Drug Development and Industrial Pharmacy最新文献

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In vitro anticancer efficacy of Calendula Officinalis extract-loaded chitosan nanoparticles against gastric and colon cancer cells. 金盏花提取物负载壳聚糖纳米粒子对胃癌和结肠癌细胞的体外抗癌功效
IF 3.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-13 DOI: 10.1080/03639045.2024.2404143
Rabia Yilmaz Ozturk,Rabia Cakir
{"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}
引用次数: 0
Poly(lactic acid hydroxyacetic acid)-poly(ethylene glycol)-modified ginsenoside Rg3 nanomedicine enhances anti-tumor effect in hepatocellular carcinoma. 聚(乳酸羟基乙酸)-聚(乙二醇)改性人参皂苷 Rg3 纳米药物增强肝细胞癌的抗肿瘤效果
IF 3.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-11 DOI: 10.1080/03639045.2024.2402769
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}
引用次数: 0
A comparative anticancer analysis of iron oxide nanoparticles of Hippophae rhamnoides and Cichorium intybus found in the Karakoram Range of Gilgit Baltistan against liver cancer targeting the RhoA gene. 吉尔吉特-巴尔蒂斯坦喀喇昆仑山脉发现的鼠李和苣苔的氧化铁纳米粒子针对 RhoA 基因对肝癌的抗癌作用比较分析。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-10 DOI: 10.1080/03639045.2024.2400209
Rukhsana Tabassum, Erum Dilshad
{"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}
引用次数: 0
Quality by design (QbD) based approach for development of itraconazole-loaded transferosomes for skin cancer: in vitro, ex vivo and cell line studies. 基于质量源于设计(QbD)的方法,开发治疗皮肤癌的伊曲康唑负载转移体:体外、体内和细胞系研究。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-10 DOI: 10.1080/03639045.2024.2400203
Priya Kudi, Srijita Sen, Satyajit Murkute, Purusottam Mohapatra, Om Prakash Ranjan
{"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}
引用次数: 0
Deciphering the cytotoxic potential of acamprosate and acamprosate loaded mesoporous silica nanoparticles in hepatocellular carcinoma: an in vitro and in silico approach. 解密阿坎酸和阿坎酸负载介孔二氧化硅纳米粒子在肝细胞癌中的细胞毒性潜力:一种体外和硅学方法。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-09 DOI: 10.1080/03639045.2024.2400202
Suhail Ahmad Bhat, Sathyapriya Chandramohan, Srividya Subramanian, Sankar Pajaniradje, Neena Yadav, Rukkumani Rajagopalan
{"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}
引用次数: 0
Chrysin-functionalized gold nanoparticles and paclitaxel exhibit synergistic impact on lung cancer cell lines via regulating the AKT/PPAR-ϒ/β-catenin pathway. 蛹虫草素功能化金纳米粒子和紫杉醇通过调节 AKT/PPAR-ϒ/β-Catenin 通路对肺癌细胞株产生协同作用。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-03 DOI: 10.1080/03639045.2024.2393327
Saheli Roy, Shashi Kant, Krishna Das Saha, Tarun Jha
{"title":"Chrysin-functionalized gold nanoparticles and paclitaxel exhibit synergistic impact on lung cancer cell lines via regulating the AKT/PPAR-ϒ/β-catenin pathway.","authors":"Saheli Roy, Shashi Kant, Krishna Das Saha, Tarun Jha","doi":"10.1080/03639045.2024.2393327","DOIUrl":"10.1080/03639045.2024.2393327","url":null,"abstract":"<p><p>Lung cancer has become progressively widespread, posing a challenge to traditional chemotherapeutic drugs such as platinum compounds and paclitaxel (PTX) owing to growing resistance. Along with that, the chemotherapeutic drugs infer major side effects. The usage of natural compounds as chemosensitizers to boost the efficacy of these chemotherapeutic drugs and minimizing their toxicity is a plausible approach. In our investigation, we employed PTX as the standard chemotherapeutic agent and utilized chrysin-functionalized gold nanoparticles (CHR-AuNPs) to augment its cytotoxicity. Gold nanoparticles were chosen for their inherent cytotoxic properties and ability to enhance chrysin's bioavailability and solubility. Characterization of CHR-AuNP revealed spherical nanoparticles within the nano-size range (35-70 nm) with a stable negative zeta potential of -22 mV, confirmed by physicochemical analyses including UV-visible spectroscopy, Fourier transform infrared (FTIR) spectral analysis, and visual observation of the wine-red coloration. