Drug Development and Industrial Pharmacy最新文献

{"title":"Ferric ions crosslinked hyaluronic acid beads: potentials for drug delivery use.","authors":"Hadeia Mashaqbeh, Rana Obaidat, Meriem Rezigue, Derar Omari, Ghyda'a Shakhatreh","doi":"10.1080/03639045.2024.2422497","DOIUrl":"10.1080/03639045.2024.2422497","url":null,"abstract":"<p><strong>Introduction and purpose: </strong>Despite the attractive properties of hyaluronic acid (HA), The preparation of HA beads is still challenging. This article reports the preparation of pH-sensitive gel HA beads. The ionic gelation method was used to prepare the HA gel beads using ferric ions. This cross-linking type is based on forming coordination bonds, which enhance the mechanical properties of the prepared beads.</p><p><strong>Methods: </strong>The developed beads were characterized using Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Scanning electron microscopy (SEM) examined the bead's morphology. Furthermore, the potential of HA gel beads as an oral drug delivery system was investigated using metformin as a hydrophilic model drug. The entrapment efficiency and <i>in vitro</i>, release, and release kinetics were evaluated. The crosslinking density and HA concentration effect on drug release and bead swelling capacity under pH 1.2 and 7.4 were also investigated.</p><p><strong>Results: </strong>The entrapment efficiency of metformin in HA beads was found to be 79.56 ± 3.89%. FTIR analysis indicated the ionic interaction between ferric ions and the carboxylic groups on the HA molecule. At the same time, there was no substantial interaction between metformin and the polymeric bead. Morphological evaluation and DSC analysis suggested the successful incorporation of metformin within the beads. The <i>in vitro</i> drug release evaluation showed pH-dependent extended release where the release kinetics followed the first-order mathematical model.</p><p><strong>Conclusions: </strong>This study provides a value-added formulation with the potential for drug delivery use, which can be further investigated for biomedical applications.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"865-877"},"PeriodicalIF":2.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142521344","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":"Formulation, characterization and evaluation of minocycline hydrochloride loaded polyurethane/collagen nanofibers via electrospinning as wound dressings.","authors":"Tugba Eren Boncu, Çiğdem Yücel, Ahmet Ceylan, Mehmet Cadir, Ertugrul Sahmetlioglu","doi":"10.1080/03639045.2024.2426581","DOIUrl":"10.1080/03639045.2024.2426581","url":null,"abstract":"<p><strong>Objective: </strong>It was aimed to formulate minocyline. HCI loaded electrospun polyurethane/collagen (PU/Col) and polyurethane/collagen/polycaprolactone (PU/Col/PCL) nanofibers are intended for use as a wound dressing.</p><p><strong>Methods: </strong>The effect of polymer ratio and addition of PCL on the morphology, diameter, drug delivery, encapsulation efficiency, mechanical properties, antibacterial activity against <i>Escherichia coli</i> and <i>Staphylococcus aureus</i>, cytotoxicity, cell adhesion and proliferation were investigated. 3-(4,5-dimethyldiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to test the cytotoxicity of the nanofibers on the human dermal fibroblast (HDF) cell line. Cell proliferation/adhesion was also determined by imaging HDF cells seeded on mats with scanning electron microscopy/fluorescence microscopy.</p><p><strong>Results: </strong>All nanofibers were bead-free and smooth in the diameter range of 866.7-882.4 nm. They had favorable encapsulation efficiency (≥79.3%), controlled drug release up to 24 h and did not have cytotoxic effects. Although collagen was preferred for cell adhesion and proliferation, its spinnability and mechanical properties were poor. While PU improved the spinnability of collagen, its mechanical properties also enhanced with the addition of PCL. Nevertheless, all mats led to favorable cell adhesion and proliferation. All the nanofibers had antimicrobial activity against <i>Escherichia coli</i> and <i>Staphylococcus aureus</i>.</p><p><strong>Conclusion: </strong>In conclusion, PU/Col and PU/Col/PCL nanofiber mats, which had favorable encapsulation efficiency, controlled drug release and antibacterial activity at least 24 h, cell viability, proliferation, adhesion, mechanical properties to be used as wound dressing, were successfully prepared.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"892-906"},"PeriodicalIF":2.