Pharmaceutical Development and Technology最新文献

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Fabrication and characterization of Coenzyme Q10-loaded nanofibers for potential biomedical applications. 用于潜在生物医学应用的辅酶q10负载纳米纤维的制备和表征。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-10-11 DOI: 10.1080/10837450.2025.2570281
Esra Oğuz, Tuğçe Tayyar, Aysun Özdemir, Onur İnam, Serdar Tort
{"title":"Fabrication and characterization of Coenzyme Q10-loaded nanofibers for potential biomedical applications.","authors":"Esra Oğuz, Tuğçe Tayyar, Aysun Özdemir, Onur İnam, Serdar Tort","doi":"10.1080/10837450.2025.2570281","DOIUrl":"10.1080/10837450.2025.2570281","url":null,"abstract":"<p><p>Coenzyme Q10 (CoQ10) is an essential molecule that plays a role in mitochondrial oxidative phosphorylation and acts as a powerful antioxidant. In this study, CoQ10-loaded nanofibers were developed and characterized <i>via</i> electrospinning method. SEM analyses showed that the fiber diameters ranged between 487 and 2163 nm, and that CoQ10 loading did not disrupt the fiber structure but reduced the diameter. It was determined that bead formation was observed only in the F1 formulation due to the low viscosity (73.09 mPas) and conductivity (1.66 mS/cm) values. The F4 formulation, containing Eudragit RL100 and Kollidon 90F, was selected as the final formulation because it exhibited the highest tensile strength (1.49 MPa) and the smallest fiber diameter (1306 nm). <i>In vitro</i> drug release studies demonstrated that the F4 formulation released only 4% of CoQ10 within 24 h, indicating a controlled release profile. The biocompatibility of this formulation was evaluated through a cytotoxicity assay using the SH-SY5Y neuroblastoma cell line. After seven days of treatment, the CoQ10-loaded nanofiber group showed a cell viability of 101.65%. This result indicates that the nanofibers did not exhibit any cytotoxic effect; on the contrary, they demonstrated potential to support cell proliferation. These findings suggest that CoQ10-loaded nanofibers hold promise for biomedical applications.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.5,"publicationDate":"2025-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145239456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design and characterization of quercetin-embedded biocomposite hydrogel for the management of polycystic ovary syndrome: a dual in vitro and in vivo approach. 槲皮素包埋生物复合水凝胶治疗多囊卵巢综合征的设计和表征:体外和体内双重方法
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-10-06 DOI: 10.1080/10837450.2025.2566901
Koushik Ghosh, Ahana Hazra, Ishika Dey, Supriya Dey, Pratibha Bhowmick, Mithun Bhowmick
{"title":"Design and characterization of quercetin-embedded biocomposite hydrogel for the management of polycystic ovary syndrome: a dual <i>in vitro</i> and <i>in vivo</i> approach.","authors":"Koushik Ghosh, Ahana Hazra, Ishika Dey, Supriya Dey, Pratibha Bhowmick, Mithun Bhowmick","doi":"10.1080/10837450.2025.2566901","DOIUrl":"10.1080/10837450.2025.2566901","url":null,"abstract":"<p><strong>Background: </strong>Polycystic ovarian syndrome (PCOS) is the most prevalent endocrine disorder in women of reproductive age, leading to issues such as androgen excess, insulin resistance, obesity, and menstrual irregularities. Quercetin (QCT), a plant polyphenol, is effective in treating PCOS by regulating steroidogenic activity and helping to correct hormonal imbalances.</p><p><strong>Methods: </strong>In this research, a hydrogel formulation containing QCT-loaded chitosan (CS) and polyvinyl alcohol (PVA) was developed for the treatment of polycystic ovary syndrome (PCOS). The hydrogel was evaluated for various characteristics including pH (ranging from 4.3 to 5.3), spreadability (11.4 to 36.4 g cm/s), swelling index, viscosity, and in vitro drug release, revealing suitable parameters for its application. The release behavior indicated a non-Fickian diffusion mechanism, with a diffusional exponent of 'n ≥ 0.5,' demonstrating effective in vitro QCT delivery. Characterization techniques such as FT-IR, SEM, and DSC were employed to confirm the properties of the hydrogel. Subsequent in vivo studies on PCOS rat models showed significant results, including the recruitment and proliferation of normal ovarian follicles and the normalization of hormone levels, supporting the hydrogel's potential for effective PCOS therapy.</p><p><strong>Conclusion: </strong>The study indicates that QCT-hydrogel is more effective than commercial preparations and represents a safe, natural topical therapy for PCOS.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-18"},"PeriodicalIF":2.5,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145150433","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Current and emerging therapies for dry and neovascular age-related macular degeneration. 干性和新生血管性年龄相关性黄斑变性的当前和新兴治疗方法。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-10-01 DOI: 10.1080/10837450.2025.2562196
