{"title":"Superior doxorubicin cellular delivery effect established by optically active mesoporous silica nanoparticles.","authors":"Lijie Wang, Dahai Yu, Dan Li, Jing Li","doi":"10.1007/s13346-024-01537-6","DOIUrl":"10.1007/s13346-024-01537-6","url":null,"abstract":"<p><p>The impact of optically active biomaterials on drug delivery remains a vital and hot topic. To reveal special advantages of optically active mesoporous silica nanoparticles in delivering drug in cells, optically active mesoporous silica nanoparticles deliver doxorubicin (DOX) with chiral behavior in cancer cells was studied. The present work focused on two types of optically active mesoporous silica nanoparticles named as levorotatory optically active mesoporous silica nanoparticles (LOA-MSNs) and dextrorotatory optically active mesoporous silica nanoparticles (DOA-MSNs) and examined their effects on cellular DOX delivery in cancer cells. The obtained LOA-MSNs and DOA-MSNs were regular spheres with particle diameters ranging from 200 to 250 nm, and their shell layer was filled with interlaced channels. Our results indicated that LOA-MSNs and DOA-MSNs did not exhibit cytotoxicity towards MCF-7 cells and B16 cells. The cytotoxicity of DOX-loaded LOA-MSNs and DOX-loaded DOA-MSNs were stronger than DOX owing to the synergistic retention and accumulation effect of nanoparticles. More importantly, DOX-loaded DOA-MSNs presented stronger cytotoxicity due to the higher synergistic retention and accumulation effect of DOA-MSNs. These findings suggest that DOA-MSNs with superior cellular delivery of DOX have great potential to advance the development of optical anti-tumor delivery system.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":"3163-3172"},"PeriodicalIF":5.7,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139912278","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sha Liu, Daoyuan Chen, Xiaosu Zhu, Xiaowen Wang, Xiao Li, Yuan Du, Peng Zhang, Jingwei Tian, Yingjian Song
{"title":"Inhaled delivery of cetuximab-conjugated immunoliposomes loaded with afatinib: A promising strategy for enhanced non-small cell lung cancer treatment.","authors":"Sha Liu, Daoyuan Chen, Xiaosu Zhu, Xiaowen Wang, Xiao Li, Yuan Du, Peng Zhang, Jingwei Tian, Yingjian Song","doi":"10.1007/s13346-024-01536-7","DOIUrl":"10.1007/s13346-024-01536-7","url":null,"abstract":"<p><p>Afatinib (AT), an FDA-approved aniline-quinazoline derivative, is a first-line treatment for metastatic non-small cell lung cancer (NSCLC). Combining it with cetuximab (CX), a chimeric human-murine derivative immunoglobulin-G1 monoclonal antibody (mAb) targeting the extracellular domain of epidermal growth factor receptor (EGFR), has shown significant improvements in median progression-free survival. Previously, we developed cetuximab-conjugated immunoliposomes loaded with afatinib (AT-MLP) and demonstrated their efficacy against NSCLC cells (A549 and H1975). In this study, we aimed to explore the potential of pulmonary delivery to mitigate adverse effects associated with oral administration and intravenous injection. We formulated AT-MLP dry powders (AT-MLP-DPI) via freeze drying using tert-butanol and mannitol as cryoprotectants in the hydration medium. The physicochemical and aerodynamic properties of dry powders were well analyzed firstly. In vitro cellular uptake and cytotoxicity study revealed concentration- and time-dependent cellular uptake behavior and antitumor efficacy of AT-MLP-DPI, while Transwell assay demonstrated the superior inhibitory effects on NSCLC cell invasion and migration. Furthermore, in vivo pharmacokinetic study showed that pulmonary delivery of AT-MLP-DPI significantly increased bioavailability, prolonged blood circulation time, and exhibited higher lung concentrations compared to alternative administration routes and formulations. The in vivo antitumor efficacy study carried on tumor-bearing nude mice indicated that inhaled AT-MLP-DPI effectively suppressed lung tumor growth.