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Mucoadhesive polymeric film with plant-based compounds for dental applications: formulation, characterization and evaluation. 牙科用植物基聚合物粘接膜:配方、表征和评价。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-05-05 DOI: 10.1080/10837450.2025.2498368
Yuliia Maslii, Nataliia Herbina, Lina Dene, Liudas Ivanauskas, Gintaras Matulis, Jurga Bernatoniene
{"title":"Mucoadhesive polymeric film with plant-based compounds for dental applications: formulation, characterization and evaluation.","authors":"Yuliia Maslii, Nataliia Herbina, Lina Dene, Liudas Ivanauskas, Gintaras Matulis, Jurga Bernatoniene","doi":"10.1080/10837450.2025.2498368","DOIUrl":"10.1080/10837450.2025.2498368","url":null,"abstract":"<p><p>Polymeric films are promising formulations for oromucosal drug delivery, particularly for localized treatment of dental diseases. This study focused on developing mucoadhesive films for dental applications, incorporating clove CO<sub>2</sub> extract and essential oils of lavender and grapefruit as active ingredients. The films were prepared using the solvent casting method, with various film-forming agents (sodium alginate, sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl alcohol) used individually and in combinations, without or with plasticizers (glycerol, polyethylene glycol 400, or their mixtures). To optimize the selection of mucoadhesive polymer and plasticizer, properties such as appearance, thickness, pH, moisture content, bursting strength, tensile capacity, elasticity, dissolution, and adhesion, were evaluated. The combination of hydroxyethyl cellulose and hydroxypropyl cellulose with polyethylene glycol 400 was proved most suitable, ensuring superior organoleptic, physicochemical, and textural characteristics. The films demonstrated strong mucoadhesion (9.20 ± 0.58 N), contributing prolonged retention on the mucosa and enhanced bioavailability of the active ingredients. <i>In vitro</i> release studies showed sustained release profile, with approximately 90% of eugenol released during the final film dissolution phase (360-420 min), supporting prolonged therapeutic effects and enhanced local therapy efficacy. The films also exhibited significant antimicrobial activity against a broad spectrum of microorganisms, confirming their potential for treating infectious and inflammatory oral diseases.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"505-520"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144023629","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 characterization of memantine and donepezil loaded 3D scaffolds. 美金刚和多奈哌齐负载3D支架的设计与表征。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-23 DOI: 10.1080/10837450.2025.2493256
Betül Topçu İnce, Samuel Guieu, Selin Seda Timur, Tuba Reçber, Emirhan Nemutlu, Maria Helena Vaz Fernandes, Hakan Eroğlu
{"title":"Design and characterization of memantine and donepezil loaded 3D scaffolds.","authors":"Betül Topçu İnce, Samuel Guieu, Selin Seda Timur, Tuba Reçber, Emirhan Nemutlu, Maria Helena Vaz Fernandes, Hakan Eroğlu","doi":"10.1080/10837450.2025.2493256","DOIUrl":"10.1080/10837450.2025.2493256","url":null,"abstract":"<p><p>Memantine HCl (MEM) and Donepezil HCl (DON) are widely used separately and in combination to treat Alzheimer's disease, and some studies suggest that these drugs may also prevent bone fractures and promote bone regeneration. For this purpose, we formulated fiber-based 3D scaffolds for local delivery of MEM/DON to improve the regeneration process of bone fractures. First, Poly (ε-caprolactone) (PCL)-based MEM/DON-loaded nanofibrous membranes were produced by electrospinning, and then these nanofibrous membranes were transformed into 3D scaffolds using the thermally induced self-agglomeration (TISA) method. Encapsulation efficiency after these two steps was found to be around 20%. Analyses confirmed that the 3D scaffolds have a morphology similar to the extracellular matrix, and that their hydrophilicity, swelling ratio, porosity, and degradation rate were adequate for bone tissue regeneration. Release studies show that the scaffolds provide an initial burst release of the drugs, followed by a sustained release for 21 days. These 3D scaffolds did not show any cytotoxic effect on the L-929 cell line, and increased cell viability over time indicates that they can be used in tissue engineering applications.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"488-504"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144030985","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