Ghayth M Abdulrazzaq, Marwan M Merkhan, Nashiru Billa, Raid G Alany, Winfried Mk Amoaku, Naing L Tint, Zeeshan Ahmad, Omar Qutachi
{"title":"Current and emerging therapies for dry and neovascular age-related macular degeneration.","authors":"Ghayth M Abdulrazzaq, Marwan M Merkhan, Nashiru Billa, Raid G Alany, Winfried Mk Amoaku, Naing L Tint, Zeeshan Ahmad, Omar Qutachi","doi":"10.1080/10837450.2025.2562196","DOIUrl":"10.1080/10837450.2025.2562196","url":null,"abstract":"<p><p>Age-related macular degeneration (AMD), first identified in the 1840s, is now considered the leading cause of visual impairment in elderly people in Western societies. This condition affects the macula, a region rich with photoreceptors essential for detailed visual resolution and colour vision. Advanced AMD can be either atrophic (dry) or exudative (wet), and both forms may coexist. Exudative AMD is characterised by choroidal neovascularisation, where abnormal blood vessels invade the retina and the retinal pigment epithelium (RPE), leading to fluid accumulation in sub- and intra-retinal compartments and photoreceptor dysfunction. In contrast, atrophic AMD involves the gradual degeneration of the RPE and outer retinal layers. Current treatments, such as anti-vascular endothelial growth factor (anti-VEGF) therapies for exudative AMD, can slow or halt disease progression but do not offer a cure. Over the past decade, extensive research programs have focused on various pathogenetic mechanisms of AMD, including oxidative stress, inflammation, and complement pathway dysregulation. This review aims to highlight current theories for developing new treatments, compile recent discoveries and insights into AMD pathogenesis and disease progression, and place special emphasis on therapeutic approaches that have reached clinical trials, evaluating their findings wherever possible.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-36"},"PeriodicalIF":2.5,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145086760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Innovative nanotechnological approaches to diabetes treatment: the role of metal oxide nanoparticles. 创新纳米技术方法治疗糖尿病:金属氧化物纳米颗粒的作用。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-30 DOI: 10.1080/10837450.2025.2566460
Eman E Shaban, Mahmoud E Abd El-Aziz
{"title":"Innovative nanotechnological approaches to diabetes treatment: the role of metal oxide nanoparticles.","authors":"Eman E Shaban, Mahmoud E Abd El-Aziz","doi":"10.1080/10837450.2025.2566460","DOIUrl":"10.1080/10837450.2025.2566460","url":null,"abstract":"<p><p>Diabetes mellitus (DM) is among the most prevalent illnesses in the world. DM and its complications lead to high mortality rates. The negative effects of traditional diabetic therapies, such as insulin and metformin, include weight gain, hypoglycemia, and gastrointestinal problems. In addition to the limited compliance of patients using insulin injections as a treatment for diabetes, these injections cause pain, discomfort, and local infections. This review illustrates the application of nanotechnology (NT) in the treatment of diabetes, especially since it has become an important area of research over the past several decades owing to its application in various sectors, such as biomedicine, cosmetics, and food. This review focuses on the different uses of nanoparticles (NPs), for example zinc oxide (ZnO-NPs), manganese oxide (MnO-NPs), magnesium oxide (MgO-NPs), and selenium (Se-NPs), and their role in controlling diabetes. The application of ZnO-, MnO-, MgO-, and Se-NPs allows the administration of relatively small but more effective doses in the treatment of DM to reduce side effects and increase therapeutic effects by decreasing oxidative stress and increasing antioxidants, insulin sensitivity, and glucose consumption. NT can also be used to improve drug formulations by enhancing drug solubility and altering pharmacokinetics, to prolong drug release and bioavailability.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-23"},"PeriodicalIF":2.5,"publicationDate":"2025-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145150384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Self-assembled Zanubrutinib-loaded lipid polymer hybrid nanoparticles for enhanced oral absorption by lymphatic uptake: in vitro, ex vivo and in vivo evaluations. 自组装zanubrutinib负载脂质聚合物杂化纳米颗粒,通过淋巴吸收增强口服吸收:体外,离体和体内评估。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-29 DOI: 10.1080/10837450.2025.2565783