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":"3147-3162"},"PeriodicalIF":5.7,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139912277","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development of the novel formulations of perospirone for the treatment of schizophrenia.","authors":"Zijun Zhang, Famin Ke, Jili Wu, Xiyao Li, Xin Chen, Lanxing Zhang, Pei Jing, Zerong Liu, Zhongbing Liu, Ruilin Lu, Shihua Fu, Meiling Zhou, Yan Lin, Xiaoduan Sun, Zhirong Zhong","doi":"10.1007/s13346-024-01730-7","DOIUrl":"10.1007/s13346-024-01730-7","url":null,"abstract":"<p><p>Schizophrenia is a severe mental illness. Its clinical features include positive symptoms (hallucinations, delusions, thought disorders), negative symptoms (avolition, anhedonia, poverty of thought, social withdrawal), and cognitive dysfunction. A large number of antipsychotic drugs with traditional dosage forms are available to mitigate the symptoms of schizophrenia but the duration of action is commonly short, often requiring frequent administration. The perospirone hydrochloride hydrate (PER), as a second-generation antipsychotic drug, shows therapeutic effects on both positive and negative symptoms of schizophrenia, with less impact on cognitive function. However, it suffers from a short half-life, fluctuating blood concentration, instability in the circulating leading to peak-trough fluctuations, and poor patient compliance due to the required frequent administration. Based on the hydrophilic matrix, we developed novel formulations of PER, including the extended-release and the controlled-release tablets of PER. The resulting formulations delayed the drug release and prolonged the persistence of PER, leading to an extended half-life and reduced fluctuations in blood concentration with stable therapeutic levels and an improved absorption with higher bioavailability, thus reducing dosing frequency. These oral extended-release and controlled-release tablets promise to alleviate patients' medication discomfort and provide long-term sustained drug release. They would provide a platform with broad prospects for the clinical treatment of schizophrenia.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142557416","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Topical delivery of baricitinib-impregnated nanoemulgel: a promising platform for inhibition of JAK -STAT pathway for the effective management of atopic dermatitis.","authors":"Shweta Nene, Geetanjali Devabattula, Ganesh Vambhurkar, Kamatham Pushpa Tryphena, Dharmendra Kumar Khatri, Chandraiah Godugu, Pankaj Kumar Singh, Saurabh Srivastava","doi":"10.1007/s13346-024-01732-5","DOIUrl":"https://doi.org/10.1007/s13346-024-01732-5","url":null,"abstract":"<p><p>Baricitinib, an inhibitor of Janus kinase 1/2 receptors majorly involved in the dysregulation of immune responses in atopic dermatitis, is currently approved for managing atopic dermatitis in Europe. The delivery of baricitinib through oral route is associated to several adverse effects due to off-target effects. Therefore, the current study is aimed at formulation of baricitinib loaded nanoemulgel for evaluation of topical delivery potential in the treatment of atopic dermatitis. The baricitinib-loaded nanoemulsions (0.05 and 0.1% w/w) revealed an average globule size of 162.86 ± 0.37 and 173.66 ± 4.88 nm respectively with narrow PDI. The optimized batch of baricitinib nanoemulsion was converted to nanoemulgel by the addition of the mixture of gel bases SEPINEO™ DERM and SEPINEO™ P 600 along with propylene glycol, resulting in pseudoplastic shear thinning behaviour. The optimized nanoemulgels have shown prominent retention of baricitinib in the skin along with permeation. The skin distribution study of coumarin-6 loaded nanoemulgel demonstrated high fluorescence in the epidermal layer. The western blot analysis revealed significant inhibition of phosphorylated signal transducers and activators of transcriptions 1 (##p < 0.01) and 3 (#p < 0.05) by application of 0.05 and 0.1% baricitinib nanoemulgel. The baricitinib nanoemulgels have shown anti-inflammatory activity by significantly reducing expressions of various inflammatory markers. Histopathological analysis of skin tissues treated with baricitinib nanoemulgel has demonstrated a marked reduction in acanthosis, hyperkeratosis, and intact outer epidermis. These results supported the potential role of baricitinib-loaded nanoemulgel in reducing the inflammation and disease severity associated with atopic dermatitis.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142521298","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Cristina Pangua, Socorro Espuelas, Jon Ander Simón, Samuel Álvarez, Cristina Martínez-Ohárriz, María Collantes, Iván Peñuelas, Alfonso Calvo, Juan M Irache
