Pharmaceutical Development and Technology最新文献_第4页

Nanoparticles co-loaded with sorafenib and emodin: preparation and efficacy against liver cancer in vitro and in vivo. 索拉非尼和大黄素共载纳米颗粒：体外和体内抗肝癌的制备和疗效。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-21 DOI: 10.1080/10837450.2025.2489743

Yichun Jiang, Qiulan Li, Yan Chen, Xiaoshi Zhou, Yunzhong Luo, Tong Qiu, Zhen Meng, Xue Ying, Min Wu

{"title":"Nanoparticles co-loaded with sorafenib and emodin: preparation and efficacy against liver cancer in vitro and in vivo.","authors":"Yichun Jiang, Qiulan Li, Yan Chen, Xiaoshi Zhou, Yunzhong Luo, Tong Qiu, Zhen Meng, Xue Ying, Min Wu","doi":"10.1080/10837450.2025.2489743","DOIUrl":"10.1080/10837450.2025.2489743","url":null,"abstract":"Liver cancer is common worldwide and associated with relatively high mortality. Sorafenib is a first-line treatment for advanced liver cancer, but its efficacy is limited by its high toxicity, wide distribution in the body and low water solubility. Combination therapy with multiple drugs can lead to greater therapeutic efficacy, and nano-delivery systems can facilitate such therapy by solubilizing drugs and thereby increasing their bioavailability. Here nanoparticles of sorafenib and emodin encapsulated in the copolymer PEG-PLGA were constructed for liver therapy. Nanoparticles carrying sorafenib and emodin were prepared using a double emulsion method, and showed a diameter around 290 nm and uniform morphology. The encapsulation rates of sorafenib and emodin were 77.4 ± 0.71% and 80.78 ± 0.05%, the drug loading rates were 12.0 ± 0.1% and 13.0 ± 0.21%, and the cumulative drug release rates in pH 5.0 medium were 83.6% and 80.2%. The dual-loaded nanoparticles demonstrated significantly suppressed cellular proliferation and markedly enhanced apoptotic induction compared to free drug formulations or monotherapy nanoparticles. In murine xenograft models, the nanoparticles achieved superior tumor growth suppression (p < 0.01 vs free drugs). These findings collectively indicate that the sorafenib-emodin co-encapsulated PEG-PLGA nanoparticles represent a promising therapeutic platform for hepatocellular carcinoma intervention and may provide more therapeutic options against advanced liver cancer.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"450-462"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144049779","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 skin penetration and clinical antifungal activity of eugenol encapsulated in aspasomes. 丁香酚包封在Aspasomes中增强皮肤渗透和临床抗真菌活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-07 DOI: 10.1080/10837450.2025.2486808

Muhammad Salah Eleleemy, Maha H Ragaie, Basma Hamdy Amin, Maha Nasr, Omaima A Sammour

{"title":"Enhanced skin penetration and clinical antifungal activity of eugenol encapsulated in aspasomes.","authors":"Muhammad Salah Eleleemy, Maha H Ragaie, Basma Hamdy Amin, Maha Nasr, Omaima A Sammour","doi":"10.1080/10837450.2025.2486808","DOIUrl":"10.1080/10837450.2025.2486808","url":null,"abstract":"Fungal infections are among the common diseases affecting the skin, which necessitate either topical or systemic delivery of antifungal agents. Eugenol was reported to exhibit antifungal properties, but owing to its poor skin-penetration ability, it requires encapsulation within delivery carriers. This study aimed to enhance the skin penetration and antifungal efficacy of eugenol through encapsulation in novel aspasomal formulations. Cationic and anionic aspasomes were prepared using ascorbyl palmitate, transcutol, and charge inducers, achieving high encapsulation efficiencies (90.55% for cationic, 63.32% for anionic) and stable formulations. Ex-vivo skin deposition studies showed significant eugenol retention in deeper skin layers, with 82.2% (cationic) and 77.2% (anionic) total skin deposition. Both formulations demonstrated superior antifungal activity compared to eugenol solution, with larger zones of inhibition against Candida albicans and Trichophyton rubrum. Clinical trials in patients with candidiasis and dermatophytosis revealed complete resolution of symptoms in 100% of patients treated with aspasomes, while eugenol solution showed partial improvement. These findings suggest that aspasomal encapsulation significantly enhances eugenol's therapeutic potential, offering a promising strategy for improving the treatment of fungal skin infections.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"372-384"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143753850","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

