International Journal of Pharmaceutics: X最新文献

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Evaluating a targeted Palbociclib-Trastuzumab loaded smart niosome platform for treating HER2 positive breast cancer cells 评估用于治疗 HER2 阳性乳腺癌细胞的靶向 Palbociclib-Trastuzumab 负载智能 niosome 平台
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-03-11 DOI: 10.1016/j.ijpx.2024.100237
Shaghayegh Saharkhiz , Negar Nasri , Nazanin Naderi , Ghasem Dini , Saeid Shirzadi Ghalehshahi , Fateme Firoozbakht
{"title":"Evaluating a targeted Palbociclib-Trastuzumab loaded smart niosome platform for treating HER2 positive breast cancer cells","authors":"Shaghayegh Saharkhiz ,&nbsp;Negar Nasri ,&nbsp;Nazanin Naderi ,&nbsp;Ghasem Dini ,&nbsp;Saeid Shirzadi Ghalehshahi ,&nbsp;Fateme Firoozbakht","doi":"10.1016/j.ijpx.2024.100237","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100237","url":null,"abstract":"<div><p>In this study, we present a targeted and pH-sensitive niosomal (pHSN) formulation, incorporating quantum dot (QD)-labeled Trastuzumab (Trz) molecules for the specific delivery of Palbociclib (Pal) to cells overexpressing human epidermal growth factor receptor 2 (HER2). FTIR analyses confirmed the successful preparation of the pHSNs and their bioconjugation. The labeled Trz-conjugated Pal-pHSNs (Trz-Pal-pHSNs) exhibited a size of approximately 170 nm, displaying a spherical shape with a neutral surface charge of −1.2 mV. Pal encapsulation reached ∼86%, and the release pattern followed a two-phase pH-dependent mechanism. MTT assessments demonstrated enhanced apoptosis induction, particularly in HER2-positive cells, by Trz-Pal-pHSNs. Fluorescence imaging further validated the internalization of particles into cells. In conclusion, Trz-Pal-pHSNs emerge as a promising platform for personalized medicine in the treatment of HER2-positive breast cancer.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100237"},"PeriodicalIF":4.7,"publicationDate":"2024-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000094/pdfft?md5=72f0b03793377c22e7fd9492588d41d1&pid=1-s2.0-S2590156724000094-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140134297","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Rationalized landscape on protein-based cancer nanomedicine: Recent progress and challenges 基于蛋白质的癌症纳米医学的合理前景:最新进展与挑战
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-03-11 DOI: 10.1016/j.ijpx.2024.100238
Zhechen Fan , Haroon Iqbal , Jiang Ni , Naveed Ullah Khan , Shahla Irshad , Anam Razzaq , Mohammad Y. Alfaifi , Serag Eldin I. Elbehairi , Ali A. Shati , Jianping Zhou , Hao Cheng
{"title":"Rationalized landscape on protein-based cancer nanomedicine: Recent progress and challenges","authors":"Zhechen Fan ,&nbsp;Haroon Iqbal ,&nbsp;Jiang Ni ,&nbsp;Naveed Ullah Khan ,&nbsp;Shahla Irshad ,&nbsp;Anam Razzaq ,&nbsp;Mohammad Y. Alfaifi ,&nbsp;Serag Eldin I. Elbehairi ,&nbsp;Ali A. Shati ,&nbsp;Jianping Zhou ,&nbsp;Hao Cheng","doi":"10.1016/j.ijpx.2024.100238","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100238","url":null,"abstract":"<div><p>The clinical advancement of protein-based nanomedicine has revolutionized medical professionals' perspectives on cancer therapy. Protein-based nanoparticles have been exploited as attractive vehicles for cancer nanomedicine due to their unique properties derived from naturally biomacromolecules with superior biocompatibility and pharmaceutical features. Furthermore, the successful translation of Abraxane™ (paclitaxel-based albumin nanoparticles) into clinical application opened a new avenue for protein-based cancer nanomedicine. In this mini-review article, we demonstrate the rational design and recent progress of protein-based nanoparticles along with their applications in cancer diagnosis and therapy from recent literature. The current challenges and hurdles that hinder clinical application of protein-based nanoparticles are highlighted. Finally, future perspectives for translating protein-based nanoparticles into clinic are identified.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100238"},"PeriodicalIF":4.7,"publicationDate":"2024-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000100/pdfft?md5=2a1875e2e0561c02f64b4fb2ab03e865&pid=1-s2.0-S2590156724000100-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140122571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dual-responsive chondroitin sulfate self-assembling nanoparticles for combination therapy in metastatic cancer cells 用于转移性癌细胞联合治疗的双响应硫酸软骨素自组装纳米粒子
