Objective: To develop ionically cross-linked pH-responsive interpenetrating polysaccharide network hydrogel tablets for the colon-targeted delivery of budesonide (BUD).
Context: The pH-responsive behaviour ensures protection of the drug during its transit through the stomach and small intestine, limiting drug release to less than 10% over a 5 h period.
Methods: We developed a series of BUD loaded pH-responsive single network and interpenetrating double network hydrogel tablets using natural polysaccharides cross-linked with Ca2+ ions.
Results: Both the single network hydrogel and the interpenetrating polymer network (IPN) double network hydrogel were unable to restrict drug release during the initial 5 h transit through the gastrointestinal tract (GIT). An important finding of the study was that the semi-interpenetrating polymer network (semi-IPN) hydrogel matrix tablets exhibited acceptable swelling, erosion, and drug release profiles compared to the single network and IPN hydrogels. The optimized semi-IPN hydrogel matrix tablets, prepared with equal amounts of guar gum (GG) and carboxymethyl cellulose (CMC) cross-linked with calcium ions, exhibited no drug release within the first 4 h, and only a small amount of drug of about 9% was released after 5 h of the dissolution study.
Conclusion: This semi-IPN hydrogel matrix was found to be suitable for the effective colon-specific delivery of the hydrophobic drug BUD.
{"title":"Ionically cross-linked pH-responsive interpenetrating polysaccharide network hydrogel tablets for colon-targeted delivery of budesonide.","authors":"Pallobi Dutta, Kaushik Mukherjee, Tapan Kumar Giri","doi":"10.1080/03639045.2025.2597499","DOIUrl":"10.1080/03639045.2025.2597499","url":null,"abstract":"<p><strong>Objective: </strong>To develop ionically cross-linked pH-responsive interpenetrating polysaccharide network hydrogel tablets for the colon-targeted delivery of budesonide (BUD).</p><p><strong>Context: </strong>The pH-responsive behaviour ensures protection of the drug during its transit through the stomach and small intestine, limiting drug release to less than 10% over a 5 h period.</p><p><strong>Methods: </strong>We developed a series of BUD loaded pH-responsive single network and interpenetrating double network hydrogel tablets using natural polysaccharides cross-linked with Ca<sup>2+</sup> ions.</p><p><strong>Results: </strong>Both the single network hydrogel and the interpenetrating polymer network (IPN) double network hydrogel were unable to restrict drug release during the initial 5 h transit through the gastrointestinal tract (GIT). An important finding of the study was that the semi-interpenetrating polymer network (semi-IPN) hydrogel matrix tablets exhibited acceptable swelling, erosion, and drug release profiles compared to the single network and IPN hydrogels. The optimized semi-IPN hydrogel matrix tablets, prepared with equal amounts of guar gum (GG) and carboxymethyl cellulose (CMC) cross-linked with calcium ions, exhibited no drug release within the first 4 h, and only a small amount of drug of about 9% was released after 5 h of the dissolution study.</p><p><strong>Conclusion: </strong>This semi-IPN hydrogel matrix was found to be suitable for the effective colon-specific delivery of the hydrophobic drug BUD.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"345-365"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145647614","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}
Pub Date : 2026-02-01Epub Date: 2025-12-01DOI: 10.1080/03639045.2025.2595494
Yara N Al-Shdifat, Yazan H Akkam, Abdel-Monem M Rawashdeh, Musa I El-Barghouthi, Osama M Abuhasan
Introduction: Valrubicin (VAL) is an N-trifluoroacetyl 14-valerate derivative of the anthracycline doxorubicin (DOX)and is known to have anti-tumor activity. Unfortunately, itis characterized by low solubility and instability in aqueous solutions, which hampers its applications and reduces its therapeutic efficacy.
Objective: To address this limitation, different types of cucurbiturils (CBs) were employed to explore VAL-CB complexation to enhance VAL's physicochemical characteristics in aqueous solutions.
Methods: Complexes were prepared and characterized using entrapment efficiency (EE %). UV-Vis spectroscopic titration, molecular dynamics (MD), and quantum mechanics (QM) simulations were used to predict binding interactions. In vitro release studies assessed drug release, while stability in water-based solutions was analyzed at 4, 25, and 50 °C.
Results: VAL formed stable host-guest complexes within CB in 1:1 stoichiometry, with a binding affinity of (6.29 ± 0.32 × 103M-1) and (2.02 ± 0.11 × 104 M-1), respectively. Additionally, molecular modeling supported a partial inclusion of the VAL structure in the CB cavity. The VAL-CB complex exhibited a 220,000-fold solubility increase, enhanced stability, and a sustained release profile.
Conclusion: The CB-VAL complex significantly enhanced physicochemical properties of VAL in aqueous solutions, with superiority for CB8. These results highlight the potential of CB7 and CB8 as novel drug delivery systems for hydrophobic drugs, offering a strategy to overcome the limitations of existing solubilization approaches in cancer therapy.