Chitosan nanoparticle encapsulation of thymus capitatus essential oil: in vitro release, antioxidant, antibacterial activity and cytotoxicity in MDA-MB-231 cells. 壳聚糖纳米颗粒包封胸腺精油：体外释放、抗氧化、抗菌活性及MDA-MB-231细胞毒性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-08 DOI: 10.1080/10837450.2025.2487255

Huseyin Beyaz, Doga Kavaz, Nahit Rizaner

{"title":"Chitosan nanoparticle encapsulation of thymus capitatus essential oil: in vitro release, antioxidant, antibacterial activity and cytotoxicity in MDA-MB-231 cells.","authors":"Huseyin Beyaz, Doga Kavaz, Nahit Rizaner","doi":"10.1080/10837450.2025.2487255","DOIUrl":"10.1080/10837450.2025.2487255","url":null,"abstract":"Thymus capitatus (Th. Ca) is known to treat mouth ulcers and respiratory infections in Cyprus. However, antioxidant, antibacterial, and cytotoxic potential of Th. Ca. EO on MDA-MB-231 cells and its' encapsulation into nanoparticles has not been well studied. Therefore, we aimed to analyze the antioxidant, antibacterial, cytotoxic potential, loading efficiency, and in vitro release profile of both Th. Ca. EO and Chitosan Nanoparticle (Ch. Np) - Th. Ca. EO. GC-MS analysis revealed 53.97% carvacrol, 14.53% borneol, and 12.09% sabinene presence in EO. The loading efficiency of Th. Ca. EO into Ch. Np. was calculated as 35.27% and the in vitro release profile reached a maximum of 68% in pH 7 for two weeks. The Minimum Inhibitory Concentration (MIC) assay showed that E. coli had an MIC50 of 0.3215 mg/ml while B. subtilis had an MIC50 of 0.5304 mg/ml. The antioxidant activity of the EO was assessed by performing a DPPH assay with an IC50 = 440 μg/ml. Trypan Blue Assay revealed that 60 µg/ml Th. Ca. EO significantly reduced the cell viability of MDA-MB-231 cells by 10.7% at 48h and 20.06% at 72h. Overall, Ch. Np. - Th. Ca. EO has shown a promising formulation for the pharmaceutical industry.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"385-399"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143753920","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

Mucoadhesive polymeric film with plant-based compounds for dental applications: formulation, characterization and evaluation. 牙科用植物基聚合物粘接膜：配方、表征和评价。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-05-05 DOI: 10.1080/10837450.2025.2498368

Yuliia Maslii, Nataliia Herbina, Lina Dene, Liudas Ivanauskas, Gintaras Matulis, Jurga Bernatoniene

{"title":"Mucoadhesive polymeric film with plant-based compounds for dental applications: formulation, characterization and evaluation.","authors":"Yuliia Maslii, Nataliia Herbina, Lina Dene, Liudas Ivanauskas, Gintaras Matulis, Jurga Bernatoniene","doi":"10.1080/10837450.2025.2498368","DOIUrl":"10.1080/10837450.2025.2498368","url":null,"abstract":"Polymeric films are promising formulations for oromucosal drug delivery, particularly for localized treatment of dental diseases. This study focused on developing mucoadhesive films for dental applications, incorporating clove CO2 extract and essential oils of lavender and grapefruit as active ingredients. The films were prepared using the solvent casting method, with various film-forming agents (sodium alginate, sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl alcohol) used individually and in combinations, without or with plasticizers (glycerol, polyethylene glycol 400, or their mixtures). To optimize the selection of mucoadhesive polymer and plasticizer, properties such as appearance, thickness, pH, moisture content, bursting strength, tensile capacity, elasticity, dissolution, and adhesion, were evaluated. The combination of hydroxyethyl cellulose and hydroxypropyl cellulose with polyethylene glycol 400 was proved most suitable, ensuring superior organoleptic, physicochemical, and textural characteristics. The films demonstrated strong mucoadhesion (9.20 ± 0.58 N), contributing prolonged retention on the mucosa and enhanced bioavailability of the active ingredients. In vitro release studies showed sustained release profile, with approximately 90% of eugenol released during the final film dissolution phase (360-420 min), supporting prolonged therapeutic effects and enhanced local therapy efficacy. The films also exhibited significant antimicrobial activity against a broad spectrum of microorganisms, confirming their potential for treating infectious and inflammatory oral diseases.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"505-520"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144023629","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 memantine and donepezil loaded 3D scaffolds. 美金刚和多奈哌齐负载3D支架的设计与表征。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-23 DOI: 10.1080/10837450.2025.2493256

