Pharmaceutical Development and Technology最新文献_第2页

Development of sustained release oral disintegrating tablet of fluvoxamine maleate. 马来酸氟伏沙明口服缓释崩解片的研制。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-08-12 DOI: 10.1080/10837450.2025.2546942

Esraa A Shetaa, Mona F Arafa, Sally E Abu-Risha, Gamal M El Maghraby

{"title":"Development of sustained release oral disintegrating tablet of fluvoxamine maleate.","authors":"Esraa A Shetaa, Mona F Arafa, Sally E Abu-Risha, Gamal M El Maghraby","doi":"10.1080/10837450.2025.2546942","DOIUrl":"https://doi.org/10.1080/10837450.2025.2546942","url":null,"abstract":"Fluvoxamine maleate is efficient in treatment of depression and obsessive-compulsive disorder. However, it has several side effects which are believed to be minimized by administration of slow-release formulation. This work introduces geriatric friendly rapidly disintegrating sustained release (RDSR) tablets for fluvoxamine intraoral administration. Fluvoxamine was subjected to wet co-processing with increasing weight ratios of Eudragit S100 in presence and absence of avicel. Fluvoxamine release was monitored using continuous pH variation strategy using USP II dissolution apparatus. Formulations exhibiting acceptable sustained release pattern were subjected to different investigations. Optimized systems were fabricated as RDSR tablets. Optimized systems were also assessed in vivo using forced swimming test using albino rats. Incorporation of avicel in the co-processed formulations showed faster release with avicel-free systems sustaining fluvoxamine release. Optimum formulations contained fluvoxamine and Eudragit at weight ratios of 4:12 (F2), 4:15 (F4) and 4:16 (F6) which liberated the drug with release efficiency of 61.65, 41.76 and 34.5%, respectively. Thermal analysis and XRD reflected dispersion of fluvoxamine in amorphous form in Eudragit with no significant chemical interaction being reflected from FTIR. The developed RDSR tablets showed acceptable sustained release. In vivo studies reflected the superiority of sustained release systems compared to unprocessed fluvoxamine. The study developed RDSR tablets for sustained delivery of fluvoxamine.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-15"},"PeriodicalIF":2.5,"publicationDate":"2025-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144837296","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 stabilizing agents to prevent crystal growth or aggregation in PTX-NCs generated via diverse nanocrystallization technologies. 探索稳定剂，以防止晶体生长或聚集的PTX-NCs通过不同的纳米晶化技术。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-08-10 DOI: 10.1080/10837450.2025.2544579

Farzaneh Amiri, Ali Nokhodchi, Mohammad Barzegar-Jalali, Hadi Valizadeh

{"title":"Exploring stabilizing agents to prevent crystal growth or aggregation in PTX-NCs generated via diverse nanocrystallization technologies.","authors":"Farzaneh Amiri, Ali Nokhodchi, Mohammad Barzegar-Jalali, Hadi Valizadeh","doi":"10.1080/10837450.2025.2544579","DOIUrl":"10.1080/10837450.2025.2544579","url":null,"abstract":"This study aimed to prepare paclitaxel nanocrystals (PTX-NCs) for developing a delivery platform for this poorly water-soluble drug. Using biocompatible polymers as stabilizers, paclitaxel (PTX) was formulated as a nanosuspension using two techniques: (I) ultrasonication followed by freeze-drying and (II) melt-based precipitation (MBP) approach. The effectiveness of stabilizers in inhibiting crystal growth and agglomeration of PTX-NCs was discussed. Nanosuspensions developed using the MBP method by employing polyethylene glycol (PEG) derivatives offered superior results compared to the ultrasonication method. Among the various stabilizers, Pluronic F-68 and myrj 52 were more efficient against particle size enlargement. The optimized formulation containing PTX/PEG/Pluronic F-68/myrj 52 produced re-dispersible particles of about 74 nm with a smooth spherical morphology, which were stable for ∼8 h in water, indicating good physical stability following reconstitution. The particles obtained after redispersion of MBP-PTX-NCs enhanced the dissolution of PTX compared to plain crystals and had superior chemical stability. A 6-month stability test showed no significant changes in drug content or X-ray powder diffraction (XRPD) pattern. These findings highlighted the potential of forming fine particles from MBP method using biocompatible polymers as a promising method for producing drug nanocrystals (NCs) for poorly soluble drugs without expensive, time-consuming freeze-drying steps.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-18"},"PeriodicalIF":2.5,"publicationDate":"2025-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144789684","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 characterization of a fixed-dose microemulsion containing efavirenz, emtricitabine, and tenofovir. 含有依非韦伦、恩曲他滨和替诺福韦的固定剂量微乳的配方和特性。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-29 DOI: 10.1080/10837450.2025.2537128

