Pharmaceutical Development and Technology最新文献_第4页

Development and optimization of cilostazol loaded transethosomal gel for improved performance. 西洛他唑运载酶体凝胶的研制与优化。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-07-01 Epub Date: 2025-06-24 DOI: 10.1080/10837450.2025.2521055

Midhat Rehman, Saba Sohail, Zakir Ali, Ali H Alamri, Ahmed A Lahiq, Taha Alqahtani, Saleh Alyahya, Fakhar Ud Din

{"title":"Development and optimization of cilostazol loaded transethosomal gel for improved performance.","authors":"Midhat Rehman, Saba Sohail, Zakir Ali, Ali H Alamri, Ahmed A Lahiq, Taha Alqahtani, Saleh Alyahya, Fakhar Ud Din","doi":"10.1080/10837450.2025.2521055","DOIUrl":"10.1080/10837450.2025.2521055","url":null,"abstract":"Deep vein thrombosis (DVT) is the third major leading cause of mortality and morbidity after cardiovascular disease and stroke. Cilostazol (CLZ) being one of the antiplatelet agents is effectively used in DVT. However, its oral administration is associated with several problems, such as gastrointestinal side effects and extensive first-pass metabolism. Herein, CLZ-loaded transethosomes (CLZ-TEs) were prepared and incorporated in chitosan gel (CLZ-TEG) for transdermal administration. Box-Behnken Design Expert® software was used to statistically optimize CLZ-TEs. Particle properties, Transmission electron microscopy (TEM), and Fourier Transform Infrared spectroscopy (FTIR) analyses of CLZ-TEs were accomplished followed by in vitro release and permeation studies and its comparison with CLZ-TEG, CLZ-dispersion (Ds) and CLZ-G. Moreover, skin irritation and pharmacokinetics studies of the optimized CLZ-TEG were executed. The optimized CLZ-TEs showed a mean particle size of 174 nm, polydispersity index of 0.173, zeta potential of -30 mV, and entrapment efficiency of 99%. TEM exhibited spherical nanovesicles and FTIR demonstrated compatibility of the excipients. Moreover, CLZ-TEG was homogeneous, smooth, and spreadable. Similarly, CLZ-TEG displayed sustained release and enhanced permeation of the CLZ. Furthermore, pharmacokinetic study showed significantly improved (p < 0.05) bioavailability of CLZ-TEG when compared with CLZ-G and CLZ-Ds. It was concluded that CLZ-TEG may be a potential candidate for the management of DVT.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"821-839"},"PeriodicalIF":2.5,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144326547","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

Enzyme-sensitive peptide KC26 modifies milk exosomes encapsulating carboplatin for the treatment of retinoblastoma. 酶敏感肽KC26修饰乳外泌体包封卡铂治疗视网膜母细胞瘤。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-05-22 DOI: 10.1080/10837450.2025.2505005

Hetong Wang, Wei Wang, Qin Tang, Xun Liu, Limin Zhu, Di Sun, Tingting Lin

{"title":"Enzyme-sensitive peptide KC26 modifies milk exosomes encapsulating carboplatin for the treatment of retinoblastoma.","authors":"Hetong Wang, Wei Wang, Qin Tang, Xun Liu, Limin Zhu, Di Sun, Tingting Lin","doi":"10.1080/10837450.2025.2505005","DOIUrl":"10.1080/10837450.2025.2505005","url":null,"abstract":"Milk exosomes have also been widely used as emerging delivery vehicles for various therapeutic cargoes. Retinoblastoma (RB) is the most common primary intraocular malignancy of childhood. However, the therapeutic efficacy is severely hampered by the presence of blood-retinal barrier (BRB) and systemic side effects. Legumain (LGMN) can be used as a target for tumor microenvironment responsive delivery design and therapeutic applications. Here, a LGMN-sensitive peptide KC26-modified milk exosomes loaded with carboplatin (CBP-KC26-MExos). The system enables milk exosomes loaded with carboplatin (CBP) to reach the target cells by binding to LGMN, improves tumor targeting, enhances cellular uptake and apoptosis, inhibits cell proliferation, invasion and migration. Intravenous injection of CBP-KC26-MExos cross the BRB significantly inhibited intraocular tumor progression and reduced CBP toxicity. We have developed a 'drug-target-carrier' approach and proposed an enzyme sensitive peptide (KC26) modified milk exosomes loaded with CBP, providing a perspective for exploring targeted therapy of tumor cells and tumor microenvironment, and offering a promising clinical strategy for the treatment of retinoblastoma.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"621-631"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144026693","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