{"title":"Host-guest complexes of cucurbituril with the neutral guest valrubicin: an experimental and computational study.","authors":"Yara N Al-Shdifat, Yazan H Akkam, Abdel-Monem M Rawashdeh, Musa I El-Barghouthi, Osama M Abuhasan","doi":"10.1080/03639045.2025.2595494","DOIUrl":"10.1080/03639045.2025.2595494","url":null,"abstract":"<p><strong>Introduction: </strong>Valrubicin (VAL) is an N-trifluoroacetyl 14-valerate derivative of the anthracycline doxorubicin (DOX)and is known to have anti-tumor activity. Unfortunately, itis characterized by low solubility and instability in aqueous solutions, which hampers its applications and reduces its therapeutic efficacy.</p><p><strong>Objective: </strong>To address this limitation, different types of cucurbiturils (CBs) were employed to explore VAL-CB complexation to enhance VAL's physicochemical characteristics in aqueous solutions.</p><p><strong>Methods: </strong>Complexes were prepared and characterized using entrapment efficiency (EE %). UV-Vis spectroscopic titration, molecular dynamics (MD), and quantum mechanics (QM) simulations were used to predict binding interactions. <i>In vitro</i> release studies assessed drug release, while stability in water-based solutions was analyzed at 4, 25, and 50 °C.</p><p><strong>Results: </strong>VAL formed stable host-guest complexes within CB in 1:1 stoichiometry, with a binding affinity of (6.29 ± 0.32 × 10<sup>3</sup>M<sup>-1</sup>) and (2.02 ± 0.11 × 10<sup>4</sup> M<sup>-1</sup>), respectively. Additionally, molecular modeling supported a partial inclusion of the VAL structure in the CB cavity. The VAL-CB complex exhibited a 220,000-fold solubility increase, enhanced stability, and a sustained release profile.</p><p><strong>Conclusion: </strong>The CB-VAL complex significantly enhanced physicochemical properties of VAL in aqueous solutions, with superiority for CB8. These results highlight the potential of CB7 and CB8 as novel drug delivery systems for hydrophobic drugs, offering a strategy to overcome the limitations of existing solubilization approaches in cancer therapy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"313-327"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145603078","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}
Pub Date : 2026-02-01Epub Date: 2025-12-11DOI: 10.1080/03639045.2025.2598618
Khaldoun A Al-Sou'od, Gaith M Al-Qudah, Rajab Abu-El-Halawa
<p><strong>Objective: </strong>Indapamide, a thiazide-like diuretic, exhibits very low aqueous solubility, which restricts its oral bioavailability and therapeutic efficacy. This study aimed to enhance its solubility and stability by forming inclusion complexes with various cyclodextrins.</p><p><strong>Significance: </strong>Poor aqueous solubility remains a major challenge for oral delivery of many diuretics and other BCS class II drugs. Cyclodextrin inclusion offers a safe and pharmaceutically accepted strategy to overcome these limitations. By quantitatively bridging phase-solubility/van't Hoff thermodynamics (ΔG°, ΔH°, ΔS°) with molecular modeling metrics (ΔE, orientation Approach A vs B), this work provides a mechanistic explanation of host-guest recognition and stability that goes beyond prior indapamide-CD reports. The study identifies SBE-β-CD as superior on mechanistic grounds (synergistic electrostatic and H-bonding interactions consistent with enthalpy-driven binding; ΔE = -28.8 kcal·mol<sup>-1</sup>; ∼8.7-fold solubility gain) and benchmarks preparation methods (freeze-drying > co-evaporation > kneading) while linking amorphization and HPLC retention shifts to complexation efficiency. Collectively, these advances yield a practical, generalizable decision framework for rational excipient and process selection in formulations of poorly water-soluble drugs.</p><p><strong>Methods: </strong>Five cyclodextrins (α-CD, β-CD, γ-CD, hydroxypropyl-β-CD, and sulfobutylether-β-CD) were systematically evaluated using an integrated experimental-computational approach. Phase-solubility studies were performed to determine stoichiometry and stability constants, and thermodynamic parameters (ΔG°, ΔH°, ΔS°) were derived from van't Hoff analysis conducted over the temperature range of 293-313 K. Solid-state characterization was carried out using SEM, XRD, and HPLC. Molecular modeling with HyperChem was performed at the MM+ and PM3 levels to assess host-guest orientations, binding energies, and electronic properties.</p><p><strong>Results: </strong>Phase solubility analysis confirmed the formation of 1:1 A<sub>L</sub>-type complexes, with sulfobutylether-β-CD achieving the highest solubilization (∼8.7-fold), followed by hydroxypropyl-β-CD and γ-CD, while α-CD showed minimal effect. Thermodynamic evaluation revealed that the inclusion process was spontaneous, exothermic, and enthalpy-driven. SEM and XRD demonstrated transformation of indapamide from crystalline to amorphous state, and HPLC confirmed efficient encapsulation. Molecular modeling showed favorable host-guest interactions, with sulfobutylether-β-CD providing the most stable binding (ΔE = -28.8 kcal·mol<sup>-1</sup>).</p><p><strong>Conclusions: </strong>The integrated findings highlight the superior potential of modified cyclodextrins, particularly sulfobutylether-β-CD, as excipients for improving solubility, dissolution, and oral bioavailability of indapamide. These results establish a mechanisti