Samantha Mabvira, Sandile M Khamanga, Roderick B Walker

{"title":"Formulation and characterization of a fixed-dose microemulsion containing efavirenz, emtricitabine, and tenofovir.","authors":"Samantha Mabvira, Sandile M Khamanga, Roderick B Walker","doi":"10.1080/10837450.2025.2537128","DOIUrl":"10.1080/10837450.2025.2537128","url":null,"abstract":"Despite a marked decrease in HIV/AIDS-related mortality, HIV remains one of the leading causes of death in specific populations. Despite concerted efforts to find a cure for HIV, to date, none exists. Current antiretroviral therapy inhibits replication of the virus without completely eradicating it. The successful inhibition of viral replication is only achieved using a combination of antiretrovirals, which inhibit viral replication at different stages of the HIV lifecycle. Efavirenz (EFV), emtricitabine (FTC), and tenofovir disoproxil fumarate (TDF) is one combination used for HIV management. The development of a novel fixed-dose microemulsion formulation of EFV, FTC, and TDF was undertaken. Microemulsions (ME) were manufactured using phase titration and drug loading, particle size, transparency, Zeta potential, and pH were determined. Transmission Electron Microscopy was used to visualize the microemulsion. In vitro release testing was used to evaluate active pharmaceutical ingredient release behavior. The optimized ME had an average Zeta potential of 33.8 mV and droplet size of 117 nm, determined using Dynamic Light Scattering and confirmed using Transmission Electron Microscopy. Powder X-ray diffraction and Differential Scanning Calorimetry analysis revealed the presence of a molecular dispersion of drugs. These findings demonstrate the potential value of using ME as a fixed-dose combination technology for the delivery of EFV, FTC, and TDF.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.5,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144699198","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

Novel vanillic acid-loaded in situ gels: development, characterization, in vitro evaluation for enhanced wound healing and skin irritation test. 新型香草酸负载原位凝胶：开发，表征，体外评估促进伤口愈合和皮肤刺激试验。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-25 DOI: 10.1080/10837450.2025.2534867

Gökçe Mutlu Sonat, Emre Şefik Çağlar, Dilara Güreşçi, Ahmet Aydın, Hande Sipahi, Neslihan Üstündağ Okur

{"title":"Novel vanillic acid-loaded in situ gels: development, characterization, in vitro evaluation for enhanced wound healing and skin irritation test.","authors":"Gökçe Mutlu Sonat, Emre Şefik Çağlar, Dilara Güreşçi, Ahmet Aydın, Hande Sipahi, Neslihan Üstündağ Okur","doi":"10.1080/10837450.2025.2534867","DOIUrl":"10.1080/10837450.2025.2534867","url":null,"abstract":"This study aimed to develop in situ gel formulations containing vanillic acid to enhance patient compliance and accelerate wound healing. Vanillic acid-loaded in situ gels were prepared, and their physicochemical properties were evaluated through in vitro release and ex vivo permeation studies. Additionally, antioxidant capacity, cytotoxicity, wound healing, prostaglandin E2 levels, IL-6 inhibition, and skin irritation tests were conducted. The optimized IN3-VA formulation exhibited a gelling temperature of 32.394 ± 0.842, a pH value of 4.780 ± 0.010 and a viscosity of 2473.33 ± 11.54 cP. It demonstrated specific mechanical properties, including hardness of 27.94 ± 1.30 g and adhesiveness of -97.00 ± 14.60 g.mm. The IN15-VA formulation showed improved parameters, with a hardness of 38.84 ± 3.33 g, adhesiveness of -126.35 ± 22.78 g.mm, pH value of 4.870 ± 0.010, viscosity of 3853.33 ± 30.55 cP, and a gelling temperature of 31.854 ± 0.345. Both formulations demonstrated sustained release behavior, releasing 60% of the medication in vitro over 6 h with no cytotoxic effects. They also decreased copper ion reduction and the release of nitric oxide, with cellular proliferation rates of 63% for IN3-VA and 73% for IN15-VA. Moreover, IN15-VA significantly reduced prostaglandin E2 levels, controlled IL-6 increase, and exhibited non-irritating properties. The results suggest that these vanillic acid-loaded in situ gels hold promising potential in wound treatment due to their sustained release over 48 h.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-18"},"PeriodicalIF":2.6,"publicationDate":"2025-07-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144643106","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Self-assembled mumio-stabilized bioactive gel systems for topical therapeutics of rheumatoid arthritis: structural, rheological, cytocompatibility, and antimicrobial properties. 用于类风湿性关节炎局部治疗的自组装mumo稳定生物活性凝胶系统：结构、流变学、细胞相容性和抗菌特性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-10 DOI: 10.1080/10837450.2025.2529894