Mitali Patel, Rahul Parmar, Vrushti Kansara, Bhavin Vyas, Rutvi Vaidya
{"title":"Self-assembled Zanubrutinib-loaded lipid polymer hybrid nanoparticles for enhanced oral absorption by lymphatic uptake: in vitro, ex vivo and in vivo evaluations.","authors":"Mitali Patel, Rahul Parmar, Vrushti Kansara, Bhavin Vyas, Rutvi Vaidya","doi":"10.1080/10837450.2025.2565783","DOIUrl":"10.1080/10837450.2025.2565783","url":null,"abstract":"<p><p>The application of zanubrutinib (ZBR) is limited by poor aqueous solubility (0.0103 mg/ml) and low oral bioavailability (15%) owing to extensive metabolism by CYP3A4 enzyme and P-glycoprotein efflux. Hence, self-assembled lipid-polymer hybrid nanoparticles (LPHNPs) were developed to overcome pitfalls by intestinal lymphatic transport. The ZBR loaded LPHNPs (ZBR-LPHNPs) were prepared by nanoprecipitation method using lipoid P-45, PLGA, and MPEG-2000 DSPE. The ZBR-LPHNPs showed a particle size of 98.17 ± 2.38 nm, a zeta potential of -30.5 ± 2.78 mV, and entrapment efficiency of 82.15 ± 3.70%. The lyophilization of ZBR-LPHNPs was carried out using trehalose at a 1:3 ratio. The DSC and XRD analyses displayed the conversion of ZBR into amorphous form. The particles were spherical, with a core-shell hybrid structure. The ZBR-LPHNPs showed 99.85 ± 2.37% release in phosphate buffer pH 6.8 at 72 h and followed the Higuchi model. The fluorescein isothiocyanate loaded LPHNPs accumulated in intestinal villi and Peyer's patches within 2 h. The bioavailability study revealed 36.11-fold increase in bioavailability with ZBR-LPHNPs as compared to free ZBR. The AUC<sub>total</sub> of ZBR-LPHNPs was reduced by 60.37% in cycloheximide treated group of rats, indicating uptake by intestinal lymphatic system. Overall, this study establishes LPHNP-mediated intestinal lymphatic transport as an effective strategy to enhance oral bioavailability of ZBR.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-13"},"PeriodicalIF":2.5,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145113747","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Enhanced solubility and controlled release of probucol using electrospun nanofibers prepared with different pharmaceutical polymers. 用不同药物聚合物制备的静电纺丝纳米纤维增强普罗布考的溶解度和控释。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-29 DOI: 10.1080/10837450.2025.2562205
Saki Arakawa, Kouji Hara, Yoko Koide, Mayumi Yamada, Eriko Yamazoe, Takaaki Ito, Kohei Tahara
{"title":"Enhanced solubility and controlled release of probucol using electrospun nanofibers prepared with different pharmaceutical polymers.","authors":"Saki Arakawa, Kouji Hara, Yoko Koide, Mayumi Yamada, Eriko Yamazoe, Takaaki Ito, Kohei Tahara","doi":"10.1080/10837450.2025.2562205","DOIUrl":"10.1080/10837450.2025.2562205","url":null,"abstract":"<p><p>We aimed to improve the water solubility and control the release of probucol using electrospinning technology. The effects of multiple polymer matrices and surfactants on the water solubility of probucol were evaluated. Probucol-loaded nanofibers were prepared using four polymers: polyvinylacetal diethylaminoacetate (AEA), methacrylic acid/ethyl acrylate (1/1) copolymer (Kollicoat MAE), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG, Soluplus), and polyvinylpyrrolidone (PVP). Each polymer exhibited different solubility characteristics, and optimal manufacturing conditions were determined. Probucol was in an amorphous state within the nanofibers. The pH-sensitive polymers, including AEA and MAE, enhanced probucol solubility, enabling controlled release in response to pH changes. Additionally, incorporating the surfactants, Tween 80 and Span 20, improved the wettability of Soluplus nanofibers, further enhancing probucol solubility. The addition of surfactants reduced the fiber diameter of the nanofibers, increased the initial dissolution rate, and approximately doubled the drug release rate after 24 h. These findings indicate that the choice of polymer matrix and surfactant is critical for improving solubility and controlling the release of drugs with poor water solubility in electrospun nanofiber solid dispersions. These results provide valuable insights for the development of nanofiber formulations.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-15"},"PeriodicalIF":2.5,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145125750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ex vivo and in vivo evaluation of an in situ nanogel composite loaded with carmustine: implications for efficient nose-to-brain delivery. 卡莫司汀原位纳米凝胶复合材料的体外和体内评价:对有效的鼻到脑输送的影响。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-26 DOI: 10.1080/10837450.2025.2564714
Olufemi D Akilo, Pradeep Kumar, Lisa C du Toit, Girish Modi, Yahya E Choonara
