avenues for drug system modifications and enhancements, highlighting their multifaceted potential in both catalytic and chemo sensing applications.

目的:研究以短链阿魏酸(FA)为稳定剂的新型金纳米粒子(AuNps)的合成及性能评价。方法:分析FA-TSC-AuNps和FA-NaBH4-AuNps的大小和分布,以及Au3 +还原到Au0的动力学。这些AuNps的电子和光学性质使用紫外可见,AFM和FT-IR进行了仔细检查。结果:AFM显示明显的球形颗粒,FA-TSC-AuNps系统的平均直径为4±1 nm, FA-NaBH4-AuNps系统的平均直径为11±1 nm。在DPPH实验中,FA的抗清除活性记录值为15.4%±0.32,FA- tsc - aunps的抗清除活性记录值为86.8%±0.32,FA- nabh4 - aunps的抗清除活性记录值为61.5%±0.22。ABTS测定的结果是:FA为13%,FA- tsc - aunps为70.14%,FA- nabh4 - aunps为92.8%。催化研究表明,两者都促进了对硝基酚到对氨基酚的快速转化。此外,评估了成功的化学感应能力,特别是环丙沙星抗生素,通过颜色的明显变化表明两种感觉系统对药物的有效检测能力。此外,FA-TSC-AuNps对铝表现出显著的敏感性。结论:这些纳米颗粒为药物系统修饰和增强提供了有希望的途径,突出了它们在催化和化学传感应用中的多方面潜力。
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引用次数: 0
Drug delivery systems incorporating bile salts: advancements since the conception of bilosomes. 含胆盐的药物输送系统:自胆囊体概念以来的进展。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-03-24 DOI: 10.1080/20415990.2025.2469488
Mohammad A Obeid, Marta Ruano-Aldea, Reinaldo Acevedo, Virgil Schjins, Manal M Alsaadi, Valerie A Ferro

This review explores the advancements in drug delivery systems that incorporate bile salts since bilosomes that were developed over 20 years ago. Bile salts, recognized for their unique amphiphilic properties, have emerged as versatile agents in enhancing solubility, stability, and bioavailability of various therapeutics. We discuss the innovative formulations developed, including micelles, liposomes, and nanoparticles, that leverage bile salts to facilitate targeted and sustained release. The review also highlights the mechanisms by which bile salts improve drug absorption, particularly for hydrophobic compounds, and examines the evolving regulatory landscape surrounding these systems. Furthermore, we address challenges faced in clinical translation and future directions for research, emphasizing the potential of bile salt-based systems in personalized medicine. Our evaluation highlights the significant role of bile salts in advancing drug delivery technologies and their promise for improving therapeutic outcomes.

本文综述了胆汁酸盐给药系统自20多年前胆汁酸盐被开发出来以来的进展。胆汁盐因其独特的两亲性而被公认,已成为提高各种治疗药物的溶解度、稳定性和生物利用度的多用途药物。我们讨论了开发的创新配方,包括胶束,脂质体和纳米颗粒,利用胆汁盐促进靶向和持续释放。该综述还强调了胆盐改善药物吸收的机制,特别是疏水化合物,并研究了围绕这些系统的不断发展的监管格局。此外,我们讨论了临床转化和未来研究方向所面临的挑战,强调了胆盐基系统在个性化医疗中的潜力。我们的评估强调了胆盐在推进药物输送技术和改善治疗结果方面的重要作用。
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引用次数: 0
Effective release of Eryngium maritimum L. callus extract via encapsulation in multilayered liposomes for skin delivery. 通过封装在多层脂质体中有效释放海腥草茧提取物,用于皮肤给药。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-02-28 DOI: 10.1080/20415990.2025.2470614
Euihyun Kim, Jihyeon Jang, Myeong-Jin Lim, Soo-Yun Kim, Seon Kyu Yun, Jihyeok Song, Hyo Hyun Seo, Jeong Hun Lee, Sang Hyun Moh

Aims: This study aimed to evaluate the potential of Eryngium maritimum L. (EM) callus media filtrate (ECMF) for enhanced skin delivery through multilayered liposomes (MLs).

Materials & methods: ECMF was applied to human skin cells to assess its antioxidant, anti-inflammatory, and skin barrier-enhancing properties. ECMF was encapsulated in MLs to enhance delivery efficiency, creating a formulation called Cellbiome. Clinical trials involving human participants were conducted to compare its effects with traditional formulations, assessing parameters such as skin density, hydration, elasticity, and wrinkle reduction.