Evaluating the color stability of titanium dioxide-free film coats under environmental and light stress. 评价无二氧化钛薄膜涂层在环境和光胁迫下的颜色稳定性。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-10 DOI: 10.1080/10837450.2025.2489005
Jamie C L Chuvalo-Abraham, David Harris, Hyunho Kang, Chiamaka U Ukachukwu, Catherine Guarino
{"title":"Evaluating the color stability of titanium dioxide-free film coats under environmental and light stress.","authors":"Jamie C L Chuvalo-Abraham, David Harris, Hyunho Kang, Chiamaka U Ukachukwu, Catherine Guarino","doi":"10.1080/10837450.2025.2489005","DOIUrl":"10.1080/10837450.2025.2489005","url":null,"abstract":"<p><p>Titanium dioxide (TiO<sub>2</sub>) is an opacifier/colorant in tablet film coatings and capsule shells. Recently, questions about its safety have raised concerns that it may be banned from medicinal products in the European Union (EU); however, little information exists on alternatives to enable the pharmaceutical industry to pivot. This study evaluated the color stability of film coats containing alternate opacifiers, calcium carbonate (CaCO<sub>3</sub>), and rice starch. Placebo tablets were coated with film coating systems containing different polymers (hydroxypropyl methylcellulose (HPMC) or polyvinyl alcohol (PVA)), opacifiers (CaCO<sub>3</sub>, rice starch, or TiO<sub>2</sub>) and pigments (FD&C Blue No. 2, iron oxides, or non-pigmented); the coated tablets were exposed to environmental stress (temperature/humidity) and light stress and color changes were quantified spectrophotometrically. The HPMC-formulated coats containing CaCO<sub>3</sub> or rice starch showed comparable stability to TiO<sub>2</sub>. The PVA-based coats containing FD&C Blue No. 2 or iron oxide colorants exhibited color changes when exposed to elevated temperature/humidity, which was more pronounced with CaCO<sub>3</sub> than with TiO<sub>2</sub>. No meaningful color changes were observed under white or UV light stress for any coat. This study demonstrated PVA coating systems pose a stability risk, whereas these alternate opacifiers presented an overall low color stability risk, offering potential TiO<sub>2</sub> alternatives.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"441-449"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143811978","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
Preparation and characterization of duloxetine-loaded nanofiber scaffold composed of polyvinyl alcohol and chitosan as wound healing agent, fabricated by electrospinning method. 聚乙烯醇-壳聚糖复合伤口愈合剂负载度洛西汀纳米纤维支架的制备及表征
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-11 DOI: 10.1080/10837450.2025.2486797
Kimiya Pourdehghan, Faraz Najafi, Fatemeh Majdi, Nooshafarin Amani, Nasrin Samadi, Hamid Akbari Javar
{"title":"Preparation and characterization of duloxetine-loaded nanofiber scaffold composed of polyvinyl alcohol and chitosan as wound healing agent, fabricated by electrospinning method.","authors":"Kimiya Pourdehghan, Faraz Najafi, Fatemeh Majdi, Nooshafarin Amani, Nasrin Samadi, Hamid Akbari Javar","doi":"10.1080/10837450.2025.2486797","DOIUrl":"10.1080/10837450.2025.2486797","url":null,"abstract":"<p><p>Wound is a disruption in the epithelial integrity of the skin or mucosa, which is caused by internal or external pathological processes. In this study, a nanofiber as wound dressing loaded with Duloxetine was produced by electrospinning technique. The diameter of nanofibers containing 20% and 40% Duloxetine was around 236 nm and 272 nm, respectively. Tensile testing results showed that elongation at break percentage soared from 11.5% for drug-free nanofibers to 40.01% for nanofibers containing 40% Duloxetine. All nanofibers had uniform bead-free structure. Contact angle of nanofibers with and without drug was 84.3° and 99.3°, respectively. The drug release profile revealed that after the burst release over the first 8 h, the curve witnessed a slow sustained release for a longer period. The nanofibers had antibacterial activity against gram-positive and gram-negative bacteria and the crosslinked nanofibers with 40% duloxetine had the largest diameter of inhibition zone at roughly 43 mm for <i>Staphylococcus aureus</i>, 40 mm for <i>Escherichia coli</i>, and 30 mm for <i>Pseudomonas aeruginosa</i>. Clinical studies showed that the percentage of wound area reduction was approximately 96.41% for nanofibers containing 40% duloxetine which was higher than positive control containing phenytoin at around 92.24% and also the other group with 20% duloxetine at 81.68%.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"351-371"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143753928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation and optimization of glycyrrhetinic acid-modified pH-sensitive curcumin liposomes for anti-hepatocellular carcinoma. 甘草次酸修饰ph敏感型抗肝癌姜黄素脂质体的制备及优化。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-02-13 DOI: 10.1080/10837450.2025.2465549
