Çiğdem Yücel, Ozgur Esim, Nurgül K Bakırhan, Sevilay Erdoğan Kablan, Engin Koçak, Meryem Sebla Ertuğrul, Cansel Köse Özkan, Emirhan Nemutlu, Ayhan Savaşer, Sibel A Özkan, Yalçın Özkan, Ahmet Rıfat Balık, Taner Özgürtaş
{"title":"Metabolomic profiles altered by erlotinib encapsulated in poly(lactide-co-glycolide) nanoparticles in non-small cell lung cancer.","authors":"Çiğdem Yücel, Ozgur Esim, Nurgül K Bakırhan, Sevilay Erdoğan Kablan, Engin Koçak, Meryem Sebla Ertuğrul, Cansel Köse Özkan, Emirhan Nemutlu, Ayhan Savaşer, Sibel A Özkan, Yalçın Özkan, Ahmet Rıfat Balık, Taner Özgürtaş","doi":"10.1080/03639045.2025.2484326","DOIUrl":"10.1080/03639045.2025.2484326","url":null,"abstract":"<p><strong>Objective: </strong>This research is focused on the metabolomics and cytotoxic effects of the anticancer drug erlotinib encapsulated in poly(lactide-co-glycolide) nanoparticles on non-small cell lung cancer (NSCLC) cell lines.</p><p><strong>Methods: </strong>Uniform-sized nanoparticles (0.325 and 0.068 PDI) with mean diameters of 264.5 and 268.4 nm for blank and erlotinib-PLGA nanoparticles (nanodrugs-NDs) were formulated, respectively. The encapsulation efficiency of prepared nanoparticles was found to be 90.1%. 36% of erlotinib was released from PLGA nanoparticles within 24 h, and the maximum sustained release was 43% at 72 h. The metabolomic and cytotoxic effects of ND were evaluated.</p><p><strong>Results: </strong>The Bax/Bcl-2 ratio was the lowest in the nanodrug group at 72 h, showing increased apoptosis, indicating that the most effective drug formulation is the combined nanoparticle at 72 h. The metabolomic studies revealed changing amino acids, antioxidant molecules, and carbohydrate profiles. The most significant changes were obtained in pathways related to the synthesis of p-glycoprotein, which is the principal protein for drug efflux and causes drug resistance. The lowest levels of amino acids and polyamines like serine, threonine, spermine, and spermidine were obtained at 72 h with erlotinib encapsulated in poly(lactide-co-glycolide) (PLGA) nanoparticles, showing that the drug resistance may in part be overcome with this nanoparticles.</p><p><strong>Conclusion: </strong>The encapsulation of erlotinib with PLGA showed effects and influenced critical metabolic pathways, especially pointing out the need to lower drug resistance and signifying it's potential use as an effective treatment strategy for NSCLC.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143691506","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}
{"title":"Nanoparticle-based delivery systems for phytochemicals in cancer therapy: molecular mechanisms, clinical evidence, and emerging trends.","authors":"Mahmoud A H Mostafa, Hani M J Khojah","doi":"10.1080/03639045.2025.2483425","DOIUrl":"10.1080/03639045.2025.2483425","url":null,"abstract":"<p><strong>Objective: </strong>This review examines recent advancements in nanoparticle-based delivery systems for phytochemicals, focusing on their role in overcoming multidrug resistance, improving therapeutic efficacy, and facilitating clinical translation.</p><p><strong>Significance: </strong>This review highlights recent advances in nanoparticle-enabled phytochemical delivery to enhance bioavailability, improve therapeutic outcomes, and enable targeted applications. By comparing various nanoparticle systems, formulation methods, and efficacy data, it identifies gaps in current research and guides the development of more effective, next-generation phytochemical-loaded nanocarriers.</p><p><strong>Methods: </strong>A systematic review of literature published between 2000 and 2024 was conducted using PubMed, Scopus, and Web of Science. Articles focusing on nanoparticle-based phytochemical delivery in cancer therapy were included.</p><p><strong>Key findings: </strong>Compounds such as curcumin, resveratrol, quercetin, and epigallocatechin gallate demonstrate enhanced anti-cancer efficacy when encapsulated in nanoparticles, leading to improved bioavailability, increased tumor cell targeting, and reduced toxicity. Clinical trials indicate tumor regression and fewer adverse effects. Emerging approaches-such as nanogels, hybrid nanoparticles, and combination therapies with immune checkpoint inhibitors-further refine treatment efficacy.</p><p><strong>Conclusions: </strong>Nanoparticle-based delivery systems significantly improve the therapeutic potential of phytochemicals, making them promising candidates for safer, more effective cancer treatments. However, challenges related to regulatory guidelines, scalability, and long-term safety must be addressed to fully realize their clinical potential.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-17"},"PeriodicalIF":2.4,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143673477","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}