Results: Cellbiome significantly improved skin density and moisturization, outperforming conventional formulations. ML encapsulation facilitated deeper penetration of active ingredients beyond the stratum corneum, leading to synchronized improvements in multiple skin parameters, including elasticity, wrinkle reduction, and overall skin health. Transcriptomic and metabolomic analyses further confirmed ECMF's bioactivity and its role in skin improvement.

Conclusions: ML-based formulations, such as Cellbiome, offer superior efficacy in skincare applications compared to conventional methods. This study underscores the importance of advanced delivery technologies in cosmetics and highlights the need for further research to optimize the benefits of natural extracts like EM for human skin, potentially advancing dermatological and cosmeceutical applications.

目的:本研究旨在评估海百合(EM)愈伤组织培养基滤液(ECMF)通过多层脂质体(MLs)增强皮肤递送的潜力。材料与方法:将ECMF应用于人体皮肤细胞,评估其抗氧化、抗炎和增强皮肤屏障的性能。ECMF被封装在ml中以提高递送效率,创造了一种称为Cellbiome的配方。研究人员进行了涉及人体参与者的临床试验,以比较其与传统配方的效果,评估皮肤密度、水合作用、弹性和皱纹减少等参数。结果:Cellbiome显着改善皮肤密度和保湿,优于传统配方。ML包封促进活性成分深入渗透到角质层之外,从而同步改善多种皮肤参数,包括弹性,皱纹减少和整体皮肤健康。转录组学和代谢组学分析进一步证实了ECMF的生物活性及其在皮肤改善中的作用。结论:与传统方法相比,基于ml的制剂,如Cellbiome,在护肤应用中具有优越的功效。这项研究强调了先进的给药技术在化妆品中的重要性,并强调了进一步研究的必要性,以优化EM等天然提取物对人体皮肤的益处,潜在地推进皮肤病学和药妆应用。
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引用次数: 0
Advantages and drawbacks of eco-friendly nano-delivery systems. 生态友好型纳米输送系统的优缺点。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-03-11 DOI: 10.1080/20415990.2025.2477441
Constantin Cerbu, Emilia Trif
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引用次数: 0
Exosomes in glioma: mechanistic insights on biological, therapeutic, and diagnostic perspective. 神经胶质瘤中的外泌体:生物学、治疗和诊断角度的机制见解。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-02-16 DOI: 10.1080/20415990.2025.2466410
Reetika Tandon, Samarth Kumar, Mayank Handa, Nidhi Srivastava

Gliomas are prominent and frequent primary malignant brain tumors, with a generally poor prognosis. Current treatment involves radiation, surgery and chemotherapy. Exosomes are nanoscale extracellular vesicles released by cells that enable biological molecule movement and encourage intercellular communication in the tumor microenvironment. This contributes to glioma development, radiation resistance, and overcomes chemotherapy. Exosome functional and structural properties are essential for understanding cancer molecular mechanisms. They can also treat invasive tumors like glioblastomas and serve as diagnostic markers. Recent research depicted exosomes' prominent role in cancer cell maintenance, intercellular signaling, and microenvironment modification. Exosomes hold nucleic acids, proteins, lipids, mRNAs, lncRNAs, miRNAs, and immunological regulatory molecules depending on the origin of the cell. This paper reviews exosomes, their role in glioma etiology, and perspective diagnostic and therapeutic uses.

胶质瘤是一种突出的、常见的原发性恶性脑肿瘤,通常预后较差。目前的治疗方法包括放疗、手术和化疗。外泌体是细胞释放的纳米级细胞外囊泡,可促进肿瘤微环境中的生物分子运动和细胞间通讯。这有助于胶质瘤的发展、放射抵抗和克服化疗。外泌体的功能和结构特性对了解癌症分子机制至关重要。它们还可以治疗侵袭性肿瘤,如胶质母细胞瘤,并作为诊断标志物。最近的研究描述了外泌体在癌细胞维持、细胞间信号传导和微环境修饰方面的突出作用。外泌体含有核酸、蛋白质、脂质、mrna、lncrna、mirna和免疫调节分子,这取决于细胞的来源。本文综述了外泌体及其在胶质瘤病因学中的作用,并对其诊断和治疗应用进行了展望。
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引用次数: 0
Novel nanostructured lipid carriers with lurasidone hydrochloride for intranasal administration for improved bioavailability. 新型纳米结构脂质载体盐酸鲁拉西酮鼻内给药以提高生物利用度。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-05-01 Epub Date: 2025-03-24 DOI: 10.1080/20415990.2025.2477440
Tanvi Kadam, Surendra Agrawal, Saritha Shetty

Aim: This research aims to develop nanostructured lipid carriers containing Lurasidone hydrochloride (LH) with Quality by Design (QbD) methodology to enhance its bioavailability, given LH's low water solubility (0.224 mg/ml) and bioavailability (9-19%).