{"title":"Enhancing bevacizumab efficacy in a colorectal tumor mice model using dextran-coated albumin nanoparticles.","authors":"Cristina Pangua, Socorro Espuelas, Jon Ander Simón, Samuel Álvarez, Cristina Martínez-Ohárriz, María Collantes, Iván Peñuelas, Alfonso Calvo, Juan M Irache","doi":"10.1007/s13346-024-01734-3","DOIUrl":"https://doi.org/10.1007/s13346-024-01734-3","url":null,"abstract":"<p><p>Bevacizumab is a monoclonal antibody (mAb) that prevents the growth of new blood vessels and is currently employed in the treatment of colorectal cancer (CRC). However, like other mAb, bevacizumab shows a limited penetration in the tumors, hampering their effectiveness and inducing adverse reactions. The aim of this work was to design and evaluate albumin-based nanoparticles, coated with dextran, as carriers for bevacizumab in order to promote its accumulation in the tumor and, thus, improve its antiangiogenic activity. These nanoparticles (B-NP-DEX50) displayed a mean size of about 250 nm and a payload of about 110 µg/mg. In a CRC mice model, these nanoparticles significantly reduced tumor growth and increased tumor doubling time, tumor necrosis and apoptosis more effectively than free bevacizumab. At the end of study, bevacizumab plasma levels were higher in the free drug group, while tumor levels were higher in the B-NP-DEX50 group (2.5-time higher). In line with this, the biodistribution study revealed that nanoparticles accumulated in the tumor core, potentially improving therapeutic efficacy while reducing systemic exposure. In summary, B-NP-DEX can be an adequate alternative to improve the therapeutic efficiency of biologically active molecules, offering a more specific biodistribution to the site of action.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497024","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Emre Tunçel, Serdar Tort, Sevtap Han, Çiğdem Yücel, Figen Tırnaksız
{"title":"Development and optimization of hydrogel-forming microneedles fabricated with 3d-printed molds for enhanced dermal diclofenac sodium delivery: a comprehensive in vitro, ex vivo, and in vivo study.","authors":"Emre Tunçel, Serdar Tort, Sevtap Han, Çiğdem Yücel, Figen Tırnaksız","doi":"10.1007/s13346-024-01728-1","DOIUrl":"https://doi.org/10.1007/s13346-024-01728-1","url":null,"abstract":"<p><p>With the developing manufacturing technologies, the use of 3D printers in microneedle production is becoming widespread. Hydrogel-forming microneedles (HFMs), a variant of microneedles, demonstrate distinctive features such as a high loading capacity and controlled drug release. In this study, the conical microneedle master molds with approximately 500 μm needle height and 250 μm base diameter were created using a Stereolithography (SLA) 3D printer and were utilized to fabricate composite HFMs containing diclofenac sodium. Using Box-Behnken Design, the effects of different polymers on swelling index and mechanical strength of the developed HFMs were evaluated. The optimum HFMs were selected according to experimental design results with the aim of the highest mechanical strength with varying swelling indexes, which was needed to use 20% Gantrez S97 and 0.1% (F22), 0.42% (F23), and 1% (F24) hyaluronic acid. The skin penetration and drug release properties of the optimum formulations were assessed. Ex vivo studies were conducted on formulations to determine drug penetration and accumulation. F24, which has the highest mechanical strength and optimized swelling index, achieved the highest drug accumulation in the skin tissue (17.70 ± 3.66%). All optimum HFMs were found to be non-cytotoxic by the MTT cell viability test (> 70% cell viability). In in vivo studies, the efficacy of the F24 was assessed for the treatment of xylene-induced ear edema by contrasting it to the conventional dosage form. It was revealed that HFMs might be an improved replacement for conventional dosage forms in terms of dermal diseases such as actinic keratosis.