Shimaa Mazyed, Soha M El-Masry, Haidy Abbas, Mohammad M Abd-Alhaseeb, Heba M Elbedaiwy
{"title":"Gliclazide loaded spanlastic nanovesicles: empowering bioavailability and antidiabetic efficacy.","authors":"Shimaa Mazyed, Soha M El-Masry, Haidy Abbas, Mohammad M Abd-Alhaseeb, Heba M Elbedaiwy","doi":"10.1080/03639045.2025.2480183","DOIUrl":"10.1080/03639045.2025.2480183","url":null,"abstract":"<p><strong>Objective: </strong>This work aimed to prepare spanlastics nanovesicles (SNVs) loaded with gliclazide (GCZ) to increase the drug's oral bioavailability and anti-diabetic effects.</p><p><strong>Methods: </strong>Two types of edge activators (tween 80 and/or brij35) and two types of spans (span 60 and span 80) were used to prepare SNVs using the ethanol injection method,2<sup>3</sup> factorial design was used to investigate the effects of various span types, edge activator types, and the ratio of span to edge activator.</p><p><strong>Results: </strong>The optimum formulation (F6) was selected and its <i>in-vitro</i> drug release, <i>in-vivo</i> pharmacokinetics, and pharmacodynamics were evaluated. A transition electron microscope (TEM) showed spherical particles with smooth surfaces, (F6) drug release was (Q<sub>12</sub> 97.05 ± 4.85) while GCZ powder was (97.89 ± 4.56 after 4 h) also showed better entrapment efficiency (EE% 95.1 ± 3.8). <i>In- vivo</i> pharmacokinetic study showed an increase in C<sub>max</sub> and t<sub>max</sub> (12.93 ± 1.34, 3.2 ± 0.83) compared to unprocessed GCZ powder (2.88 ± 1.59, 1.8 ± 0.74). <i>In-vivo</i> pharmacodynamics study of diabetic rats demonstrated that GCZ-loaded SNVs has a higher % maximum decrease in blood glucose levels (MR) 58.31 ± 5.70 compared to 38.33 ± 8.18 for free drug and % total drop in blood glucose levels (TD) 25.78 ± 5.31% for GCZ-SNVs compared to 20.26 ± 6.05% for free drug. Histopathological examination revealed no cytotoxic signs in any of the examined samples.</p><p><strong>Conclusion: </strong>Results revealed a significant rise in relative bioavailability, sustained and prolonged drug release when compared to the unprocessed GCZ powder.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2025-03-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143647552","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}
{"title":"Formation of self-assembled polyelectrolyte complex derived from BSA and nanogels: a study to optimize processing parameters and preserve protein integrity.","authors":"Jahanzeb Mudassir, Aamir Jalil, Khizar Abbas, Yusrida Darwis","doi":"10.1080/03639045.2025.2479758","DOIUrl":"10.1080/03639045.2025.2479758","url":null,"abstract":"<p><strong>Objective: </strong>The aim of this work was to identify, optimize, and use nondestructive process to develop nano-formulation using polyelectrolyte complexation (PEC) between polymeric nanocarrier and bovine serum albumin.</p><p><strong>Significance: </strong>Proteins are mostly degraded during preparation and loading into nano-carriers which hinders success in protein delivery.</p><p><strong>Method: </strong>Herein, novel PEC consisting of model protein BSA and nanogels (NGs), were prepared to form self-assembled polyelectrolyte nanocomplexes <b>(</b>BSA/NGs-PEC). The BSA/NGs-PEC were obtained by mixing BSA and nanogels at various weight ratios (1:2, 1:4, 1:5, 1:6, 1:8, 1:10), pH values of solution (1.2, 4.0, 6.0), incubation time (2, 4, 6, 8 h), and stirring rate (without, 100, 200 rpm). The prepared PEC were evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and percentage of complexation efficiency (%CE). To study insights into structural integrity and biological activity, the SDS-PAGE and esterase activity assay was performed on BSA released from final optimized formulation.</p><p><strong>Results: </strong>The optimized parameters were BSA/nanogels mixing ratios at 1:8, pH of complex-forming medium at 4.0, incubation time of 6 h, and stirring rate at 100 rpm. The SDS-PAGE and esterase activity assay revealed that the primary structure and bioactivity, respectively, of BSA was still intact.</p><p><strong>Conclusion: </strong>The results suggest that current scheme for optimization has considerable potential for creating protein-based delivery system by using PEC <i>via</i> electrostatic interaction.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2025-03-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143656401","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}
