Journal of Liposome Research最新文献_第4页

Phytosterol ester-based liposomes for improved oral delivery of puerarin: enhanced stability and mucus penetration. 改善葛根素口服给药的植物甾醇酯脂质体：增强稳定性和黏液渗透性。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-13 DOI: 10.1080/08982104.2026.2685610

Pu Yang, Xiqi Wu, Jingjian Liu, Tarun Belwal, Luyao Qi, Xiaotian Li, Jingjing Liang, Simin Feng, Liuqing Yang

{"title":"Phytosterol ester-based liposomes for improved oral delivery of puerarin: enhanced stability and mucus penetration.","authors":"Pu Yang, Xiqi Wu, Jingjian Liu, Tarun Belwal, Luyao Qi, Xiaotian Li, Jingjing Liang, Simin Feng, Liuqing Yang","doi":"10.1080/08982104.2026.2685610","DOIUrl":"https://doi.org/10.1080/08982104.2026.2685610","url":null,"abstract":"Puerarin (Pue), an isoflavone with diverse pharmacological activities, exhibits poor oral bioavailability due to its low solubility and permeability. To improve its oral delivery, phytosterol ester (PE) was employed as a membrane stabilizer to replace cholesterol (CH) in liposomal formulations. Two Pue-loaded nanoliposomes, CH-Pue-NLs and PE-Pue-NLs, were successfully prepared via ethanol injection. PE-Pue-NLs exhibited a particle size of 219.80 ± 1.81 nm, a zeta potential of 48.76 ± 1.65 mV, and an encapsulation efficiency (EE) of 74.59 ± 1.25%, outperforming CH-Pue-NLs. FTIR and DSC analyses confirmed successful encapsulation of Pue. During 15 days of storage at 4 °C, PE-Pue-NLs showed superior physical stability, maintaining PDI < 0.3, zeta potential > +35 mV, and higher EE (59.42 ± 1.17%) than CH-Pue-NLs, which exhibited marked aggregation and drug leakage. In simulated gastrointestinal fluids, PE-Pue-NLs demonstrated enhanced structural stability and a slower biphasic release profile, with a lower cumulative release in simulated intestinal fluid at 6 h (36.87 ± 1.47%) compared with CH-Pue-NLs (50.29 ± 2.57%). Furthermore, PE-Pue-NLs exhibited reduced binding with mucin and a 1.32-fold higher apparent permeability coefficient (Papp) in Transwell studies, indicating enhanced mucus penetration. In vivo intestinal fluorescence imaging further confirmed improved mucosal permeability of PE-Pue-NLs. These findings suggest that phytosterol ester is a promising alternative to cholesterol for constructing liposomes with improved gastrointestinal stability and intestinal permeability for poorly soluble bioactive compounds.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-12"},"PeriodicalIF":4.3,"publicationDate":"2026-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148239545","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

Ultrasound-responsive drug nanocarriers in oncology: key determinants of therapeutic performance. 肿瘤超声反应药物纳米载体：治疗效果的关键决定因素。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-08 DOI: 10.1080/08982104.2026.2681623

Fahima Reete, Zimei Wu, Sachin S Thakur

引用次数: 0

Transnasal Zolmitriptan-Ginkgolide B loaded liposomes for migraine therapy: formulation, optimisation and in vitro characterisation. 经鼻佐米曲坦-银杏内酯B负载脂质体用于偏头痛治疗：配方，优化和体外表征。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-05 DOI: 10.1080/08982104.2026.2682487

Aparna Rajesh, Abhirami Subramony, Nethish Kumaar R, Siva Syam Kumar, Anand Biju, Sreeja C Nair

