Drug Development and Industrial Pharmacy最新文献

{"title":"Hypolipidemic and HMG-CoA reductase inhibitory effects of 15-oxoursolic acid from <i>Rhododendron arboreum</i>: An <i>In-vivo</i> and <i>In-silico</i> study.","authors":"Sajid Ali, Usman Ali, Muhammad Ishtiaq Jan","doi":"10.1080/03639045.2025.2519976","DOIUrl":"10.1080/03639045.2025.2519976","url":null,"abstract":"<p><strong>Background: </strong>Hyperlipidemia is an identified risk factor for metabolic syndrome, obesity and cardiovascular complications characterized by elevated levels of lipids in blood.</p><p><strong>Objective: </strong>The present study aimed to inhibit HMG-CoA reductase with 15-oxoursolic acid through <i>in-vivo</i> and <i>in-silico</i> assessments.</p><p><strong>Methods: </strong>The amorphous compound 15-oxoursolic acid was obtained from plant material through purification with a rotary evaporator and column chromatography. The male BALB/c mice were maintained under stabilized ambient conditions and sustained with standard food and water ad libitum. HFD was used to induce hyperlipidemia in rats.</p><p><strong>Results: </strong>HFD-induced hyperlipidemia in rats was developed with a marked increase in total cholesterol (58.34 ± 0.21 mg/dL), triglycerides (45.45 ± 0.39 mg/dL), LDL-c (66.12 ± 0.10 mg/dL), VLDL-c (19.34 ± 0.16 mg/dL), and a decrease in HDL-c (10.34 ± 0.18 mg/dL). The oral administration of 15-oxoursolic acid at a concentration of 30 mg/Kg b.w significantly reduced the serum concentration of total cholesterol (42.65 ± 0.54 mg/dL), triglycerides (32.33 ± 0.16 mg/dL), LDL-c (50.34 ± 0.15 mg/dL) and VLDL-c (13.15 ± 0.45 mg/dL), respectively and an increased in the serum HDL-c (18.56 ± 0.34 mg/dL). 15-oxoursolic acid also caused a decrease in the coronary risk index and atherogenic risk index. <i>In-silico</i> studies of 15-oxoursolic acid with HMG-CoA reductase showed significant interaction capability with binding energy (-9.26805 Kcal/mol).</p><p><strong>Conclusions: </strong>It is concluded that 15-oxoursolic acid could significantly reduce the total cholesterol, triglycerides and LDL levels in HFD-induced hyperlipidemia rats, which might lead to new medication with significant hypolipidemic potential.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-8"},"PeriodicalIF":2.4,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144274413","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":"Reducing residual solvent levels in poly (D, L-lactic-co-glycolic acid) microspheres: a roadmap for scalable industrial production.","authors":"Somayeh Khanmohammadi, Samira Sadeghi, Samira Ansari, Milad Jafari-Nodoushan, Mahdieh Farhangi","doi":"10.1080/03639045.2025.2514214","DOIUrl":"10.1080/03639045.2025.2514214","url":null,"abstract":"<p><strong>Objective: </strong>Poly (D, L-lactic-co-glycolic acid) (PLGA) microspheres have garnered significant attention as biocompatible and biodegradable carriers for sustained drug delivery. However, the production of PLGA microspheres typically involves organic solvents, such as ethyl acetate and benzyl alcohol. Residual solvents are undesirable given their potential toxicity and adverse effects on product stability. Effective solvent removal is critical for ensuring the safety and functionality of microspheres.</p><p><strong>Method: </strong>In this study, 12 formulations were designed by altering the conditions of solvent extraction, washing, and solvent evaporation steps to reduce residual solvents and determine critical parameters in process. Microspheres were evaluated based on residual solvent content, drug loading, size, morphology, moisture content, injectability, and release kinetics.</p><p><strong>Result: </strong>In five formulations (F06-F10), at least the residual amount of one organic solvent was significantly reduced. Prolonging the microspheres' residence time in ethanolic solution during the second extraction phase (F11) resulted in notable organic solvent reductions (ethyl acetate 93% and benzyl alcohol 60% compared to formulation F01). Further, these microparticles were spherical with a geometric diameter of 75.8 μm, a drug loading percentage of 33.7%, and a reasonable release profile, representing significant achievements.</p><p><strong>Conclusion: </strong>This study highlighted the importance of some modifications in preparing PLGA microspheres that have not been reported previously. These modifications greatly affected the residual solvent amount as well as other physicochemical properties of microspheres including size, morphology, and release profile. Overall, some practical methods could be used for feasible industrial production of PLGA microspheres.