Drug Development and Industrial Pharmacy最新文献

{"title":"Advancements in nanotechnology for targeted drug delivery in idiopathic pulmonary fibrosis: a focus on solid lipid nanoparticles and nanostructured lipid carriers.","authors":"Suriya Prakaash K K, Damodharan Narayansamy","doi":"10.1080/03639045.2025.2468811","DOIUrl":"10.1080/03639045.2025.2468811","url":null,"abstract":"<p><strong>Objective: </strong>This review aims to explore innovative therapeutic strategies, with a particular focus on recent advancements in drug delivery systems using bioinspired nanomaterials such as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for the idiopathic pulmonary fibrosis (IPF).</p><p><strong>Significance of the review: </strong>Current treatments for IPF, including the FDA-approved anti-fibrotic agents pirfenidone and nintedanib, primarily aim to slow disease progression rather than reverse fibrosis. Bioinspired nanomaterials like SLNs and NLCs have shown promise in enhancing the efficacy of anti-fibrotic agents by improving drug solubility, stability, and targeted delivery. These systems not only minimize systemic side effects but also maximize therapeutic impact in lung tissues, offering a new hope for improved patient management and outcomes in this debilitating disease.</p><p><strong>Key findings: </strong>SLNs facilitate sustained drug release and have demonstrated potential in delivering phosphodiesterase type 5 inhibitors effectively to lung cells. NLCs, on the other hand, exhibit superior biocompatibility and controlled release properties, making them suitable for pulmonary applications. Studies indicate that both SLNs and NLCs can enhance the bioavailability of drugs like ciprofloxacin and montelukast, thereby improving treatment outcomes in pulmonary conditions.</p><p><strong>Conclusion: </strong>The integration of nanotechnology into anti-fibrotic therapy represents a significant advancement in addressing the challenges posed by IPF. By leveraging the unique properties of SLNs and NLCs, there is potential to overcome the limitations of current treatments and provide new therapeutic options that offer better management and improved outcomes for patients suffering from this debilitating disease.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"285-294"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143440108","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":"A novel synthetic approach for the piperazynyl pyrimidine intermediate: focus on the cost cutting of buspirone drug at commercial level.","authors":"Anjan Kumar Nayak, Divya Bajpai Tripathy, Dhananjay Pendharkar, Vijay Kumar Sharma, Gaurav Sharma","doi":"10.1080/03639045.2025.2473505","DOIUrl":"10.1080/03639045.2025.2473505","url":null,"abstract":"<p><strong>Background: </strong>Buspirone is a critical in treatment for generalized anxiety disorder (GAD), but the synthesis of its key intermediate, 2-(piperazin-1-yl) pyrimidine faces challenges in terms of cost, yield and purity. Traditional synthesis methods are hindered by high material costs and significant by-product formation, necessitating a more efficient and economical approach.</p><p><strong>Objective: </strong>To develop a novel, cost-effective synthesis strategy for the 2-(piperazin-1-yl) pyrimidine intermediate that improves yield and purity while reducing production costs and environmental impact.</p><p><strong>Methods: </strong>A four-step synthesis process was optimized as follows: First, piperazine reacts with sulfuric acid and cyanamide, followed by precipitation with cold methanol. Next, 1,1,3,3-tetramethoxypropane reacts with hydrochloric acid and amidine, and the mixture was extracted with dichloromethane (DCM). In the third step, the product was dissolved in isopropanol (IPA), treated with charcoal and converted to the oxalate salt using oxalic acid. Finally, the oxalate salt was converted to the freebase with ammonia, followed by a final extraction with DCM. Key variables such as reagent equivalents, reaction conditions and purification techniques were systematically optimized throughout the process.</p><p><strong>Results: </strong>The optimized process achieved a purity level of over 99% and reduced production costs by 25-30%. Significant improvements included controlled bis-product formation with cyanamide, effective addition of 1,1,3,3-tetramethoxypropane and efficient removal of by-products through oxalate salt formation and charcoal treatment.</p><p><strong>Conclusion: </strong>The developed synthesis method for 2-(piperazin-1-yl) pyrimidine was both cost-effective and efficient, significantly enhancing the yield and purity. This method is highly suitable for large-scale pharmaceutical production, aligning with industry goals of improved process efficiency, cost reduction and environmental sustainability.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"365-374"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143540528","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":"Preformulation studies and <i>in vitro</i> cytotoxicity of naringin.","authors":"A Gaitán, S Ravetti, A G Garro, M Bonaterra, R V Alasino, S D Palma","doi":"10.1080/03639045.2025.2471912","DOIUrl":"10.1080/03639045.2025.2471912","url":null,"abstract":"<p><strong>Objective: </strong>This study evaluates the chemical and enzymatic stability of naringin (NRG), identifies its degradation metabolites, assesses its <i>in vitro</i> cytotoxicity, and validates a high-performance liquid chromatography (HPLC) method for precise quantification.</p><p><strong>Significance: </strong>NRG, a flavonoid with antioxidant, anti-inflammatory, and anticancer properties, faces clinical limitations due to poor solubility, rapid degradation, and low bioavailability. While research efforts on this promising compound have largely focused on overcoming these limitations through formulation strategies, it is equally necessary and complementary to focus on preformulation studies to enhance NRG's therapeutic potential. These studies represent a fundamental step in drug development, providing key insights into the physicochemical and biological properties of NRG and serving as the basis for the rational design of safe and effective formulations in future research.</p><p><strong>Methods: </strong>NRG stability was analyzed under various temperature and pH conditions. Cytotoxicity was evaluated in 3T3 cells, and an HPLC method was developed and validated to quantify NRG and its primary metabolite, naringenin (NRGN).