{"title":"Cyclodextrin-based inclusion complexes to enhance the solubility and oral bioavailability of indapamide: experimental and computational approaches.","authors":"Khaldoun A Al-Sou'od, Gaith M Al-Qudah, Rajab Abu-El-Halawa","doi":"10.1080/03639045.2025.2598618","DOIUrl":"10.1080/03639045.2025.2598618","url":null,"abstract":"<p><strong>Objective: </strong>Indapamide, a thiazide-like diuretic, exhibits very low aqueous solubility, which restricts its oral bioavailability and therapeutic efficacy. This study aimed to enhance its solubility and stability by forming inclusion complexes with various cyclodextrins.</p><p><strong>Significance: </strong>Poor aqueous solubility remains a major challenge for oral delivery of many diuretics and other BCS class II drugs. Cyclodextrin inclusion offers a safe and pharmaceutically accepted strategy to overcome these limitations. By quantitatively bridging phase-solubility/van't Hoff thermodynamics (ΔG°, ΔH°, ΔS°) with molecular modeling metrics (ΔE, orientation Approach A vs B), this work provides a mechanistic explanation of host-guest recognition and stability that goes beyond prior indapamide-CD reports. The study identifies SBE-β-CD as superior on mechanistic grounds (synergistic electrostatic and H-bonding interactions consistent with enthalpy-driven binding; ΔE = -28.8 kcal·mol<sup>-1</sup>; ∼8.7-fold solubility gain) and benchmarks preparation methods (freeze-drying > co-evaporation > kneading) while linking amorphization and HPLC retention shifts to complexation efficiency. Collectively, these advances yield a practical, generalizable decision framework for rational excipient and process selection in formulations of poorly water-soluble drugs.</p><p><strong>Methods: </strong>Five cyclodextrins (α-CD, β-CD, γ-CD, hydroxypropyl-β-CD, and sulfobutylether-β-CD) were systematically evaluated using an integrated experimental-computational approach. Phase-solubility studies were performed to determine stoichiometry and stability constants, and thermodynamic parameters (ΔG°, ΔH°, ΔS°) were derived from van't Hoff analysis conducted over the temperature range of 293-313 K. Solid-state characterization was carried out using SEM, XRD, and HPLC. Molecular modeling with HyperChem was performed at the MM+ and PM3 levels to assess host-guest orientations, binding energies, and electronic properties.</p><p><strong>Results: </strong>Phase solubility analysis confirmed the formation of 1:1 A<sub>L</sub>-type complexes, with sulfobutylether-β-CD achieving the highest solubilization (∼8.7-fold), followed by hydroxypropyl-β-CD and γ-CD, while α-CD showed minimal effect. Thermodynamic evaluation revealed that the inclusion process was spontaneous, exothermic, and enthalpy-driven. SEM and XRD demonstrated transformation of indapamide from crystalline to amorphous state, and HPLC confirmed efficient encapsulation. Molecular modeling showed favorable host-guest interactions, with sulfobutylether-β-CD providing the most stable binding (ΔE = -28.8 kcal·mol<sup>-1</sup>).</p><p><strong>Conclusions: </strong>The integrated findings highlight the superior potential of modified cyclodextrins, particularly sulfobutylether-β-CD, as excipients for improving solubility, dissolution, and oral bioavailability of indapamide. These results establish a mechanisti","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"377-391"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145707821","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}
Pub Date : 2026-02-01Epub Date: 2025-12-26DOI: 10.1080/03639045.2025.2600006
Ping Li, Rongqin Zhang, Xin Li, Hong Chen, Ping Zheng, Li Xie
Objective: To establish an in vitro release (IVR) method for butenafine hydrochloride cream using Immersion Cells and compare the drug release characteristics of commercial samples.
Significance: Reevaluating post-listing semisolid drug products based on quality attributes of IVR performance is crucial for guaranteeing clinical efficacy.
Methods: An in vitro release testing (IVRT) method using Immersion Cells was developed and validated for sensitivity, linearity, and reproducibility. It was adapted for use with Vertical Diffusion Cells (VDCs) to compare two devices. Univariate tests were conducted to assess the effect of excipients on in vitro release rates (IVRRs). Three regulatory guidelines recommended by FDA, NMPA and EMA for IVR performance consistency assessment were compared to evaluate the sameness of marketed samples.
Results: For IVRT of butenafine hydrochloride cream, Immersion Cells exhibited the same functionality as VDCs. Stearyl alcohol which serves as oil phase matrix and thickener in the cream had a significant impact on IVRRs. Regarding the consistency of marketed samples, FDA guidelines supported a consistent conclusion, while NMPA and EMA guidelines reached the opposite conclusion, which were primarily attributed to different acceptance criteria outlined in the three regulatory guidelines.
Conclusions: Additional strategies are needed to ensure consistent therapeutic outcomes of butenafine hydrochloride cream throughout its life cycles, such as stricter control of stearyl alcohol dosage during manufacturing. Further research is needed to explore appropriate limits for consistency assessment of it. Immersion Cells offers the advantage of lower cost in routine quality control and its application in IVRT for semisolid formulations merits further expansion.
