Agnieszka Wiesner , Paweł Zagrodzki , Alicja Gawalska , Monika Marcinkowska , Agnieszka Cios , Paweł Paśko
{"title":"Navigating through chemometrics: Unveiling antibiotic-food interactions for improved pediatric formulations ahead","authors":"Agnieszka Wiesner , Paweł Zagrodzki , Alicja Gawalska , Monika Marcinkowska , Agnieszka Cios , Paweł Paśko","doi":"10.1016/j.ejpb.2025.114652","DOIUrl":"10.1016/j.ejpb.2025.114652","url":null,"abstract":"<div><h3>Background</h3><div>Given the challenges of pediatric antibacterial therapy, it is crucial to formulate antibiotics with a lower potential for interaction with dietary interventions and tailor them for optimal administration in children. Chemometric methods allow us to analyze multiple interrelated variables simultaneously and uncover correlations.</div></div><div><h3>Aim</h3><div>We applied a chemometric approach to examine how food, beverages, antacids, and mineral supplements affect antibiotic bioavailability in adults and children, aiming to explore relationships between antibiotic structure, physicochemical properties, and post-meal changes in pharmacokinetic (PK) parameters.</div></div><div><h3>Methods</h3><div>We selected 95 antibacterial drugs for analysis, including beta-lactams (32), quinolones (25), macrolides (13), tetracyclines (16), and others (9). The input dataset comprised information from published clinical trials, chemical records, and calculations. We constructed hierarchical partial least squares (PLS) models with changes in PK parameters (ΔAUC, ΔC<sub>max</sub>, ΔT<sub>max</sub>, and Δ t ½) as response parameters and nine groups of molecular descriptors (M1-M9) as predictor parameters. We performed analyses separately in children and adults for different dietary interventions.</div></div><div><h3>Results</h3><div>In the final 10 PLS models, significant components explained 61–90% and 10.3–54.4% of the variance in the predictor and response parameter sets, respectively. We obtained 59 significant positive and negative correlations between antibiotic structure or physicochemical properties (molecular descriptors) and action in the human body in the presence of food, antacids, or mineral supplements (changes in PK parameters), of which 41 concern pediatric patients.</div></div><div><h3>Conclusions</h3><div>Chemometric methods can be helpful and valuable in investigating the interactions between antibiotics and dietary interventions. Using chemometrics may pave the way for formulating antibiotics for children with a lower potential to interact with food.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114652"},"PeriodicalIF":4.4,"publicationDate":"2025-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143058492","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Nils Christian Böck , Julius Sundermann , Mirko Koziolek , Benjamin-Luca Keller , Karsten Mäder
{"title":"Impact of stabilizers on particle size and dispersion behavior in biorelevant media in solid nanocrystal formulations","authors":"Nils Christian Böck , Julius Sundermann , Mirko Koziolek , Benjamin-Luca Keller , Karsten Mäder","doi":"10.1016/j.ejpb.2025.114651","DOIUrl":"10.1016/j.ejpb.2025.114651","url":null,"abstract":"<div><div>Nanocrystalline formulations typically contain stabilizing additives to minimize the risk of particle growth or agglomeration. This risk is particularly relevant when the nanosuspension is converted into a solid drug product as the original state of the nanosuspension should be restored upon redispersion of the drug product <em>in vivo</em>. In this work, the behavior of different nonionic and anionic surfactants in solid nanocrystalline formulations and their effects on redispersibility under biorelevant conditions were investigated. For this purpose, nanocrystalline formulations of basic (itraconazole, ritonavir), acidic (naproxen), and neutral (fenofibrate) API containing nonionic polymers acting as steric stabilizers combined either with anionic (sodium dodecyl sulfate, deoxycholate sodium, docusate sodium) or non-ionic surfactants (polysorbate 80, vitamin E-TPGS) were manufactured by nano-milling. These formulations were turned into a solid drug product by lyophilization and their redispersibility was tested by dispersing them in biorelevant media with different pH values and by characterizing their particle size distribution (PSD) and surface charge. In the absence of an anionic surfactant, it was difficult to achieve particle sizes below 500 nm. However, formulations stabilized anionically were at risk of agglomeration in gastric media. For basic API, the agglomeration was reversible for formulations containing sodium deoxycholate after increasing the pH from acidic to neutral levels, but it was found to be irreversible for those containing sodium dodecyl sulfate and docusate sodium. In summary, the type of anionic stabilizer and its interplay with the physicochemical properties of the API (basic, acidic, or neutral) should be considered in the development of solid nanocrystal formulations.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114651"},"PeriodicalIF":4.4,"publicationDate":"2025-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143052096","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Lanlan Song , Huihui Ye , Zhanghang Lv , Yichen Liu , Ziyi Lu , Jun Chen , Haofeng Pan , Luqiong Cai , Yuxin Chen , Shiqing Huang , Xingjie Zan , Xiaoying Huang , Chang Yu