Topical hyalubilosomes of dantrolene sodium as muscle targeted nanocarrier for muscle spasms: fabrication, ex-vivo permeation and behavioral animal model. 作为肌肉痉挛靶向纳米载体的丹曲林钠局部透明体：制备、体外渗透和行为动物模型。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-05-17 DOI: 10.1080/10837450.2025.2504999

Abdelrahaman M M Othman, Ossama Y Abdallah, Yosra S R Elnaggar

{"title":"Topical hyalubilosomes of dantrolene sodium as muscle targeted nanocarrier for muscle spasms: fabrication, ex-vivo permeation and behavioral animal model.","authors":"Abdelrahaman M M Othman, Ossama Y Abdallah, Yosra S R Elnaggar","doi":"10.1080/10837450.2025.2504999","DOIUrl":"10.1080/10837450.2025.2504999","url":null,"abstract":"Topical muscle relaxants are gaining interest in pharmaceuticals. Dantrolene sodium (DS), an FDA-approved relaxant targeting ryanodine receptors, is limited in topical use by poor physicochemical properties, delayed onset, and hepatotoxicity. This study introduces the first optimized hyalubilosome-based nanocarrier for non-invasive DS delivery. Two anionic surfactants were used as edge activators to improve drug encapsulation and permeation. The optimized nanocarrier had a spherical shape, 165 nm particle size, -31.2 mV zeta potential, and 97.47% entrapment efficiency. Ex vivo studies showed superior permeation compared to DS suspension (10% in water, pH 6.8), with 30% of the dose permeating within 15 min. In vivo, efficacy was tested in Wistar mice using the Straub tail test with a single 30 mg/kg topical dose. Behavioral analysis showed a fivefold increase in muscle relaxation vs. untreated controls (p < 0.0001). The formulation had an onset within one minute and complete relief within two minutes, unlike the conventional topical DS, which showed no effect for 90 min. This highlights hyaluronic acid-based transbilosomes as a promising nanoplatform for fast, effective topical DS delivery and potential muscle spasm treatment.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"590-603"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144079545","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

Solid supersaturated self-nanoemulsifying drug delivery system for abiraterone acetate: improved drug loading, dissolution, cellular uptake, and anticancer activity. 醋酸阿比特龙固体过饱和自纳米乳化给药系统：改善药物负载、溶出、细胞摄取和抗癌活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-05-23 DOI: 10.1080/10837450.2025.2505003

Ayush Nair, Mayur Aalhate, Srushti Mahajan, Ujala Gupta, Indrani Maji, Pankaj Kumar Singh

{"title":"Solid supersaturated self-nanoemulsifying drug delivery system for abiraterone acetate: improved drug loading, dissolution, cellular uptake, and anticancer activity.","authors":"Ayush Nair, Mayur Aalhate, Srushti Mahajan, Ujala Gupta, Indrani Maji, Pankaj Kumar Singh","doi":"10.1080/10837450.2025.2505003","DOIUrl":"10.1080/10837450.2025.2505003","url":null,"abstract":"Abiraterone acetate (ABT) is an androgen biosynthesis inhibitor approved for the treatment of prostate cancer. However, the treatment course of ABT is constrained by its high dose, poor solubility and permeability issues. A solid supersaturated self-nanoemulsifying drug delivery system (ssSNEDDS) is an excellent approach for improving drug loading. The aim was to increase the solubility and drug loading of ABT in SNEDDS via supersaturation by using a polymeric precipitation inhibitor (HPMC E5). Liquid SNEDDS were thoroughly optimized with a mixture design followed by solidification with Aerosil® 200 by the adsorption method. The developed ABT-ssSNEDDS showed a nano-ranged particle size of 106.23 ± 4.15 nm and PDI of 0.234 ± 0.0069. Furthermore, the powder showed an angle of repose of 34.86 ± 0.30° indicating good flow properties with smooth morphology under SEM analysis. DSC and PXRD studies revealed amorphization of ABT in the ABT-ssSNEDDS group. Furthermore, the dissolution study demonstrated significantly higher ABT release from ABT-ssSNEDDS in comparison to free ABT after 2 h in pH 1.2 and 6.8 pH buffer. In-vitro cell culture studies in the PC-3 cell line denoted significantly enhanced anticancer activity and cellular uptake. Thus, ABT-ssSNEDDS could be an encouraging approach for improved oral therapy and enhanced drug loading of ABT.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"604-620"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015402","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