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-03-05 DOI: 10.1016/j.ijpx.2024.100235
Ensieh Poursani , Giuseppe Cirillo , Manuela Curcio , Orazio Vittorio , Michele De Luca , Antonella Leggio , Fiore Pasquale Nicoletta , Francesca Iemma
{"title":"Dual-responsive chondroitin sulfate self-assembling nanoparticles for combination therapy in metastatic cancer cells","authors":"Ensieh Poursani ,&nbsp;Giuseppe Cirillo ,&nbsp;Manuela Curcio ,&nbsp;Orazio Vittorio ,&nbsp;Michele De Luca ,&nbsp;Antonella Leggio ,&nbsp;Fiore Pasquale Nicoletta ,&nbsp;Francesca Iemma","doi":"10.1016/j.ijpx.2024.100235","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100235","url":null,"abstract":"<div><p>In this study, we developed self-assembling nanoparticles (LCPs) able to trigger the release of Chlorambucil (Chl) and Doxorubicin (DOX) to MDA-MB-231 cells by exploiting the enzyme and redox signals. The DOX loaded LCPs was prepared by the self-assembly of two chondroitin sulphate (CS) derivatives, obtained by the covalent conjugation of Lipoic Acid (LA) and Chlorambucil (Chl) to the CS backbone. After the physic-chemical characterization of the conjugates by FT-IR, <sup>1</sup>H NMR, and determination of the critical aggregation concentration, spherical nanoparticles with mean hydrodynamic diameter of 45 nm (P.D.I. 0.24) and <em>Z</em>-potential of - 44 mV were obtained by water addition/solvent evaporation method. In vitro experiments for the release of Chl and DOX were performed in healthy and cancer cells, using a cell culture media to maintain the physiological intracellular conditions (pH 7.4) (and concentration of esterase and GSH. The results allowed the selective release of the payloads to be detected: Chl release of 0 and 41% were obtained after 2 h incubation in normal and in cancer cells respectively, while values of 35 (in healthy cells) and 60% (in cancer cells) were recorded for DOX release after 96 h. Finally, viability studies proved the ability of the newly proposed nanosystem to enhance the cytotoxic activity of the two drugs against cancer cells.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100235"},"PeriodicalIF":4.7,"publicationDate":"2024-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000070/pdfft?md5=625bb0fe8f8d17a646ce9861a6328e0a&pid=1-s2.0-S2590156724000070-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140051728","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design and validation of a custom-made system to measure transepithelial electrical impedance in human corneas preserved in active storage machine 设计和验证定制系统,测量保存在活性存储机中的人类角膜的经皮层电阻抗
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-02-09 DOI: 10.1016/j.ijpx.2024.100234
Marielle Mentek , Benjamin Peyret , Siwar Zouari , Sébastien Urbaniak , Jean-Marie Papillon , Emmanuel Crouzet , Chantal Perrache , Sophie Hodin , Xavier Delavenne , Zhiguo He , Philippe Gain , Gilles Thuret
{"title":"Design and validation of a custom-made system to measure transepithelial electrical impedance in human corneas preserved in active storage machine","authors":"Marielle Mentek ,&nbsp;Benjamin Peyret ,&nbsp;Siwar Zouari ,&nbsp;Sébastien Urbaniak ,&nbsp;Jean-Marie Papillon ,&nbsp;Emmanuel Crouzet ,&nbsp;Chantal Perrache ,&nbsp;Sophie Hodin ,&nbsp;Xavier Delavenne ,&nbsp;Zhiguo He ,&nbsp;Philippe Gain ,&nbsp;Gilles Thuret","doi":"10.1016/j.ijpx.2024.100234","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100234","url":null,"abstract":"<div><p>Corneal epithelial barrier represents one of the major limitations to ocular drug delivery and can be explored non-invasively through the evaluation of its electrical properties. Human corneas stored in active storage machine (ASM) could represent an interesting physiological model to explore transcorneal drug penetration. We designed a new system adapted to human corneas preserved in ASM to explore corneal epithelial barrier function ex-vivo. A bipolar set-up including Ag/AgCl electrodes adaptors to fit the corneal ASM and a dedicated software was designed and tested on freshly excised porcine corneas (<em>n</em> = 59) and human corneas stored 14 days in ASM (<em>n</em> = 6). Porcine corneas presented significant and proportional decrease in corneal impedance in response to increasing-size epithelial ulcerations and acute exposure to benzalkonium chloride (BAC) 0.01 and 0.05%. Human corneas stored 14 days in ASM presented a significant increase in corneal impedance associated with the restoration of a multi-layer epithelium and an enhanced expression of tight junctions markers zonula occludens 1, claudin 1 and occludin. These results support the relevance of the developed approach to pursue the exploration and development of human corneas stored in ASM as a physiological pharmacological model.