{"title":"An in vitro release test method with Immersion Cells for evaluation of drug release performance of butenafine hydrochloride cream.","authors":"Ping Li, Rongqin Zhang, Xin Li, Hong Chen, Ping Zheng, Li Xie","doi":"10.1080/03639045.2025.2600006","DOIUrl":"10.1080/03639045.2025.2600006","url":null,"abstract":"<p><strong>Objective: </strong>To establish an <i>in vitro</i> release (IVR) method for butenafine hydrochloride cream using Immersion Cells and compare the drug release characteristics of commercial samples.</p><p><strong>Significance: </strong>Reevaluating post-listing semisolid drug products based on quality attributes of IVR performance is crucial for guaranteeing clinical efficacy.</p><p><strong>Methods: </strong>An <i>in vitro</i> release testing (IVRT) method using Immersion Cells was developed and validated for sensitivity, linearity, and reproducibility. It was adapted for use with Vertical Diffusion Cells (VDCs) to compare two devices. Univariate tests were conducted to assess the effect of excipients on <i>in vitro</i> release rates (IVRRs). Three regulatory guidelines recommended by FDA, NMPA and EMA for IVR performance consistency assessment were compared to evaluate the sameness of marketed samples.</p><p><strong>Results: </strong>For IVRT of butenafine hydrochloride cream, Immersion Cells exhibited the same functionality as VDCs. Stearyl alcohol which serves as oil phase matrix and thickener in the cream had a significant impact on IVRRs. Regarding the consistency of marketed samples, FDA guidelines supported a consistent conclusion, while NMPA and EMA guidelines reached the opposite conclusion, which were primarily attributed to different acceptance criteria outlined in the three regulatory guidelines.</p><p><strong>Conclusions: </strong>Additional strategies are needed to ensure consistent therapeutic outcomes of butenafine hydrochloride cream throughout its life cycles, such as stricter control of stearyl alcohol dosage during manufacturing. Further research is needed to explore appropriate limits for consistency assessment of it. Immersion Cells offers the advantage of lower cost in routine quality control and its application in IVRT for semisolid formulations merits further expansion.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"423-434"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145761595","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}
Pub Date : 2026-02-01Epub Date: 2025-12-13DOI: 10.1080/03639045.2025.2600647
Soji Soman, Priyanka Venkatesan, P N Remya
Objective: To provide a comprehensive overview of recent advancements in transdermal drug delivery systems (TDDSs), with a focus on their design, development, evaluation, and therapeutic importance.
Significance of review: TDDSs offer a noninvasive route of drug administration that bypasses gastrointestinal metabolism, enhances patient compliance, and improves pharmacokinetic profiles. Over the past two decades, their role in controlled drug delivery has increased significantly.
Key findings: This review traces the evolution of TDDSs from first-generation systems to modern formulations, highlighting key properties such as drug lipophilicity, molecular size, optimal pH, and potential for skin irritation. Major formulation strategies-membrane permeation, matrix diffusion, and microreservoir systems-are discussed. Testing methodologies, including physicochemical characterization, in vitro diffusion studies, and in vivo evaluations, have also been explored. Advancements in TDDSs have led to the development of more effective transdermal patches capable of increasing skin permeability and expanding the range of drugs that can be delivered. Despite limitations such as difficulty in delivering large- or high-dose molecules, TDDSs demonstrate improved therapeutic efficiency and better patient adherence.
Conclusions: TDDSs represent a significant innovation in drug delivery, offering several advantages over conventional routes. The ongoing development of these materials holds promise for broader clinical applications and improved therapeutic outcomes.
{"title":"Advancing transdermal drug delivery systems: breakthrough innovations, comprehensive evaluation approaches for optimized therapeutic efficacy and patient outcomes.","authors":"Soji Soman, Priyanka Venkatesan, P N Remya","doi":"10.1080/03639045.2025.2600647","DOIUrl":"10.1080/03639045.2025.2600647","url":null,"abstract":"<p><strong>Objective: </strong>To provide a comprehensive overview of recent advancements in transdermal drug delivery systems (TDDSs), with a focus on their design, development, evaluation, and therapeutic importance.</p><p><strong>Significance of review: </strong>TDDSs offer a noninvasive route of drug administration that bypasses gastrointestinal metabolism, enhances patient compliance, and improves pharmacokinetic profiles. Over the past two decades, their role in controlled drug delivery has increased significantly.</p><p><strong>Key findings: </strong>This review traces the evolution of TDDSs from first-generation systems to modern formulations, highlighting key properties such as drug lipophilicity, molecular size, optimal pH, and potential for skin irritation. Major formulation strategies-membrane permeation, matrix diffusion, and microreservoir systems-are discussed. Testing methodologies, including physicochemical characterization, <i>in vitro</i> diffusion studies, and <i>in vivo</i> evaluations, have also been explored. Advancements in TDDSs have led to the development of more effective transdermal patches capable of increasing skin permeability and expanding the range of drugs that can be delivered. Despite limitations such as difficulty in delivering large- or high-dose molecules, TDDSs demonstrate improved therapeutic efficiency and better patient adherence.</p><p><strong>Conclusions: </strong>TDDSs represent a significant innovation in drug delivery, offering several advantages over conventional routes. The ongoing development of these materials holds promise for broader clinical applications and improved therapeutic outcomes.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"213-227"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145713654","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}
Pub Date : 2026-02-01Epub Date: 2025-12-15DOI: 10.1080/03639045.2025.2599468
Pelin Eroglu, Selda Doğan Çalhan, Hamide Doğan
Objective: Silver nanoparticles (AgNPs) are widely utilized in anti-migratory applications due to their beneficial physicochemical and biological properties. This study aimed to evaluate the in vitro cytotoxic and anti-migratory effects of AgNPs synthesized using the above-ground parts (stems, flowers, and leaves) of Onosma mutabilis (O. mutabilis).