{"title":"Transnasal Zolmitriptan-Ginkgolide B loaded liposomes for migraine therapy: formulation, optimisation and in vitro characterisation.","authors":"Aparna Rajesh, Abhirami Subramony, Nethish Kumaar R, Siva Syam Kumar, Anand Biju, Sreeja C Nair","doi":"10.1080/08982104.2026.2682487","DOIUrl":"https://doi.org/10.1080/08982104.2026.2682487","url":null,"abstract":"Migraine is a chronic neurological disorder that necessitates swift and efficient treatment. Zolmitriptan (ZMT) is a first-line agent with low oral bioavailability and a slow onset of action. Intranasal delivery represents one of the noninvasive routes, directly targeting the nose-to-brain pathway. Therefore, a nano-liposomal system for the co-encapsulation of Zolmitriptan and Ginkgolide B (GB) was developed for efficient intranasal synergistic migraine therapy. The preparation of co-loaded liposomes was performed by thin-film hydration and then optimized by means of DoE. The nanoparticles of the optimal formulation had a mean diameter of 73.13 ± 10.45 nm, high entrapment efficiencies for both ZMT and GB (94.88 ± 2.0% and 95.41 ± 1.3%, respectively) and a biphasic pattern of drug release: a fast burst release of ZMT during the first 2 hours (95.69 ± 4.58%), followed by sustained release of GB within 8 hours (cumulative amount of 98.37 ± 2.87%). The ex vivo permeation study further demonstrated an increased transport across the olfactory mucosa compared to the control treatments. The formulation was well cytocompatible against the nasal cell line (>80% cell viability) and stable upon storage at refrigerated conditions. In this way, it is emphasized that this new dual-drug co-loaded liposomal system may be of great promise in providing improved migraine management through direct brain delivery, but needs in vivo experimentation.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-20"},"PeriodicalIF":4.3,"publicationDate":"2026-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148163523","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

Liposomes in oral delivery: mechanisms, advances, challenges, and future perspectives. 口服给药脂质体：机制、进展、挑战和未来展望。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-03 DOI: 10.1080/08982104.2026.2675542

Patrick Pan, Yuhong Ma, Seeun Kong, Kamel Ahmed, Zimei Wu

{"title":"Liposomes in oral delivery: mechanisms, advances, challenges, and future perspectives.","authors":"Patrick Pan, Yuhong Ma, Seeun Kong, Kamel Ahmed, Zimei Wu","doi":"10.1080/08982104.2026.2675542","DOIUrl":"https://doi.org/10.1080/08982104.2026.2675542","url":null,"abstract":"Oral liposome drug delivery system has gained attention due to their potential to improve patient compliance, enhance the bioavailability of encapsulated poorly soluble drugs, and protect drugs from gastrointestinal degradation. Liposomes structurally mimic the human cell membrane, and so are biocompatible and facilitate interactions with cell membranes. However, liposome drug delivery remains inherently challenging due to limitations such as physicochemical instability, limited permeability across GI barriers, and manufacturing scalability constraints. This review first summarizes the current innovative oral liposome products such as Meriva®, Lipicur, and silymarin liposomes. This is followed by a comprehensive overview of the biological barriers for liposome absorption. The report further reviews current understanding the mechanisms for liposomes to cross the GI track and enter the bloodstream, including cellular uptake, transepithelial transport, and lymphatic transport. Formulation strategies to improve absorption such as lipid composition, surface modification techniques such as PEGylation and chitosan are discussed. Understanding these properties is essential for enhancing transepithelial transport efficiency and designing effective oral liposome delivery systems. Finally, the recent development in manufacturing scalability is also covered. Owing to their favorable properties, oral liposome delivery systems remain an active area for innovations in expanding their applications. It is anticipated that demand for oral liposomal drug‑delivery systems will continue to grow, driven by the rising prevalence of chronic diseases that require long‑term therapeutic management.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-21"},"PeriodicalIF":4.3,"publicationDate":"2026-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148150222","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 novel cyclodextrin-lipid complex method for formulating asymmetric liposomes and the complexation and asymmetry validations. 一种新的环糊精-脂质络合制备不对称脂质体的方法及其络合和不对称的验证。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-02 DOI: 10.1080/08982104.2026.2681620