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142581700","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":"Application of cocoa butter for formulation of fast melt tablets containing memantine hydrochloride.","authors":"Ying Hui Loke, Hiu Ching Phang, Ganesan Gobal, Palanirajan Vijayaraj Kumar, Phei Er Kee, Riyanto Teguh Widodo, Bey Hing Goh, Kai Bin Liew","doi":"10.1080/03639045.2024.2417999","DOIUrl":"10.1080/03639045.2024.2417999","url":null,"abstract":"<p><strong>Introduction: </strong>Fast melt tablets (FMTs) provide a convenient dosage form that rapidly dissolves on the tongue without the need for water. Cocoa butter serves as a suitable matrix system for FMTs formulation, facilitating rapid disintegration at body temperature.</p><p><strong>Objectives: </strong>This study aimed to formulate FMTs using cocoa butter as a base and investigate the effect of various disintegrants and superdisintegrants on their characteristics.</p><p><strong>Methods: </strong>Cocoa butter-based FMTs were prepared <i>via</i> the fusion molding technique. Different disintegrants and superdisintegrants were added at varying concentrations and subjected to characterization. The optimal formulation was selected and incorporated with 10 mg memantine hydrochloride.</p><p><strong>Results: </strong>The optimal FMT formulation consisted of 340 mg cocoa butter, 75 mg starch, and 75 mg crospovidone, exhibiting a hardness of 17.12 ± 0.31 N and a disintegration time of 32.67 ± 0.17 s. Furthermore, FMTs demonstrated a faster release profile compared to the commercially available product, Ebixa. SEM micrographs revealed homogenous blending of individual ingredients within the cocoa butter matrix and FT-IR analysis confirmed the chemical stability of memantine hydrochloride in the formulation. The dissolution profile of F17 suggested that the drug in FMTs released faster compared to Ebixia. Memantine hydrochloride achieved 98.07% of drug release in FMTs at 10 min. Moreover, the prepared FMTs exhibited stability for at least 6 months.</p><p><strong>Conclusion: </strong>The successful development of cocoa butter-based FMTs containing memantine hydrochloride highlights the potential of cocoa butter as viable alternative matrix-forming material for FMTs production. This innovative formulation offers patients a convenient alternative for medication administration.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"845-855"},"PeriodicalIF":2.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142460409","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":"TGF-β1 and FOXM1 siRNA co-loaded nanoparticles by Disulfide crosslinked PEG-PDMAEMA for the treatment of triple negative breast cancer and its bone metastases in vitro.","authors":"Xingbo Wang,Hong Huang,Wenxiu Xu,Yanling Gong,Songbo Shi,Xu Wan,Li Pengbiao","doi":"10.1080/03639045.2024.2404979","DOIUrl":"https://doi.org/10.1080/03639045.2024.2404979","url":null,"abstract":"INTRODUCTIONTriple negative breast cancer (TNBC) is characterized with higher malignancy and mortality and is prone to distant metastasis, among which bone is the most common site. It's urgent to explore new strategies for treatment of TNBC and its bone metastases.METHODSA tumor environment responsive vector, poly-(dimethylaminoethyl methacrylate)-SS-poly(ethylene glycol)-SS-poly-(dimethylaminoethyl methacrylate) (PDMAEMA-SS-PEG-SS-PDMAEMA), was constructed to co-delivery transforming growth factor-β1 (TGF-β1) siRNA and forkhead box M1 (FOXM1) siRNA in MDA-MB-231 cells. The preparation, characterization, in vitro release, stability, and transfection efficiency of nanoparticles were measured. Cell viability, migration and invasion of MDA-MB-231 cells were determined. Cell chemotactic migration and cell heterogeneity adhesion of MDA-MB-231 cells to the human osteoblast-like cell line MG-63 were determined.RESULTSPDMAEMA-SS-PEG-SS-PDMAEMA self assembled with siRNA at N/P of 15:1 into nanoparticles with particle size of 122 nm. In vitro release exhibited redox and pH sensitivity, and the nanoparticles protected siRNA from degradation by RNase and serum protein, remaining stable at 4 °C with similar transfection efficiency with lipo2000. Nanoparticles co-loaded with TGF-β1 siRNA and FOXM1 siRNA inhibited the cell viability, migration and invasion of MDA-MB-231 cells, as well as chemotactic migration and heterogeneous adhesion of MDA-MB-231 cells to MG-63 cells, showing a synergetic effect. After gene silencing on TGF-β1 and FOXM1, the epithelial to mesenchymal transition (EMT) related molecules vimentin mRNA expression decreased while E-cadherin increased.CONCLUSIONPDMAEMA-SS-PEG-SS-PDMAEMA was suitable for TGF-β1 siRNA and FOXM1 siRNA delivery, exhibiting synergetic inhibition effect on TNBC