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100234"},"PeriodicalIF":4.7,"publicationDate":"2024-02-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000069/pdfft?md5=1415dea1eb2579fd72e98a2f249aba2c&pid=1-s2.0-S2590156724000069-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139725760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Colon targeting in rats, dogs and IBD patients with species-independent film coatings 在大鼠、狗和 IBD 患者中使用与物种无关的薄膜涂层进行结肠靶向治疗
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-02-08 DOI: 10.1016/j.ijpx.2024.100233
F. Ferraro , L.M. Sonnleitner , C. Neut , S. Mahieux , J. Verin , J. Siepmann , F. Siepmann
{"title":"Colon targeting in rats, dogs and IBD patients with species-independent film coatings","authors":"F. Ferraro ,&nbsp;L.M. Sonnleitner ,&nbsp;C. Neut ,&nbsp;S. Mahieux ,&nbsp;J. Verin ,&nbsp;J. Siepmann ,&nbsp;F. Siepmann","doi":"10.1016/j.ijpx.2024.100233","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100233","url":null,"abstract":"<div><p>Polysaccharides were identified, which allow for colon targeting in human Inflammatory Bowel Disease (IBD) patients, as well as in rats and dogs (which are frequently used as animals in preclinical studies). The polysaccharides are degraded by colonic enzymes (secreted by bacteria), triggering the onset of drug release at the target site. It has to be pointed out that the microbiota in rats, dogs and humans substantially differ. Thus, the performance of this type of colon targeting system observed in animals might not be predictive for patients. The aim of this study was to limit this risk. Different polysaccharides were exposed to culture medium inoculated with fecal samples from IBD patients, healthy dogs and “IBD rats” (in which colonic inflammation was induced). Dynamic changes in the pH of the culture medium were used as an indicator for the proliferation of the bacteria and, thus, the potential of the polysaccharides to serve as their substrate. Fundamental differences were observed with respect to the extent of the pH variations as well as their species-dependency. The most promising polysaccharides were used to prepare polymeric film coatings surrounding 5-aminosaliciylic acid (5-ASA)-loaded starter cores. To limit premature polysaccharide dissolution/swelling in the upper gastro intestinal tract, ethylcellulose was also included in the film coatings. Drug release was monitored upon exposure to culture medium inoculated with fecal samples from IBD patients, healthy dogs and “IBD rats”. For reasons of comparison, also 5-ASA release in pure culture medium was measured. Most film coatings showed highly species-dependent drug release kinetics or limited colon targeting capacity. Interestingly, extracts from aloe vera and reishi (a mushroom) showed a promising potential for colon targeting in <em>all</em> species.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100233"},"PeriodicalIF":4.7,"publicationDate":"2024-02-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000057/pdfft?md5=c0b0a088fe205558dd451ddd92066b61&pid=1-s2.0-S2590156724000057-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139733356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development and optimization of vildagliptin solid lipid nanoparticles loaded ocuserts for controlled ocular delivery: A promising approach towards treating diabetic retinopathy 开发和优化用于眼部控制给药的维达列汀固体脂质纳米颗粒:治疗糖尿病视网膜病变的有效方法
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-02-04 DOI: 10.1016/j.ijpx.2024.100232
Abd El hakim Ramadan , Mahmoud M.A. Elsayed , Amani Elsayed , Marwa A. Fouad , Mohamed S. Mohamed , Sangmin Lee , Reda A. Mahmoud , Shereen A. Sabry , Mohammed M. Ghoneim , Ahmed H.E. Hassan , Reham A. Abd Elkarim , Amany Belal , Ahmed A. El-Shenawy