Significance: Green-synthesized AgNPs derived from O. mutabilis exhibit notable cytotoxic and anti-migratory effects on A549 cells, offering dual-functional potential. Their biocompatibility and capacity for targeted release in acidic tumor microenvironments make them promising candidates for sustainable cancer therapies.
Methods: AgNPs were green-synthesized using aqueous plant extracts and characterized by ultraviolet-visible spectroscopy (UV-Vis spectroscopy), X-ray diffraction (XRD), fourier transform infrared (FTIR), and scanning electron microscopy (SEM). Cytotoxicity against A549 cells was assessed via the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay and anti-migratory effects were examined using a scratch assay.
Results: UV-Vis spectroscopy confirmed the formation of AgNPs synthesized from O. mutabilis extracts by showing a characteristic absorption band around 420-480 nm. XRD analysis revealed their crystalline structure, while SEM demonstrated predominantly spherical morphology. MTT assay indicated that the AgNPs, especially those derived from the flower extract, significantly reduced A549 cell viability in a dose- and time-dependent manner, with an IC50 value of 5.28 µg/mL. In addition, wound healing assays confirmed their strong anti-migratory activity.
Conclusion: These findings suggest that green-synthesized AgNPs induce cytotoxic and anti-migratory effects, highlighting their potential as therapeutic agents against A549 lung cancer cells.
目的银纳米颗粒（AgNPs）具有良好的物理化学和生物学特性，在抗迁移方面得到了广泛的应用。本研究旨在评价以野牡丹（Onosma mutabilis， O. mutabilis）地上部分（茎、花和叶）合成的AgNPs的体外细胞毒和抗迁移作用。绿色合成的来自O. mutabilis的AgNPs对A549细胞具有显著的细胞毒性和抗迁移作用，具有双重功能潜力。它们的生物相容性和在酸性肿瘤微环境中靶向释放的能力使它们成为可持续癌症治疗的有希望的候选者。方法采用植物水提液绿色合成sagnps，并采用紫外可见光谱（UV-Vis）、x射线衍射（XRD）、傅里叶变换红外光谱（FTIR）和扫描电镜（SEM）对其进行表征。通过3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四唑（MTT）法评估对A549细胞的细胞毒性，并通过划痕法检测抗迁移作用。结果紫外-可见光谱在420 ~ 480nm处显示了AgNPs的形成。XRD分析显示其晶体结构，SEM分析显示其主要呈球形。MTT实验表明，AgNPs，特别是来自花提取物的AgNPs，显著降低A549细胞的活力，且呈剂量和时间依赖性，IC50值为5.28 µg/mL。此外，伤口愈合实验证实其具有较强的抗迁移活性。结论绿色合成的AgNPs具有细胞毒性和抗迁移作用，具有治疗A549肺癌的潜力。
{"title":"<i>Onosma mutabilis-</i>mediated silver nanoparticles target lung cancer cell viability and migration: <i>in vitro</i> evidence from A549 model.","authors":"Pelin Eroglu, Selda Doğan Çalhan, Hamide Doğan","doi":"10.1080/03639045.2025.2599468","DOIUrl":"10.1080/03639045.2025.2599468","url":null,"abstract":"<p><strong>Objective: </strong>Silver nanoparticles (AgNPs) are widely utilized in anti-migratory applications due to their beneficial physicochemical and biological properties. This study aimed to evaluate the <i>in vitro</i> cytotoxic and anti-migratory effects of AgNPs synthesized using the above-ground parts (stems, flowers, and leaves) of <i>Onosma mutabilis (O. mutabilis).</i></p><p><strong>Significance: </strong>Green-synthesized AgNPs derived from <i>O. mutabilis</i> exhibit notable cytotoxic and anti-migratory effects on A549 cells, offering dual-functional potential. Their biocompatibility and capacity for targeted release in acidic tumor microenvironments make them promising candidates for sustainable cancer therapies.</p><p><strong>Methods: </strong>AgNPs were green-synthesized using aqueous plant extracts and characterized by ultraviolet-visible spectroscopy (UV-Vis spectroscopy), X-ray diffraction (XRD), fourier transform infrared (FTIR), and scanning electron microscopy (SEM). Cytotoxicity against A549 cells was assessed <i>via</i> the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay and anti-migratory effects were examined using a scratch assay.</p><p><strong>Results: </strong>UV-Vis spectroscopy confirmed the formation of AgNPs synthesized from <i>O. mutabilis</i> extracts by showing a characteristic absorption band around 420-480 nm. XRD analysis revealed their crystalline structure, while SEM demonstrated predominantly spherical morphology. MTT assay indicated that the AgNPs, especially those derived from the flower extract, significantly reduced A549 cell viability in a dose- and time-dependent manner, with an IC<sub>50</sub> value of 5.28 µg/mL. In addition, wound healing assays confirmed their strong anti-migratory activity.</p><p><strong>Conclusion: </strong>These findings suggest that green-synthesized AgNPs induce cytotoxic and anti-migratory effects, highlighting their potential as therapeutic agents against A549 lung cancer cells.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"366-376"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145687339","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}
Pub Date : 2026-02-01Epub Date: 2025-12-12DOI: 10.1080/03639045.2025.2592675
Malik Muhammad Imtiaz, Sheikh Abdur Rashid, Faiza Naseem, Nauman Rahim Khan, Kalim Ullah, Muhammad Khalid Khan, Pervaiz Akhtar Shah, Farooq Bashir Butt, Amina Riaz, Khalid J Alzahrani, Khalaf F Alsharif, Abul Kalam Azad
Background: Metformin is gold standard for polycystic ovary syndrome (PCOS), but associated with gastrointestinal side effects, leading to poor patient adherence. Present oral fast-dissolving films (OFDFs) offer rapid disintegration, improving drug delivery, therapeutic outcomes, and patient compliance.
