Pharmaceutical Development and Technology最新文献_第3页

The chrysin solid dispersion prepared using polyvinylpyrrolidone K40 demonstrates enhanced solubility and a thermogenesis-promoting effect on adipocytes. 用聚乙烯吡咯烷酮K40制备的菊花素固体分散体具有增强溶解度和促进脂肪细胞生热的作用。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-07-28 DOI: 10.1080/10837450.2026.2708937

Wenchen Tao, Jinwei Wang, Yan Lin, Xian Zhang, Juan Chen, Jian Liu

{"title":"The chrysin solid dispersion prepared using polyvinylpyrrolidone K40 demonstrates enhanced solubility and a thermogenesis-promoting effect on adipocytes.","authors":"Wenchen Tao, Jinwei Wang, Yan Lin, Xian Zhang, Juan Chen, Jian Liu","doi":"10.1080/10837450.2026.2708937","DOIUrl":"10.1080/10837450.2026.2708937","url":null,"abstract":"Chrysin, a natural flavonoid compound found in honey, propolis, and various plant sources, was reported to promote adipocyte thermogenesis and improve metabolism in obese mice. However, its clinical application is hindered by poor water solubility and low bioavailability. In this study, water-soluble chrysin solid dispersions were prepared using polyvinylpyrrolidone (K10, K40, K90), polyethylene glycol (1000, 2000, 6000), and maltitol. Among these, polyvinylpyrrolidone K40 (PVPK40) was identified as the optimal carrier for preparing PVPK40-chrysin solid dispersion (PVPK40-Chy SD), achieving a 1200-fold higher aqueous solubility than crystalline chrysin. The PVPK40-Chy SD exhibited a more soluble amorphous structure compared to crystalline chrysin. Hydrogen bonding interactions were observed between chrysin and the carrier. Additionally, an in vitro digestion model confirmed the improved dissolution behavior of chrysin. Finally, in vivo and in vitro experiments have demonstrated that the water-soluble chrysin solution, which was formed by dissolving PVPK40-Chy SD in water, can effectively promote adipocyte thermogenesis in C3H10T1/2 cells and mice. The mean UCP1 protein level in the water-soluble chrysin-treated group reached 2.02-fold that of the control group, thereby stimulating adipocyte thermogenesis. Following 2 h of cold exposure, mice in the water-soluble chrysin-treated group exhibited a mean rectal temperature 3.2 °C higher than animals in the PVPK40 carrier group, indicating remarkably enhanced cold tolerance.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1109-1125"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148550004","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

Enhanced solubility and bioavailability of zanubrutinib nanocrystals: physicochemical and pharmacokinetic evaluation. 扎鲁替尼纳米晶体的溶解度和生物利用度增强：物理化学和药代动力学评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-08 DOI: 10.1080/10837450.2026.2696448

Vrushti Kansara, Yashraj Mahajan, Bhavin Vyas, Vishweshwari Chauhan, Mitali Patel