Jie Wang, Xuemei Gu, Xia Gao, Jing Chen, Zhiyang Lv, Siyu Zhang, Siyu Ni, Fei Shi, Xialin Chen, Liang Cao, Zhenzhong Wang, Wei Xiao
{"title":"Formulation and optimization of glycyrrhetinic acid-modified pH-sensitive curcumin liposomes for anti-hepatocellular carcinoma.","authors":"Jie Wang, Xuemei Gu, Xia Gao, Jing Chen, Zhiyang Lv, Siyu Zhang, Siyu Ni, Fei Shi, Xialin Chen, Liang Cao, Zhenzhong Wang, Wei Xiao","doi":"10.1080/10837450.2025.2465549","DOIUrl":"10.1080/10837450.2025.2465549","url":null,"abstract":"<p><p>In order to enhance the therapeutic value of curcumin in liver cancer treatment, glycyrrhetinic acid-modified pH-sensitive curcumin liposomes (GA-pH-Lip@Cur) was developed.GA-pH-Lip@Cur was prepared using a thin film dispersion ultrasonication method, and the optimal formulation process was selected through single-factor experiments and a Box-Behnken design-response surface methodology. The liposomes were evaluated for their morphological appearance, particle size, <i>in vitro</i> release at different pH levels, and biocompatibility. The anti-tumor effect of GA-pH-Lip@Cur was assessed using cell viability assays (CCK-8). The <i>in vivo</i> hepatic targeting and anti-liver tumor efficacy of GA-pH-Lip@Cur were evaluated through pharmacokinetic and pharmacological experiments. The results indicated that optimized GA-pH-Lip@Cur exhibited uniform particle size distribution, good stability, pH-sensitive <i>in vitro</i> release with sustained behavior. Compared to conventional liposomes, GA-pH-Lip@Cur showed prolonged average retention time <i>in vivo</i> and significantly increased curcumin distribution in liver tissues, indicating excellent liver targeting. Both <i>in vitro</i> and <i>in vivo</i> evaluations demonstrated the effectiveness of GA-pH-Lip@Cur in inhibiting liver cancer cell proliferation and suppressing liver tumor growth in tumor-bearing mice. In conclusion, GA-pH-Lip@Cur, by leveraging the acidic tumor microenvironment and overexpression of glycyrrhetinic acid receptors in liver cells, encapsulates curcumin to improve its bioavailability, and target its delivery to the liver tumor sites.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"233-245"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399752","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
Ocular polymeric nanomicelles for the posterior eye segment in the management of retinoblastoma: formulation, optimization, in vitro and ex vivo evaluations. 眼后段聚合物纳米胶束治疗视网膜母细胞瘤:配方、优化、体外和离体评估。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-02-23 DOI: 10.1080/10837450.2025.2469321
Mudassir Ansari, Yogesh A Kulkarni, Kavita Singh
{"title":"Ocular polymeric nanomicelles for the posterior eye segment in the management of retinoblastoma: formulation, optimization, <i>in vitro</i> and <i>ex vivo</i> evaluations.","authors":"Mudassir Ansari, Yogesh A Kulkarni, Kavita Singh","doi":"10.1080/10837450.2025.2469321","DOIUrl":"10.1080/10837450.2025.2469321","url":null,"abstract":"<p><p>The existing study focuses on the development, optimization, and evaluation of sorafenib-loaded polymeric nanomicelles for posterior segment delivery in treating retinoblastoma. The formulation involved adjusting various process and product parameters to create effective drug-loaded polymeric nanomicelles. The particle size, PDI, and zeta potential of optimized formulation were found to be 65.52 ± 1.18 nm, 0.14 ± 0.01, and -3.26 ± 0.66 mV, respectively. The entrapment efficiency and drug release were estimated to be 98.84% ± 0.001 and 99.99% in 6 h, respectively. Additionally, the optimized formulation demonstrated acceptable outcomes for solid-state analysis, osmolality, pH, residual solvent, and morphological properties. After 8 h, the <i>ex vivo</i> transcleral permeation and scleral deposition were 629.05 ± 124.11 ng/cm<sup>2</sup> and 4.10 ± 0.54 µg, respectively. Y-79 (human retinoblastoma) cell line study using standard drug, test drug, and optimized formulation revealed anticancer potential at all time points (6, 12, 18, and 24 h) with comparable IC50 values. Furthermore, the optimized formulation exhibited no toxicity on the ARPE-19 (human retinal pigmented epithelium) cell line over 24 h. The optimized formulation was non-irritating to the eye (HET-CAM) and remained stable for 6 months. Thus, drug delivery to the posterior eye segment for the treatment of retinoblastoma appears to be possible with the help of established technology.