Betül Topçu İnce, Samuel Guieu, Selin Seda Timur, Tuba Reçber, Emirhan Nemutlu, Maria Helena Vaz Fernandes, Hakan Eroğlu

{"title":"Design and characterization of memantine and donepezil loaded 3D scaffolds.","authors":"Betül Topçu İnce, Samuel Guieu, Selin Seda Timur, Tuba Reçber, Emirhan Nemutlu, Maria Helena Vaz Fernandes, Hakan Eroğlu","doi":"10.1080/10837450.2025.2493256","DOIUrl":"10.1080/10837450.2025.2493256","url":null,"abstract":"Memantine HCl (MEM) and Donepezil HCl (DON) are widely used separately and in combination to treat Alzheimer's disease, and some studies suggest that these drugs may also prevent bone fractures and promote bone regeneration. For this purpose, we formulated fiber-based 3D scaffolds for local delivery of MEM/DON to improve the regeneration process of bone fractures. First, Poly (ε-caprolactone) (PCL)-based MEM/DON-loaded nanofibrous membranes were produced by electrospinning, and then these nanofibrous membranes were transformed into 3D scaffolds using the thermally induced self-agglomeration (TISA) method. Encapsulation efficiency after these two steps was found to be around 20%. Analyses confirmed that the 3D scaffolds have a morphology similar to the extracellular matrix, and that their hydrophilicity, swelling ratio, porosity, and degradation rate were adequate for bone tissue regeneration. Release studies show that the scaffolds provide an initial burst release of the drugs, followed by a sustained release for 21 days. These 3D scaffolds did not show any cytotoxic effect on the L-929 cell line, and increased cell viability over time indicates that they can be used in tissue engineering applications.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"488-504"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144030985","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

Evaluating the color stability of titanium dioxide-free film coats under environmental and light stress. 评价无二氧化钛薄膜涂层在环境和光胁迫下的颜色稳定性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-10 DOI: 10.1080/10837450.2025.2489005

Jamie C L Chuvalo-Abraham, David Harris, Hyunho Kang, Chiamaka U Ukachukwu, Catherine Guarino

{"title":"Evaluating the color stability of titanium dioxide-free film coats under environmental and light stress.","authors":"Jamie C L Chuvalo-Abraham, David Harris, Hyunho Kang, Chiamaka U Ukachukwu, Catherine Guarino","doi":"10.1080/10837450.2025.2489005","DOIUrl":"10.1080/10837450.2025.2489005","url":null,"abstract":"Titanium dioxide (TiO2) is an opacifier/colorant in tablet film coatings and capsule shells. Recently, questions about its safety have raised concerns that it may be banned from medicinal products in the European Union (EU); however, little information exists on alternatives to enable the pharmaceutical industry to pivot. This study evaluated the color stability of film coats containing alternate opacifiers, calcium carbonate (CaCO3), and rice starch. Placebo tablets were coated with film coating systems containing different polymers (hydroxypropyl methylcellulose (HPMC) or polyvinyl alcohol (PVA)), opacifiers (CaCO3, rice starch, or TiO2) and pigments (FD&C Blue No. 2, iron oxides, or non-pigmented); the coated tablets were exposed to environmental stress (temperature/humidity) and light stress and color changes were quantified spectrophotometrically. The HPMC-formulated coats containing CaCO3 or rice starch showed comparable stability to TiO2. The PVA-based coats containing FD&C Blue No. 2 or iron oxide colorants exhibited color changes when exposed to elevated temperature/humidity, which was more pronounced with CaCO3 than with TiO2. No meaningful color changes were observed under white or UV light stress for any coat. This study demonstrated PVA coating systems pose a stability risk, whereas these alternate opacifiers presented an overall low color stability risk, offering potential TiO2 alternatives.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"441-449"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143811978","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 and characterization of duloxetine-loaded nanofiber scaffold composed of polyvinyl alcohol and chitosan as wound healing agent, fabricated by electrospinning method. 聚乙烯醇-壳聚糖复合伤口愈合剂负载度洛西汀纳米纤维支架的制备及表征