{"title":"Glimepiride/hydroxypropyl-β-cyclodextrin inclusion compound: preparation, characterization, and evaluation.","authors":"Xin Quan, Shurui Wang, Jiamin Lu, Xingyi Zhu, Yunfen Hua","doi":"10.1080/03639045.2025.2479748","DOIUrl":"10.1080/03639045.2025.2479748","url":null,"abstract":"<p><strong>Objective: </strong>To enhance solubility and bioavailability of GM, an inclusion compound of glimepiride/hydroxypropyl-β-cyclodextrin (GM/HP-β-CD) was prepared using mechanical ball milling.</p><p><strong>Significance: </strong>Based on response surface optimization for the ball milling preparation of the inclusion compound, this study investigates its <i>in vitro</i> and <i>in vivo</i> release and pharmacokinetics.</p><p><strong>Methods: </strong>GM/HP-β-CD inclusion compound was prepared by optimized ball milling based on response surface methodology and characterized using powder x-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier transform infrared spectroscopy, and the stability of the compound was studied. In addition, GM/HP-β-CD inclusion compound's <i>in vitro</i> release and <i>in vivo</i> release assays were performed.</p><p><strong>Results: </strong>Optimal ball milling conditions for a 1:1 molar ratio of GM/HP-β-CD were a milling speed of 296 rpm, a milling time of 88 min, and a filling rate of 17.7%. Solubility and dissolution rate experiments indicated that the solubility of the GM/HP-β-CD inclusion compound was 20 times higher than that of GM, and the dissolution rate was 12.7 times faster. Additionally, the thermal stability and photostability of the inclusion compound were improved. <i>In vivo</i> pharmacokinetics and pharmacodynamics studies showed that, compared to GM, the GM/HP-β-CD inclusion compound shortened the T<sub>max</sub> by 1 h, increased the maximum plasma concentration by nearly 3.5 times, and significantly enhanced bioavailability.</p><p><strong>Conclusion: </strong>GM/HP-β-CD inclusion compound demonstrates potential for developing sustained-release formulations, thereby prolonging the hypoglycemic effect of GM, reducing dosing frequency, and improving patient compliance with oral administration.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-11"},"PeriodicalIF":2.4,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143623983","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}
Khadija Rouaz-El-Hajoui, Pilar Pérez-Lozano, Àlex Fraschi-Nieto, Xavier Mula-Roldán, Marc Suñé-Pou, Blanca Chiclana-Rodríguez, Josep María Suñé-Negre, Encarnación García-Montoya
{"title":"Optimization of the manufacturing process of a pediatric omeprazole enteric pellets suspension: Full Factorial Design.","authors":"Khadija Rouaz-El-Hajoui, Pilar Pérez-Lozano, Àlex Fraschi-Nieto, Xavier Mula-Roldán, Marc Suñé-Pou, Blanca Chiclana-Rodríguez, Josep María Suñé-Negre, Encarnación García-Montoya","doi":"10.1080/03639045.2025.2476651","DOIUrl":"10.1080/03639045.2025.2476651","url":null,"abstract":"<p><strong>Objective: </strong>The purpose of the present study was to apply the design of experiments (DoE) to develop an omeprazole enteric pellets suspension for use in the pediatric population.</p><p><strong>Methodology: </strong>This experimental study employed a Full Factorial Design for drug development, encompassing three factors (Aerosil<sup>®</sup> R972, cetostearyl alcohol, and Span 80) at two levels (2% and 6% for factor A (Aerosil<sup>®</sup> R972) and 2% and 4% for factors B and C (cetostearyl alcohol and Span 80, respectively)).</p><p><strong>Results: </strong>Following the statistical optimization, the suspension F10 was formulated and subjected to a stability study for one month. The dissolution test results were suboptimal, achieving only an 22% release. Subsequently, eight additional suspensions were devised using hydrophilic oily vehicles (Labraphac Hydrophile WL 1219, Labrafil M2125 CS, and Labrafil M 1944 CS) and excipients (Gelucire 44/14 and Aerosil<sup>®</sup> 200) to enhance the dissolution profile. Suspension F17 showed over 75% within 30 min, displaying superior sedimentation time when compared to all other formulations, along with effortless resuspension.