Oyunchimeg Zandraa, Fahanwi Asabuwa Ngwabebhoh, Smarak Bandyopadhyay, Nabanita Saha, Tomas Saha, Petr Saha

{"title":"Self-assembled mumio-stabilized bioactive gel systems for topical therapeutics of rheumatoid arthritis: structural, rheological, cytocompatibility, and antimicrobial properties.","authors":"Oyunchimeg Zandraa, Fahanwi Asabuwa Ngwabebhoh, Smarak Bandyopadhyay, Nabanita Saha, Tomas Saha, Petr Saha","doi":"10.1080/10837450.2025.2529894","DOIUrl":"10.1080/10837450.2025.2529894","url":null,"abstract":"This study presents the development of salicylate polyacrylic copolymer gel systems incorporating mumio particulates as a bioactive agent for the topical treatment of rheumatoid arthritis. Using an experimental design, formulations were optimized based on mumio, salicylic acid, and polyacrylate copolymer ratios. Rheological behavior was assessed through frequency, temperature, and time sweep tests to evaluate shear response, stability, and application suitability. Spectral and morphological analyses confirmed the uniformity and surface characteristics of the gels. Antimicrobial activity was tested against Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans, and Aspergillus niger. Cytotoxicity was evaluated using NIH-3T3 mouse fibroblast cells. Results showed over 60% microbial inhibition after 24 hours and maintained cell viability above 70% at both 24 and 48 hours, indicating good biocompatibility. The gels also exhibited smooth texture, consistent bioactive dispersion, and non-irritating properties. Overall, these findings support the potential of mumio-loaded salicylate-polyacrylic gels as stable, biocompatible, and effective topical therapeutics for rheumatoid arthritis.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-14"},"PeriodicalIF":2.6,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144591898","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

Development of fenofibrate solid dispersion via hot melt extrusion and 3D printing technologies. 利用热熔挤压和3D打印技术研制非诺贝特固体分散体。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-01 Epub Date: 2025-06-27 DOI: 10.1080/10837450.2025.2522802

Janhavi Deshmukh, Kavish Sanil, Achref Cherif, Eman A Ashour

{"title":"Development of fenofibrate solid dispersion via hot melt extrusion and 3D printing technologies.","authors":"Janhavi Deshmukh, Kavish Sanil, Achref Cherif, Eman A Ashour","doi":"10.1080/10837450.2025.2522802","DOIUrl":"10.1080/10837450.2025.2522802","url":null,"abstract":"This study aimed to develop an amorphous solid dispersion (ASD) of fenofibrate using Hot Melt Extrusion (HME) and 3D printing to evaluate the impact of preparation methods on ASD properties. Fenofibrate (10% w/w) was processed with Soluplus® and Polyethylene oxide-N80 to produce HME filaments. These filaments were either used as feedstock for Fused Deposition Modeling (FDM) 3D printing to fabricate tablets with 90%, 70%, and 50% infill densities or milled and filled into gelatin capsules. Printability was assessed via a three-point bend test. The fenofibrate formulations were evaluated for drug content, physical state, surface morphology, and release profile. The SEM images of pure fenofibrate showed large cylindrical crystals while the 3D-printed tablets showed a smooth surface with no record of any crystals. This observation is in line with the DSC results and confirms the conversion of fenofibrate from crystalline to an amorphous state. The in- vitro drug release for the 3D printed tablets and capsules was increased 2-fold as compared to pure fenofibrate. Statistical comparisons further supported these findings, highlighting infill density as a tunable parameter for modulating release kinetics.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"852-862"},"PeriodicalIF":2.5,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507524","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

HPMCAS-solidified supersaturated baicalin self-nanoemulsifying drug delivery systems: development and anti-colitis evaluation. hpmcas固化过饱和黄芩苷自纳米乳化给药系统：开发和抗结肠炎评价。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-01 Epub Date: 2025-06-13 DOI: 10.1080/10837450.2025.2518567