{"title":"Development and optimization of vildagliptin solid lipid nanoparticles loaded ocuserts for controlled ocular delivery: A promising approach towards treating diabetic retinopathy","authors":"Abd El hakim Ramadan ,&nbsp;Mahmoud M.A. Elsayed ,&nbsp;Amani Elsayed ,&nbsp;Marwa A. Fouad ,&nbsp;Mohamed S. Mohamed ,&nbsp;Sangmin Lee ,&nbsp;Reda A. Mahmoud ,&nbsp;Shereen A. Sabry ,&nbsp;Mohammed M. Ghoneim ,&nbsp;Ahmed H.E. Hassan ,&nbsp;Reham A. Abd Elkarim ,&nbsp;Amany Belal ,&nbsp;Ahmed A. El-Shenawy","doi":"10.1016/j.ijpx.2024.100232","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100232","url":null,"abstract":"<div><p>Diabetes mellitus (DM) is the most prevalent cause of diabetic retinopathy (DRP). DRP has been recognized for a long time as a microvascular disease. Many drugs were used to treat DRP, including vildagliptin (VLD). In addition to its hypoglycemic effect, VLD minimizes ocular inflammation and improves retinal blood flow for individuals with type 2 diabetes mellitus. Nevertheless, VLD can cause upper respiratory tract infections, diarrhea, nausea, hypoglycemia, and poor tolerability when taken orally regularly due to its high water solubility and permeability. Effective ocular administration of VLD is achieved using solid lipid nanoparticles (SLNPs), which improve corneal absorption, prolonged retention, and extended drug release. Ocuserts (OCUs) are sterile, long-acting ocular dosage forms that diminish the need for frequent dosing while improving residence time and stability. Therefore, this study intends to develop VLD solid lipid nanoparticle OCUs (VLD-SLNPs-OCUs) to circumvent the issues commonly associated with VLD. SLNPs were prepared using the double-emulsion/melt dispersion technique. The optimal formula has been implemented in OCUs. Optimization and development of VLD-SLNPs-OCUs were performed using a Box-Behnken Design (BBD). VLD-SLNPs-OCUs loading efficiency was 95.28 ± 2.87%, and differential scanning calorimetry data (DSC) showed the full transformation of VLD to an amorphous state and the excellent distribution in the prepared OCUs matrices. The <em>in vivo</em> release of VLD from the optimized OCUs after 24 h was 35.12 ± 2.47%, consistent with <em>in vitro</em> drug release data of 36.89 ± 3.11. The optimized OCUs are safe to use in the eye, as shown by the ocular irritation test. VLD-SLNPs-OCUs provide extended VLD release, an advantageous alternative to conventional oral dose forms, resulting in fewer systemic adverse effects and less variation in plasma drug levels. VLD-SLNPs-OCUs might benefit retinal microvascular blood flow beyond blood glucose control and may be considered a promising approach to treating diabetic retinopathy.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100232"},"PeriodicalIF":4.7,"publicationDate":"2024-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000045/pdfft?md5=fbb4415e298afe0eccf06c47aa046056&pid=1-s2.0-S2590156724000045-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139710150","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Magnetic nanosystem a tool for targeted delivery and diagnostic application: Current challenges and recent advancement 磁性纳米系统是定向输送和诊断应用的工具:当前挑战与最新进展
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-01-23 DOI: 10.1016/j.ijpx.2024.100231
Nilesh Rarokar , Sakshi Yadav , Suprit Saoji , Pratiksha Bramhe , Rishabh Agade , Shailendra Gurav , Pramod Khedekar , Vetriselvan Subramaniyan , Ling Shing Wong , Vinoth Kumarasamy
{"title":"Magnetic nanosystem a tool for targeted delivery and diagnostic application: Current challenges and recent advancement","authors":"Nilesh Rarokar ,&nbsp;Sakshi Yadav ,&nbsp;Suprit Saoji ,&nbsp;Pratiksha Bramhe ,&nbsp;Rishabh Agade ,&nbsp;Shailendra Gurav ,&nbsp;Pramod Khedekar ,&nbsp;Vetriselvan Subramaniyan ,&nbsp;Ling Shing Wong ,&nbsp;Vinoth Kumarasamy","doi":"10.1016/j.ijpx.2024.100231","DOIUrl":"10.1016/j.ijpx.2024.100231","url":null,"abstract":"<div><p>Over the last two decades, researchers have paid more attention to magnetic nanosystems due to their wide application in diverse fields. The metal nanomaterials' antimicrobial and biocidal properties make them an essential nanosystem for biomedical applications. Moreover, the magnetic nanosystems could have also been used for diagnosis and treatment because of their magnetic, optical, and fluorescence properties. Superparamagnetic iron oxide nanoparticles (SPIONs) and quantum dots (QDs) are the most widely used magnetic nanosystems prepared by a simple process. By surface modification, researchers have recently been working on conjugating metals like silica, copper, and gold with magnetic nanosystems. This hybridization of the nanosystems modifies the structural characteristics of the nanomaterials and helps to improve their efficacy for targeted drug and gene delivery. The hybridization of metals with various nanomaterials like micelles, cubosomes, liposomes, and polymeric nanomaterials is gaining more interest due to their nanometer size range and nontoxic, biocompatible nature. Moreover, they have good injectability and higher targeting ability by accumulation at the target site by application of an external magnetic field. The present article discussed the magnetic nanosystem in more detail regarding their structure, properties, interaction with the biological system, and diagnostic applications.