An insight into cell-penetrating peptides: perspectives on design, optimization, and targeting in drug delivery systems. 洞察细胞穿透肽：在药物输送系统的设计，优化和靶向的观点。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-05-23 DOI: 10.1080/10837450.2025.2505000

Ali Asghar Khakshur, Elham Khodaverdi, Hossein Kamali, Ali Nokhodchi

{"title":"An insight into cell-penetrating peptides: perspectives on design, optimization, and targeting in drug delivery systems.","authors":"Ali Asghar Khakshur, Elham Khodaverdi, Hossein Kamali, Ali Nokhodchi","doi":"10.1080/10837450.2025.2505000","DOIUrl":"10.1080/10837450.2025.2505000","url":null,"abstract":"The authors carried out a comprehensive review of the application of peptides known as cell-penetrating peptides (CPPs) in various drug delivery systems (DDS), with the prospect of achieving novel solutions and ideas to overcome the challenges of DDS, by making them more able to penetrate cells and biological membranes. A conceptual search was conducted in relevant literature databases (Scopus, PubMed, Web of Science, and Google Scholar) up to 1 April 2025 using keywords such as drug delivery systems, cell-penetrating peptides, CPPs, complexes, conjugates, nanoparticles, dendrimers, exosomes, liquid crystalline, liposomes, micelles, nanospheres and lipid nanoparticles. The studies demonstrate that the antimicrobial effect of drugs, including curcumin, gentamicin, and antifungal drugs like imidazoacridinone derivatives, can be enhanced when they are conjugated or complexed with CPPs. CPPs possess positive charges, which make them suitable for gene therapy applications by facilitating the delivery of plasmids and siRNAs with negative charges in modern delivery systems. Medicinal formulations containing CPPs in combination with liquid crystals or nanostructured lipid carriers (NLCs) increase drugs penetration to the skin. Additionally, several investigations showed that CPPs could have a positive impact on the pharmacokinetic and pharmacodynamic of chemotherapy agents, reducing their side effects. CPPs have significant potential in enhancing penetration, bioavailability, targeting, and optimization of DDS. By using computer modeling and designing CPPs with more desirable features and conducting more clinical studies, new methods for treating diseases and better formulations can be achieved.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"521-547"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Formulation and characterization of novel oral pH-sensitive electrospun nanofibers for boosting dissolution and penetration of model class IV drug. 促进IV类药物溶出渗透的新型口服ph敏感静电纺丝纳米纤维的配方与表征。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-06-13 DOI: 10.1080/10837450.2025.2517709

Omar Y Mady, Safaa Khaled, Asmaa A Hedaya, Noorelhoda Abdine, Yusuf Haggag

{"title":"Formulation and characterization of novel oral pH-sensitive electrospun nanofibers for boosting dissolution and penetration of model class IV drug.","authors":"Omar Y Mady, Safaa Khaled, Asmaa A Hedaya, Noorelhoda Abdine, Yusuf Haggag","doi":"10.1080/10837450.2025.2517709","DOIUrl":"10.1080/10837450.2025.2517709","url":null,"abstract":"Sulpiride (a model class IV drug) is a central dopamine antagonist, that is commonly used in the treatment of various psychiatric and gastrointestinal conditions. However, its poor aqueous solubility and low oral bioavailability (20-30%) limit its therapeutic efficacy. Electrospun nanofibers offer a promising method to enhance the oral absorption of poorly water-soluble drugs. This study, for the first time, aimed to investigate the feasibility of electrospun Eudragit S100-loaded Sulpiride nanofibers as an enhanced oral delivery system, compared to drug-loaded solid dispersion. The physicochemical properties of the nanofibers were characterized. The drug's intestinal permeability was evaluated using an ex vivo non-everted sac technique. Sulpiride-loaded nanofibers exhibited uniform morphology with a very narrow nanosize range of (98.4-123.6 nm) and a high drug-loading efficiency of >98%. In vitro, dissolution demonstrated a significant enhancement in the Sulpiride's dissolution rates from the nanofiber formulations (>94% of the drug released within 4 h) compared to the solid dispersion formulation (˂77% of the drug released). The nanofiber formulations exhibited a 2-fold increase in the drug's intestinal permeability and a 4-fold increase in apparent permeability (Papp) compared to the free drug. The improved dissolution and intestinal permeability of Sulpiride-loaded nanofibers suggest their potential application for enhancing the oral delivery and therapeutic efficacy of class IV drugs.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"712-727"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144258693","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Formulation and characterization of transfersomes for ocular delivery of tonabersat. 托那伯沙眼给药转移体的制备与表征。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-05-15 DOI: 10.1080/10837450.2025.2501991

