Drug Development and Industrial Pharmacy最新文献

{"title":"Protective effects of oral pharmaceutical solution of fucoxanthin against paracetamol-induced liver injury: modulation of drug-metabolizing enzymes, oxidative stress, and apoptotic pathways in rats.","authors":"Safaa Y Eid, Maimonah F Koshak, Mohamed E Elzubier, Bassem Refaat, Riyad A Almaimani, Mohammad Althubiti, Essam Eldin M Nour Eldin, Nawaf H Alahmadi, Sameer H Fatani, Akhmed Aslam, Elshiekh Babiker Adam Khidir, Ahmed A H Abdellatif, Mahmoud Zaki El-Readi","doi":"10.1080/03639045.2025.2469808","DOIUrl":"10.1080/03639045.2025.2469808","url":null,"abstract":"<p><strong>Background: </strong>Paracetamol (PAC) overdose causes acute liver injury through oxidative stress, inflammation, and apoptosis. While N-acetyl cysteine (NAC) is the standard treatment, fucoxanthin (FUC), a carotenoid from brown seaweed, has shown hepatoprotective effects in animal studies, but its role in PAC toxicity is unclear.</p><p><strong>Objective: </strong>Compared to NAC, this study assessed the hepatoprotective potential of oral FUC solution toward PAC-induced injury to the rat's liver.</p><p><strong>Method: </strong>FUC was formulated as a pharmaceutical solution and characterized <i>via</i> UV-VIS spectroscopy. Six groups of male Wistar rats each contain five animal which are in total 30 rats: negative control (NC), positive control (PC, 2 g/kg PAC), NAC (1200 mg/kg), and three oral FUC doses (100, 200, and 500 mg/kg) for seven days, with PAC administered on day-8. Liver tissues were analyzed for oxidative stress, gene expression, and histology.</p><p><strong>Results: </strong>FUC solution was clear with absorbance at 433 nm. PAC caused 30% mortality (<i>p</i> < .01 vs. others). NAC reduced ALT (56%), AST (78%), ALP (28%), and increased TP by 25% (<i>p</i> < .001 vs. PC). FUC at 500 mg/kg (F500) was superior, reducing ALT (82%), AST (93%), ALP (40%), and increasing TP (35%) (<i>p</i> < .001 vs. NAC). PAC increased oxidative stress, CYP2E1/CYP3A2 expression, apoptosis markers, and suppressed Nrf2/AMPK/AKT1. F500 improved antioxidants, reduced oxidative stress, and apoptosis, enhanced the Nrf2/AMPK pathway, and downregulated CYP2E1/CYP3A2 (<i>p</i> < .01).</p><p><strong>Conclusion: </strong>FUC, particularly at 500 mg/kg, offers significant hepatoprotection against PAC-induced liver injury by modulating drug metabolizing enzymes and enhancing antioxidant defenses, warranting further research.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"332-343"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143482500","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":"Green Synthesis and Biomedical Potential of L-Ascorbic Acid-Stabilized Copper Sulfide Nanoparticles as Antibacterial and Antioxidant Agents.","authors":"Shafiul Haque, Saba Siddiqui, Abdullah Mashraqi, Raju K Mandal, Mohd Wahid, Faraz Ahmad, Bushra Fatima","doi":"10.1080/03639045.2025.2487939","DOIUrl":"https://doi.org/10.1080/03639045.2025.2487939","url":null,"abstract":"<p><strong>Background: </strong>Copper sulfide nanoparticles (CuS NPs) are promising materials for a variety of biomedical applications, particularly as antimicrobial and antioxidant agents. The main objective of this study was to synthesize CuS NPs and evaluate their efficiency as an antioxidant and antibacterial agent.</p><p><strong>Methods: </strong>CuS NPs were prepared in a single step process using L-ascorbic acid as the stabilizing agent. Systematic structural and morphological characterization was performed using standard techniques of X-ray diffraction (XRD), Fourier-transform infrared (FT-IR) spectroscopy, and scanning (SEM) and transmission electron microscopy (TEM). Further, agar well disk-diffusion method was applied for determination of the antibacterial sensitivity and minimum inhibitory concentration (MIC) against multiple pathogenic bacterial strains. The antioxidant potential was evaluated by performing total reduction capability, and nitric oxide (NO) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activities at multiple doses, with L-ascorbate as the reference.