Drug Development and Industrial Pharmacy最新文献

{"title":"A Novel image processing technique for weighted particle size distribution assessment.","authors":"Pierre-Luc Latreille, Ajay Babu Pazhayattil, Sam Turner, Naresh Talwar","doi":"10.1080/03639045.2024.2358366","DOIUrl":"10.1080/03639045.2024.2358366","url":null,"abstract":"<p><p>The objective of the study was to create a reliable method that could be used to evaluate the particle size distribution of samples and pre-mixes in real-world situations, particularly those consisting of typical formulation blends. The goal was to use this method to assess the uniformity of the samples and ensure that they met the required quality standards. The researchers aimed to create a method that could be easily incorporated into the manufacturing process, providing a practical and efficient solution. This study demonstrates the use of ImageJ software to analyze the particle size distribution (PSD) of powders. The technique produces qualitative data from microscopy images and quantitative data from analysis of parameters including average diameter, <i>D</i>₁₀, <i>D</i>₅₀<i>, D</i>₉₀, and standard deviation. The method was tested with various treatments, showing differentiating outcomes in all cases. The alternate technique provides a rapid and cost-effective method for PSD analysis, surpassing the limitations of sieve analysis. Extensive testing of the method, using a variety of sample types, including typical formulation blends, was performed. The results suggest that the method can effectively assess the morphology of changing materials during batch manufacturing and characterize uniformity in blends. The methodology has the capability to identify attributes related to PSD that are typically required to be monitored during manufacturing. The technique allows for accurate and reliable quantification of the attributes through image capture technology. The technique has future potential and has important implications for material science, powder rheology, pharmaceutical formulation development, and continual process monitoring.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"550-560"},"PeriodicalIF":2.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141086354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synergistic effects of quercetin-loaded CoFe₂O₄@Liposomes regulate DNA damage and apoptosis in MCF-7 cancer cells: based on biophysical magnetic hyperthermia.","authors":"Shehab Elbeltagi, Abo Bakr Abdel Shakor, Hanan M Alharbi, Hesham M Tawfeek, Basmah N Aldosari, Zienab E Eldin, Basma H Amin, Mohamed Abd El-Aal","doi":"10.1080/03639045.2024.2363231","DOIUrl":"10.1080/03639045.2024.2363231","url":null,"abstract":"<p><strong>Introduction: </strong>Breast cancer (BC) is the most common malignancy in women globally. Significant progress has been made in developing structural nanoparticles (NPs) and formulations for targeted smart drug delivery (SDD) of pharmaceuticals, improving the precision of tumor cell targeting in therapy.</p><p><strong>Significance: </strong>Magnetic hyperthermia (MHT) treatment using magneto-liposomes (MLs) has emerged as a promising adjuvant cancer therapy.</p><p><strong>Methods: </strong>CoFe₂O₄ magnetic NPs (MNPs) were conjugated with nanoliposomes to form MLs, and the anticancer drug quercetin (Que) was loaded into MLs, forming Que-MLs composites for antitumor approach. The aim was to prepare Que-MLs for DD systems (DDS) under an alternating magnetic field (AMF), termed chemotherapy/hyperthermia (chemo-HT) techniques. The encapsulation efficiency (EE), drug loading capacity (DL), and drug release (DR) of Que and Que-MLs were evaluated.</p><p><strong>Results: </strong>The results confirmed successful Que-loading on the surface of MLs, with an average diameter of 38 nm and efficient encapsulation into MLs (69%). <i>In vitro</i>, experimental results on MCF-7 breast cells using MHT showed high cytotoxic effects of novel Que-MLs on MCF-7 cells. Various analyses, including cytotoxicity, apoptosis, cell migration, western blotting, fluorescence imaging, and cell membrane internalization, were conducted. The Acridine Orange-ethidium bromide double fluorescence test identified 35% early and 55% late apoptosis resulting from Que-MLs under the chemo-HT group. TEM results indicated MCF-7 cell membrane internalization and digestion of Que-MLs, suggesting the presence of early endosome-like vesicles on the cytoplasmic periphery.</p><p><strong>Conclusions: </strong>Que-MLs exhibited multi-modal chemo-HT effects, displaying high toxicity against MCF-7 BC cells and showing promise as a potent cytotoxic agent for BC chemotherapy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"561-575"},"PeriodicalIF":2.