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-11 DOI: 10.1080/10837450.2025.2486797

Kimiya Pourdehghan, Faraz Najafi, Fatemeh Majdi, Nooshafarin Amani, Nasrin Samadi, Hamid Akbari Javar

{"title":"Preparation and characterization of duloxetine-loaded nanofiber scaffold composed of polyvinyl alcohol and chitosan as wound healing agent, fabricated by electrospinning method.","authors":"Kimiya Pourdehghan, Faraz Najafi, Fatemeh Majdi, Nooshafarin Amani, Nasrin Samadi, Hamid Akbari Javar","doi":"10.1080/10837450.2025.2486797","DOIUrl":"10.1080/10837450.2025.2486797","url":null,"abstract":"Wound is a disruption in the epithelial integrity of the skin or mucosa, which is caused by internal or external pathological processes. In this study, a nanofiber as wound dressing loaded with Duloxetine was produced by electrospinning technique. The diameter of nanofibers containing 20% and 40% Duloxetine was around 236 nm and 272 nm, respectively. Tensile testing results showed that elongation at break percentage soared from 11.5% for drug-free nanofibers to 40.01% for nanofibers containing 40% Duloxetine. All nanofibers had uniform bead-free structure. Contact angle of nanofibers with and without drug was 84.3° and 99.3°, respectively. The drug release profile revealed that after the burst release over the first 8 h, the curve witnessed a slow sustained release for a longer period. The nanofibers had antibacterial activity against gram-positive and gram-negative bacteria and the crosslinked nanofibers with 40% duloxetine had the largest diameter of inhibition zone at roughly 43 mm for Staphylococcus aureus, 40 mm for Escherichia coli, and 30 mm for Pseudomonas aeruginosa. Clinical studies showed that the percentage of wound area reduction was approximately 96.41% for nanofibers containing 40% duloxetine which was higher than positive control containing phenytoin at around 92.24% and also the other group with 20% duloxetine at 81.68%.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"351-371"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143753928","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

Formulation and optimization of glycyrrhetinic acid-modified pH-sensitive curcumin liposomes for anti-hepatocellular carcinoma. 甘草次酸修饰ph敏感型抗肝癌姜黄素脂质体的制备及优化。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-02-13 DOI: 10.1080/10837450.2025.2465549

Jie Wang, Xuemei Gu, Xia Gao, Jing Chen, Zhiyang Lv, Siyu Zhang, Siyu Ni, Fei Shi, Xialin Chen, Liang Cao, Zhenzhong Wang, Wei Xiao

{"title":"Formulation and optimization of glycyrrhetinic acid-modified pH-sensitive curcumin liposomes for anti-hepatocellular carcinoma.","authors":"Jie Wang, Xuemei Gu, Xia Gao, Jing Chen, Zhiyang Lv, Siyu Zhang, Siyu Ni, Fei Shi, Xialin Chen, Liang Cao, Zhenzhong Wang, Wei Xiao","doi":"10.1080/10837450.2025.2465549","DOIUrl":"10.1080/10837450.2025.2465549","url":null,"abstract":"In order to enhance the therapeutic value of curcumin in liver cancer treatment, glycyrrhetinic acid-modified pH-sensitive curcumin liposomes (GA-pH-Lip@Cur) was developed.GA-pH-Lip@Cur was prepared using a thin film dispersion ultrasonication method, and the optimal formulation process was selected through single-factor experiments and a Box-Behnken design-response surface methodology. The liposomes were evaluated for their morphological appearance, particle size, in vitro release at different pH levels, and biocompatibility. The anti-tumor effect of GA-pH-Lip@Cur was assessed using cell viability assays (CCK-8). The in vivo hepatic targeting and anti-liver tumor efficacy of GA-pH-Lip@Cur were evaluated through pharmacokinetic and pharmacological experiments. The results indicated that optimized GA-pH-Lip@Cur exhibited uniform particle size distribution, good stability, pH-sensitive in vitro release with sustained behavior. Compared to conventional liposomes, GA-pH-Lip@Cur showed prolonged average retention time in vivo and significantly increased curcumin distribution in liver tissues, indicating excellent liver targeting. Both in vitro and in vivo evaluations demonstrated the effectiveness of GA-pH-Lip@Cur in inhibiting liver cancer cell proliferation and suppressing liver tumor growth in tumor-bearing mice. In conclusion, GA-pH-Lip@Cur, by leveraging the acidic tumor microenvironment and overexpression of glycyrrhetinic acid receptors in liver cells, encapsulates curcumin to improve its bioavailability, and target its delivery to the liver tumor sites.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"233-245"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399752","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