{"title":"Enhanced solubility and bioavailability of zanubrutinib nanocrystals: physicochemical and pharmacokinetic evaluation.","authors":"Vrushti Kansara, Yashraj Mahajan, Bhavin Vyas, Vishweshwari Chauhan, Mitali Patel","doi":"10.1080/10837450.2026.2696448","DOIUrl":"10.1080/10837450.2026.2696448","url":null,"abstract":"The present study focuses on the development of zanubrutinib nanocrystals (ZBR-NCs) to enhance its solubility, dissolution rate and oral bioavailability. The ZBR-NCs were successfully prepared by antisolvent precipitation method and subjected to physicochemical and pharmacokinetic evaluations. The resulting nanocrystals exhibited a particle size of 258.8 ± 12.56 nm, a polydispersity index value of 0.24 ± 0.02, a zeta potential of -18.4 ± 1.40 mV, and drug content of 93.56 ± 2.5%. The solubility studies revealed a 57-fold increase in ZBR solubility as compared to the pure drug. The solid-state characterization studies confirmed reduced crystallinity of the ZBR within the nanocrystals and its compatibility with Poloxamer 188® as a stabilizing agent. The spherical shape of ZBR-NCs was demonstrated by high-resolution transmission electron microscopy study. The ZBR-NCs exhibited 98.67 ± 3.49% release at 10 h, showing an increased ZBR release as compared to free ZBR. Pharmacokinetic evaluation of ZBR-NCs after oral administration displayed a 4.41-fold increase (p < 0.001) in bioavailability. The stability study of ZBR-NCs showed good stability over a 2-month period at refrigerated (2-8 °C) condition, with retention of their physicochemical properties. Collectively, these findings emphasize the potential of ZBR-NCs as a promising strategy to improve solubility and oral absorption of ZBR. HIGHLIGHTSThe ZBR-NCs were prepared using PVPK-30, Poloxamer 407® and Poloxamer 188®.The solubility of ZBR was improved 57-fold with NCs.The ZBR-NCs showed higher drug release than free ZBR.The ZBR-NCs achieved a 4.41-fold increase in bioavailability.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"977-989"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148346099","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

Compression equations in pharmaceutical tableting: from classical compaction models to data-driven and mechanistic approaches. 药物压片中的压缩方程：从经典压片模型到数据驱动和机械方法。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-06-24 DOI: 10.1080/10837450.2026.2694094

Tansel Comoglu

{"title":"Compression equations in pharmaceutical tableting: from classical compaction models to data-driven and mechanistic approaches.","authors":"Tansel Comoglu","doi":"10.1080/10837450.2026.2694094","DOIUrl":"10.1080/10837450.2026.2694094","url":null,"abstract":"Powder compaction remains the key step in pharmaceutical tablet manufacturing, but its multiscale and path-dependent nature makes accurate prediction of tablet properties difficult. Compression equations have long been used to relate applied pressure to densification, porosity, and mechanical strength, providing descriptors for material comparison and formulation design. Classical models such as Heckel, Kawakita-Lüdde, and Cooper-Eaton remain widely used, although they are limited by pressure-range dependence, sensitivity to in-die versus out-of-die measurements, and restricted mechanistic interpretation. Recent developments have expanded compression modeling to include extended in-die formulations incorporating solid compressibility, continuum constitutive laws for finite-element simulations, particle-scale discrete-element approaches, and data-driven process analytical technology (PAT) frameworks. These approaches are critically evaluated alongside classical equations with respect to constitutive validity, calibration transferability, contact-law realism, computational cost, data governance, model drift, and regulatory acceptability. Together, they form a hierarchical modeling framework spanning empirical screening, mechanistic prediction, and real-time process control. This review integrates classical and emerging compaction models and discusses their relevance to critical quality attributes, scale-up, and digital-twin-enabled pharmaceutical manufacturing.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"935-956"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148302607","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

Taste-Masked orodispersible tablets of alfuzosin hydrochloride: response surface methodology (RSM) based approach for enhanced patient compliance in BPH management. 盐酸阿呋唑星掩味或分散片：基于响应面法（RSM）的BPH治疗依从性提高方法。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-29 DOI: 10.1080/10837450.2026.2707519