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141237560","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Statistical design and optimization of nano-transfersomes based chitosan gel for transdermal delivery of cefepime.","authors":"Rashna Mirza, Kifayat Ullah Shah, Atif Ullah Khan, Mohsin Fawad, Asim Ur Rehman, Naveed Ahmed, Asif Nawaz, Shefaat Ullah Shah, Abdullah F Alasmari, Metab Alharbi, Fawaz Alasmari, Zeeshan Hafeez, Sami Ul Haq","doi":"10.1080/03639045.2024.2353098","DOIUrl":"10.1080/03639045.2024.2353098","url":null,"abstract":"<p><strong>Objectives: </strong>This research aimed to overcome challenges posed by cefepime excessive elimination rate and poor patient compliance by developing transdermal delivery system using nano-transfersomes based chitosan gel.</p><p><strong>Methods: </strong>Rotary evaporation-sonication method and the Box-Behnken model were used to prepare cefepime loaded nano-transfersomes (CPE-NTFs). The physiochemical characterization of CPE-NTFs were analyzed including DLS, deformability index, DSC and antimicrobial study. Optimized CPE-NTFs loaded into chitosan gel and appropriately characterized. <i>In vitro</i> release, <i>ex vivo</i> and <i>in vivo</i> studies were performed.</p><p><strong>Results: </strong>The CPE-NTFs were physically stable with particle size 222.6 ± 1.8 nm, polydispersity index 0.163 ± 0.02, zeta potential -20.8 ± 0.1 mv, entrapment efficiency 81.4 ± 1.1% and deformability index 71 ± 0.2. DSC analysis confirmed successful drug loading and thermal stability. FTIR analysis showed no chemical interaction among the excipients of CPE-NTFs gel. The antibacterial activity demonstrated a remarkable reduction in the minimum inhibitory concentration of cefepime when incorporated into nano-transfersomes. CPE-NTFs based chitosan gel (CPE-NTFs gel) showed significant physicochemical properties. <i>In vitro</i> release studies exhibited sustained release behavior over 24 h, and <i>ex vivo</i> studies indicated enhanced permeation and retention compared to conventional cefepime gel. <i>In vivo</i> skin irritation studies confirmed CPE-NTFs gel was nonirritating and biocompatible for transdermal delivery.</p><p><strong>Conclusion: </strong>This research showed nano-transfersomes based chitosan gel is a promising approach for cefepime transdermal delivery and provides sustained release of cefepime.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"511-523"},"PeriodicalIF":2.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140890920","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An insight into viscosity and conductivity in the formulation of co-axial electrospun <i>Carica papaya</i> leaf extract.","authors":"Siew Mei Tan, Reem Abou Assi, Roza Dianita, Vikneswaran Murugaiyah, Siok Yee Chan","doi":"10.1080/03639045.2024.2335527","DOIUrl":"10.1080/03639045.2024.2335527","url":null,"abstract":"<p><p><b>Objective:</b> This research aimed to investigate the application of the coaxial electrospun method for the production of natural extracts (papaya leaf extract) fibre films. This was achieved through utilising different polymers and with a focus on the conductivity and the viscosity of polymer solutions as critical parameters to generate successful fibres.<b>Significance:</b> Electrospinning is a promising trending manufacturing method for incorporating thermolabile herbal extracts using coaxial electrospun features. However, the complexity of the electrospinning process and the feasibility of the product required precise scrutiny.<b>Methods:</b> The electrospinning solution parameters (conductivity and viscosity) were evaluated by employing various ratios of Eudragit L100 (EL100) and Eudragit L100-55 (EL100-55) pre-spinning polymeric blend solutions. The electrospinning process and ambient parameters were optimised. Following that, the <i>in-silico</i> physicochemical properties of phytochemical marker, rutin, were illustrated using SwissADME web tool. Both freeze-dried <i>Carica papaya</i> leaf extract and its produced films were characterised using Scanning Electron Microscopy (SEM), Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR), polarised light microscopy, and X-ray Powder Diffraction (XRPD).<b>Results:</b> The optimal values of conductivity (≈40-44 × 10^-4 S/m) and viscosity (≈32-42 × 10^-3Pa·s) were determined for producing evenly distributed and small fibre diameters in SEM images. These parameters significance was highlighted in acquiring and maintaining adequate tangential stress for fibre elongation, which would consequently affect the morphology and diameter of the fibres formed.<b>Conclusion:</b> In conclusion, the solution, process, and ambient parameters are significant in developing natural extracts into films via electrospinning technology, and this includes the promising <i>Carica papaya</i> leaf extract films produced by coaxial electrospinning.