Material and methods: The optimized LH-NLC formulation contains Glyceryl monostearate (GMS) as solid lipid, Caproyl 90 as liquid lipid and co-surfactant, and Tween 80 as surfactant. The hot emulsification method was used to formulate the LH-NLC using a three-factor, three-level Box-Behnken design (BBD)for ascertaining functional relationships between particle size and entrapment efficiency (EE). Particle size, polydispersity index (PDI), zeta potential, surface morphology, percentage EE, and in vitro and ex-vivo release were assessed. Wistar rats were used to estimate plasma drug concentration after LH-NLC administration.

Results: The developed formulation exhibited a particle size of 190.98 ± 4.72 nm, zeta potential of + 17.47 mV, and encapsulation efficiency of 94 ± 1.26% w/w. LH-NLCs showed a drug release rate of 95.37% within 24 hours. Intranasal administration of LH-NLCs resulted in 5.16 times higher bioavailability compared to intranasally administered lurasidone.

Conclusion: The study successfully applied QbD methodology to develop NLCs for LH with enhanced bioavailability, demonstrating improved drug entrapment and delivery efficacy for treating psychosis.

目的:考虑到盐酸鲁拉西酮(LH)水溶性低(0.224 mg/ml),生物利用度低(9-19%),本研究旨在利用质量设计(QbD)方法开发含有盐酸鲁拉西酮(LH)的纳米结构脂质载体,以提高其生物利用度。材料与方法:优化后的LH-NLC配方以单硬脂酸甘油酯(GMS)为固体脂质,以己烷酰90为液体脂质和助表面活性剂,以吐温80为表面活性剂。采用三因素三水平Box-Behnken设计(BBD)确定粒径与捕集效率(EE)之间的函数关系,采用热乳化法制备了LH-NLC。评估了颗粒大小、多分散性指数(PDI)、zeta电位、表面形貌、EE百分比以及体外和离体释放。用Wistar大鼠测定给药后血药浓度。结果:该配方粒径为190.98±4.72 nm, zeta电位为+ 17.47 mV,包封效率为94±1.26% w/w。h - nlcs在24 h内释药率为95.37%。经鼻给药的hl - nlcs的生物利用度比经鼻给药的鲁拉西酮高5.16倍。结论:该研究成功地应用QbD方法开发了LH的NLCs,提高了生物利用度,证明了治疗精神病的药物包裹和递送效果。
{"title":"Novel nanostructured lipid carriers with lurasidone hydrochloride for intranasal administration for improved bioavailability.","authors":"Tanvi Kadam, Surendra Agrawal, Saritha Shetty","doi":"10.1080/20415990.2025.2477440","DOIUrl":"10.1080/20415990.2025.2477440","url":null,"abstract":"<p><strong>Aim: </strong>This research aims to develop nanostructured lipid carriers containing Lurasidone hydrochloride (LH) with Quality by Design (QbD) methodology to enhance its bioavailability, given LH's low water solubility (0.224 mg/ml) and bioavailability (9-19%).</p><p><strong>Material and methods: </strong>The optimized LH-NLC formulation contains Glyceryl monostearate (GMS) as solid lipid, Caproyl 90 as liquid lipid and co-surfactant, and Tween 80 as surfactant. The hot emulsification method was used to formulate the LH-NLC using a three-factor, three-level Box-Behnken design (BBD)for ascertaining functional relationships between particle size and entrapment efficiency (EE). Particle size, polydispersity index (PDI), zeta potential, surface morphology, percentage EE, and in vitro and ex-vivo release were assessed. Wistar rats were used to estimate plasma drug concentration after LH-NLC administration.</p><p><strong>Results: </strong>The developed formulation exhibited a particle size of 190.98 ± 4.72 nm, zeta potential of + 17.47 mV, and encapsulation efficiency of 94 ± 1.26% w/w. LH-NLCs showed a drug release rate of 95.37% within 24 hours. Intranasal administration of LH-NLCs resulted in 5.16 times higher bioavailability compared to intranasally administered lurasidone.</p><p><strong>Conclusion: </strong>The study successfully applied QbD methodology to develop NLCs for LH with enhanced bioavailability, demonstrating improved drug entrapment and delivery efficacy for treating psychosis.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"419-429"},"PeriodicalIF":3.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12135687/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143693350","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Industry update: the latest developments in the field of therapeutic delivery, February 2025. 行业更新:治疗递送领域的最新进展,2025年2月。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-04-16 DOI: 10.1080/20415990.2025.2492539
Louise Rosenmayr-Templeton
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引用次数: 0
Naturally derived hydrogels for wound healing. 用于伤口愈合的天然水凝胶。
IF 2.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-04-01 Epub Date: 2025-01-27 DOI: 10.1080/20415990.2025.2457928
Duy Toan Pham, Ngo Thi Ngoc Thuy, Nguyen Thi Phuong Thao, Le Thi Nhi, Bui Thi Phuong Thuy