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497022","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development of FK506-loaded maleimide-functionalized cationic niosomes for prolonged retention and therapeutic efficacy in dry eye disease.","authors":"Zhixin Guo, Yutong Song, Zhihong Liu, Jiansheng Dai, Zhenzhen Chen, Xianquan Feng, Wenhao Gao, Lingjun Zeng, Hongtao Song","doi":"10.1007/s13346-024-01726-3","DOIUrl":"https://doi.org/10.1007/s13346-024-01726-3","url":null,"abstract":"<p><p>Tacrolimus (FK506) is widely used in ocular diseases such as corneal transplantation-host disease, uveitis, conjunctivitis, and dry eye disease (DED). However, its low aqueous solubility and poor ocular retention pose challenges for its application in the eye diseases. This study developed a novel FK506-loaded maleimide-functionalized cationic niosomes (FK506 M-CNS), aiming to prolong the retention time of FK506 in the eye and enhance its therapeutic efficacy. FK506 M-CNS had a particle size of 87.69 ± 1.05 nm and zeta potential of 22.06 ± 1.01 mV. Results of histological evaluation through H&E staining and in vitro cytotoxicity of human corneal epithelial cells consistently revealed the excellent biocompatibility of FK506 M-CNS. FK506 M-CNS exhibited superior ocular retention compared to the market product Talymus<sup>®</sup>. FK506 M-CNS significantly alleviated the symptoms of DED and promoted the recovery of corneal epithelia. FK506 M-CNS group had the lowest expression levels of inflammatory factors associated with DED. These superiorities might be due to the electrostatic interaction between cationic niosomes and negatively charged mucin in the eye, and the covalent binding of maleimide with the thiol group in the mucin. The maleimide group improved the ocular retention and efficacy of FK506, but did not increase the toxicity. Results indicated that FK506 M-CNS had great potential as a nanopharmaceutical in the treatment of ocular diseases, and M-CNS could be a promising drug carrier for ophthalmic drug delivery systems.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497023","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Human epidermal growth factor receptor 2(Her2)-targeted pH-responsive MR/NIRF bimodal imaging-mediated nano-delivery system for the diagnosis and treatment of undifferentiated thyroid cancer.","authors":"Qiushi Jia, Fulin Li, Chunxiang Li, Changzhi Guo, Shuang Wu, Liguo Hao, Zhongyuan Li","doi":"10.1007/s13346-024-01727-2","DOIUrl":"10.1007/s13346-024-01727-2","url":null,"abstract":"<p><p>Undifferentiated thyroid cancer (ATC) is highly malignant and does not respond well to sorafenib (SRF) treatment owing to the lack of specificity of SRF targeting. Drug delivery nanosystems can improve the efficiencies of drug in treating various cancer types. However, many conventional drug delivery nanosystems lack targeting and exhibit unresponsive drug release. Therefore, we developed a pH-responsive nano-targeted drug delivery systems using human serum albumin (HSA) as a carrier to generate manganese dioxide (MnO<sub>2</sub>)@HSA nanoparticles (NPs), then encapsulated SRF and the fluorescent dye indocyanine green (ICG) and finally modifyed the targeting antibody pertuzumab in the outer layer of the nano complexes, resulting in SRF/ICG/MnO<sub>2</sub>@HSA-pertuzumab (HISMP) NPs. This system targets human epidermal growth factor receptor 2 on the cell membrane surface of thyroid cancer cells and is designed to accumulate at tumor sites. Then, pH-responsive release of divalent manganese ions, ICG, and SRF enables magnetic resonance/fluorescence (MR/NIRF) dual-modality imaging and precise drug delivery for diagnostic and therapeutic integration. Various characterization analyses including transmission electron microscopy, Fourier infrared spectroscopy, and particle size analysis confirm that we successfully synthesized HISMP NPs with a diameter of 150.709 nm. The results of CCK8 cytotoxicity and apoptosis assays show that HISMP NPs exhibited high cytotoxicity and induce apoptosis in thyroid cancer cells. In vivo MR/NIRF imaging experiments confirmed that the HISMP NPs specifically aggregated at tumor sites and have good in vivo MR/NIRF imaging ability and effective anti-tumor activity. The nano-delivery system is expected to provide a theoretical foundation for the efficient ATC diagnosis and therapy.