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2025-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144293507","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":"Development, characterization and <i>in vitro</i> evaluation of capecitabine-loaded chitosan nanoparticles.","authors":"Debarati Ghosh, Ketousetuo Kuotsu","doi":"10.1080/03639045.2025.2518304","DOIUrl":"10.1080/03639045.2025.2518304","url":null,"abstract":"<p><strong>Objective: </strong>To formulate capecitabine-loaded nanoparticles by the ionotropic gelation method, using low molecular weight (LMW) chitosan polymer and sodium tripolyphosphate (STPP) as the cross-linking agent.</p><p><strong>Methods: </strong>Nanoparticles were prepared using the ionotropic gelation method. They were characterized for particle size, polydispersity index (PDI), entrapment efficiency (%), and percentage yield (%) using dynamic light scattering (DLS), UV-Visible spectrophotometry, and other analytical techniques.</p><p><strong>Results: </strong>The optimized formulation (CN-4) showed a particle size of 166.5 nm ± 2.3 nm, PDI of 0.346 ± 0.01, entrapment efficiency of 65.34 ± 1.8%, and percentage yield of 90.32 ± 2.1%. The zeta potential of CN-4 was found to be +37.4 mV, confirming its colloidal stability and cationic surface characteristics. An increase in particle size and PDI was observed with higher concentrations of chitosan.</p><p><strong>Conclusions: </strong>No appreciable difference in particle size, polydispersity index (PDI) and percentage intensity was observed for CN-4 formulation after storing it for a period of 15 days at 2-4 °C. However, significant changes were observed after 30 days of storage, indicating destabilization and precipitation of the formulation.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-13"},"PeriodicalIF":2.4,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144257604","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":"Dextran-based prodrug-nanoassemblies responsively releasing pidotimod and camptothecin for anti-breast cancer.","authors":"Peng-Fei Gao, Jia-Jun Cui, Jia-Min Li, Bing-Feng Zhang","doi":"10.1080/03639045.2025.2517726","DOIUrl":"10.1080/03639045.2025.2517726","url":null,"abstract":"<p><strong>Objective: </strong>The aim of this study was to develop a pH/GSH-responsive dextran-based drug delivery system, co-delivering camptothecin (CPT) and pidotimod (PTD), to increase anti-breast cancer efficacy.</p><p><strong>Methods: </strong>CPT was grafted onto dextran <i>via</i> disulfide bond, and PTD were concurrently conjugated into dextran by the instrumentality of ester bond. The synthesized conjugate could self-assemble to form prodrug-nanoassemblies (CPT-SS-DEX-PTD NPs) in solution. The feature of prodrug-nanoassemblies was assayed, and the synergetic effect of chemo-immunotherapy against solid tumor was investigated in 4T1 breast cancer xenograft models.</p><p><strong>Results: </strong>The CPT-SS-DEX-PTD NPs were approximately spherical and about 180 nm. In drug release experiment, the prodrug-nanoassemblies showed more prolonged circulation time and selective pH or GSH-responsive release profile. The PTD was released in weak acidity tumor microenvironment (TME), then induced immune cells to activate and secret anti-tumor cytokines. The CPT was released <i>via</i> GSH-responsive in tumor cell to exert anti-tumor efficiency. In 4T1 breast cancer model, the CPT-SS-DEX-PTD NPs displayed synergistic anti-tumor efficacy and lower side effects of CPT due to the combination of chemo-immunotherapy.</p><p><strong>Conclusions: </strong>The dextran-based pH/GSH-responsive prodrug-nanoassemblies with synergistic therapy efficacy and low systemic toxicity may offer a novel strategy for breast cancer therapy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144246975","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 overview of novel formulations for ocular viral infections: focused on nanomedicines.","authors":"Shalu Verma, Nidhi Nainwal, Divya Juyal","doi":"10.1080/03639045.2025.2515998","DOIUrl":"10.1080/03639045.2025.2515998","url":null,"abstract":"<p><p>Ocular viral infections are a common cause of blindness globally. Many ocular viral infections are mistakenly identified as bacterial infections. In these situations, treatment is initiated belatedly and fails to address the root cause of the infection, which frequently results in serious ocular complications like corneal infiltrates, conjunctival scarring, and decreased visual acuity. The efficacy of conventional treatments for viral infections suffers from poor bioavailability, which requires the development