Jie Wang, Xuemei Gu, Zhiyang Lv, Jing Chen, Zihan Gao, Xinyun Hu, Wei Xiao

{"title":"HPMCAS-solidified supersaturated baicalin self-nanoemulsifying drug delivery systems: development and anti-colitis evaluation.","authors":"Jie Wang, Xuemei Gu, Zhiyang Lv, Jing Chen, Zihan Gao, Xinyun Hu, Wei Xiao","doi":"10.1080/10837450.2025.2518567","DOIUrl":"10.1080/10837450.2025.2518567","url":null,"abstract":"This study developed a hydroxypropyl methylcellulose acetate succinate (HPMCAS)-functionalized supersaturated self-nanoemulsifying drug delivery system (HPMCAS-SNEDDS@BA) to address the poor solubility and bioavailability of baicalin (BA), a flavonoid with anti-colitis efficacy. The formulation was systematically optimized through solubility screening, emulsification efficiency evaluation, and pseudo-ternary phase diagram analysis. Central composite design-response surface methodology (CCD-RSM) was employed to identify the optimal SNEDDS@BA composition, followed by HPMCAS ratio optimization based on supersaturation maintenance in biorelevant media. Comprehensive characterization included emulsification performance, droplet morphology, solid-state properties, in vitro release, and stability. The optimized formulation (mass ratio: HPMCAS-castor oil-RH40-PEG400-BA = 151.5:20:40:40:1) generated homogeneous, transparent nanoemulsions with spherical droplets, achieving an emulsification time of 48.30 ± 0.74 s, a mean particle size of 47.77 ± 2.32 nm, and a polydispersity index (PDI) of 0.259 ± 0.007. HPMCAS-SNEDDS@BA effectively prevented premature gastric emulsification while enhancing intestinal dissolution rates and sustaining BA supersaturation. Pharmacokinetic studies demonstrated a 5.84-fold improvement in BA bioavailability compared to unmodified formulations. In a dextran sulfate sodium (DSS)-induced colitis model, HPMCAS-SNEDDS@BA outperformed BA suspension and SNEDDS@BA, normalizing colon length, reducing inflammatory cytokines, and restoring mucosal architecture. These findings validate the dual functionality of HPMCAS as a pH-responsive polymer and crystallization inhibitor, enabling targeted intestinal delivery and optimized therapeutic outcomes for ulcerative colitis.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"743-758"},"PeriodicalIF":2.5,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144267016","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

Investigating the in vivo distribution characteristics of gel-in-water nanogel emulsions and demonstrating their efficacy in treating C26 tumor-bearing mice. 研究水凝胶纳米乳的体内分布特征及对C26荷瘤小鼠的治疗作用。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-01 Epub Date: 2025-06-20 DOI: 10.1080/10837450.2025.2518564

Yi Zhang, Jannatul Fardous, Ryota Doi, Yuuta Inoue, Yasuhiro Ikegami, Hiroyuki Ijima

{"title":"Investigating the in vivo distribution characteristics of gel-in-water nanogel emulsions and demonstrating their efficacy in treating C26 tumor-bearing mice.","authors":"Yi Zhang, Jannatul Fardous, Ryota Doi, Yuuta Inoue, Yasuhiro Ikegami, Hiroyuki Ijima","doi":"10.1080/10837450.2025.2518564","DOIUrl":"10.1080/10837450.2025.2518564","url":null,"abstract":"Nanotechnology has been advancing drug delivery systems (DDSs) for decades. Nanoparticle DDSs, in which nanometric carriers deliver drugs to the target site, are highly valued for cancer treatment. In this study, based on nanoemulsion technology, gel-in-water (G/W) nanoemulsion was developed by using an organogel, i.e. 12-hydroxystearic acid and castor oil, followed by encapsulation of the model anticancer drug paclitaxel (PTX) within the nanogel droplets. The G/W was prepared using ultrasound and stabilized with a nonionic surfactant. The enhanced permeability and retention of G/W were investigated by encapsulating coumarin-6 and comparing it with an oil-in-water (O/W) nanoemulsion. Temporal changes in tissue distribution of both nanoemulsions were used to assess the effect of gelation on drug distribution. Regardless of the tissue type, the extraction efficiency of G/W was lower compared to O/W. The fluorescence intensity of coumarin-6 in G/W was higher compared to O/W. The size of G/W nanoparticles affects lung distribution and blood retention. PTX-loaded G/W (PTX-G/W) nanoparticles effectively treated colon cancer in vivo. They also exhibited antitumor activity against colon26 (C26) cells in vitro. The impact of particle size on the in vivo tissue distribution of G/W nanoemulsions suggests an improvement in drug delivery to the tumor site via nanoparticles.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"729-742"},"PeriodicalIF":2.5,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144286042","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