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100231"},"PeriodicalIF":4.7,"publicationDate":"2024-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000033/pdfft?md5=cee03f07eda27af8fd23e76f73a2b37a&pid=1-s2.0-S2590156724000033-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139631332","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation, optimization and evaluation of ocular gel containing nebivolol Hcl-loaded ultradeformable spanlastics nanovesicles: In vitro and in vivo studies 含有盐酸奈必洛尔的超可塑spanlastics纳米颗粒的眼用凝胶的配制、优化和评估:体外和体内研究
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-01-16 DOI: 10.1016/j.ijpx.2023.100228
Mohamed Yasser , Eman E. El Naggar , Nehal Elfar , Mahmoud H. Teaima , Mohamed A. El-Nabarawi , Sammar Fathy Elhabal
{"title":"Formulation, optimization and evaluation of ocular gel containing nebivolol Hcl-loaded ultradeformable spanlastics nanovesicles: In vitro and in vivo studies","authors":"Mohamed Yasser ,&nbsp;Eman E. El Naggar ,&nbsp;Nehal Elfar ,&nbsp;Mahmoud H. Teaima ,&nbsp;Mohamed A. El-Nabarawi ,&nbsp;Sammar Fathy Elhabal","doi":"10.1016/j.ijpx.2023.100228","DOIUrl":"10.1016/j.ijpx.2023.100228","url":null,"abstract":"<div><p>The study aims to improve the ocular delivery of Nebivolol HCL (NBV) belonging to the Biopharmaceutics classification system (BCSII) by using spanlastic nanovesicles (SNVs) for ophthalmic delivery and incorporating them into hydroxypropyl methylcellulose gel with ketorolac tromethamine (KET) as an anti-inflammatory to improve glaucoma complications like Conjunctivitis. SNVs were prepared by ethanol injection technique using span (60) as a surfactant and labrasol as an edge activator (EA). The impact of formulation factors on SNVs properties was investigated using a Box-Behnken design. In vitro evaluations showed that the formulations (F1, F4, and F14), containing Span 60 and labrasol as EA (25%, 50%, and 25%), exhibited high EE% with low PS and high ZP and DI. Additionally, 61.72 ± 0.77%, 58.97 ± 1.44%, and 56.20 ± 2.32% of the NBV amount were released from F1, F4, and F14 after 5 h, compared to 93.94 ± 1.21% released from drug suspension. The selected formula (G1), containing F1 in combination with KET and 2% <em>w</em>/w HPMC, exhibited 76.36 ± 0.90% drug release after 12 h. Ex vivo Confocal laser scanning revealed a high penetration of NBV-SNVs gel that ascertained the results of the in-vitro <em>study</em>. In vivo studies showed a significant decrease in glaucoma compared to drug suspension, and histopathological studies showed improvement in glaucomatous eye retinal atrophy. G1 is considered a promising approach to improving ocular permeability, absorption, and anti-inflammatory activity, providing a safer alternative to current regimens.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100228"},"PeriodicalIF":4.7,"publicationDate":"2024-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156723000725/pdfft?md5=b2ff799666c90e95ea2c791759c45b4b&pid=1-s2.0-S2590156723000725-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139631782","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Everolimus-encapsulation in Pluronic P123 self-assembled micelles as drug delivery systems for drug-coated balloons 将埃维莫司封装在 Pluronic P123 自组装胶束中,作为药物涂层球囊的给药系统
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-01-10 DOI: 10.1016/j.ijpx.2024.100230
Mohammad Akrami-Hasan-Kohal , Adrien Chouchou , Sébastien Blanquer , Tahmer Sharkawi