Objective: This project aimed to fabricate metformin-loaded OFDFs to enhance patient compliance and drug efficacy in treatment of PCOS.
Methods: Metformin-loaded OFDFs were prepared using solvent casting method with hydroxypropyl methylcellulose (HPMC) and gelatin as film-forming polymers and propylene glycol as a plasticizer. The Box-Behnken experimental design was utilized for optimization. Various physico-chemical characterization tests, including thickness, weight, folding endurance, percent elongation, water content, and moisture uptake, were conducted. In vitro drug release, disintegration time, and mechanical strength were analyzed. Additionally, a pharmacokinetic study in rats was conducted to compare plasma concentrations of optimized formulation with those of metformin intragastric solution.
Results: A stable drug-loaded formulations with a uniform surface and an amorphous nature of drug were prepared in OFDFs. The optimized formulation demonstrated significant drug release at 5 min (98.9%), a rapid disintegration time (19.2 sec), and good mechanical strength (7.4 MPa) (ANOVA, p < .05). Furthermore, increased values of Cmax as well as AUC0-t were also observed in plasma of rats treated with optimized formulation (MF7) as compared to those administered with metformin intragastric solution (Student t-test, p < .05).
Conclusion: Results cemented a very rapid disintegration and dissolution of OFDF, suggesting a promising substitute to enhance patient adherence and reduce metformin onset time in treating PCOS.
{"title":"Polymeric oral fast dissolving films of metformin: fabrication, optimization, <i>in vitro,</i> and <i>in vivo</i> evaluation.","authors":"Malik Muhammad Imtiaz, Sheikh Abdur Rashid, Faiza Naseem, Nauman Rahim Khan, Kalim Ullah, Muhammad Khalid Khan, Pervaiz Akhtar Shah, Farooq Bashir Butt, Amina Riaz, Khalid J Alzahrani, Khalaf F Alsharif, Abul Kalam Azad","doi":"10.1080/03639045.2025.2592675","DOIUrl":"10.1080/03639045.2025.2592675","url":null,"abstract":"<p><strong>Background: </strong>Metformin is gold standard for polycystic ovary syndrome (PCOS), but associated with gastrointestinal side effects, leading to poor patient adherence. Present oral fast-dissolving films (OFDFs) offer rapid disintegration, improving drug delivery, therapeutic outcomes, and patient compliance.</p><p><strong>Objective: </strong>This project aimed to fabricate metformin-loaded OFDFs to enhance patient compliance and drug efficacy in treatment of PCOS.</p><p><strong>Methods: </strong>Metformin-loaded OFDFs were prepared using solvent casting method with hydroxypropyl methylcellulose (HPMC) and gelatin as film-forming polymers and propylene glycol as a plasticizer. The Box-Behnken experimental design was utilized for optimization. Various physico-chemical characterization tests, including thickness, weight, folding endurance, percent elongation, water content, and moisture uptake, were conducted. <i>In vitro</i> drug release, disintegration time, and mechanical strength were analyzed. Additionally, a pharmacokinetic study in rats was conducted to compare plasma concentrations of optimized formulation with those of metformin intragastric solution.</p><p><strong>Results: </strong>A stable drug-loaded formulations with a uniform surface and an amorphous nature of drug were prepared in OFDFs. The optimized formulation demonstrated significant drug release at 5 min (98.9%), a rapid disintegration time (19.2 sec), and good mechanical strength (7.4 MPa) (ANOVA, <i>p</i> < .05). Furthermore, increased values of C<sub>max</sub> as well as AUC<sub>0-t</sub> were also observed in plasma of rats treated with optimized formulation (MF7) as compared to those administered with metformin intragastric solution (Student t-test, <i>p</i> < .05).</p><p><strong>Conclusion: </strong>Results cemented a very rapid disintegration and dissolution of OFDF, suggesting a promising substitute to enhance patient adherence and reduce metformin onset time in treating PCOS.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"277-290"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145582026","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}
Objective: The main objective of this article was to explore the therapeutic potential of intranasally administered metal/metal oxide nanoparticles (NPs) for treating central nervous system (CNS) disorders. Significance of review Metal/metal oxide NPs offer new possibilities for brain imaging and targeted drug delivery. These NPs can be delivered intranasally with minimal invasiveness, offering a patient-friendly approach for therapeutic applications. The current article synthesizes research studies on the potential of intranasal metal/metal oxide NPs for treating CNS disorders, focusing on their unique features, transport pathways, therapeutic and diagnostic benefits, and neurotoxicological challenges.