and its bone metastases, which might be related to its synergetic inhibition on EMT.","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":"15 1","pages":"1-20"},"PeriodicalIF":3.4,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142251134","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":"Enhancement in the Antibacterial Activity of Rifaximin by Delivery through Gelatin Nanoparticles.","authors":"Nida Iqbal,Amber Bano,Daim Asif Raja,Ali Raza,Rabia Ilyas,Rafia Akhlaq,Imran Saleem,Ayaz Ahmed,Syed Ghulam Musharraf,Muhammad Imran Malik","doi":"10.1080/03639045.2024.2405622","DOIUrl":"https://doi.org/10.1080/03639045.2024.2405622","url":null,"abstract":"OBJECTIVESBacterial infections are a noteworthy global health concern that necessitates the development of new strategies to enhance the potency and efficacy of antibiotics. Rifaximin (RFX), a broad-spectrum antibiotic, exhibits promising antibacterial activity against several bacterial strains. However, its insolubility and impermeability impede the exploitation of its full potential. The objective of the current study is to overcome the inherent caveats of RFX in order to exploit its maximum potential.SIGNIFICANCEThe exploitation of the full potential of antibiotics is necessary for reduction in their dosage and to minimize antibiotic pollution. This is a preliminary study aiming for maximum utilization of RFX at the target site and reduction in its release in unmetabolized form.METHODSGelatin is a biopolymer that has gained significant attention for biomedical applications owing to its inherent biocompatibility and biodegradability. In this study, bovine gelatin nanoparticles (BGNPs) were fabricated by the self-assembly method for their application as a carrier of RFX to enhance its antibacterial activity. The study employs a comprehensive range of experimental techniques to characterize the fabricated BGNPs such as DLS, Zeta Potential, FT-IR, AFM, SEM-EDX, and UV-Vis spectrophotometry.RESULTSThe average size of the fabricated BGNPs was 100 nm with a zeta potential value of -15.3 mV. The loading of RFX on BGNPs rendered an increase in its size to 136 nm with a zeta potential value of -16 mV. In-vitro assays and microscopic analyses were conducted to compare the antibacterial efficacy of RFX and RFX@BGNPs. An excellent loading capacity followed by sustained release of RFX from RFX@BGNPs rendered a significant enhancement in its pharmaceutical efficacy. The release of RFX from RFX@BGNPs followed the Higuchi and Korsmeyer-Peppasmodels. The antibacterial efficacy of RFX against Staphylococcus aureus has doubled by delivery through RFX@BGNPs, assessed by inhibitory and biofilm inhibitory assays. The enhancement in the antibacterial efficiency was further endorsed by SEM and microscopic imaging of the control and treated bacterial colonies.CONCLUSIONThe study demonstrates an enhancement in the antimicrobial efficacy of RFX by its delivery in the form of RFX@BGNPs to exploit its full potential for practical applications.","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":"37 1","pages":"1-15"},"PeriodicalIF":3.4,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142251166","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":"In vitro anticancer efficacy of Calendula Officinalis extract-loaded chitosan nanoparticles against gastric and colon cancer cells.","authors":"Rabia Yilmaz Ozturk,Rabia Cakir","doi":"10.1080/03639045.2024.2404143","DOIUrl":"https://doi.org/10.1080/03639045.2024.2404143","url":null,"abstract":"OBJECTIVEThis study assessed the anticancer activities of calendula officinalis-loaded chitosan nanoparticles in gastric and colon cancer cells compared to fibroblast cells and examined the balance between ROS and antioxidants.METHODSConsidering this information, we synthesized Calendula officinalis-loaded chitosan nanoparticles (CO-CSNPs) via the ionic gelation method. Their characterizations were carried out with ZetaSizer, UV-Vis, FTIR and SEM devices including size, morphology and surface zeta potential analysis, loading capacity, encapsulation efficiency, in vitro drug release, and chemical interactions. The anticancer activities of CO, CSNPs, and CO-CSNPs were tested against AGS, Caco-2, and normal NIH-3T3 cells using an XTT assay. The anticancer effects were evaluated with the DAPI staining, scratch assay, reactive oxygen species (ROS) detection and CUPRAC method on cellular and non-cellular processes that promote anticancer mechanisms.RESULTSResults showed that CO and CO-CNPs exhibited anticancer activity against AGS and Caco-2. Further, the formulation of CO with CSNPs enhanced the anticancer activity of CO while