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-13"},"PeriodicalIF":3.4,"publicationDate":"2024-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140293090","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of a novel human stratum corneum mimetic phospholipid -vesicle-based permeation assay models for <i>in vitro</i> permeation studies.","authors":"Yuerong Qian, Xuchao Wei, Yiwei Wang, Shaoping Yin, Jun Chen, Jie Dong","doi":"10.1080/03639045.2024.2331242","DOIUrl":"10.1080/03639045.2024.2331242","url":null,"abstract":"<p><strong>Objectives: </strong>To develop and evaluate a novel human stratum corneum (SC) mimetic phospholipid vesicle-based permeation assay (PVPA_SC) model for <i>in vitro</i> permeation studies.</p><p><strong>Significance: </strong>Due to the increasing restrictions on the use of human and animal skins, artificial skin models have attracted substantial interest in pharmaceuticals and cosmetic industries. In this study, a modified PVPA_SC model containing both SC lipids and proteins was developed.</p><p><strong>Methods: </strong>The PVPA_SC model was optimized by altering the lipid composition and adding keratin in the formulation of large liposomes. The barrier properties were monitored by measuring the electrical resistance (ER) and permeability of Rhodamine B (RB). The modified PVPA_SC model was characterized in terms of the surface topography, solvent influence and storage stability. The permeation studies of the active components in Compound Nanxing Zhitong Plaster (CNZP) were performed to examine the capability of PVPA_SC in the application of skin penetration.</p><p><strong>Results: </strong>The ER and <i>P</i>_app values of RB obtained from the optimized PVPA_SC model indicated a similar barrier property to porcine ear skin. Scanning electron microscope analysis demonstrated a mimic 'brick-and-mortar' structure. The PVPA_SC model can be stored for three weeks at -20 °C, and withstand the presence of different receptor medium for 24 h. The permeation studies of the active components demonstrated a good correlation (<i>r</i>² = 0.9136) of <i>P</i>_app values between the drugs' permeation through the PVPA_SC model and porcine ear skin.</p><p><strong>Conclusion: </strong>Keratin contained composite phospholipid vesicle-based permeation assay models have been proven to be potential skin tools in topical/transdermal permeation studies.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"410-419"},"PeriodicalIF":3.4,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140142995","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Temozolomide nano-in-nanofiber delivery system with sustained release and enhanced cellular uptake by U87MG cells.","authors":"Karishma Shetty, Khushwant S Yadav","doi":"10.1080/03639045.2024.2332906","DOIUrl":"10.1080/03639045.2024.2332906","url":null,"abstract":"<p><strong>Objective: </strong>The study was aimed at formulating temozolomide (TMZ) loaded gelatin nanoparticles (GNPs) encapsulated into polyvinyl alcohol (PVA) nanofibers (TMZ-GNPs-PVA NFs) as the nano-in-nanofiber delivery system. The secondary objective was to explore the sustained releasing ability of this system and to assess its enhanced cellular uptake against U87MG glioma cells <i>in vitro.</i></p><p><strong>Significance: </strong>Nano-in-nanofibers are the emerging drug delivery systems for treating a wide range of diseases including cancers as they overcome the challenges experienced by nanoparticles and nanofibers alone.</p><p><strong>Methods: </strong>The drug-loaded GNPs were formulated by one-step desolvation method. The Design of Experiments (DoE) was used to optimize nanoparticle size and entrapment efficiency. The optimized drug-loaded nanoparticles were then encapsulated within nanofibers using blend electrospinning technique. The U87MG glioma cells were used to investigate the uptake of the formulation.</p><p><strong>Results: </strong>A 3² factorial design was used to optimize the mean particle size (145.7 nm) and entrapment efficiency (87.6%) of the TMZ-loaded GNPs which were subsequently ingrained into PVA nanofibers by electrospinning technique. The delivery system achieved a sustained drug release for up to seven days (<i>in vitro</i>). The SEM results ensured that the expected nano-in-nanofiber delivery system was achieved. The uptake of TMZ-GNPs-PVA NFs by cells was increased by a factor of 1.964 compared to that of the pure drug.</p><p><strong>Conclusion: </strong>The nano-in-nanofiber drug delivery system is a potentially useful therapeutic strategy for the management of glioblastoma multiforme.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"420-431"},"PeriodicalIF":3.4,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140157814","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Improving cellular uptake and synergetic anti-tumor effects of magnolol and <i>Brucea javanica</i> oil through self-microemulsion.","authors":"Huiyun Zhang, Yu Zhang, Yunfei Hu, Shunru Wei, Michael Adu-Frimpong, Congyong Sun, Gang Qi","doi":"10.1080/03639045.2024.2329730","DOIUrl":"10.1080/03639045.2024.2329730","url":null,"abstract":"<p><strong>Objective: </strong>Magnolol (MG) and <i>Brucea javanica</i> (L.) Merr. oil (BJO) possess synergetic anti-tumor effects, but have poor water solubility and stability, which results in low oral bioavailability.