of novel methods of drug delivery, accurate diagnosis, and efficient treatment choices. As nanotechnology in medicine advances at a rapid pace, multifunctional nanosystems are being prioritized more and more to address the problems brought on by viral infections of the eyes offering targeted delivery, increased bioavailability and decreased systemic toxicity. This study delivers a thorough overview of the use of nanomedicines in the treatment of ocular viral infections, with a particular emphasis on how they may enhance the safety and efficacy of antiviral drugs. We address a range of nanocarrier systems, such as liposomes, nanoparticles, nanosuspension, proniosomes, in-situ gels, dendrimers, and nanogels, emphasizing their distinct characteristics that facilitate the effective transportation of antiviral drugs to ocular tissues. This article also highlighted the regulatory barriers of ocular nanoformulation. The transition of <i>in-vitro</i> studies to <i>in-vivo</i> and clinical models has been discussed. This review also highlights the Preclinical studies of ocular viral treatment, ocular nanotoxicology and advancement of ocular antiviral treatments in the form of patents, ongoing clinical trials and marketed formulations.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-23"},"PeriodicalIF":2.4,"publicationDate":"2025-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144233421","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":"Innovative strategies in the formulation and applications of mouth dissolving films for enhanced oral drug delivery.","authors":"Varun S, Keerthy H S","doi":"10.1080/03639045.2025.2510581","DOIUrl":"10.1080/03639045.2025.2510581","url":null,"abstract":"<p><strong>Objective: </strong>The main objective is to provide an overview of the advantages of mouth dissolving films (MDFs) by addressing the limitations of traditional oral dosage forms such as tablets and capsules, particularly for pediatric and geriatric patients with dysphagia. Also to explore its potential to revolutionize the oral drug delivery system supported by advancements in technology.</p><p><strong>Significance: </strong>Mouth dissolving films offer a transformative approach for the delivery of drugs with rapid disintegration, ease of administration, and water-free administration that improve patient compliance significantly. This review highlights the MDFs formulation strategies, applications, patent portfolio, and role of emerging technologies like 3D printing and artificial intelligence in enhancing drug absorption and bioavailability with substantial commercial potential and versatility, offering a patient-centric solution to modern pharmaceutical challenges.</p><p><strong>Key findings: </strong>Mouth dissolving film helps in addressing potential limitations in the traditional drug delivery system by enhancing patient compliance. This formulation relies on hydrophilic polymers and excipients to achieve desired characteristics, with techniques like solvent casting and 3D printing playing a pivotal role in their development, ensuring critical quality parameters that are essential for maintaining the efficacy and safety of the film with significant market potential. These dosage forms can offer good absorption and bioavailability by the use of artificial intelligence and microfabrication.</p><p><strong>Conclusion: </strong>Mouth dissolving films are a transformative progress in oral drug delivery with future advancements in AI, robotics, and microfabrication that hold promise to further enhance bioavailability, targeted delivery, and sustained release solidifying their role in modern pharmaceutics.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2025-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144136141","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":"Establishing virtual bioequivalence and bio-related dissolution specifications for naproxen using physiologically based pharmacokinetic modeling and <i>in vitro</i> biorelevant dissolution testing.","authors":"Chenxia Bai, Jiaming Zhang, Xiaolan Xu, Xiaoting Li, Tianhong Zhang","doi":"10.1080/03639045.2025.2515999","DOIUrl":"10.1080/03639045.2025.2515999","url":null,"abstract":"<p><strong>Objective: </strong>The aim of the present study was to assess the accuracy of the PBPK model in predicting the pharmacokinetic behavior of weakly acidic BCS class II drugs in humans through a multipronged approach of <i>in vitro</i> dissolution, <i>in vivo</i> studies, and in silico simulations.