Ocular polymeric nanomicelles for the posterior eye segment in the management of retinoblastoma: formulation, optimization, in vitro and ex vivo evaluations. 眼后段聚合物纳米胶束治疗视网膜母细胞瘤：配方、优化、体外和离体评估。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-02-23 DOI: 10.1080/10837450.2025.2469321

Mudassir Ansari, Yogesh A Kulkarni, Kavita Singh

{"title":"Ocular polymeric nanomicelles for the posterior eye segment in the management of retinoblastoma: formulation, optimization, in vitro and ex vivo evaluations.","authors":"Mudassir Ansari, Yogesh A Kulkarni, Kavita Singh","doi":"10.1080/10837450.2025.2469321","DOIUrl":"10.1080/10837450.2025.2469321","url":null,"abstract":"The existing study focuses on the development, optimization, and evaluation of sorafenib-loaded polymeric nanomicelles for posterior segment delivery in treating retinoblastoma. The formulation involved adjusting various process and product parameters to create effective drug-loaded polymeric nanomicelles. The particle size, PDI, and zeta potential of optimized formulation were found to be 65.52 ± 1.18 nm, 0.14 ± 0.01, and -3.26 ± 0.66 mV, respectively. The entrapment efficiency and drug release were estimated to be 98.84% ± 0.001 and 99.99% in 6 h, respectively. Additionally, the optimized formulation demonstrated acceptable outcomes for solid-state analysis, osmolality, pH, residual solvent, and morphological properties. After 8 h, the ex vivo transcleral permeation and scleral deposition were 629.05 ± 124.11 ng/cm2 and 4.10 ± 0.54 µg, respectively. Y-79 (human retinoblastoma) cell line study using standard drug, test drug, and optimized formulation revealed anticancer potential at all time points (6, 12, 18, and 24 h) with comparable IC50 values. Furthermore, the optimized formulation exhibited no toxicity on the ARPE-19 (human retinal pigmented epithelium) cell line over 24 h. The optimized formulation was non-irritating to the eye (HET-CAM) and remained stable for 6 months. Thus, drug delivery to the posterior eye segment for the treatment of retinoblastoma appears to be possible with the help of established technology.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"246-258"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143476825","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

Exploring the application of single-step drying in lyophilization of high protein concentration formulations. 探索单步干燥法在高蛋白浓度制剂冻干中的应用

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-03-18 DOI: 10.1080/10837450.2025.2476707

Qi Zeng, Zhaowei Jin, Jeremy Guo

{"title":"Exploring the application of single-step drying in lyophilization of high protein concentration formulations.","authors":"Qi Zeng, Zhaowei Jin, Jeremy Guo","doi":"10.1080/10837450.2025.2476707","DOIUrl":"10.1080/10837450.2025.2476707","url":null,"abstract":"Objectives: Single-step drying integrates sublimation and desorption process in one step. The applicability of single-step drying in high protein concentration formulations with or without viscosity reducers remains to be explored. And drying behavior of single-step drying remains to be monitored.Methods: Firstly, in formulations without viscosity reducers (sucrose and mannitol), the method of single-step drying at shelf temperature (Ts) of 25 °C and chamber pressure (Pc) of 0.3 mbar with aggressive annealing (-3 °C) was tested; secondly, two viscosity reducers (ArgHCl and NaCl) were applied to further explore the application of single-step drying in viscosity reducer-containing formulations; finally, drying behavior of single-step drying was monitored in real time by tunable diode laser absorption spectroscopy(TDLAS).Results: In single-step drying process, significant cycle time reduction (68%) was achieved compared to traditional two-step drying. Good cake appearance was observed in all formulation combinations with comparable pre- and post-lyophilization quality attributes as well as reconstitution time. Three times faster sublimation rate was monitored in single-step drying process compared to traditional two-step drying.Conclusion: Single-step drying was proved to be applicable to high protein concentration formulations with or without viscosity reducers. Significant cycle time reduction in drying process was achieved. Sublimation rate resulted in a more efficient drying cycle as a whole even though an increase of product resistance.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"342-349"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143625508","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