Yaqeen Nadheer Al Badri, Cheng Shu Chaw, Amal Ali Elkordy

{"title":"A novel cyclodextrin-lipid complex method for formulating asymmetric liposomes and the complexation and asymmetry validations.","authors":"Yaqeen Nadheer Al Badri, Cheng Shu Chaw, Amal Ali Elkordy","doi":"10.1080/08982104.2026.2681620","DOIUrl":"https://doi.org/10.1080/08982104.2026.2681620","url":null,"abstract":"Liposomes have long been explored as versatile drug delivery systems. Recently, achieving and maintaining asymmetry of liposomes has been the focus of liposomal research. This research aims to provide a novel method for formulating asymmetric liposomes, it focuses on development and optimization of asymmetric liposomes using a cyclodextrin (CD)-lipid exchange method, firstly created by E. London and coworkers, the innovative method has not yet in any publications. The method involves dissolving cyclodextrin in HEPES buffer. The lipid is then dissolved in methanol and added in dropwise approach to cyclodextrin solution. Complexation of the lipid and cyclodextrin is confirmed by several methods involving: infrared spectroscopy which showed shifts of some peaks and disappearance of others, thermogravimetric analysis, differential scanning calorimetry, and nuclear magnetic resonance (the spectra were different compared to the raw materials and physical mixtures). Large unilamellar vesicles (acceptor) are formulating with required lipids via thin film method. Finally, equal volumes of the cyclodextrin-lipid complex and acceptor vesicles suspension are mixed using a shaking water bath (22 °C) for 45mins-1 hour to allow lipid exchange, then asymmetric liposomes, via centrifugation at 15,000RPM at 4 °C for 1 hour, were collected from the rest of vehicle containing the CD-complex on. The asymmetry of liposomes was confirmed by using zetapotential and fluorescence quenching methods. The study showed more stable liposomes compared to those prepared by the conventional method. In future, those asymmetric liposomes prepared by the cyclodextrin-lipid complexation method will be evaluated for their encapsulation efficiency for both small and large drug molecules.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-20"},"PeriodicalIF":4.3,"publicationDate":"2026-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148143659","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

Engineered berberine and berberrubine nanobilosomes as a sustainable approach for reversing the toxic metals contamination-induced hepatorenal injuries in rats. 工程小檗碱和小檗碱纳米粒体作为逆转有毒金属污染引起的大鼠肝肾损伤的可持续方法。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-02 DOI: 10.1080/08982104.2026.2678892

Mona M Youssef, Doaa A Ghareeb, Aya M Helal, Inas K Seif, Sally A El-Zahaby, Noha A Elsokary, Nadia Z Shaban

{"title":"Engineered berberine and berberrubine nanobilosomes as a sustainable approach for reversing the toxic metals contamination-induced hepatorenal injuries in rats.","authors":"Mona M Youssef, Doaa A Ghareeb, Aya M Helal, Inas K Seif, Sally A El-Zahaby, Noha A Elsokary, Nadia Z Shaban","doi":"10.1080/08982104.2026.2678892","DOIUrl":"https://doi.org/10.1080/08982104.2026.2678892","url":null,"abstract":"Berberine (BB) is recognized for its medicinal properties; however, its clinical application is limited by its poor bioavailability. This study prepared ecologically friendly albumin-modified nanobilosomes (ABL) to enhance and compare the therapeutic efficacies of BB and berberrubine (BR) in managing hepatic and renal damages. Hepatic and renal injuries were induced in rats through their daily consumption of toxic metal-contaminated water portion (TM/W) containing lead (20 mg/kg), aluminum (10 mg/kg), and cadmium (5 mg/kg) for 90 days. Rats were subsequently treated with free BB, BR, or BB-ABL/BR-ABL (25 mg/kg/day) for 45 days. Biochemical parameters, oxidative stress, inflammation, and autophagy markers were evaluated. The optimized formulations possessed high drug entrapment efficiencies of 83.2 ± 1.35% for BB-ABL and 84.5 ± 0.06% for BR-ABL. BB-ABL and BR-ABL exhibited significantly greater therapeutic efficacy than free drugs in attenuating TM/W-induced hepatic and renal injuries as evidenced by significant reductions in nitric oxide (NO), microtubule-associated protein light chain 3-II (LC3-II), interleukins (IL-1β and IL-6), and AMP-activated protein kinase (AMPK) protein levels (p < 0.05). Hepatic mTOR levels were significantly elevated by 32.4% and 37.5% in the TM/BB-ABL and TM/BB-ABL treated groups, respectively, while renal mTOR levels increased by 39.6% and 42.8% compared with the TM/W group. Likewise, hepatic PI3K levels increased by 37.9% and 47.4%, whereas renal PI3K levels increased by 33.1% and 37.8% in the TM/BB-ABL and TM/BR-ABL-treated groups, respectively, relative to the TM/W group. Engineered albumin-modified nanobilosomes enhanced the antioxidant, anti-inflammatory, anti-apoptotic, and autophagy-modulatory properties of BB and BR for the treatment of toxic metal-induced hepatorenal damage.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-21"},"PeriodicalIF":4.3,"publicationDate":"2026-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148150175","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

Optimizing liposomal drug release via γ-irradiation and iron-based radiosensitization. 通过γ辐照和铁基放射增敏优化脂质体药物释放。

IF 4.7 4区医学

Journal of Liposome Research Pub Date : 2026-06-01 Epub Date: 2026-02-03 DOI: 10.1080/08982104.2026.2625077