Majid Imam, Neeraj Gupta, Somesh Narayan, Kalpana Nagpal

{"title":"Taste-Masked orodispersible tablets of alfuzosin hydrochloride: response surface methodology (RSM) based approach for enhanced patient compliance in BPH management.","authors":"Majid Imam, Neeraj Gupta, Somesh Narayan, Kalpana Nagpal","doi":"10.1080/10837450.2026.2707519","DOIUrl":"10.1080/10837450.2026.2707519","url":null,"abstract":"Alfuzosin hydrochloride, an α1-adrenergic antagonist used in the treatment of benign prostatic hyperplasia (BPH), was formulated as orodispersible tablets (ODTs) to improve patient compliance, particularly in geriatric patients with dysphagia. Tablets were prepared by direct compression using microcrystalline cellulose as a filler-binder, crospovidone as a superdisintegrant, magnesium stearate as a lubricant, and aspartame (2%) as a taste-masking agent. Pre-compression studies confirmed satisfactory flow properties, compressibility, and drug-excipient compatibility. A Box-Behnken Design (BBD) was employed to evaluate the effects of crospovidone, microcrystalline cellulose, and magnesium stearate on friability, hardness, disintegration time, and drug release, enabling optimization of critical quality attributes. Numerical desirability optimization identified the optimized formulation containing 9.44% crospovidone, 49.49% microcrystalline cellulose, and 0.50% magnesium stearate, with an overall desirability of 0.997. The optimized formulation showed rapid disintegration (10.72 sec), low friability (0.261%), adequate hardness (5.28 kg/cm2), and 99.21% drug release within initial 15 min. Taste evaluation using an Alpha MOS electronic tongue confirmed effective masking of the drug's inherent bitterness and the study demonstrated the potential of optimized ODTs as a patient-friendly dosage form for effective BPH management.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1050-1070"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148550016","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

Intradermal delivery of lidocaine hydrochloride using dissolving microneedles: in vitro dermatokinetic test and in vivo anesthetic activity assessment. 溶解微针法给药盐酸利多卡因：体外皮动学试验及体内麻醉活性评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-04 DOI: 10.1080/10837450.2026.2695295

Delly Ramadon, Okto Tri Hamda, Ellizabeth Natawidjaya, Choon Fu Goh, Yahdiana Harahap, Fadlina Chany Saputri, Pietradewi Hartrianti, Faradilla Muliawardani, Nadhifa Ayu Nisrina, Callista Andinie Mulyadi, Yohan Baptista Adidharma Willie

{"title":"Intradermal delivery of lidocaine hydrochloride using dissolving microneedles: in vitro dermatokinetic test and in vivo anesthetic activity assessment.","authors":"Delly Ramadon, Okto Tri Hamda, Ellizabeth Natawidjaya, Choon Fu Goh, Yahdiana Harahap, Fadlina Chany Saputri, Pietradewi Hartrianti, Faradilla Muliawardani, Nadhifa Ayu Nisrina, Callista Andinie Mulyadi, Yohan Baptista Adidharma Willie","doi":"10.1080/10837450.2026.2695295","DOIUrl":"10.1080/10837450.2026.2695295","url":null,"abstract":"Lidocaine hydrochloride (LiH) is a widely used local anesthetic administered topically or parenterally. However, passive delivery of LiH through the skin is hindered by its hydrophilicity and discomfort associated with injections. Dissolving microneedles (DMNs) offer a minimally invasive alternative for intradermal delivery. This study developed LiH-loaded DMNs (LiH-DMNs) using a combination of poly(vinylpyrrolidone) K-29/32 (PVP) and hyaluronic acid (HA). LiH-DMNs were evaluated in terms of their mechanical properties, insertion ability, dissolution, drug content, in vitro dermatokinetic tests, and in vivo local anesthetic tests on rats. Nine formulations were prepared, among which DMN-7 (PVP 30%; HA 1.25%) and DMN-8 (PVP 30%; HA 2.5%) showed needle height reduction of <10% and drug content of 97-100%. Both formulations penetrated skin to a depth of approximately 500 μm and fully dissolved within 1 h In vitro dermatokinetic studies demonstrated higher drug accumulation for DMN-7 (Cmax of 6.75 ± 1.36 μg/mL in the dermis and 7.47 ± 0.97 μg/mL in the epidermis) compared to DMN-8. Consequently, DMN-7 was selected for in vivo evaluation. DMN-7 caused no erythema or edema in irritation studies and produced significant local anesthetic effects in rats. Overall, PVP-HA-based DMNs represent a promising, safe, and effective approach for intradermal delivery of LiH.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"957-976"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148332108","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