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Iontophoresis and electroporation-assisted microneedles: advancements and therapeutic potentials in transdermal drug delivery.","authors":"Mehrnaz Abbasi, Braeden Heath","doi":"10.1007/s13346-024-01722-7","DOIUrl":"https://doi.org/10.1007/s13346-024-01722-7","url":null,"abstract":"<p><p>Transdermal drug delivery (TDD) using electrically assisted microneedle (MN) systems has emerged as a promising alternative to traditional drug administration routes. This review explores recent advancements in this technology across various therapeutic applications. Integrating iontophoresis (IP) and electroporation (EP) with MN technology has shown significant potential in improving treatment outcomes for various conditions. Studies demonstrate their effectiveness in enhancing vaccine and DNA delivery, improving diabetes management, and increasing efficacy in dermatological applications. The technology has also exhibited promise in delivering nonsteroidal anti-inflammatory drugs (NSAIDs), treating multiple sclerosis, and advancing obesity and cancer therapy. These systems offer improved drug permeation, targeted delivery, and enhanced therapeutic effects. While challenges remain, including safety concerns and technological limitations, ongoing research focuses on optimizing these systems for broader clinical applications. The future of electrically assisted MN technologies in TDD appears promising, with potential advancements in personalized medicine, smart monitoring systems, and expanded therapeutic applications.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142460532","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Matthias Sandmeier, Fabrizio Ricci, Dennis To, Sera Lindner, Daniel Stengel, Michaela Schifferle, Saadet Koz, Andreas Bernkop-Schnürch
{"title":"Design of self-emulsifying oral delivery systems for semaglutide: reverse micelles versus hydrophobic ion pairs.","authors":"Matthias Sandmeier, Fabrizio Ricci, Dennis To, Sera Lindner, Daniel Stengel, Michaela Schifferle, Saadet Koz, Andreas Bernkop-Schnürch","doi":"10.1007/s13346-024-01729-0","DOIUrl":"https://doi.org/10.1007/s13346-024-01729-0","url":null,"abstract":"<p><p>It was the aim of this study to evaluate the potential of reverse micelles (RM) and hydrophobic ion pairs (HIP) for incorporation of semaglutide into self-emulsifying oral drug delivery systems. Reverse micelles loaded with semaglutide were formed with a cationic (ethyl lauroyl arginate, ELA) and an anionic surfactant (docusate, DOC), whereas HIP were formed between semaglutide and ELA. Maximum solubility of the peptide and the rate of dissolution was evaluated in various lipophilic phases (glycerol monocaprylocaprate:caprylic acid 1:4 (m/m), glycerol monolinoleate:caprylic acid 1:4 (m/m) and glycerol monocaprylocaprate:glycerol monolinoleate 1:4 (m/m)). Self-emulsifying drug delivery systems (SEDDS) loaded with RM and HIP were characterized regarding size distribution, zeta potential, cytocompatibility and Caco-2 permeability. Droplet sizes between 50 and 300 nm with polydispersity index (PDI) around 0.3 and zeta potentials between - 45 mV (RM<sub>DOC</sub>) and 36 mV (RM<sub>ELA</sub>) were obtained. RM provided an almost 2-fold higher lipophilicity of semaglutide than HIP resulting in a 4.2-fold higher payload of SEDDS compared to HIP. SEDDS containing RM or HIP showed high cytocompatibilities with a cell survival above 75% for concentrations up to 0.1% on Caco-2 cells and acceptable hemolytic activity. Permeation studies across Caco-2 monolayer revealed an at least 2-fold increase in permeability of semaglutide for the developed formulations.</p>","PeriodicalId":11357,"journal":{"name":"Drug Delivery and Translational Research","volume":" ","pages":""},"PeriodicalIF":5.7,"publicationDate":"2024-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142460531","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}