E Loscertales, S España

{"title":"Optimizing liposomal drug release via γ-irradiation and iron-based radiosensitization.","authors":"E Loscertales, S España","doi":"10.1080/08982104.2026.2625077","DOIUrl":"10.1080/08982104.2026.2625077","url":null,"abstract":"Chemotherapy remains a cornerstone of cancer treatment, yet its lack of tumor specificity often leads to systemic toxicity and limits the maximum tolerable dose. To address these limitations, drug-loaded nanocarriers responsive to ionizing radiation have emerged as a promising strategy to achieve localized drug release within irradiated tumor regions, thereby enhancing therapeutic efficacy while minimizing off-target effects. However, current radiation-responsive nanosystems often exhibit limited drug release at clinically relevant radiation doses. In our previous work, we evaluated liposomal formulations varying lipid composition, sensitizers, and particle size. While these systems demonstrated moderate immediate release upon irradiation followed by sustained passive leakage, they were incompatible with remote drug loading and failed to achieve rapid release. In the present study, we optimized the liposomal membrane composition through modulation of polyunsaturated and saturated phospholipids to enhance radiation sensitivity and colloidal stability. Furthermore, we introduced a radiosensitization mechanism based on the encapsulation of Fe³+ ions, which are reduced to Fe2+ upon γ-irradiation. This redox transition triggers a Fenton-like reaction that catalyzes the degradation of lipid hydroperoxides, leading to localized lipid peroxidation and membrane disruption. This dual strategy, membrane composition tuning and iron-mediated oxidative activation, resulted in significantly enhanced drug release upon exposure to low-dose radiation.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"199-207"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146113109","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

Enhanced buccal bioavailability of olmesartan through ultradeformable bilosomes loaded film: a novel approach for hypertension management. 通过超可成形的脂质体负载膜提高奥美沙坦的口腔生物利用度：一种治疗高血压的新方法。

IF 4.7 4区医学

Journal of Liposome Research Pub Date : 2026-06-01 Epub Date: 2026-01-19 DOI: 10.1080/08982104.2026.2616857

Amira N Abd Elrady, Mona M Elkhatib, Magdy I Mohamed, Ahmed M Fatouh

{"title":"Enhanced buccal bioavailability of olmesartan through ultradeformable bilosomes loaded film: a novel approach for hypertension management.","authors":"Amira N Abd Elrady, Mona M Elkhatib, Magdy I Mohamed, Ahmed M Fatouh","doi":"10.1080/08982104.2026.2616857","DOIUrl":"10.1080/08982104.2026.2616857","url":null,"abstract":"This study investigated the use of ultradeformable bilosomes (UBs)-loaded buccal films to overcome the limited oral bioavailability of olmesartan medoxomil (OLM), a poorly water-soluble antihypertensive. UBs were prepared via thin film hydration technique, and a 24 factorial design evaluated the effects of phosphatidylcholine to bile salt (PC: BS) ratio, permeation enhancer (PE) type and amount, and sonication time on entrapment efficiency (EE), particle size (PS), zeta potential (ZP), and polydispersity index (PDI). The optimized formulation (UBs-12), comprising 50 mg Labrasol® at an 8:1 PC: BS ratio and sonicated for 4 minutes, showed EE% of 67.9 ± 1.9%, PS of 279.8 ± 3.5 nm, ZP of -46.9 ± 1.4 mV, and PDI of 0.46 ± 0.02. It showed a markedly higher OLM release after 24 h (78.5 ± 2.4%) compared to conventional bilosomes and aqueous OLM suspension, as well as a significantly greater deformability index (18.2 ± 0.3) (p = 0.008) than conventional bilosomes. UBs-12 was incorporated into buccal films with favorable in vitro characteristics. Pharmacodynamic assessment in dexamethasone-induced hypertensive male rats demonstrated that UBs-12 films achieved a more pronounced and sustained blood pressure reduction compared to oral suspension. The films yielded a 1.68-fold increase in area under the antihypertensive effect-time curve and a 1.75-fold longer effect half-life. These results support UBs-loaded buccal films as a promising approach to enhance OLM bioavailability.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"142-155"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146003641","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

Assessing liposomal compositions for posterior ocular therapeutics: revelations from animal model research-a systematic review. 评估后眼治疗的脂质体组成：来自动物模型研究的启示-系统综述。

IF 4.3 4区医学

Journal of Liposome Research Pub Date : 2026-06-01 Epub Date: 2026-02-01 DOI: 10.1080/08982104.2026.2618747