Camellia sinensis silver nanoparticles inhibit proliferation and induce PARP-dependent apoptosis in A549 cells: formulation, characterization, and biological evaluation. 茶树银纳米颗粒抑制A549细胞增殖并诱导parp依赖性细胞凋亡：配方、表征和生物学评价

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-18 DOI: 10.1080/10837450.2026.2699219

Waad A Samman, Hesham M Tawfeek, Rawan Bafail, Mahmoud Zaki El-Readi, Safaa Y Eid, Ahmed A H Abdellatif

{"title":"Camellia sinensis silver nanoparticles inhibit proliferation and induce PARP-dependent apoptosis in A549 cells: formulation, characterization, and biological evaluation.","authors":"Waad A Samman, Hesham M Tawfeek, Rawan Bafail, Mahmoud Zaki El-Readi, Safaa Y Eid, Ahmed A H Abdellatif","doi":"10.1080/10837450.2026.2699219","DOIUrl":"10.1080/10837450.2026.2699219","url":null,"abstract":"In this work, the potential anti-cancer activity of silver nanoparticles (AgNPs-CS) prepared using Camellia sinensis, C. sinensis (CS) aqueous extract and its pro-apoptotic effects on human lung adenocarcinoma alveolar (A549) cells were investigated. AgNPs-CS were prepared by reduction of AgNO3 using C. sinensis aqueous extract, CSaq. Furthermore, they were characterized for their size, polydispersity index (PDI), ζ-potentials, morphology, and antioxidant activity. of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), acridine orange/ethidium bromide (AO/EB) staining, and Western blotting techniques were used to measure cell proliferation, apoptosis, and poly (ADP-ribose) polymerase, PARP cleavage. AgNPs-CS had a size, PDI and ζ-potential of 101 nm, 0.12, and -21 ± 1.2 mV, respectively. Furthermore, they are spherical with a core size of ∼20-40 nm and have significant antioxidant activity compared with quercetin. A sigmoidal dose-response curve exhibiting significant concentration-dependent reductions in cell viability was obtained. AgNPs-CS had an IC50 of 6.5 µg/ml and a significant level of apoptosis (∼57%) compared to CSaq and doxorubicin (Dox). Western blot analysis showed a higher level of cleaved PARP, with cPARP/β-actin ratios of 1.8 and 2.9 for CSaq and AgNPs-CS, respectively, confirmed the caspase-dependent apoptosis. AgNPs-CS is a promising green-based nanotherapeutic for treating lung cancer with an enhanced ability to kill cells and cause apoptosis in A549 cells.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"990-1002"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148376669","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

Design and in vivo pharmacokinetic evaluation of a once-daily immediate- and extended-release bilayer tablet of bepotastine salicylate. 每日一次水杨酸贝钾他汀速释和缓释双层片的设计和体内药动学评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-28 DOI: 10.1080/10837450.2026.2706525

Do Hwan Kim, Wookyung Kim, Jinsu Yang, Seonyeong Jeong, Min Young Jeong, In Gyu Yang, Myung Joo Kang, Sun Ho Kim

{"title":"Design and in vivo pharmacokinetic evaluation of a once-daily immediate- and extended-release bilayer tablet of bepotastine salicylate.","authors":"Do Hwan Kim, Wookyung Kim, Jinsu Yang, Seonyeong Jeong, Min Young Jeong, In Gyu Yang, Myung Joo Kang, Sun Ho Kim","doi":"10.1080/10837450.2026.2706525","DOIUrl":"10.1080/10837450.2026.2706525","url":null,"abstract":"Aiming to provide rapid and extended drug release and increase patient adherence, bepotastine salicylate (BEP-S), a selective antihistamine, was formulated into a once-daily bilayer tablet (BLT). The BLT, consisting of immediate-release (IR) and extended-release (ER) layers, was prepared via direct compression and optimized based on mechanical strength, content uniformity, and dissolution performance. The optimized BLT first rapidly released 50% of the BEP-S within 1 h and then provided extended BEP-S release for more than 12 h. In a pharmacokinetic study in beagle dogs, the maximum drug concentration and extent of drug absorption of the once-daily BLT system were comparable to those of the twice-daily IR tablet. The half-life of the once-daily BLT under fasted and fed conditions was longer than that of the twice-daily tablet, with no significant differences in maximum plasma concentration or area under the plasma concentration-time curve between the tablet types. The optimized BLT was stable for 6 months under accelerated conditions (40 °C/75% relative humidity); the appearance, drug content, impurities, and dissolution of the BLT did not notably change during this period. In conclusion, the developed BEP-S BLT is a promising once-daily oral formulation with appropriate IR/ER release characteristics and a bioequivalent pharmacokinetic profile.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1033-1049"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148497871","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