</p><p><strong>Conclusion: </strong>The findings suggest that the optimal vehicle for the administration of omeprazole enteric pellets in suspension is the formulation comprising Labrafil M 1944 CS, Span 80, and Aerosil<sup>®</sup> 200. This study has paved the way for an oily suspension vehicle, opening new avenues of research for developing pediatric omeprazole formulations that fulfill gastro-resistance requirements.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-12"},"PeriodicalIF":2.4,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143566306","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}
{"title":"Optimization and assessment of three generation solid dispersion for enhancement of solubility and dissolution for montelukast sodium.","authors":"Kirti Rashmi, Kaushiki Ash, Abhimanyu Dev","doi":"10.1080/03639045.2025.2477722","DOIUrl":"10.1080/03639045.2025.2477722","url":null,"abstract":"<p><strong>Objective: </strong>To enhance the solubility of Montelukast sodium using three generation polymers by solid dispersion method.</p><p><strong>Material and method: </strong>Montelukast sodium with selected generation of carriers were used for phase solubility and to optimize the stoichiometric ratio for the preparation of SD with MS. Various characterization techniques (FTIR, DSC and XRD) have been used to evaluate the MS-SD formulations with selected hydrophilic carriers. Dissolution and stability study were also investigated.</p><p><strong>Result and discussion: </strong>The two best-selected formulations (MS-PVP & MS-HPMC SD) have shown the highest dissolution profile as compared to pure drug, physical mixture and commercially available marketed product (Montel-10, Cipla). The FTIR, DSC and XRD results of these SD formulations have shown interaction between drug and polymers, decrease in enthalpy compared to the drug and amorphous behavior respectively. Finally, MS-PVP & MS-HPMC SD formulations have shown good stability for one-month period under accelerated storage condition.</p><p><strong>Conclusion: </strong>The study showed increase in solubility of Montelukast sodium with second generation polymers (PVP & HPMC) in comparison to pure drug as well as marketed formulation.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143584908","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}
Jasmine Southward, Fang Liu, Sam R Aspinall, Tochukwu C Okwuosa
{"title":"Exploring the potential of mucoadhesive buccal films in geriatric medicine.","authors":"Jasmine Southward, Fang Liu, Sam R Aspinall, Tochukwu C Okwuosa","doi":"10.1080/03639045.2025.2467329","DOIUrl":"10.1080/03639045.2025.2467329","url":null,"abstract":"<p><p>As the global demographic shifts toward an aging society, the geriatric patient population is steadily increasing. These patients often suffer from comorbidities and require numerous oral medications, which can be especially challenging for dysphagic geriatric patients. Mucoadhesive buccal films (MBFs) seem promising and could reduce pill burden, simplify administration, and enable individualized drug therapy. This review aims to explore the age-related changes in the oral cavity and their impact on MBF delivery, including potential strategies to overcome these age-related barriers to drug delivery. It was observed that aging impacts the oral mucosa as well the properties of the saliva. There are several studies in the application of buccal films including the use of a wide range of permeation enhancers. The 3D printing of buccal films seems to introduce dosing flexibility to buccal film manufacturing.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-21"},"PeriodicalIF":2.4,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143440121","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}
Muzzamil Ilyas, Asim Ur Rehman, Muhammad Tayyab, Marya Nawaz Malik, Naveed Ahmed, Humaira Fatima