{"title":"<i>Ex vivo</i> and <i>in vivo</i> evaluation of an <i>in situ</i> nanogel composite loaded with carmustine: implications for efficient nose-to-brain delivery.","authors":"Olufemi D Akilo, Pradeep Kumar, Lisa C du Toit, Girish Modi, Yahya E Choonara","doi":"10.1080/10837450.2025.2564714","DOIUrl":"10.1080/10837450.2025.2564714","url":null,"abstract":"<p><p>In this study, the efficacy of a Nanogel Composite was evaluated and compared to the conventional drug carmustine (BCNU) through <i>ex vivo</i> and <i>in vivo</i> studies using New Zealand White rabbits. The Nanogel Composite is a thermosensitive, electro-responsive, and mucoadhesive gel containing BCNU-loaded paramagnetic nanoparticles known as Nano-co-Plex (NCP). Following intranasal administration, electrical stimulation (ES) was applied to the rabbit's nasal cavity, initiating the release of BCNU-NCP. Subsequently, a magnetic headband placed on the rabbit's head rapidly attracted the released nanoparticles toward the brain. The <i>in vivo</i> results showed high amount of BCNU in cerebrospinal fluid (CSF) and the brain of the rabbit for Nanogel Composite compared to the conventional drug with BCNU concentration values in the CSF, brain and plasma being 0.2571 µg/mL, 0.199 µg/g and 0.0078 µg/mL, respectively, after 30 min of administration with the application of ES and MF; and 0.0087 µg/mL, 0.0076 µg/g and 0.0078 µg/mL without the application. The system enabled a pulsatile 'on-off' release profile, improving drug localization in the brain while minimizing systemic exposure. The applied ES and MF conditions (5 V and 0.4 Tesla) were found to be safe and well-tolerated, indicating the potential of this dual-stimuli-responsive platform for effective, non-invasive, and controlled nose-to-brain drug delivery.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.5,"publicationDate":"2025-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145125599","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An injectable ropivacaine and lornoxicam sustained-release gel regulated by low molecular weight poly(ortho esters). 一种低分子量聚邻苯二甲酸酯调控的注射用罗哌卡因氯诺西康缓释凝胶。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-19 DOI: 10.1080/10837450.2025.2559717
Xianzhi Wu, Xiaoan Li, Zhannuan Yin, Huiying Zhong, Haibing He, Guoqing Zhang, Liu Hongfei, Xinggang Yang
{"title":"An injectable ropivacaine and lornoxicam sustained-release gel regulated by low molecular weight poly(ortho esters).","authors":"Xianzhi Wu, Xiaoan Li, Zhannuan Yin, Huiying Zhong, Haibing He, Guoqing Zhang, Liu Hongfei, Xinggang Yang","doi":"10.1080/10837450.2025.2559717","DOIUrl":"10.1080/10837450.2025.2559717","url":null,"abstract":"<p><p>Persistent postoperative pain is commonly occurred after surgical procedures, while over half of patients suffer from poorly controlled pain, due to the limited therapeutic period of commercial drugs and suboptimal drug delivery strategy. Herein, an injectable sustained-release gel was developed by a combination of ropivacaine (a local anesthetic) and lornoxicam (a nonsteroidal anti-inflammatory drug), which formulated by poly(ortho esters) (POE) to regulate the sustained-release behavior. POE with low molecular weight was synthesized and employed to prepare the ropivacaine and lornoxicam sustained-release gel (RL-SRG) with the rheological characteristics of temperature-sensitivity. <i>In vitro</i> release studies demonstrated that RL-SRG exhibited sustained release for 72 h. The RL-SRG was stable for 3 months at 40 ± 2 °C and a relative humidity of 75 ± 5%. <i>In vivo</i> pharmacokinetic studies in rats indicated that RL-SRG maintained the plasma concentrations of ropivacaine and lornoxicam for 3 days. Compared to commercial products, RL-SRG prolonged the time of peak concentration (<i>T</i><sub>max</sub>), mean residence time (MRT), and elimination half life (<i>t</i><sub>1/2</sub>), as well as possessed similar the area under the plasma concentration-time curve (AUC<sub>0-</sub><i><sub>t</sub></i>). Therefore, RL-SRG has been validated as a novel sustained release system to the application for the long-term treatment of postoperative pain.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-11"},"PeriodicalIF":2.5,"publicationDate":"2025-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145054897","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation, characterization and drug release properties of 5-(p-carboxyphenoxy) valeric anhydride microspheres loaded with nimodipine. 负载尼莫地平的5-(对羧基苯氧基)戊酸酐微球的制备、表征及释药性能
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-15 DOI: 10.1080/10837450.2025.2559719
Sibo Su, Jingguo Liu, Yongxue Guo