{"title":"Everolimus-encapsulation in Pluronic P123 self-assembled micelles as drug delivery systems for drug-coated balloons","authors":"Mohammad Akrami-Hasan-Kohal ,&nbsp;Adrien Chouchou ,&nbsp;Sébastien Blanquer ,&nbsp;Tahmer Sharkawi","doi":"10.1016/j.ijpx.2024.100230","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100230","url":null,"abstract":"<div><p>Drug-coated balloons (DCBs) are effective tools for cardiovascular interventions, ensuring uniform drug delivery to occluded arteries. This research investigates the potential of Pluronic P123 (P123), a micelle-forming polymer, to solubilize and release Everolimus (EVE) from DCBs. Furthermore, it seeks to understand how the ratio of P123 to EVE affects release rates and micelle formation under physiological conditions. We tested three P123 to EVE ratios: 90:10, 75:25, and 50:50. Microscopy revealed that increasing EVE proportions resulted in more uniform coatings. Fourier-transform infrared spectroscopy (FTIR) analysis confirmed the successful incorporation of EVE into the P123 matrix without altering its chemical properties. Differential scanning calorimetry (DSC) studies showed that EVE incorporation affected the crystalline structure of P123, leading to more uniform coatings. In vitro release studies showed that all formulations had &lt;1% drug loss in the first minute (the tracking phase); furthermore, the 90:10 ratio exhibited optimal drug release in the following 3 min, corresponding to the deployment phase in DCB angioplasty. Analysis of micelle loading capacity (LC), encapsulation efficiency (EE), size, and structure indicated an increase in both LC and EE with higher EVE content and a corresponding enlargement in micelle size. Given these findings, the optimized formula provided a consistent coating on commercial balloons, highlighting the potential of using P123 for DCB drug coating and release.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100230"},"PeriodicalIF":4.7,"publicationDate":"2024-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000021/pdfft?md5=c594d2ed3f793f14634838a04c5b3943&pid=1-s2.0-S2590156724000021-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139433425","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of treatment with original or biosimilar adalimumab on SARS-CoV2 vaccination antibody titers 使用阿达木单抗原药或生物类似药治疗对 SARS-CoV2 疫苗抗体滴度的影响
IF 4.7 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-01-06 DOI: 10.1016/j.ijpx.2024.100229
Eva Dokoupilová , David Vetchý , Sylvie Pavloková , Markéta Hanuštiaková
{"title":"Effect of treatment with original or biosimilar adalimumab on SARS-CoV2 vaccination antibody titers","authors":"Eva Dokoupilová ,&nbsp;David Vetchý ,&nbsp;Sylvie Pavloková ,&nbsp;Markéta Hanuštiaková","doi":"10.1016/j.ijpx.2024.100229","DOIUrl":"10.1016/j.ijpx.2024.100229","url":null,"abstract":"<div><p>The technological process of production of biosimilars determines the degree of biosimilarity to the original biological drug. In particular, the focus is on the similarity of immunogenic responses. The primary endpoint of our retrospective study was to find the differences in SARS-CoV-2 antibody amount between patients treated with original adalimumab and biosimilar adalimumab MSB11022 (Idacio) and the differences in the SARS-CoV-2 antibody amount between patients treated with and without biological treatment. We collected the gender, autoimmune disease type, age, and treatment data of the patients in the outpatient clinic MEDICAL PLUS, s.r.o., Uherske Hradiste. These patients suffer from autoimmune rheumatic diseases. All patients received the mRNA vaccine (Pfizer/BioNTech – BNT162b2), with a 21-day (interquartile range, 21–24) gap between the two vaccinations. Patients receiving adalimumab were able to develop cellular immune responses after the second vaccination dose, as well as the individuals without adalimumab. In the period of 6–23 weeks after the second vaccination dose (D63 – D182), the SARS-CoV-2 antibody levels did not change significantly in the patients receiving the original adalimumab, while in the patients receiving biosimilar adalimumab a significant decrease was revealed. A statistically significant difference in the SARS-CoV-2 antibody amount between the patients without biological treatment (median: 504.3 U/mL) and with biological treatment (Original and Biosimilar – median: 47.2 and 28.2 U/mL, respectively) was confirmed on day 182. According to our observation, the effect of the treatment type on the increase/decrease of antibodies over time is dominant, while the impact of other variables (gender, methotrexate treatment, autoimmune disease type, and age) was confirmed as insignificant or minor.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100229"},"PeriodicalIF":4.7,"publicationDate":"2024-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S259015672400001X/pdfft?md5=ee42becd18e7a46e551fcbc81f1c9731&pid=1-s2.0-S259015672400001X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139392470","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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