Natural hydrogels have garnered increasing attention due to their natural origins and beneficial roles in wound healing. Hydrogel water-retaining capacity and excellent biocompatibility create an ideal moist environment for wound healing, thereby enhancing cell proliferation and tissue regeneration. For this reason, naturally derived hydrogels formulated from biomaterials such as chitosan, alginate, gelatin, and fibroin are highly promising due to their biodegradability and low immunogenic responses. Recent integrated approaches to utilizing new technologies with bioactive agents have significantly improved the mechanical properties of hydrogels and the controlled release and delivery of active compounds, thereby increasing the efficiency of the treatment processes. Herein, this review highlights the advantages and the challenges of natural hydrogels in wound healing, focusing on their mechanical strength, controlled degradation rates, safety and efficiency validation, and the potential for incorporating advanced technologies such as tissue engineering and gene therapy for utilization in personalized medicine.

天然水凝胶由于其天然来源和在伤口愈合中的有益作用而受到越来越多的关注。水凝胶保水能力和优异的生物相容性为伤口愈合创造了理想的湿润环境,从而促进细胞增殖和组织再生。因此,由壳聚糖、海藻酸盐、明胶和丝蛋白等生物材料制成的天然水凝胶因其生物可降解性和低免疫原性反应而具有很高的前景。最近利用新技术与生物活性剂的综合方法显着改善了水凝胶的机械性能和活性化合物的可控释放和递送,从而提高了处理过程的效率。在此,本文综述了天然水凝胶在伤口愈合中的优势和挑战,重点关注其机械强度、可控制的降解率、安全性和效率验证,以及结合组织工程和基因治疗等先进技术用于个性化医疗的潜力。
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引用次数: 0
Next-generation pharmaceuticals: the rise of sildenafil citrate ODF for the treatment of men with erectile dysfunction. 下一代药物:柠檬酸西地那非用于治疗男性勃起功能障碍的兴起。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-04-01 Epub Date: 2025-01-12 DOI: 10.1080/20415990.2024.2445501
Emmanuele A Jannini, Shivani Ohri Vignesh, Tarek Hassan

Orodispersible film (ODF) is one of the novel formulations that disintegrate rapidly in the mouth without the requisite for water compared to other conventional oral solid dosage formulations. This delivery system serves as a convenient mode of administration, especially in patients who have dysphagia and fluid restriction, being beneficial to pediatric, geriatric, and bedridden patients. A novel sildenafil ODF containing sildenafil citrate is formulated to be used in patients with erectile dysfunction (ED). This review discusses the advantages of ODF in improving compliance and satisfaction in these patients and describes the manufacturing techniques, evaluation tests, bioequivalence, and stability studies of sildenafil ODF. This formulation offers unique benefit to patients with ED by improving their acceptance and compliance and respecting their privacy and the need for a discreet treatment. Moreover, the comparison of pharmacokinetic parameters between the sildenafil ODF administered with and without water and the conventional film-coated tablet were similar. It also demonstrated reliable performance that yielded a consistent product, meeting all specifications at release and after three weeks of storage under stressed conditions (60°C). Sildenafil ODF warrants improved ease of intake, taste, portability, storage, and compliance among ED patients, making it the potential most preferred formulation and drug of choice.

与其他传统的口服固体剂型相比,孔分散膜(ODF)是一种无需水即可在口腔中快速分解的新型剂型。这种给药系统是一种方便的给药方式,特别是对于吞咽困难和液体限制的患者,对儿童、老年人和卧床不起的患者都有益。一种新型西地那非ODF含有柠檬酸西地那非配制用于患者勃起功能障碍(ED)。这篇综述讨论了ODF在提高这些患者的依从性和满意度方面的优势,并描述了西地那非ODF的制造技术、评价试验、生物等效性和稳定性研究。这种配方通过提高ED患者的接受度和依从性,尊重他们的隐私和谨慎治疗的需要,为ED患者提供了独特的好处。此外,加水和不加水给药的西地那非ODF与常规薄膜包衣片的药动学参数比较相似。它还显示出可靠的性能,产生一致的产品,在发布时和在压力条件下(60°C)储存三周后符合所有规格。西地那非ODF保证易于摄入,口味,便携性,储存和依从性在ED患者中,使其成为潜在的首选配方和药物选择。
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引用次数: 0
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Therapeutic delivery
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