A process-free setup for the preparation of probiotic-loaded electrospun mat as a tailored dressing. 一种无工艺装置，用于制备益生菌负载电纺垫作为定制敷料。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-27 DOI: 10.1080/10837450.2026.2707533

Dorrin Mohtadi Haghighi, Hamid Akbari Javar, Nasrin Samadi, Mohammad Abdollahi, Fatemeh Moraffah, Helia Behrouzfar, Omid Ghaderzadeh, Alireza Vatanara

{"title":"A process-free setup for the preparation of probiotic-loaded electrospun mat as a tailored dressing.","authors":"Dorrin Mohtadi Haghighi, Hamid Akbari Javar, Nasrin Samadi, Mohammad Abdollahi, Fatemeh Moraffah, Helia Behrouzfar, Omid Ghaderzadeh, Alireza Vatanara","doi":"10.1080/10837450.2026.2707533","DOIUrl":"10.1080/10837450.2026.2707533","url":null,"abstract":"Infected burn wounds remain difficult to treat because increasing antibiotic resistance can limit the effectiveness of conventional antimicrobial therapy. Probiotic offers an alternative, but many probiotic dressings require fabrication, encapsulation, or drying procedures that reduce cell viability. This study developed a post-fabrication method for loading probiotics onto electrospun mats and assessed it in a rat model of infected burn wounds, with mupirocin as the control. Poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) electrospun mats were characterized for fiber morphology, water vapor transmission rate, and mechanical properties. Lactiplantibacillus plantarum was loaded onto the prefabricated mats by soaking or spraying, without prior encapsulation or immobilization. Viable cell loading, release, and short-term survival after loading were quantified. Spraying cells suspended in MRS broth, followed by drying at room temperature, produced the highest viable counts on both mats. Agar diffusion and co-culture assays confirmed that the loaded mats retained antimicrobial activity and released active bacterial metabolites. PLA was selected for the in vivo study because it provided suitable mechanical properties, slower cell detachment, and a lower material cost. The L. plantarum-loaded PLA mats accelerated wound closure, collagen organization, and re-epithelialization. This scalable method may simplify manufacturing while supporting point-of-care preparation of wound dressings.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1090-1107"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148549991","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 and biological evaluation of a Cotinus coggygria extract-loaded Pluronic F127-HPMC buccal gel formulation. 载Pluronic F127-HPMC口腔凝胶制剂的研制及生物学评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-08-05 DOI: 10.1080/10837450.2026.2707530

Hayrullah Pakkan, Zehra Keskin, Hümeyra Şahin Bektay, Gülbahar Özge Alim Toraman, Fatma Göç, Zeynep Büşra Erarslan, Ali Asram Sağıroğlu, Meltem Güleç, Gülaçtı Topçu, Aysenur Gunaydin Akyildiz