Key findings: The small size and high surface area of metal/metal oxide NPs enable efficient drug encapsulation and direct delivery to the brain via the olfactory and trigeminal pathways, bypassing the blood-brain barrier. These NPs exhibit tunable surface chemistry, allowing functionalization with ligands or coatings to enhance biocompatibility and reduce neurotoxicity. Additionally, these NPs can show inherent therapeutic properties, such as antioxidant or anti-inflammatory effects, which further support neuroprotection.
Conclusions: Intranasal delivery of metallic NPs is an emerging strategy for drug delivery and imaging, particularly for targeting CNS disorders. However, the development of novel NPs with minimal neurotoxicity is crucial to ensuring their safety and efficacy for clinical applications.
{"title":"Intranasal delivery of metal/metal oxide nanoparticles for the management of CNS-related diseases: theranostic and toxicity issues.","authors":"Samin Hamidi, Zahra Esmaeili Moghaddam, Mitra Alami-Milani, Maryam Azarfarin, Shirin Ahmadi, Fereshteh Valipour, Sara Salatin","doi":"10.1080/03639045.2025.2603418","DOIUrl":"10.1080/03639045.2025.2603418","url":null,"abstract":"<p><strong>Objective: </strong>The main objective of this article was to explore the therapeutic potential of intranasally administered metal/metal oxide nanoparticles (NPs) for treating central nervous system (CNS) disorders. Significance of review Metal/metal oxide NPs offer new possibilities for brain imaging and targeted drug delivery. These NPs can be delivered intranasally with minimal invasiveness, offering a patient-friendly approach for therapeutic applications. The current article synthesizes research studies on the potential of intranasal metal/metal oxide NPs for treating CNS disorders, focusing on their unique features, transport pathways, therapeutic and diagnostic benefits, and neurotoxicological challenges.</p><p><strong>Key findings: </strong>The small size and high surface area of metal/metal oxide NPs enable efficient drug encapsulation and direct delivery to the brain <i>via</i> the olfactory and trigeminal pathways, bypassing the blood-brain barrier. These NPs exhibit tunable surface chemistry, allowing functionalization with ligands or coatings to enhance biocompatibility and reduce neurotoxicity. Additionally, these NPs can show inherent therapeutic properties, such as antioxidant or anti-inflammatory effects, which further support neuroprotection.</p><p><strong>Conclusions: </strong>Intranasal delivery of metallic NPs is an emerging strategy for drug delivery and imaging, particularly for targeting CNS disorders. However, the development of novel NPs with minimal neurotoxicity is crucial to ensuring their safety and efficacy for clinical applications.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"248-260"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145740260","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}
Objective: This review article outlines the transformative impact of Artificial Intelligence (AI) in the pharmaceutical sciences, focusing on its integration with modern technologies and its role in advancing medication research, development, production, and digital transformation.
Significance: AI, through its synergy with machine learning (ML), deep learning (DL), and Industry 4.0 technologies such as the Internet of Things (IoT), robotics, blockchain, and digital twins, is pivotal in advancing personalized healthcare and adaptive manufacturing processes.
Methods: This article reviews AI technologies to analyze complex datasets, enhancing real-time decision-making, predictive analytics, and supply chain optimization. This approach allows for the development of personalized medicines using genomic, clinical, and environmental data.
Results: The application of AI has significantly improved operational efficiency and facilitated the tailored production of medications. However, challenges such as data privacy, algorithmic bias, and the need for updated regulations remain prevalent.
Conclusions: Addressing these issues through ethical frameworks and comprehensive training is essential. The ongoing evolution of AI promises to bolster digital transformation, promote sustainable manufacturing, and improve global healthcare outcomes, setting a course toward innovation and patient-centric solutions in pharmaceutical sciences.