</p><p><strong>Significance: </strong>We envision that accurate prediction of <i>in vivo</i> pharmacokinetic behavior of drugs is expected to be achieved if physiological pharmacokinetic models can be organically combined with the physicochemical and bio pharmacological properties of the drugs, as well as their <i>in vitro</i> dissolution behavior.</p><p><strong>Methods: </strong>In the current study, using naproxen, a BCS class II drug, as a model drug, GastroPlus^® was applied to bridge the <i>in vitro</i> dissolution and <i>in vivo</i> pharmacokinetic behaviors to establish an alternative method for predicting pharmacokinetics in humans.</p><p><strong>Results: </strong>The test products with different <i>in vitro</i> dissolution profiles were shown to be bioequivalent to the reference product. In addition, a Biphasic <i>In vitro</i> Dissolution Test method of bio-related dissolution methods was constructed to correctly predict the bioequivalence of naproxen tablets. Finally, extrapolation of the combined PBPK model to humans showed that drugs with different <i>in vitro</i> dissolution profiles are bioequivalent in humans.</p><p><strong>Conclusions: </strong>These findings will help demonstrate the biowaiver of naproxen tablets, which has implications for scale-up or post-approval changes in naproxen tablets.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-12"},"PeriodicalIF":2.4,"publicationDate":"2025-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144224619","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":"Preparation and evaluation of gastrodin-ferulic acid co-loaded liposome gel patches for the treatment of migraine.","authors":"Jie Wang, Xuemei Gu, Xia Gao, Huifang Gao, Jing Chen, Zhiyang Lv, Lei Chen, Yunzhu Xu, Xialin Chen, Liang Cao, Zhenzhong Wang, Jinzhou Tian, Wei Xiao","doi":"10.1080/03639045.2025.2513408","DOIUrl":"10.1080/03639045.2025.2513408","url":null,"abstract":"<p><strong>Objective: </strong>Gastrodin (GA) and ferulic acid (FA) are the main active ingredients of the traditional Chinese medicine Da Chuan Xiong formula for migraine treatment. This study aimed to develop a gastrodin-ferulic acid co-loaded liposomal gel patch (GA/FA-Lip-GelP) as a transdermal drug delivery system (TDDS) for migraine management.</p><p><strong>Significance: </strong>TDDS overcomes the limitations of first-pass metabolism associated with oral administration and is particularly suitable for migraine patients experiencing nausea and vomiting. The system contains three key components: sodium polyacrylate (hydrophilic gel matrix), laurocapram (Azone, permeation enhancer), and GA/FA-loaded liposomes (nanocarrier). This combination enables effective systemic drug delivery.</p><p><strong>Methods: </strong>The GA/FA-Lip was prepared using central composite design optimization. Subsequently, the GA/FA-Lip-GelP formulation was developed through single-factor screening and Box-Behnken designs. The optimized GA/FA-Lip-GelP was systematically evaluated via in vitro release studies, ex vivo transdermal permeation experiments, and in vivo pharmacokinetic/pharmacodynamic analyses.</p><p><strong>Results: </strong>The GA/FA-Lip was prepared via thin-film dispersion, forming uniform spherical nanoparticles (146.34 ± 1.35 nm). These nanoparticles achieved high encapsulation efficiencies (GA: 85.26 ± 1.90%; FA: 86.92 ± 2.23%) and demonstrated excellent stability. The final GA/FA-Lip-GelP demonstrated optimal adhesion, sustained drug release, and content uniformity under low-temperature storage. Compared to oral administration and non-liposomal gel patches, GA/FA-Lip-GelP showed significantly enhanced transdermal permeation, improved pharmacokinetic profiles, and superior therapeutic efficacy.</p><p><strong>Conclusions: </strong>GA/FA-Lip-GelP demonstrated potential as an effective migraine treatment by overcoming first-pass metabolism, thereby improving bioavailability and enabling sustained drug release.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-15"},"PeriodicalIF":2.4,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144172975","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":"Amplifying therapeutic potential through optimization of bioavailability of poorly soluble flavonols via albumin-based nanoparticles.","authors":"Shayeri Chatterjee Ganguly, Ritam Maity, Priya Manna, Avisek Sardar, Swarupananda Mukherjee, Dipanjan Karati","doi":"10.1080/03639045.2025.2490281","DOIUrl":"10.1080/03639045.2025.2490281","url":null,"abstract":"<p><strong>Objective: </strong>Flavonols have different pharmacological actions that render them highly promising therapeutic targets. However, their water solubility and bioavailability are low, which restricts their therapeutic potential. ABNPs, albumin-based nanoparticles, are potential nanocarriers that enhance flavonol solubility, stability, and targeted delivery. By utilizing ABNPs, in this work we provide a detailed overview of strategies employed to attain maximum bioavailability of poorly water-soluble flavonols. The review critically evaluates ABNP-mediated delivery's pharmacokinetic advantage, physicochemical properties, and formulation principles. We also highlight existing gaps in research, such as the need for stringent <i>in vivo</i> validity tests, standardized formulation procedures, and in-depth mechanistic understanding of flavonol-albumin interactions.