{"title":"Development and biological evaluation of a Cotinus coggygria extract-loaded Pluronic F127-HPMC buccal gel formulation.","authors":"Hayrullah Pakkan, Zehra Keskin, Hümeyra Şahin Bektay, Gülbahar Özge Alim Toraman, Fatma Göç, Zeynep Büşra Erarslan, Ali Asram Sağıroğlu, Meltem Güleç, Gülaçtı Topçu, Aysenur Gunaydin Akyildiz","doi":"10.1080/10837450.2026.2707530","DOIUrl":"10.1080/10837450.2026.2707530","url":null,"abstract":"Cotinus coggygria Scop. is a polyphenol-rich medicinal plant traditionally used in topical preparations, and the formulation-dependent effects of its extracts on fibroblast behavior remain insufficiently characterized. In this study, a 60% ethanol extract of C. coggygria was prepared and chemically profiled by LC-HRMS, identifying 6-OH-luteolin-7-O-glucoside as a major constituent. In silico bioactivity prediction of this compound indicated the highest mean probability of activity within the membrane/barrier-associated category (mean Pa = 0.895). An optimized Pluronic F127-HPMC gel formulation incorporating the extract was developed and evaluated using human fibroblasts as an in vitro screening model. Intracellular ATP levels were measured to examine potential effects on cellular bioenergetics, and cell migration was assessed by scratch assay. Within the tested concentration range (5-15 µg/mL), treatment with the extract-loaded gel resulted in reduced intracellular ATP levels by 25% and decreased migration modestly, whereas the extract alone did not significantly alter these parameters, indicating a formulation-dependent modulation of cellular response. In an exploratory Caenorhabditis elegans assay, the extract exhibited a biphasic concentration-dependent response, with the lowest concentration tested (3 µg/mL) producing the greatest lifespan extension, whereas higher concentrations (3000-50 000 µg/mL) progressively reduced survival. Collectively, these findings demonstrate that incorporation of C. coggygria extract into a gel matrix alters cellular bioenergetics and motility.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1071-1089"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148550060","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

Thermosensitive hydrogels for sustained semaglutide release: overcoming weight loss plateau in diet-induced obese rats. 用于持续释放西马鲁肽的热敏水凝胶：克服饮食诱导的肥胖大鼠的体重减轻平台期。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-07-01 Epub Date: 2026-07-20 DOI: 10.1080/10837450.2026.2703559

Jing Wang, Hong Hu, Luoxin Long, Hanyu Wan, Jiatong Lv, Yi Yan, Yuji Wang, Shanhong Mao

{"title":"Thermosensitive hydrogels for sustained semaglutide release: overcoming weight loss plateau in diet-induced obese rats.","authors":"Jing Wang, Hong Hu, Luoxin Long, Hanyu Wan, Jiatong Lv, Yi Yan, Yuji Wang, Shanhong Mao","doi":"10.1080/10837450.2026.2703559","DOIUrl":"10.1080/10837450.2026.2703559","url":null,"abstract":"A series of semaglutide-loaded sustained-release formulations is developed using thermosensitive hydrogel as the release system. Micro-needle jet injection (MNJI) devices are used to deliver the highly viscous material and achieve a desired dispersion at delivery. Physicochemical properties, in vitro drug release behavior, and biocompatibility are systematically characterized. Therapeutic efficacy is evaluated in DIO rats, with non-sustained formulation as control to assess efficacy and sustainability. P407-based hydrogel has temperature-dependent sol-gel transition: at low temperature it is injectable, while at body temperature it becomes a solid gel to restrict semaglutide release. Drug incorporation did not interfere with this property. MNJI devices effectively delivered the formulation with consistency and showed favorable safety without severe inflammation. The system prolonged half-life to 15 h, extended Tmax from 8 to 24 h, and maintained effective levels to day 6. In DIO rats, GT10 50 achieved continuous weight loss over 20 days, overcoming the plateau of non-sustained formulations. Serum assays revealed significant reductions in TC (p < 0.01), ALT (p < 0.05), and AST (p < 0.01), indicating improved dyslipidemia and liver injury. Glucose tolerance tests confirmed alleviation of hyperglycemia without hypoglycemia. This study provides a strategy for obesity management with good efficacy and improved compliance via reduced dosing.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1003-1019"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148448694","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