Santosh Nandalal, Madhumitha Haridoss, Raji Rajesh Lenin

{"title":"Assessing liposomal compositions for posterior ocular therapeutics: revelations from animal model research-a systematic review.","authors":"Santosh Nandalal, Madhumitha Haridoss, Raji Rajesh Lenin","doi":"10.1080/08982104.2026.2618747","DOIUrl":"10.1080/08982104.2026.2618747","url":null,"abstract":"Despite advances in retinal therapeutics, drug delivery remains hindered by ocular barriers and rapid clearance. Liposomes provide a promising strategy due to their capacity to enhance drug retention, protect labile compounds, and enable targeted delivery to the retina. Conventional eye drop formulations are inadequate for sustained retinal delivery, highlighting the need for optimized nanocarriers. Our systematic review examined how variations in liposomal composition influence drug delivery efficiency in posterior segment eye diseases. In vivo and ex vivo studies published until November 11, 2025 were systematically searched in PubMed-MEDLINE and SCOPUS. Fourteen studies were included, focusing on liposome preparation methods, particle size, and ocular targeting. Risk of bias (ROB) was assessed using the SYRCLE tool, and the review adhered to PRISMA 2020 guidelines (protocol registered in PROSPERO: CRD42024513400). Findings indicated that lipid-to-cholesterol ratios, surface modifications, and polymer coatings substantially affected particle size, encapsulation efficiency, and drug bioavailability at the retina. While these modifications improved therapeutic outcomes, challenges persist in achieving sustained release and clinical reproducibility. ROB assessment revealed methodological limitations across studies. Due to heterogeneity, we performed semi-quantitative weight-of-evidence data correlation to compare the studies. Standardizing formulation strategies and preparation protocols is essential. Future research should prioritize optimized lipid compositions and noninvasive delivery methods to enhance retinal penetration and retention.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"221-233"},"PeriodicalIF":4.3,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146099719","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

PEGylated flexosomes as a novel intranasal carrier for quetiapine: formulation, characterization, and in vivo studies. 聚乙二醇化柔体作为奎硫平的新型鼻内载体：配方、表征和体内研究。

IF 4.7 4区医学

Journal of Liposome Research Pub Date : 2026-06-01 Epub Date: 2026-02-01 DOI: 10.1080/08982104.2026.2619917

Rana M Gebreel, Alshaimaa Attia, Menna M Abdellatif, Mubarak Algahtany, Hasnaa Ali Ebrahim, Nabil A Shoman

{"title":"PEGylated flexosomes as a novel intranasal carrier for quetiapine: formulation, characterization, and in vivo studies.","authors":"Rana M Gebreel, Alshaimaa Attia, Menna M Abdellatif, Mubarak Algahtany, Hasnaa Ali Ebrahim, Nabil A Shoman","doi":"10.1080/08982104.2026.2619917","DOIUrl":"10.1080/08982104.2026.2619917","url":null,"abstract":"The present study aimed to fabricate PEGylated flexosomes (PFs) for intranasal delivery of quetiapine (QTP), addressing its poor oral bioavailability. QTP-loaded PFs were formulated via thin-film hydration and optimized using a 2³ factorial design to evaluate Brij type and concentration, with or without 0.1% cholesterol, providing ultradeformable nanovesicles capable of efficient brain targeting. Brij surfactants served dual roles as elasticity-enhancing edge activators and PEGylating agents, thereby improving steric stabilization and mucosal interactions. The formulae were assessed by determining particle size, entrapment efficiency, polydispersity, zeta potential, and drug release. The optimized formulation (QTP-OPF) was assessed for deformability, stability, morphology, and ex vivo nasal permeation. Finally, in vivo pharmacokinetic and histopathological assessments were accomplished to estimate the in vivo performance of QTP-OPF. The QTP-OPF exhibited reduced particle size and polydispersity, a high zeta potential, and enhanced drug release. Additionally, it demonstrated superior deformability and maintained stability for 90 days. Transmission electron microscopy confirmed spherical, PEG-coated vesicles. The ex vivo nasal permeation study revealed a 1.6-fold increase over QTP suspension, while in vivo pharmacokinetics revealed a 3.8-fold enhancement in brain Cmax and a 7.5-fold higher brain AUC0-∞. Histopathological evaluation confirmed the formulation's safety. PFs present a promising platform for enhanced intranasal QTP delivery.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"183-198"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146099994","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