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"246-258"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143476825","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Exploring the application of single-step drying in lyophilization of high protein concentration formulations. 探索单步干燥法在高蛋白浓度制剂冻干中的应用
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-03-18 DOI: 10.1080/10837450.2025.2476707
Qi Zeng, Zhaowei Jin, Jeremy Guo
{"title":"Exploring the application of single-step drying in lyophilization of high protein concentration formulations.","authors":"Qi Zeng, Zhaowei Jin, Jeremy Guo","doi":"10.1080/10837450.2025.2476707","DOIUrl":"10.1080/10837450.2025.2476707","url":null,"abstract":"<p><strong>Objectives: </strong>Single-step drying integrates sublimation and desorption process in one step. The applicability of single-step drying in high protein concentration formulations with or without viscosity reducers remains to be explored. And drying behavior of single-step drying remains to be monitored.</p><p><strong>Methods: </strong>Firstly, in formulations without viscosity reducers (sucrose and mannitol), the method of single-step drying at shelf temperature (Ts) of 25 °C and chamber pressure (Pc) of 0.3 mbar with aggressive annealing (-3 °C) was tested; secondly, two viscosity reducers (ArgHCl and NaCl) were applied to further explore the application of single-step drying in viscosity reducer-containing formulations; finally, drying behavior of single-step drying was monitored in real time by tunable diode laser absorption spectroscopy(TDLAS).</p><p><strong>Results: </strong>In single-step drying process, significant cycle time reduction (68%) was achieved compared to traditional two-step drying. Good cake appearance was observed in all formulation combinations with comparable pre- and post-lyophilization quality attributes as well as reconstitution time. Three times faster sublimation rate was monitored in single-step drying process compared to traditional two-step drying.</p><p><strong>Conclusion: </strong>Single-step drying was proved to be applicable to high protein concentration formulations with or without viscosity reducers. Significant cycle time reduction in drying process was achieved. Sublimation rate resulted in a more efficient drying cycle as a whole even though an increase of product resistance.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"342-349"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143625508","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
Ezetimibe oral solid lipid nanoparticle by effervescent dispersion method: in vitro characterization and in vivo pharmacokinetic study in rats. 泡腾分散法制备依折替米口服固体脂质纳米粒体外表征及大鼠体内药代动力学研究。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-03-02 DOI: 10.1080/10837450.2025.2471461
Ruba S Darweesh, Farah S Al-Qawasmi, Mai S Khanfar
{"title":"Ezetimibe oral solid lipid nanoparticle by effervescent dispersion method: <i>in vitro</i> characterization and <i>in vivo</i> pharmacokinetic study in rats.","authors":"Ruba S Darweesh, Farah S Al-Qawasmi, Mai S Khanfar","doi":"10.1080/10837450.2025.2471461","DOIUrl":"10.1080/10837450.2025.2471461","url":null,"abstract":"<p><p>Ezetimibe (EZT) is a class II drug of the Biopharmaceutics classification system (BCS), with limited aqueous solubility and high permeability. This study aims to enhance the solubility and oral bioavailability of EZT by developing EZT solid lipid nanoparticles (SLNs). EZT-SLNs were developed through the effervescent dispersion technique. Different amounts of Tween-80, Compritol ATO 888, and mannitol as cryoprotectant were used. F11 was the optimum formula with 154 nm in size and 90.26% entrapment efficiency. It demonstrates significant enhancements in solubility across various pH values. In addition, F11 shows a significantly higher drug release than pure EZT at all time points, and that's related to the reduction in the particle