</p><p><strong>Results: </strong>The results indicated amorphous nature of the CuS NPs with the size range of 8.17 to 9.63 nm. FI-IR confirmed presence of several bioactive functional groups required for the reduction of copper ions. Additionally, our CuS NPs showed robust antibacterial activities against bacterial species such as <i>Escherichia coli</i> and <i>Staphylococcus aureus</i>) in the agar well diffusion assays, with zone of inhibition values ranging between 21 and 23 mm. CuS NPs also showed potent dose-dependent antioxidant activity.</p><p><strong>Conclusion: </strong>CuS NPs prepared in this study in a cost- and time-efficient manner have excellent antibacterial and antioxidant properties with the potential to be applied for different biomedical applications.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143763373","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":"<i>In vitro</i>, <i>ex vivo</i>, and <i>in vivo</i> studies of celecoxib topical platforms for antimicrobial activity and wound healing: a comparative assessment.","authors":"Priyanka Mundankar, Pankaj Neje, Shubhada Mangrulkar, Pranav Shah, Madhur Kulkarni","doi":"10.1080/03639045.2025.2469805","DOIUrl":"10.1080/03639045.2025.2469805","url":null,"abstract":"<p><strong>Background & rationale: </strong>Celecoxib (CXB), with its anti-inflammatory and recently discovered antibacterial activity, especially against sensitive and methicillin-resistant <i>Staphylococcus aureus (MRSA),</i> could be promising in treating local pain, superficial skin infections, wounds and infected wounds. The study aims to develop and compare commercially scalable topical formulations of CXB to explore their antimicrobial and wound-healing potential.</p><p><strong>Methods: </strong>Carbopol gel, o/w cream, polyethylene glycol (PEG) ointment, and paraffin ointment were selected as the vehicles for the preparation of 3% CXB topical formulations. Appearance, pH, viscosity, spreadability, drug content, stability, <i>in vitro</i> release and permeation, and skin retention studies were performed. Further, antimicrobial assay, <i>in vivo</i> wound-healing and histopathology studies were carried out for each formulation.</p><p><strong>Results: </strong>The formulations had an acceptable appearance, viscosity, spreadability, and drug content. The drug release at 6h was the highest from gel (2428.8ug/cm²), followed by PEG ointment (2230.1ug/cm²), cream (1897.8ug/cm²), and lastly, the paraffin ointment (1217.2ug/cm²). PEG ointment and gel showed the highest skin permeation, whereas cream and gel were better able to retain the drug in the skin. All the formulations exhibited appreciable zones of inhibition against sensitive and the resistant strains of <i>Staphylococcus aureus</i>. PEG ointment exerted a significantly greater (<i>p</i> < 0.001) wound-healing effect. Accelerated stability studies confirmed good physicochemical stability of the formulations.</p><p><strong>Conclusion: </strong>PEG ointment, with its optimal drug release profile, skin permeation ability, and greater wound-healing action, can be considered as a promising topical delivery vehicle for CXB. CXB's antimicrobial potential could further aid in the prevention as well as treatment of wound infection.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"319-331"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143448502","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":"Nanoemulgel mediated enhanced skin curcumin penetration/retention for local treatment of cutaneous leishmaniasis: <i>in vitro</i> and <i>in vivo</i> assessment.","authors":"Shoaib Ur Rehman, Nauman Rahim Khan, Majeed Ullah, Shefaat Ullah Shah, Asim Ur Rehman, Qaisar Jamal, Memuna Ghafoor Shahid, Hassan A Albarqi, Ali Alasiri, Abdulsalam A Alqahtani, Ismail A Walbi","doi":"10.1080/03639045.2025.2473495","DOIUrl":"10.1080/03639045.2025.2473495","url":null,"abstract":"<p><strong>Background: </strong>Skin delivery of a therapeutically effective drug is imperative for local cutaneous leishmaniasis (CL) treatment.</p><p><strong>Objective: </strong>This study aimed to formulate, optimize, and characterize curcumin-loaded nanoemulgel for enhanced skin drug retention to treat CL locally.