</p><p><strong>Significance: </strong>The MG loaded self-microemulsion drug delivery system (MG-SMDDS) with BJO as oil phase component was utilized to improve the cellular uptake and synergetic anti-tumor effects.</p><p><strong>Methods: </strong>Compatibility study and pseudoternary phase diagram (PTPD) were respectively employed to screen for the composition and proportion of oil phase in the formulation. Central composite design-effect surface method was applied to optimize proportion of each formulation condition. The droplet size, ζ-potential, colloid stability, encapsulation rate (ER) and <i>in vitro</i> dissolution rate of MG-SMDDS were evaluated. Furthermore, cellular uptake and cytotoxicity of the microemulsion on HepG2 cells were assessed.</p><p><strong>Results: </strong>The optimal composition of MG-SMDDS was: MG (9.09%), castor oil (7.40%), BJO (2.47%), Cremophor EL 35 (54.04%) and 1, 2-propanediol (27.01%). The MG-SMDDS exhibited satisfactory droplet size, ζ-potential, colloid stability and ER, as well as faster dissolution rate than free MG. More importantly, SMEDDS containing BJO could enhance the cellular uptake and cytotoxicity of free BJO and free MG on tumor cells.</p><p><strong>Conclusions: </strong>The BJO self-microemulsion delivery technique can provide an idea for design of oral delivery vehicles based on BJO.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"401-409"},"PeriodicalIF":3.4,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140093615","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effect of mango butter on the physicochemical properties of beeswax-Moringa seed oil-based oleogels for topical application.","authors":"Gourav Kumar Indu, Sk Habibullah, Tapan Kumar Shaw, Biswaranjan Mohanty","doi":"10.1080/03639045.2024.2334314","DOIUrl":"10.1080/03639045.2024.2334314","url":null,"abstract":"<p><strong>Objective: </strong>The purpose of this research was to determine any connections between the characteristics of oleogels made of beeswax and the impact of mango butter.</p><p><strong>Methods: </strong>Oleogel was prepared through inverted tube methods, and optimized through oil binding capacity. Other evaluations like bright field and polarized microscopy, Fourier-transform infrared (FTIR) spectroscopy, crystallization kinetics, mechanical study, and X-ray diffractometry (XRD). The drug release kinetic studies and <i>in vitro</i> antibacterial studies were performed.</p><p><strong>Results: </strong>FTIR study reveals that the gelation process does not significantly alter the chemical composition of the individual components. Prepared gel exhibiting fluid-like behavior or composed of brittle networks is particularly vulnerable to disruptions in their network design. The incorporation of mango butter increases the drug permeation. <i>In-vitro</i> microbial efficacy study was found to be excellent.</p><p><strong>Conclusion: </strong>The studies revealed that mango butter can be used to modify the physico-chemical properties of the oleogels.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"432-445"},"PeriodicalIF":3.4,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140287104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Eutectic Solutions for Healing: A Comprehensive Review on Therapeutic Deep Eutectic Solvents (TheDES)","authors":"Sudhanshu Kalantri, Amisha Vora","doi":"10.1080/03639045.2024.2345131","DOIUrl":"https://doi.org/10.1080/03639045.2024.2345131","url":null,"abstract":"Objective TheDES are formed by mixing a Hydrogen Bond Donor (HBD) and a Hydrogen Bond Acceptor (HBA) in appropriate molar ratios. These solvents have been shown to enhance drug solubility, permeabi...","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":"49 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140616711","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Silibinin Solubilization: Combined Effect of Co-solvency and Inclusion Complex Formation","authors":"Azam Dehghan, Saeed Ghanbarzadeh, Majid Ghiass, Mohammad Imani","doi":"10.1080/03639045.2024.2343016","DOIUrl":"https://doi.org/10.1080/03639045.2024.2343016","url":null,"abstract":"Objective: Belonging to the class II drugs according to the biopharmaceutics classification system, silibinin (SLB) benefits from high permeability but suffers poor solubility that negatively affec...","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":"7 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140566983","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}