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay cytotoxicity studies demonstrated CHR-AuNP's superior efficacy compared to CHR alone, with synergistic effects observed in combination with PTX, validated by Compusyn software. Morphological changes indicative of apoptosis were more pronounced with combined treatment, corroborated by acridine orange/ethidium bromide (AO/EtBr) staining and Annexin V assays. Furthermore, the combination treatment amplified reactive oxygen species (ROS) production and destabilized mitochondrial membrane potential, while altering the expression of pro-apoptotic and anti-apoptotic proteins. Exploring the mechanistic pathways, we found that the drugs upregulated PPAR-γ expression while suppressing Akt and overexpressing PTEN, thereby impeding the Wnt/β-catenin pathway commonly dysregulated in lung cancer. This highlights the potential of low-dose combination therapy with PTX and CHR-AuNP as a promising strategy for addressing lung cancer's challenges.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2024-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142003872","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
Lymphatic targeting of cilnidipine by designing and developing a nanostructured lipid carrier drug delivery system. 通过设计和开发纳米结构脂质载体给药系统实现西尼地平的淋巴靶向作用
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-01 Epub Date: 2024-10-21 DOI: 10.1080/03639045.2024.2415638
Preeti Rajabhau Meshram, Nisharani Sudhakar Ranpise
{"title":"Lymphatic targeting of cilnidipine by designing and developing a nanostructured lipid carrier drug delivery system.","authors":"Preeti Rajabhau Meshram, Nisharani Sudhakar Ranpise","doi":"10.1080/03639045.2024.2415638","DOIUrl":"10.1080/03639045.2024.2415638","url":null,"abstract":"<p><strong>Objective: </strong>The objective of current research is to design, develop, and optimize a cilnidipine (CLN) nanostructured lipid carrier (NLC)-based drug delivery system for the effective treatment of hypertension (HT).</p><p><strong>Significance: </strong>Oral administration of CLN-loaded NLC (CLN NLC) containing glyceryl monostearate (GMS) as a solid and isopropyl myristate (IPM) as a liquid lipid may show remarkable lymphatic uptake through payer patches.</p><p><strong>Methods: </strong>The emulsification probe sonication technique was used followed by optimization using 3<sup>2</sup> factorial designs.</p><p><strong>Results: </strong>The optimized batch showed a mean particle size of 115.4 ± 0.22 nm with encapsulation efficiency of 98.32 ± 0.23%, polydispersity index (PDI) of 0.342 ± 0.03, and zeta potential (ZP, <i>ζ</i>) was -60.5 ± 0.24 which indicate excellent physical stability. <i>In vitro</i> studies showed a controlled release of CLN NLCs. Pharmacokinetics studies determined the <i>C</i><sub>max</sub> of NLCs (373.47 ± 15.1) indicates 2.3-fold enhancement compared with plain drug (160.64 ± 7.63). Pharmacodynamic studies indicated that CLN NLCs were maintaining systolic blood pressure in a controlled manner without any signs of side effects.</p><p><strong>Conclusion: </strong>CLN NLCs significantly improved lymphatic delivery and proved to be effective in the treatment and management of HT. It has been proved that CLN NLCs are found to be better than any traditional CLN dosage form due to enhancement in solubility, absorption, bioavailability, intestinal permeability, avoidance of first-pass metabolism, P-glycoprotein efflux and reduction in dose-related side effects, achievement of controlled and sustained release action.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"827-843"},"PeriodicalIF":2.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142460410","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
Comparison of oven drying and freeze drying methods for the production of fast melt films containing quetiapine fumarate. 比较烘箱干燥法和冷冻干燥法生产含富马酸喹硫平的快速熔融薄膜。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-01 Epub Date: 2024-10-01 DOI: 10.1080/03639045.2024.2409168
Hiu Ching Phang, Zhi Qi Ng, Najwa Mohamad, Yik Ling Chew, Ashok Balaraman, Phei Er Kee, Kenji Mishima, Bey Hing Goh, Long Chiau Ming, Kai Bin Liew
