{"title":"Preparation and characterization of soluplus-based nanosuspension for dissolution enhancement of indomethacin using ultrasonic assisted precipitation method for formulation and Box-Behnken design for optimization.","authors":"Areen Alshweiat, Eqbal Abu-Alkebash, Alaa Abuawad, Tamara Athamneh, Shorooq Abukhamees, Muna Oqal","doi":"10.1080/03639045.2024.2424307","DOIUrl":"10.1080/03639045.2024.2424307","url":null,"abstract":"<p><strong>Objectives: </strong>Nanosuspensions are increasingly recognized as a valuable technology for enhancing poorly water-soluble drugs' solubility and dissolution rate, thereby improving their bioavailability. In this study, we employed ultrasonic-assisted precipitation to fabricate nanosuspensions of indomethacin (IND), utilizing Soluplus<sup>®</sup> (Sol) as a stabilizing agent. Our objectives were driven by hypotheses centered on optimizing formulation variables and developing predictive models for optimal IND formulations.</p><p><strong>Significance: </strong>This research highlights the Box-Behnken design (BBD) as a powerful tool that optimizes the properties of IND nanosuspensions, thus significantly enhancing their dissolution rate.</p><p><strong>Methods: </strong>The impacts of the independent variables on the mean particle size (MPS), polydispersity index (PDI), and zeta potential (ZP) were investigated using BBD. The optimized nanosuspension was freeze-dried with 3% trehalose to produce a dry nanosuspension (DNS). The DNS was characterized by SEM, DSC, XRPD, solubility, and dissolution.</p><p><strong>Results: </strong>The IND: Sol ratio and sonication power significantly affected the MPS and ZP of the nanosuspensions. The optimized formulation showed MPS, PDI, and ZP of 144.77 ± 6.68 nm, 0.26 ± 0.08, and -24.6 ± 1.90 mV, respectively. The DNS exhibited spherical particle morphology. The DSC and XRPD confirmed the amorphous state of IND with enhanced solubility and dissolution of IND. DNS showed a 3.7-fold increase in drug release in the first 15 min compared with raw IND.</p><p><strong>Conclusions: </strong>This study demonstrated the critical role of BBD in accurately predicting the values of independent variables essential for formulating optimal nanosuspensions. These formulations possess specific properties that can be effectively integrated into various dosage forms tailored for different routes of administration.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"878-891"},"PeriodicalIF":2.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142581798","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":"pH sensitive lipid polymeric hybrid nanoparticle (LPHNP) of paclitaxel and curcumin for targeted delivery in breast cancer.","authors":"Hrishikesh Sarma, Ankit Dutta, Alakesh Bharali, Sheikh Sofiur Rahman, Sunayana Baruah, Nikhil Biswas, Bhanu P Sahu","doi":"10.1080/03639045.2024.2421198","DOIUrl":"10.1080/03639045.2024.2421198","url":null,"abstract":"<p><strong>Objective: </strong>The study aimed at designing a pH sensitive Lipid polymeric Hybrid nanoparticle (LPHNP) for targeted release of Paclitaxel (PTX) and Curcumin (CUR) in breast cancer.</p><p><strong>Significance: </strong>Such systems shall result in controlled triggered release in acidic microenvironment of tumor cells with improved pharmacokinetic profile.</p><p><strong>Methods: </strong>Chitosan-coated CUR and PTX coloaded pH-sensitive LPHNPs were synthesized employing nanoprecipitation technique. The synthesized NPs were characterized in terms of particle size, polydispersity index (PDI), zeta potential, and morphology.</p><p><strong>Results: </strong>LPHNPs co-loaded with curcumin (CUR) and paclitaxel (PTX) were successfully formulated, achieving a size of 146 nm, a PDI of 0.18, and an entrapment efficiency exceeding 90%. <i>In vitro</i> release studies demonstrated controlled release of CUR and PTX under tumor pH conditions showing 1.6 fold and 1.7 fold higher release in ABS pH 5 in comparison to PBS 7.4 for PTX and CUR respectively. MTT-assay studies revealed enhanced cytotoxicity of CUR and PTX as LPHNPs showing IC<sub>50</sub> value of free CUR & PTX 480.06 µg/mL decreasing to 282.97 µg/mL for CS-CUR-PTX-LPHNPs. <i>In vivo</i> pharmacokinetic evaluations in rats confirmed significantly improved bioavailability, with a 3.8-fold increase in AUC for CUR and a 6.6-fold increase for PTX. Additionally, the LPHNPs demonstrated controlled release and prolonged retention, evidenced by a 2.2-fold increase in the half-life (t1/2) of CUR and a 1.3-fold increase in the half-life of PTX.</p><p><p>The results underscores potential of chitosan-coated LPHNP as a promising delivery platform, offering high drug loading, optimal size for cellular penetration, and prolonged blood circulation for cancer.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"856-864"},"PeriodicalIF":2.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142496931","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":"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}
Tugba Eren Boncu, Çiğdem Yücel, Ahmet Ceylan, Mehmet Cadir, Ertugrul Sahmetlioglu
{"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}
Ying Hui Loke, Hiu Ching Phang, Ganesan Gobal, Palanirajan Vijayaraj Kumar, Phei Er Kee, Riyanto Teguh Widodo, Bey Hing Goh, Kai Bin Liew
{"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}
Wei Zheng,Yuqiao Huang,Qiong Wu,Pu Cheng,Song Yujun,Ben Wang,Qi Huang,Shen Hu
{"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> Fe<sub>2</sub>O<sub>3</sub> 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>Fe<sub>2</sub>O<sub>3</sub> 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> Fe<sub>2</sub>O<sub>3</sub> NPs suggested the presence of aldehydes, alcohols and polyols whereas bands of <i>C. intybus</i> Fe<sub>2</sub>O<sub>3</sub> NPs suggested the presence of carboxyl groups, hydroxyl groups, alkynes and amines. The size of Fe<sub>2</sub>O<sub>3</sub> NPs was found to be 27 ± 5nm for <i>H. rhamnoides</i> and 84 ± 4nm for <i>C. intybus.</i> The IC<sub>50</sub> value of 41.69 µM for <i>H. rhmnoides</i> and 71.04 µM for <i>C. intybus</i> Fe<sub>2</sub>O<sub>3</sub> 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}