having no cytotoxicity on NIH-3T3. DAPI staining, scratch assay, ROS, and CUPRAC method confirmed the anticancer activity of CO and CO-CSNPs, which resulted in a reduction in the number of apoptotic cells, inhibited migration, triggered apoptotic pathway via ROS, and higher antioxidant activity.CONCLUSIONSThe results of the study indicate that CO-CSNPs are a promising therapeutic formulation for gastric and colon cancer treatment. We consider that this study will lead to the investigation of molecular mechanisms of CO-CSNPs in cancer treatment and their investigation in clinical studies.","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":"4 1","pages":"1-15"},"PeriodicalIF":3.4,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142251130","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":"Poly(lactic acid hydroxyacetic acid)-poly(ethylene glycol)-modified ginsenoside Rg3 nanomedicine enhances anti-tumor effect in hepatocellular carcinoma.","authors":"Wei Zheng,Yuqiao Huang,Qiong Wu,Pu Cheng,Song Yujun,Ben Wang,Qi Huang,Shen Hu","doi":"10.1080/03639045.2024.2402769","DOIUrl":"https://doi.org/10.1080/03639045.2024.2402769","url":null,"abstract":"OBJECTIVEThis research aim to improve bioavailability and anti-hepatocellular carcinoma (HCC) efficacy of Ginsenoside Rg3 by modification with poly (lactic acid hydroxyacetic acid)-poly(ethylene glycol) (PLGA-PEG).METHODSPLGA-PEG-Rg3 was obtained by emulsification and evaluated it physiochemical characterization by FTIR, SEM, laser particle-size analyser and HPLC. The effect of the PLGA-PEG-Rg3 and Rg3 on HepG2 cells was compared in vitro studies, including cell proliferation, transwell and a series of apoptosis detection, and in-situ HCC model.RESULTSThe PLGA-PEG-Rg3 were 122 nm in size and 0.112 in polydispersity index with sustained release profile in vitro. Compared to Rg3, PLGA-PEG-Rg3 was more effective in suppressing HepG2 growth and inducing apoptosis by mitochondrial apoptosis pathway in vitro. and PLGA-PEG modification enhanced the liver-targeting ability and drug circulation time of Rg3 in vivo, resulting in PLGA-PEG-Rg3 possessed superior performance in inhibiting tumor growth and prolonging survival time of tumor-bearing mice than Rg3.CONCLUSIONSOverall, these results showed PLGA-PEG-Rg3 enhanced anti-tumor effect of Rg3 in HCC.","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":"27 1","pages":"1-39"},"PeriodicalIF":3.4,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142197660","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":"A comparative anticancer analysis of iron oxide nanoparticles of <i>Hippophae rhamnoides</i> and <i>Cichorium intybus</i> found in the Karakoram Range of Gilgit Baltistan against liver cancer targeting the <i>RhoA</i> gene.","authors":"Rukhsana Tabassum, Erum Dilshad","doi":"10.1080/03639045.2024.2400209","DOIUrl":"10.1080/03639045.2024.2400209","url":null,"abstract":"<p><strong>Objective: </strong>The current research work focused on the evaluation of of <i>H. rhamnoides</i> and <i>C. intybus</i> Fe₂O₃ NPs against liver cancer cell line (HepG2) by performing antiproliferative assay targeting the <i>RhoA</i> gene and apoptotic pathway genes and proteins.</p><p><strong>Methods: </strong>Fe₂O₃ NPs were synthesized using extracts of <i>H. rhamnoides</i> and <i>C. intybus</i> and characterized by UV-Vis spectroscopy, FTIR, SEM/EDS and XRD. MTT assay was used to study cytotoxicity against the HepG2 cells. Real-time qPCR and ELISA were used for the gene and protein analysis.</p><p><strong>Results: </strong>An absorbance peak at 300 nm for <i>H. rhamnoides</i> and 289 nm for <i>C. intybus</i> nanoparticles were observed by UV-Vis analysis. The FTIR bands of <i>H. rhamnoide</i> Fe₂O₃ NPs suggested the presence of aldehydes, alcohols and polyols whereas bands of <i>C. intybus</i> Fe₂O₃ NPs suggested the presence of carboxyl groups, hydroxyl groups, alkynes and amines. The size of Fe₂O₃ NPs was found to be 27 ± 5nm for <i>H. rhamnoides</i> and 84 ± 4nm for <i>C. intybus.</i> The IC₅₀ value of 41.69 µM for <i>H. rhmnoides</i> and 71.04 µM for <i>C. intybus</i> Fe₂O₃ NPs compared to plant extract (78.10 and 96.03 µM for <i>H. rhamnoides</i> and <i>C. intybus</i>, respectively<i>)</i> were found against HepG2 cells. The gene expression and protein levels of <i>RhoA</i> were decreased whereas those of <i>bax</i>, <i>caspase 3</i>, <i>caspase 8</i> and <i>caspase 9</i> were found increased.</p><p><strong>Conclusion: </strong>Nanoparticles and extract of <i>H. rhamnoides</i> were found more effective as compared to <i>C. intybus</i>, which was evident by the results of cytotoxicity and analysis of studied genes and proteins.