Santosh Bhujbal, Ilva D Rupenthal, Priyanka Agarwal

{"title":"Formulation and characterization of transfersomes for ocular delivery of tonabersat.","authors":"Santosh Bhujbal, Ilva D Rupenthal, Priyanka Agarwal","doi":"10.1080/10837450.2025.2501991","DOIUrl":"10.1080/10837450.2025.2501991","url":null,"abstract":"Transfersomes (TFS) are deformable vesicles, known for their ability to enhance transdermal drug penetration. This study aimed to evaluate whether TFS can also enhance ocular delivery of poorly soluble tonabersat. TFS were prepared using Phospholipon® 90G with Tween® 80 as the edge activator. The effect of formulation parameters (edge activator and cryoprotectant concentrations) on TFS characteristics were evaluated using a full factorial design. The optimized TFS eyedrop was characterized for particle size, zeta potential, deformability, entrapment efficiency (EE), drug content, pH, osmolality and TFS stability over 3 months at different storage conditions. Furthermore, drug penetration into the cornea, conjunctiva, eyelid, and sclera-choroid after topical application was studied ex vivo using a tonabersat solution in medium chain triglycerides as the control. The optimized TFS formed spherical unilamellar vesicles with a mean diameter <130 nm, EE >80%, and were stable at -20 and 5 ± 3 °C for up to 3 months. The TFS eyedrop resulted in significantly greater ocular penetration than the control without affecting the barrier properties of the tested tissues. Drug penetration into different ocular tissues was compared, shedding light on the penetration mechanism of TFS. Overall, this study demonstrates that TFS provide a promising alternative for the ocular delivery of tonabersat.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"558-571"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144009207","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

Gum tragacanth-based hemostatic sponge for enhanced hemostasis in dental surgery. 牙龈黄芪止血海绵在牙科手术中的止血作用。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-06-12 DOI: 10.1080/10837450.2025.2516238

Mirmousa Mousavai, Ramin Khajavi, Mohammadreza Kalaee, Mohammad Karim Rahimi

{"title":"Gum tragacanth-based hemostatic sponge for enhanced hemostasis in dental surgery.","authors":"Mirmousa Mousavai, Ramin Khajavi, Mohammadreza Kalaee, Mohammad Karim Rahimi","doi":"10.1080/10837450.2025.2516238","DOIUrl":"10.1080/10837450.2025.2516238","url":null,"abstract":"Regulating hemorrhage is crucial during dental procedures, particularly surgical interventions where substantial blood loss may occur. Hemostatic sponges are effective instruments for controlling hemorrhage, facilitating hemostasis, preparing the surgical area, and enhancing the healing of injuries. This work aimed to present a novel hemostatic sponge created by integrating antihemorrhagic chemicals with the natural polysaccharide tragacanth. Gum tragacanth (GT) (derived from the species Astragalus gossypinus) was solubilized in water and combined with nanoclay (NC) and tranexamic acid (TXA) at varying doses. Subsequently, they were freeze-dried in cubic silicone molds. Scanning electron micrographs revealed that the incorporation of TXA and NC significantly increased the porosity of the sponges. No evidence of chemical bonding was present in our converted infrared spectra. Prothrombin time (PT), activated partial thromboplastin time (aPTT), and whole blood coagulation index showed improvement with the administration of hemostatics, with TXA demonstrating a more pronounced impact. The cytotoxicity assay of the hemostatic GT exhibited no notable difference from the control sample. The hemostatic GT has demonstrated significant potential for medical applications, particularly in dentistry, and applies to procedures such as endodontics and prosthesis placement.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"666-690"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144234784","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

Quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery: impact of glycyrrhizic acid concentrations. 甘草酸稳定的槲皮素纳米晶体用于肝脏靶向药物递送：甘草酸浓度的影响。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-05-01 DOI: 10.1080/10837450.2025.2498370

Fengxia Wang, Chengying Shen, Fangwen Chen, Jinyun Cao, Pengfei Yue, Baode Shen

{"title":"Quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery: impact of glycyrrhizic acid concentrations.","authors":"Fengxia Wang, Chengying Shen, Fangwen Chen, Jinyun Cao, Pengfei Yue, Baode Shen","doi":"10.1080/10837450.2025.2498370","DOIUrl":"10.1080/10837450.2025.2498370","url":null,"abstract":"The purpose of this study was to investigate the impact of glycyrrhizic acid (GL) concentrations on in vitro and in vivo behavior of quercetin (QT) nanocrystals stabilized by GL (QT-NCs/GL), with a particular focus on its influence on liver targeted drug delivery. QT-NCs/GL with similar particle size around 200 nm were successfully prepared by media milling technique using different concentrations of GL, which were 10%, 20% and 40% (w/w) of the QT. All QT-NCs/GL showed oval and rod shapes, and remained in crystalline state with a reduced crystallinity as GL concentrations increased. All QT-NCs/GL exhibited significant solubility increase and drug release improvement of QT as compared to raw QT. Pharmacokinetics revealed similar plasma concentration-time profiles of QT after intravenous of all QT-NCs/GL. All QT-NCs/GL exhibited rapidly distribution of QT to liver with the maximum QT concentration more than 750 μg/g at 5 min after intravenous administration, and the AUC0∼t of QT for three formulations in liver were significant difference with the following order: QT-NCs/GL-40% > QT-NCs/GL-20% > QT-NCs/GL-10%. These results suggested that different GL concentrations exhibited significant influence on liver targeted delivery of QT-NCs/GL, and more GL used in QT-NCs/GL may contribute more liver distribution of QT.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"548-557"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144017644","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

Impact of medication swallowing lubricants on the in vitro dissolution of crushed and whole metformin tablets: dissolution kinetics study. 药物吞食润滑剂对二甲双胍碎片和整片体外溶出度的影响：溶出动力学研究。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-06-12 DOI: 10.1080/10837450.2025.2516234

Vivek Babu Nooney, Thilini Thrimawithana, Barbora de Courten, Albert Le, Filip Nikolovski, Noemi Cieleszky, Seerat Fatima, Ayman Allahham

{"title":"Impact of medication swallowing lubricants on the in vitro dissolution of crushed and whole metformin tablets: dissolution kinetics study.","authors":"Vivek Babu Nooney, Thilini Thrimawithana, Barbora de Courten, Albert Le, Filip Nikolovski, Noemi Cieleszky, Seerat Fatima, Ayman Allahham","doi":"10.1080/10837450.2025.2516234","DOIUrl":"10.1080/10837450.2025.2516234","url":null,"abstract":"Metformin is the most common drug used in patients with type 2 diabetes. Our aim is to assess if the in vitro dissolution of Metformin IR 500 mg tablets and its kinetics is altered in the presence of various medication swallowing lubricants used in vivo and to evaluate their rheological properties of tablet lubricant. The dissolution profile of metformin tablets (crushed and whole) mixed with selected medication swallowing lubricants was studied in a Distek® Dissolution apparatus at 6 different time points (n = 5). Samples were diluted and analysed using a UV-visible Spectrometer at a wavelength of 232 nm using a calibrated absorbance-concentration curve. Dissolution data will be modelled to understand the effect on its dissolution kinetics. Rheology studies were completed using an AR G2 System Rheometer. Gloup® Forte delayed the in vitro dissolution of metformin from crushed or whole tablets and produced lower peak concentrations, irrespective of the pH of the dissolution media (reduction up to 35% reduction in concentration in pH = 6.8). Gloup® Forte has changed the release to almost erosion-controlled in different media when mixed with crushed metformin tablets. Further studies evaluating the effects of commonly used thickened fluids on medication may be required to better inform clinical practice.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"632-645"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144234785","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