{"title":"Box-Behnken based furosemide-nanostructured lipid carriers (NLCs) delivery system for improving oral bioavailability.","authors":"Muzzamil Ilyas, Asim Ur Rehman, Muhammad Tayyab, Marya Nawaz Malik, Naveed Ahmed, Humaira Fatima","doi":"10.1080/03639045.2025.2460062","DOIUrl":"10.1080/03639045.2025.2460062","url":null,"abstract":"<p><strong>Objective: </strong>The fabrication of furosemide (FSM) with enhanced oral bioavailability and encapsulation was achieved using a nanostructured lipid carriers (NLCs) drug delivery system.</p><p><strong>Significance: </strong>The uniform drug distribution is a barrier due to its low dose. The lipid-based delivery system was selected based on its poor solubility and permeability, limiting its poor partitioning and solubility in water-based polymeric delivery systems. The lipophilicity of the FSM makes it favorable to partition with triglyceride-based Compritol 888 ATO and oleic acid with minimized drug expulsion, high drug payload, and sustained release over extended time frames.</p><p><strong>Methods: </strong>The Organic and aqueous phases of the microemulsion were stabilized using Tween 80, a hydrophilic surfactant. Box-Behnken design-based optimization was done using alteration in various formulation variables to obtain nano-formulation with the lowest particle size and polydispersity, maximal zeta potential and entrapment efficiency.</p><p><strong>Results: </strong>Design-Expert yielded several optimized formulations with the desirability function. Maximum desirability was obtained at a particle size of around 178 nm, a surface charge of -19.6 mV, and an EE of above 85%.The <i>in vitro</i> release profile depicted 86.5% of cumulative release after 24 h whereas, <i>in vivo</i> pharmacokinetic study revealed an increase in C<sub>max</sub> from 0.48 µg/mL (FSM-Suspension) to 0.77 µg/mL (FSM NLCs) to increase the bioavailability to approx. 241% in FSM NLCs. The half-life escalation demonstrated that the residence time of the nanoparticles prolonged at the physiologic pH.</p><p><strong>Conclusions: </strong>FSM-NLCs exhibited sustained release over a prolonged period, improved residence time in the body, and their action was prolonged.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"219-230"},"PeriodicalIF":2.4,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143051647","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}
{"title":"Central composite design (CCD) based formulation, optimization, <i>in-vitro</i> and <i>ex-vivo</i> characterization of 5-fluorouracil-loaded emulgel for enhanced dermal penetration and psoriasis management.","authors":"Simran Parhi, Naureen Afrose, Kavitha Rajendran, Damodharan Narayanasamy","doi":"10.1080/03639045.2025.2464782","DOIUrl":"10.1080/03639045.2025.2464782","url":null,"abstract":"<p><strong>Objective: </strong>Psoriasis is a condition that mostly responds to topical remedies. 5-FU is promising since it is anti-proliferative but has poor permeability. The study aimed to fabricate a novel 5-FU emulgel in order to accomplish enhanced therapy of psoriasis.</p><p><strong>Methods: </strong>A central composite design (CCD) was employed to optimize the emulgel's key characteristics, including viscosity, spreadability, drug content, and <i>in-vitro</i> release profile. This statistical approach utilized a five-level, two-factor model to construct linear and quadratic relationships between the formulation variables and the desired responses. Design-Expert software version 13 facilitated this process, requiring 13 experimental runs (FU1-FU13) to achieve optimal formulation parameters. The emulgel consisted of an oil phase (oleic acid, Span 80, and Transcutol P) and an aqueous phase (5-FU and Tween 80). High shear homogenization was utilized for emulsification. The emulsion and gel were combined in a 1:1 ratio to form the emulgel. Finally, the optimized emulgel (FU13) underwent assessments for drug-excipient compatibility, <i>ex-vivo</i> drug permeability through the skin barrier, and long-term stability.</p><p><strong>Results: </strong>The results of optimized formulation FU13 showed viscosity of 5166 ± 9.01 Pa.s, spreadability of 27.56 ± 2.69 g.cm/s, extrudability of 28.49 ± 2.25 g/cm, drug content of 87.9 ± 3.16%, <i>in-vitro</i> drug release of 96.4 ± 1.25 up to 360 min and <i>ex-vivo</i> cumulative permeability of 1056.97 ± 10.33 µg/cm<sup>2</sup>. FU13 showed no significant chemical interactions and was stable throughout stability period.</p><p><strong>Conclusion: </strong>It is within this context that the present study appears to possess significant potential for topical treatment of psoriasis, as it provides higher therapeutic gain over current treatment modalities with fewer undesired effects.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"244-261"},"PeriodicalIF":2.4,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143390350","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}