</p><p><strong>Results: </strong>NRG remained stable up to 100 °C and under physiological pH (1.2, 5.8, and 7.4) but degraded at extreme pH, forming NRGN. Cytotoxicity assays showed low toxicity at ≤1 mM (viability >80%), whereas 5 mM significantly reduced viability. The validated HPLC method exhibited high precision, specificity, and accuracy in distinguishing NRG from NRGN.</p><p><strong>Discussion: </strong>This study provides critical insights into NRG's stability, safety, and quantification, supporting its potential therapeutic development. These findings establish a foundation for future research aimed at enhancing NRG bioavailability and clinical applicability.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"344-353"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143482499","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":"An evaluation of the effect of aging on the quality attributes of orodispersible tablets prepared by the direct compression technique.","authors":"Amjad Khan, Abad Khan, Shabnam Nazir, Nauman Rahim Khan, Majeed Ullah, Naila Shahbaz, Noor Ul Ain Nawaz","doi":"10.1080/03639045.2025.2469800","DOIUrl":"10.1080/03639045.2025.2469800","url":null,"abstract":"<p><strong>Background: </strong>The presented study aimed to evaluate the effect of aging on the quality attributes of ODTs.</p><p><strong>Experimental: </strong>ODTs prepared in one of our previous studies, packed in standard blister packing, were stored at ambient conditions in a laboratory (protected from direct sunlight) for 5 years and evaluated for their quality attributes, including physical parameters, mechanical strength (crushing strength, specific crushing strength, tensile strength, and friability), disintegration behavior (<i>in vitro</i> disintegration time, oral disintegration time, and wetting time), assay and dissolution rates. Drug content of all the samples was determined by HPLC.</p><p><strong>Results: </strong>Physically, the ODTs were oval (10 mm), shallow, and convex with a bisection line, and their compression weight was 200 mg/tablet. With the passage of time, the moisture content of the ODTs increased from 2.4 ± 0.39% to 3.48 ± 0.62%. After 5 years, the drug content decreased to 92.38 ± 0.93%.</p><p><strong>Discussion: </strong>Initially, there was an increase in the crushing strength of the ODTs (up to 3 years), and then it gradually decreased. At the time of preparation, disintegration time of the ODTs was 53 s, which gradually increased up to 89 s, at the 4th year. After completion of the study, it slightly decreased to 85 s. The dissolution rate of domperidone from the ODTs remained unaffected by aging. The FTIR spectra of the ODTs showed insignificant cahnges, indicating absence of degradation during the study period.</p><p><strong>Conclusion: </strong>ODTs remained stable for five years and insignificant changes were observed in their quality attributes.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"309-318"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143448506","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":"Enhancing quality-by-design through weighted goal programming: a case study on formulation of ultradeformable liposomes.","authors":"Sonia Valverde Cabeza, Pedro Luis González-R, María Luisa González-Rodríguez","doi":"10.1080/03639045.2025.2470397","DOIUrl":"10.1080/03639045.2025.2470397","url":null,"abstract":"<p><strong>Introduction: </strong>Optimization of pharmaceutical formulations requires advanced tools to ensure quality, safety, and efficacy. quality-by-design (QbD), introduced by the FDA, emphasizes understanding and controlling processes early in development. Advanced optimization methods, such as desirability, have surpassed traditional single-objective techniques. Others, such as weighted goal programming (WGP) offers unique advantages by integrating decision-maker preferences, enabling balanced solutions for complex drug delivery systems. This study applies WGP to optimize timolol (TM)-loaded nanoliposomes aligning with QbD principles.</p><p><strong>Methods: </strong>The optimization process followed six steps: identifying factors and responses, developing a Design of Experiments (DoE) plan, defining ideal and anti-ideal points, setting aspiration levels, assigning relative weights, and applying WGP compared to desirability function. Minimized and balanced deviations from aspiration levels served as criteria for selecting the most robust optimization results. Six responses were analyzed: vesicle size <math><mo>(</mo><mrow><msub><mrow><mi>z</mi></mrow><mrow><mn>1</mn></mrow></msub></mrow><mo>)</mo></math>, polydispersity index <math><mo>(</mo><mrow><msub><mrow><mi>z</mi></mrow><mrow><mn>2</mn></mrow></msub></mrow><mo>)</mo></math>, zeta potential <math><mo>(</mo><mrow><msub><mrow><mi>z</mi></mrow><mrow><mn>3</mn></mrow></msub></mrow><mo>)</mo></math>, deformability index <math><mo>(</mo><mrow><msub><mrow><mi>z</mi></mrow><mrow><mn>4</mn></mrow></msub></mrow><mo>)</mo></math>, phosphorus content <math><mo>(</mo><mrow><msub><mrow><mi>z</mi></mrow><mrow><mn>5</mn></mrow></msub></mrow><mo>)</mo></math>, and drug entrapment efficiency <math><mo>(</mo><mrow><msub><mrow><mi>z</mi></mrow><mrow><mn>6</mn></mrow></msub></mrow><mo>)</mo></math>.</p><p><strong>Results: </strong>WGP produced a more balanced formulation that simultaneously optimized multiple responses. By incorporating the importance of each response, the WGP approach improved control over size, colloidal stability, and drug entrapment, based on its mathematical formulation. Comparative analysis with the desirability function confirmed that WGP effectively addressed potential tradeoffs without oversimplifying conflicting objectives.</p><p><strong>Conclusions: </strong>This case-study demonstrates WGP potential as an advanced multi-objective optimization tool for pharmaceutical applications, improving upon traditional methods in complex formulations. Its ability to harmonize multiple critical attributes in line with QbD highlights its value in developing high-quality pharmaceutical products.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"384-395"},"PeriodicalIF":2.4,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143491262","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":"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}