{"title":"Comparison of oven drying and freeze drying methods for the production of fast melt films containing quetiapine fumarate.","authors":"Hiu Ching Phang, Zhi Qi Ng, Najwa Mohamad, Yik Ling Chew, Ashok Balaraman, Phei Er Kee, Kenji Mishima, Bey Hing Goh, Long Chiau Ming, Kai Bin Liew","doi":"10.1080/03639045.2024.2409168","DOIUrl":"10.1080/03639045.2024.2409168","url":null,"abstract":"<p><strong>Background: </strong>Quetiapine fumarate (QTP) is commonly prescribed for schizophrenic patient, typically available in tablet or oral suspension form, presenting challenges such as administration difficulties, fear of choking and distaste for its bitter taste. Fast melt films (FMF) offer an alternative dosage form with a simple development process, ease of administration and rapid drug absorption and action onset.</p><p><strong>Objective: </strong>This study aims to prepare FMF with different formulations using solvent casting methods and to compare the effects of different drying methods, including oven drying and freeze drying, on the properties of the films.</p><p><strong>Methods: </strong>Various formulations were created by manipulating polymer types (starch, hydroxypropyl methylcellulose (HPMC) and guar gum) at different concentrations, along with fixed concentrations of QTP and other excipients. Characterization tests including surface morphology, weight, thickness, pH, tensile strength, elongation length, Young's modulus, folding endurance and disintegration time were conducted. The optimal FMF formulation was identified and further evaluated for moisture and drug content, dissolution behavior, accelerated stability, X-ray diffraction (XRD), and palatability.</p><p><strong>Results: </strong>FMF containing 10 mg guar gum/film developed using oven drying emerged as the optimum choice, exhibiting desirable film appearance, ultra-thin thickness (0.453 ± 0.002 mm), appropriate pH for oral intake (pH 5.0), optimal moisture content of 11.810%, rapid disintegration (52.67 ± 1.53 s), high flexibility (folding endurance > 300 times) and lower Young's modulus (1.308 ± 0.214).</p><p><strong>Conclusion: </strong>Oven drying method has been proven to be favorable for developing FMF containing QTP, meeting all testing criteria and providing an alternative option for QTP prescription.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"810-826"},"PeriodicalIF":2.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142343507","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
Olive oil and flaxseed oil incorporating niosomes for enhanced in vivo anti-diabetic efficacy of canagliflozin. 添加橄榄油和亚麻籽油的niosomes可增强卡格列净的体内抗糖尿病疗效。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-09-01 Epub Date: 2024-09-30 DOI: 10.1080/03639045.2024.2409167
Ghada Saad, Gamal M El Maghraby, Amal A Sultan
{"title":"Olive oil and flaxseed oil incorporating niosomes for enhanced <i>in vivo</i> anti-diabetic efficacy of canagliflozin.","authors":"Ghada Saad, Gamal M El Maghraby, Amal A Sultan","doi":"10.1080/03639045.2024.2409167","DOIUrl":"10.1080/03639045.2024.2409167","url":null,"abstract":"<p><strong>Background: </strong>Canagliflozin (CFZ) is broadly implicated for the management of type 2 diabetes mellitus. Unfortunately, it has low oral bioavailability due to poor solubility behavior and restricted membrane permeability.</p><p><strong>Objective: </strong>The current work focuses on development of CFZ encapsulated niosomes for enhanced oral anti-diabetic efficacy.</p><p><strong>Methodology: </strong>Niosomes comprising Span 60 and cholesterol were formulated both in absence and presence of olive oil or flaxseed oil. These were evaluated <i>in vitro</i> for average vesicular size, structural morphology, CFZ entrapment efficiency, and drug release. Additionally, the oral hypoglycemic effect of CFZ encapsulated niosomes was explored in diabetic rats.