size and increasing its surface area along with the transformation from a crystalline state to an amorphous state. The powder X-ray diffraction and Differential Scanning Calorimetry tests confirmed this conversion from crystalline form to amorphous. The <i>in vivo</i> animal study demonstrated that the C<sub>max</sub> and <math><mrow><msubsup><mrow><mtext>AUC</mtext></mrow><mrow><mn>0</mn></mrow><mrow><mtext>∞ </mtext></mrow></msubsup></mrow></math> of the EZT-SLNs group were significantly higher than the pure EZT group, after oral administration. In conclusion, EZT-SLNs with enhanced <i>in vitro</i> and <i>in vivo</i> properties were successfully developed using the effervescent dispersion technique.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"268-279"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143483886","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
Engineering orally disintegrating tablets for buccal delivery of cilostazol with enhanced dissolution and bioavailability: a novel dual porogenic approach, in vitro characterization, and in vivo evaluation in rats. 具有增强溶解性和生物利用度的西洛他唑口腔崩解片:一种新的双重致孔方法,体外表征和大鼠体内评价。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-02-28 DOI: 10.1080/10837450.2025.2472887
Shahinaze A Fouad, Nada Abdelaziz, Mahmoud H Teaima, Mohamed El-Nabarawi, Amal Anwar Taha, Rehab Abdelmonem, Khaled El-Refai
{"title":"Engineering orally disintegrating tablets for buccal delivery of cilostazol with enhanced dissolution and bioavailability: a novel dual porogenic approach, <i>in vitro</i> characterization, and <i>in vivo</i> evaluation in rats.","authors":"Shahinaze A Fouad, Nada Abdelaziz, Mahmoud H Teaima, Mohamed El-Nabarawi, Amal Anwar Taha, Rehab Abdelmonem, Khaled El-Refai","doi":"10.1080/10837450.2025.2472887","DOIUrl":"10.1080/10837450.2025.2472887","url":null,"abstract":"<p><p>Cilostazol (CTZ), is a BCS class II drug with limited bioavailability. In the current study, orally disintegrating tablets (ODTs) for buccal delivery of CTZ were prepared by two methods; lyophilization (Lyo-ODTs) and direct compression (DC-ODTs). All CTZ-ODTs were evaluated for <i>in vitro</i> disintegration time (DT) and wetting time (WT) tests, <i>in vitro</i> dissolution. Scanning electron microscopic (SEM) analysis was performed for the selected Lyo-ODT-7 and DC-ODT-2. Lyo-ODT-7 composed of aerosil<sup>®</sup> 200 and PEG 4000 acquired the shortest DT (13.00 ± 0.14) and WT (33.00 ± 0.26) among the prepared ODTs. It also showed a 2.3 fold significantly enhanced dissolution profile at an early time point (5 min) that was maintained till 1 h, in simulated saliva fluid (pH ∼ 6.8), compared to Pletaal<sup>®</sup> IR tablets (<i>p</i> < 0.0001). SEM analysis revealed the remarkable porosity of Lyo-ODT-7, confirming its successfully enhanced disintegration and dissolution. Lyo-ODT-7 showed significantly enhanced pharmacokinetic parameters with a 3.5 and 3.6 fold increase in C<sub>max</sub> (<i>p</i> = 0.0493) and AUC<sub>0-24</sub> (<i>p</i> = 0.0470), respectively compared to Pletaal<sup>®</sup> IR tablets. The relative bioavailability of CTZ after buccal administration of Lyo-ODT-7 to rats was 364.45%, compared to the market oral IR tablets; Pletaal<sup>®</sup>. The enhanced bioavailability imposes the successful oromucosal absorption of CTZ <i>via</i> buccal delivery of Lyo-ODT-7. Our study demonstrated that Lyo-ODT-7 could represent a favorable buccal dosage form for patients with intermittent claudication, suffering from dysphagia. It can also be used in cases of acute cerebral or myocardial infarction due to its significantly enhanced rate and extent of absorption. It is considered a promising approach for buccal delivery of BCS class II active pharmaceutical ingredients (APIs) suffering from solubility problems and hepatic first pass effect.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"280-294"},"PeriodicalIF":2.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503322","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
Assessment of therapeutic effectiveness of developed colchicine transnovasomes in treatment of recurrent aphthous ulcer as monotherapy and combination therapy with platelet-rich plasma. 秋水仙碱转新酶体单药与富血小板血浆联合治疗复发性阿弗特溃疡的疗效评价。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-03-01 Epub Date: 2025-03-10 DOI: 10.1080/10837450.2025.2475967
Soha M Kandil, Iman I Soliman, Marwa Hosni, Abeer Salama, Ebtisam M Abdou
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