Engineered gastroretentive amorphous ferulate matrix: a novel raft-forming paradigm for enhanced bioavailability. 工程胃保留无定形阿魏酸基质：提高生物利用度的新型筏形形成范例。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-01 Epub Date: 2025-06-28 DOI: 10.1080/10837450.2025.2525265

Ruedeekorn Wiwattanapatapee, Nattawat Chavasiri, Kijja Laohawiriyakamon, Saravoot Pumjan, Nattawut Leelakanok, Arpa Petchsomrit

{"title":"Engineered gastroretentive amorphous ferulate matrix: a novel raft-forming paradigm for enhanced bioavailability.","authors":"Ruedeekorn Wiwattanapatapee, Nattawat Chavasiri, Kijja Laohawiriyakamon, Saravoot Pumjan, Nattawut Leelakanok, Arpa Petchsomrit","doi":"10.1080/10837450.2025.2525265","DOIUrl":"10.1080/10837450.2025.2525265","url":null,"abstract":"This study aimed to enhance the solubility of ferulic acid using solid dispersion techniques and develop chewable tablets that neutralize stomach acid, form a protective gel layer, prevent gastric fluid reflux, and ensure prolonged retention in the stomach with controlled release of the active ingredient. Researchers developed solid dispersions of ferulic acid using Eudragit® E PO as a carrier, with a 1:2 w/w ratio, achieving the highest solubility (39.9 mg/mL). Chewable tablets were formulated by direct compression, incorporating sodium alginate as a gelling agent, calcium carbonate for calcium ions and carbon dioxide, HPMC as a release retardant, and mannitol as a diluent. All formulations rapidly formed a gel layer within 10 s, had a lower density than gastric fluid, and floated on 0.1 N hydrochloric acid for over 8 h. The optimal formulation demonstrated excellent physical properties, including a gel strength of 11.84 g, an acid neutralization capacity of 15.97 mEq, and reaching 80.58% over 8 h with gradual release. It exhibited significant antioxidant activity (IC50 6.74 µg/mL) in the DPPH assay and showed stronger anti-inflammatory effects in macrophage cells than indomethacin. These findings suggest this formulation could enhance ferulic acid's effectiveness in treating gastric ulcers and preventing acid reflux.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"875-890"},"PeriodicalIF":2.5,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144497663","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

Advancing darunavir delivery: nanoformulation strategies and innovations in HIV therapy. 推进达若那韦递送：HIV治疗的纳米制剂策略和创新。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-01 Epub Date: 2025-06-19 DOI: 10.1080/10837450.2025.2520624

Shreyash R Patil, Anjana Adhyapak, Rahul Koli

{"title":"Advancing darunavir delivery: nanoformulation strategies and innovations in HIV therapy.","authors":"Shreyash R Patil, Anjana Adhyapak, Rahul Koli","doi":"10.1080/10837450.2025.2520624","DOIUrl":"10.1080/10837450.2025.2520624","url":null,"abstract":"Darunavir, a nonpeptidic protease inhibitor, remains a cornerstone of antiretroviral therapy due to its potent activity against wild-type human immunodeficiency virus (HIV). However, its poor aqueous solubility and limited oral bioavailability, characteristic of Biopharmaceutical Classification System Class II drugs, restrict therapeutic efficacy, with an absorption rate of only 37%. To address these pharmacokinetic limitations, nanotechnology-based strategies have been explored to enhance drug solubility, systemic exposure, and targeted tissue distribution. This review critically examines the potential of nanocarrier-based formulations, including solid lipid nanoparticles, supersaturated self-nanoemulsifying drug delivery systems, lipid nanoemulsions, poly(lactic-co-glycolic acid) nanoparticles, and cubosomes, in optimizing darunavir pharmacokinetics. These approaches have demonstrated improved bioavailability, sustained drug release, lymphatic targeting, and enhanced blood-brain barrier penetration, offering promising avenues for optimizing HIV therapy while minimizing systemic toxicity. Further, this review discusses challenges associated with nanoformulation-based antiretroviral strategies, scalability, manufacturing challenges, potential toxicity, immunogenicity, long-term stability issues, and explores emerging innovations, such as multifunctional nanoparticles, targeted delivery platforms, and sustainable nanotechnology-based formulations. By systematically evaluating current advances, this analysis provides critical insights into overcoming bioavailability constraints and facilitating the clinical translation of nanocarrier-based antiretroviral therapies.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"772-820"},"PeriodicalIF":2.5,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144310302","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