{"title":"Preparation, characterization and drug release properties of 5-(p-carboxyphenoxy) valeric anhydride microspheres loaded with nimodipine.","authors":"Sibo Su, Jingguo Liu, Yongxue Guo","doi":"10.1080/10837450.2025.2559719","DOIUrl":"10.1080/10837450.2025.2559719","url":null,"abstract":"<p><p>Nimodipine (NMP), a poorly water-soluble small-molecule agent, demonstrates notable therapeutic limitations in addressing cerebral vasospasm secondary to subarachnoid hemorrhage (SAH). Owing to its inherent physicochemical properties characterized by low oral bioavailability, rapid elimination half-life, and extensive first-pass metabolism, conventional formulations necessitate frequent dosing regimens to sustain therapeutic plasma concentrations. These pharmacological challenges collectively result in suboptimal patient adherence, marked plasma concentration fluctuations, and recurrent vascular irritation. To overcome these pharmacological constraints, this investigation engineered a novel drug-loaded microsphere system utilizing poly(5-(p-carboxyphenoxy) valeric anhydride (Poly(CPV)) as a biodegradable matrix material. The sustained-release microspheres were fabricated <i>via</i> microfluidic technology to systematically address the clinical challenges associated with frequent dosing regimens. The optimized microspheres exhibited a drug loading capacity of 5.59%, an encapsulation efficiency of 70.22%, and a uniform particle size distribution (43.98 ± 4.29 μm). <i>In vitro</i> release studies demonstrated sustained drug release over 14 days. Pharmacokinetic evaluation in rats revealed that the NMP-loaded microspheres maintained relative stable plasma drug concentrations for approximately 10 days. Biocompatibility assessments, including histocompatibility tests and <i>in vitro</i> cytotoxicity assays, confirmed the excellent biocompatibility of the Poly(CPV) microsphere. These findings suggest that Poly(CPV)-based microspheres prepared by microfluidics represent a promising drug delivery platform for poorly soluble small-molecule pharmaceuticals, offering controlled release characteristics and improved therapeutic outcomes.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.5,"publicationDate":"2025-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145030252","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
D-optimal design-based optimization of etoricoxib cubogel for management of arthritis; in vitro and in vivo evaluation. 基于d -最优设计的依托昔布库博凝胶治疗关节炎的优化体外和体内评价。
IF 2.5 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-09-07 DOI: 10.1080/10837450.2025.2556062
Marwa H Abdo, Marwa A Abd El-Fattah, Heba A Eassa, Manal K Darwish
{"title":"D-optimal design-based optimization of etoricoxib cubogel for management of arthritis; in vitro and in vivo evaluation.","authors":"Marwa H Abdo, Marwa A Abd El-Fattah, Heba A Eassa, Manal K Darwish","doi":"10.1080/10837450.2025.2556062","DOIUrl":"10.1080/10837450.2025.2556062","url":null,"abstract":"<p><p>Etoricoxib (Et) is selective COX-2 inhibitor with several drawbacks after oral administration. Current study focused on formulating targeted Et cubogel for osteoarthritis management. Interaction between formulation factors; (glyceryl-monooleate (GMO) and Poloxamer407 (Px)) concentrations and process parameters (melting/solvent-evaporation preparation methods) was investigated using D-optimal design. Considered levels were 3, 5 and 7% for GMO and 0.5,0.75 and 1% for Px. Effect of selected variables on particle size (PS) and entrapment efficiency (EE) of Et cubosomes was studied using Design Expert software. Optimized formulation was studied for zeta potential, TEM, and Et release. Optimum formula was loaded into gel formulations and subjected to physical characterization and in-vitro Et release. Selected cubogel was evaluated for ex-vivo permeation, and anti-inflammatory activity using carrageenan-induced edema model. Optimum formulation (6.5% GMO,1% Px , melting preparation method) had PS of 58.6 ± 0.51 nm, EE of 96.1 ± 1.5%, zeta potential of -26.6 ± 0.66 mV and cubic structure as indicated by TEM. Formulated cubogels had acceptable physical properties with sustained release depending on gelling agent type and concentration. Ex-vivo permeation confirmed higher permeability for Et cubogel than Etgel. Anti-inflammatory study confirmed enhanced (<i>p</i> < 0.05) anti-inflammatory activity of Et cubogel as compared to Et gel. Hence, the present study presents Et cubgel formulation as anti-inflammatory remedy.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-14"},"PeriodicalIF":2.5,"publicationDate":"2025-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144993139","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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