</p><p><strong>Methods: </strong>Nanoemulsions were prepared by high-speed homogenization, characterized, and optimized for size, PDI, zeta potential, stability, morphology, drug contents, encapsulation efficiency, <i>in vitro</i> drug release, antileishmanial activity, and cell viability. The optimized nanoemulsion (C3) was then incorporated into a carbopol-based gel and evaluated for pH, viscosity, spreadability, and <i>in vitro</i> drug release. Both formulations were then assessed for <i>ex-vivo</i> and <i>in vivo</i> skin permeation/retention, and pharmacokinetic analysis.</p><p><strong>Results: </strong>All nanoemulsion formulations had size in nano range with negative surface charge, homogeneously distributed, with spherical droplet geometries, where C3 being highly stable, had good encapsulation efficiency and drug contents (85 ± 5.4 and 68 ± 3.2%), released 90% of drug within 4 h, while C3 gel released the drug significantly sustained up to 46% in 24 h. The C3 formulation demonstrated significant <i>in vitro</i> antileishmanial activity across all tested concentrations, while the IC₅₀ value against NIH3T3 fibroblasts was 0.6202 mM (Log IC₅₀: 2.7, <i>R</i>²: 0.98). The C3 gel showed significantly low skin permeation (341.7 ± 43.6 and 52.6 ± 8.9 µg) with significantly higher skin drug retention (129.5 ± 16.7 and 190.2 ± 33.4 µg) <i>ex-vivo</i> and <i>in vivo</i>, with significantly lower <i>C</i>_max, AUC_0-<i>_t</i>, and AUC_0-∞.</p><p><strong>Conclusion: </strong>These results suggested that curcumin nanoemulgel could be an effective alternative strategy for treating CL locally.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"354-364"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143531279","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":"Improved pharmacokinetic parameters and reduced tissue distribution of prodrug of triamcinolone acetonide in lipid nanospheres - a preliminary investigation.","authors":"Siddharth Maity, Amisha Vora, Ashish M Kanhed, Ambikanandan Misra, Sarika Wairkar","doi":"10.1080/03639045.2025.2475333","DOIUrl":"10.1080/03639045.2025.2475333","url":null,"abstract":"<p><strong>Objective: </strong>In the current research work, we synthesized triamcinolone acetonide palmitate (TAP), a lipophilic prodrug of triamcinolone acetonide (TA) and formulated it into lipid nanospheres (TAP-LN) to improve pharmacokinetics and tissue distribution on intravenous administration.</p><p><strong>Significance: </strong>Triamcinolone acetonide is a parenteral glucocorticoid used to treat several inflammatory disorders. It has a short plasma half-life (2-3 h) and its parenteral administration causes severe side effects.</p><p><strong>Methods: </strong>-TAP-LNs were composed of soy lecithin, soybean oil, Miglyol 812N as a lipid phase and poloxamer 188 and glycerol in distilled water as an aqueous phase. The coarse emulsion was subjected to probe sonication followed by a microfluidizer by applying 20,000 psi pressure with 10 cycles. Similarly, TAP-lipid microspheres (TAP-LMs) were prepared for comparative study without microfluidization.</p><p><strong>Results: </strong>The optimized TAP-LN exhibited a size of 106.8 nm, zeta potential of -45.7 mV, and entrapment efficiency of 82.35%. A pharmacokinetic study showed that in rats, TAP-LN exhibited a 4.5-fold plasma concentration and 10-fold AUC_0-<i>_t</i> than TAP-LMs. The slow clearance of TAP-LN could be associated with lower uptake by eliminating organs that eventually increased the residence time. In the spleen, TAP-LM concentrations were higher than TAP-LN; TAP-LN could not be detected in the liver, unlike TAP-LM, attributing to the carboxylesterase lipase, the metabolizing enzyme responsible for the conversion of TAP to TA.</p><p><strong>Conclusion: </strong>Thus, TAP nanospheres showed improved pharmacokinetic parameters and reduced tissue distribution, which would benefit the intravenous treatment of this glucocorticoid.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"375-383"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143556107","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":"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}

{"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,2³ 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 (Q₁₂ 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_max and t_max (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_max 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}