</p><p><strong>Significance: </strong>Despite having potential therapeutic activities, the utilization of flavonoids in the form of medication is limited. Some recent studies have shown that flavonoids exhibit low solubility, low permeability and chemical instability, thereby limiting their bioavailability and therapeutic responses.</p><p><strong>Methods: </strong>To overcome these drawbacks, multiple novel drug delivery approaches have emerged in the pharmaceutical research.</p><p><strong>Results: </strong>These novel approaches seem to offer a viable foundation for improving the bioavailability of the flavonoids and positioning them as viable therapeutic options. Out of all the polymers implemented in enhancing the solubility and bioavailability of the flavonoids, albumin-based nanomaterials have been the most efficacious one.</p><p><strong>Conclusion: </strong>Compared to all other polymeric nano-carriers, albumin nano-carriers offer a greater scale of drug entrapment and drug loading because of their capacity for surface modification, crosslinking, conjugation, coupling, and characteristics including biodegradability and biocompatibility.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"534-545"},"PeriodicalIF":2.4,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143788079","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":"Optimizing paracetamol-ascorbic acid effervescent tablet characteristics: a quality by design approach  .","authors":"Nur Tasnim Adlina Mazdi, Nur Aisyah Mior Mat Zin, Muhammad Aiman Khairul Hisham, Shaiqah Mohd Rus, Muhammad Salahuddin Haris, Bappaditya Chatterjee","doi":"10.1080/03639045.2025.2495131","DOIUrl":"10.1080/03639045.2025.2495131","url":null,"abstract":"<p><strong>Objective: </strong>This study aims to optimize paracetamol-ascorbic acid (PCM-AA) effervescent tablet characteristics through a Quality-by-Design (QbD) approach, investigating the effects of binder concentration, granulation time, and effervescent agents' ratio on hardness, disintegration, and dissolution of the tablets.</p><p><strong>Methods: </strong>The QbD approach was implemented by identifying the quality target product profile, critical quality attributes (CQAs), critical material attributes (CMAs), and critical process parameters for formulating PCM-AA effervescent tablets. An Ishikawa diagram identified risk factors for CQAs. A risk estimation matrix evaluated the levels of associated risks. A central composite design-based response surface methodology with 20 experimental runs, including six center points, identified key factors (binder concentration, granulation time, and effervescent agents' ratio) influencing tablet characteristics (hardness, disintegration, dissolution). The optimum formulation, determined by numerical analysis, was characterized for weight uniformity, tablet thickness and diameter, friability, and PCM and AA assay.</p><p><strong>Results: </strong>Optimized PCM (500 mg)-AA(200 mg) effervescent tablets with 2.9% PVP concentration, 15 min granulation time, and 1:1.5 (w/w) sodium bicarbonate-citric acid ratio achieved acceptable characteristics (hardness: 45 N ± 20 N, disintegration: <5 min, and both PCM and AA dissolution: <10 min). Model validation showed no significant difference (<i>p</i> > 0.05), indicating consistent results.</p><p><strong>Conclusion: </strong>The study successfully optimized the hardness, disintegration, and dissolution rate of PCM-AA effervescent tablets via the QbD approach. Granulation time affects hardness and PCM dissolution, binder concentration influences disintegration time, and the effervescent agents' ratio impacts both disintegration time and AA dissolution. This research enhances the understanding of pharmaceutical formulation processes, risk management, and optimization in effervescent tablet development.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"647-658"},"PeriodicalIF":2.4,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143962387","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}