{"title":"The Future trends of Artificial Intelligence and innovative technologies in the new era of pharmaceutical sciences and Industry 4.0.","authors":"Phuvamin Suriyaamporn, Boonnada Pamornpathomkul, Tanasait Ngawhirunpat, Prasert Akkaramongkolporn, Praneet Opanasopit","doi":"10.1080/03639045.2025.2590707","DOIUrl":"10.1080/03639045.2025.2590707","url":null,"abstract":"<p><strong>Objective: </strong>This review article outlines the transformative impact of Artificial Intelligence (AI) in the pharmaceutical sciences, focusing on its integration with modern technologies and its role in advancing medication research, development, production, and digital transformation.</p><p><strong>Significance: </strong>AI, through its synergy with machine learning (ML), deep learning (DL), and Industry 4.0 technologies such as the Internet of Things (IoT), robotics, blockchain, and digital twins, is pivotal in advancing personalized healthcare and adaptive manufacturing processes.</p><p><strong>Methods: </strong>This article reviews AI technologies to analyze complex datasets, enhancing real-time decision-making, predictive analytics, and supply chain optimization. This approach allows for the development of personalized medicines using genomic, clinical, and environmental data.</p><p><strong>Results: </strong>The application of AI has significantly improved operational efficiency and facilitated the tailored production of medications. However, challenges such as data privacy, algorithmic bias, and the need for updated regulations remain prevalent.</p><p><strong>Conclusions: </strong>Addressing these issues through ethical frameworks and comprehensive training is essential. The ongoing evolution of AI promises to bolster digital transformation, promote sustainable manufacturing, and improve global healthcare outcomes, setting a course toward innovation and patient-centric solutions in pharmaceutical sciences.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"183-196"},"PeriodicalIF":2.2,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145530542","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}
Objective: This study aimed to develop and evaluate a dermal gel formulation incorporating the methanolic leaf extract of Guiera senegalensis (GS) for potential topical antimicrobial application.
Significance: Dermal gel formulations of GS leaf extracts may offer safe and effective alternatives against bacterial and fungal skin infections, particularly beneficial for pediatric and geriatric individuals who are most susceptible to such conditions.
Methods: Leaves of GS were extracted by maceration using methanol and fractionated with solvents of increasing polarity. The extract and fractions underwent phytochemical screening, antibacterial evaluation, and spectral characterization (GC-MS and FT-IR). Xanthan gum-based gels were formulated and evaluated for pH, viscosity, spreadability, extrudability, swelling, erosion, and antibacterial activity.
Results: The methanolic extract (26.36% yield) contained abundant phytochemicals, including flavonoids, phenolics, tannins, and terpenoids. Fractionation revealed the polarity-based distribution of phytochemicals but did not enhance antibacterial potency. The methanolic extract showed the strongest activity against Staphylococcus aureus (22.24 ± 0.12 mm). GC-MS and FT-IR confirmed the presence of bioactive compounds and functional groups linked to antimicrobial effects. The gels exhibited skin-compatible pH (5.95-6.65), appropriate viscosity (11.23-63.23 Pa·s), and desirable spreadability. Among all, formulation F2 showed the best overall characteristics for topical use.
Conclusion: GS leaf extract-loaded gels demonstrated excellent physicochemical properties and antibacterial activity. Although fractionation provided no added antimicrobial advantage, it offered insights into phytochemical distribution. Formulation F2 represents a promising natural, plant-based topical antimicrobial candidate.
{"title":"Dermal gel formulation of <i>Guiera senegalensis</i> (sabara) leaf extract: development, characterisation, and antibacterial evaluation.","authors":"Nafiu Aminu, Abdulrahman Haliru Sidi, Zainab Attahiru, Thatayaone Monkgogi, Siok-Yee Chan, Mumuni Audu Momoh, Umar Zaki Faruq","doi":"10.1080/03639045.2026.2614374","DOIUrl":"10.1080/03639045.2026.2614374","url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to develop and evaluate a dermal gel formulation incorporating the methanolic leaf extract of <i>Guiera senegalensis</i> (GS) for potential topical antimicrobial application.</p><p><strong>Significance: </strong>Dermal gel formulations of GS leaf extracts may offer safe and effective alternatives against bacterial and fungal skin infections, particularly beneficial for pediatric and geriatric individuals who are most susceptible to such conditions.</p><p><strong>Methods: </strong>Leaves of GS were extracted by maceration using methanol and fractionated with solvents of increasing polarity. The extract and fractions underwent phytochemical screening, antibacterial evaluation, and spectral characterization (GC-MS and FT-IR). Xanthan gum-based gels were formulated and evaluated for pH, viscosity, spreadability, extrudability, swelling, erosion, and antibacterial activity.</p><p><strong>Results: </strong>The methanolic extract (26.36% yield) contained abundant phytochemicals, including flavonoids, phenolics, tannins, and terpenoids. Fractionation revealed the polarity-based distribution of phytochemicals but did not enhance antibacterial potency. The methanolic extract showed the strongest activity against <i>Staphylococcus aureus</i> (22.24 ± 0.12 mm). GC-MS and FT-IR confirmed the presence of bioactive compounds and functional groups linked to antimicrobial effects. The gels exhibited skin-compatible pH (5.95-6.65), appropriate viscosity (11.23-63.23 Pa·s), and desirable spreadability. Among all, formulation F2 showed the best overall characteristics for topical use.</p><p><strong>Conclusion: </strong>GS leaf extract-loaded gels demonstrated excellent physicochemical properties and antibacterial activity. Although fractionation provided no added antimicrobial advantage, it offered insights into phytochemical distribution. Formulation F2 represents a promising natural, plant-based topical antimicrobial candidate.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-19"},"PeriodicalIF":2.2,"publicationDate":"2026-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145932703","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}
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