</p><p><strong>Results: </strong>The fabricated niosomes were negatively charged spherical vesicles with a size range of 103.0-141.7 nm. These entrapped CFZ with efficiency ranging from 92.3% to 96.0%. Drug release investigations reflected that incorporating CFZ into niosomes significantly sustained drug release compared to the aqueous drug dispersion. Oral administration of niosomal formulations significantly enhanced the oral antidiabetic effect of CFZ. Comparing the tested niosomes, similar efficiency was shown eliminating the effect of composition.</p><p><strong>Conclusion: </strong>The enhanced oral bioavailability of niosomes' encapsulated drugs is related to niosomal vesicular structure which allows intact niosomes absorption. The study presented niosomes as promising carriers for improved oral anti-diabetic activity of CFZ.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"801-809"},"PeriodicalIF":2.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142343508","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
Fabrication and optimization of naringin-loaded MOF-5 encapsulated by liponiosomes as smart drug delivery, cytotoxicity, and apoptotic on breast cancer cells. 制作和优化脂质体包裹的 MOF-5 中的柚皮苷作为智能药物递送,对乳腺癌细胞具有细胞毒性和凋亡作用。
IF 2.4 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2024-08-12 DOI: 10.1080/03639045.2024.2388786
Lina M Alneghery, Mohammed Al-Zharani, Fahd A Nasr, Zienab E Eldin, Tayel A Al Hujran, Hesham M Tawfeek, Mohamed H Fayed, Shehab Elbeltagi
{"title":"Fabrication and optimization of naringin-loaded MOF-5 encapsulated by liponiosomes as smart drug delivery, cytotoxicity, and apoptotic on breast cancer cells.","authors":"Lina M Alneghery, Mohammed Al-Zharani, Fahd A Nasr, Zienab E Eldin, Tayel A Al Hujran, Hesham M Tawfeek, Mohamed H Fayed, Shehab Elbeltagi","doi":"10.1080/03639045.2024.2388786","DOIUrl":"10.1080/03639045.2024.2388786","url":null,"abstract":"<p><strong>Introduction: </strong>Cancers are regarded as hazardous due to their high worldwide death rate, with breast cancer (BC), which affects practically all cancer patients globally, playing a significant role in this statistic. The therapeutic approach for BC has not advanced using standard techniques, such as specialized naringin (NG) chemotherapy. Instead, a novel strategy has been utilized to enhance smart drug delivery (SDD) to tumors.</p><p><strong>Significance: </strong>Herein, we established NG-loaded zinc metal-organic framework-5 (NG-MOF-5) coated with liponiosomes (LNs) to manufacture NG-MOF-5@LNs nanoparticles (NPs) for antibacterial and cancer treatment.</p><p><strong>Methods: </strong>MOF-5, NG, and NG-MOF-5@LNs were evaluated with XRD, thermogravimetric analysis (TGA), FTIR, SEM, TEM, PDI, ZP, encapsulation efficiency (EE), loading efficiency (LE), and drug release (DR) kinetics. We examined the antibacterial activity involving minimum inhibitory concentration (MIC) and zone of inhibition by NG, MOF-5, and NG-MOF-5@LNs. The cell viability, necrosis, and total apoptosis (late and early) were evaluated for anti-cancer activity against MCF-7 BC cells.</p><p><strong>Results: </strong>TEM results demonstrated that NG-MOF-5@LNs formed monodispersed spherical-like particles with a size of 122.5 nm, PDI of 0.139, and ZP of +21 mV. The anti-microbial activity results indicated that NG-MOF-5@LNs exhibited potent antibacterial effects, as evidenced by inhibition zones and MIC values. The Higuchi model indicates an excellent fit (<i>R</i><sup>2</sup> = 0.9988). The MTT assay revealed anti-tumor activity against MCF-7 BC cells, with IC<sub>50</sub> of 21 µg/mL for NG-MOF-5@LNs and demonstrating a total apoptosis effect of 68.2% on MCF-7 cells.</p><p><strong>Conclusion: </strong>NG-MOF-5@LNs is anticipated to show as an effective antimicrobial and novel long-term-release antitumor agent and might be more suitable for MCF-7 cell therapy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2024-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141888763","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}
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