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-10"},"PeriodicalIF":2.4,"publicationDate":"2024-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142125128","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":"Quality by design (QbD) based approach for development of itraconazole-loaded transferosomes for skin cancer: <i>in vitro, ex vivo</i> and cell line studies.","authors":"Priya Kudi, Srijita Sen, Satyajit Murkute, Purusottam Mohapatra, Om Prakash Ranjan","doi":"10.1080/03639045.2024.2400203","DOIUrl":"10.1080/03639045.2024.2400203","url":null,"abstract":"<p><strong>Objective: </strong>Itraconazole (ITZ), a widely used systemic antifungal drug, has been ingeniously repurposed for its antitumor effects. In the present work, we have prepared and optimized the ITZ-loaded transferosomes by Quality by Design (QbD) approach and repurposed them for skin cancer.</p><p><strong>Methods: </strong>The transferosomal formulation was optimized by employing a QbD approach with the design of experiment. A combination of screening and optimization design was used for formulation optimization. The optimized formulation was characterized by particle size, PDI, zeta potential, FTIR, XRD, and surface morphology using TEM. <i>In vitro</i> and <i>ex vivo</i> studies were performed using Franz diffusion cells. An <i>in vitro</i> cell line study was performed on the human melanoma A375 cell line.</p><p><strong>Results: </strong>The optimized formulation has a particle size of 192.37 ± 13.19 nm, PDI of 0.41 ± 0.03, zeta potential -47.80 ± 3.66, and an entrapment efficiency of 64.11 ± 3.75%. <i>In vitro</i> release studies showed that ITZ encapsulated transferosomes offer higher and sustained release than pure drugs. <i>Ex vivo</i> drug penetration and retention studies show that the penetration and retention of transferosomes are more visible in the skin than in the drug. The cell viability study confirms that ITZ encapsulated transferosomes have almost 2-fold more potency against the A375 cell line than pure drug.</p><p><strong>Conclusion: </strong>ITZ encapsulated transferosomes were successfully prepared and optimized using a combination of screening and optimization designs. Based on <i>ex vivo</i> and cell line studies, we conclude that ITZ-loaded transferosomes could aid melanoma management alongside standard therapies.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2024-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142125130","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":"Deciphering the cytotoxic potential of acamprosate and acamprosate loaded mesoporous silica nanoparticles in hepatocellular carcinoma: an <i>in vitro</i> and <i>in silico</i> approach.","authors":"Suhail Ahmad Bhat, Sathyapriya Chandramohan, Srividya Subramanian, Sankar Pajaniradje, Neena Yadav, Rukkumani Rajagopalan","doi":"10.1080/03639045.2024.2400202","DOIUrl":"10.1080/03639045.2024.2400202","url":null,"abstract":"<p><p>Hepatocellular carcinoma (HCC) is a healthcare concern that causes most cancer-linked deaths around the world. This work was aimed at unraveling the anticancer potential of acamprosate and development of mesoporous silica nanoparticle (MSN) drug delivery system to increase the therapeutic efficacy of acamprosate. For this purpose, the MSNs were synthesized and encapsulated with acamprosate (MSN-Acamp). The MSN and MSN-Acamp were characterized by DLS, Zeta potential, UV spectroscopy, SEM, FTIR, XRD, DFT, and XPS. Biological effects were evaluated by MTT and lactate dehydrogenase assays. The apoptotic mode of cell death was evaluated by fluorescence imaging and DNA fragmentation assay. Cell cycle assessment and Annexin V-FITC/PI staining were performed to depict the phase of cell arrest and stage of apoptotic cells respectively. The acamprosate was found to exhibit cytotoxic effect and MSN-Acamp exhibited an increased cytotoxicity. Apoptotic mode of cell death was revealed by fluorescence imaging as nuclear fragmentation, production of reactive oxygen species (ROS), loss of membrane potential in mitochondria, and chromatin condensation/fragmentation were found. The docking results revealed that acamprosate had a considerable binding affinity with Bcl-2, Mcl-1, EGFR, and mTOR proteins. Overall, our results indicated that acamprosate and MSN-Acamp had a potent apoptotic effect and MSNs are propitious drug carriers to increase therapeutic effect in HCC.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-20"},"PeriodicalIF":2.4,"publicationDate":"2024-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142125129","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}