{"title":"Hexahistidine-metal assembly encapsulated fibroblast growth factor 21 for lipopolysaccharide-induced acute lung injury","authors":"Lanlan Song , Huihui Ye , Zhanghang Lv , Yichen Liu , Ziyi Lu , Jun Chen , Haofeng Pan , Luqiong Cai , Yuxin Chen , Shiqing Huang , Xingjie Zan , Xiaoying Huang , Chang Yu","doi":"10.1016/j.ejpb.2025.114650","DOIUrl":"10.1016/j.ejpb.2025.114650","url":null,"abstract":"<div><div>Acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) represents a spectrum of potentially fatal conditions that currently lack effective drug treatment. Recent researches suggest that Fibroblast Growth Factor 21 (FGF21) may protect against ALI/ARDS. However, the clinical use of FGF21 is limited by its rapid degradation, restricted targeting capabilities, and numerous adverse effects. Addressing this challenge, the study employs a pH-responsive nanoparticle delivery system known as Hexahistidine-metal Assembly (HmA) for administering FGF21. The entrapment efficiency (EE%) and loading capacity (LCwt%) of HmA exceed 90 % and 35 %, respectively, while the HmA@FGF21 nanoparticles exhibit an average size of 130 nm, a PDI value of approximately 0.28, and a zeta potential of 24 mV. In animal experiments, HmA@FGF21 administered in lipopolysaccharide (LPS)-induced lung injury significantly exceed those of standalone FGF21, including mitigating the pathological manifestations and reducing the wet/dry ratio, total protein concentration, and overall cell count in BALF of ALI, whether administered via the airway or intravenously. This therapeutic approach therefore shows promise for precise delivery of FGF21 to the lungs to treat ALI, and may offer a novel, and efficient method for delivery of potential pharmacological agents to address other lung diseases.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114650"},"PeriodicalIF":4.4,"publicationDate":"2025-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143052094","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Shubhashis Datta , Juraj Kronek , Zuzana Nadova , Ludmila Timulakova , Alzbeta Minarcikova , Pavol Miskovsky
{"title":"Effect of polymer architecture on the properties and in vitro cytotoxicity of drug formulation: A case study with mono- and di-gradient amphiphilic poly(2-Oxazoline)s","authors":"Shubhashis Datta , Juraj Kronek , Zuzana Nadova , Ludmila Timulakova , Alzbeta Minarcikova , Pavol Miskovsky","doi":"10.1016/j.ejpb.2025.114635","DOIUrl":"10.1016/j.ejpb.2025.114635","url":null,"abstract":"<div><div>Due to the straightforward single-step synthesis, amphiphilic gradient copoly(2-oxazoline)s are becoming more popular alternative to their block analogue for the development of next-generation drug delivery systems. Here, we investigated the influence of polymer architecture on the physiochemical and biological assessment of nanoformulations formed by the self-assembly of gradient copoly(2-oxazoline)s. Two different architectures were synthesized: hydrophilic-grad-hydrophobic (mono-gradient) and hydrophobic-grad-hydrophilic-grad-hydrophobic (di-gradient) which contained a hydrophilic monomer, 2-ethyl-2-oxazoline (EtOx) and a hydrophobic monomer, 2-phenyl-2-oxazoline (PhOx). Di-gradient copolymers self-assembled in the presence of a hydrophobic model drug, curcumin and formed monodispersed or slightly polydispersed nanoparticle solution. On the other hand, mono-gradient copolymers formed polydispersed nanoparticle solutions. Di-gradient copolymer was slightly more efficient to solubilize curcumin. Mono-gradient copolymer nanoparticle showed faster monomer chain exchange kinetics and comparatively less stability in the presence of serum albumin. At longer incubation times, faster drug release was observed from the mono-gradient copolymer nanoformulations. Cytotoxicity of free curcumin and curcumin loaded nanoparticles in cancer cell of U87 MG (human glioblastoma cell) was dose and time-dependent, whereby the significant cell death occurred after 48 h. Curcumin-loaded mono-gradient copolymer nanoparticles inhibited U87MG cancel cell growth to a large extent compared to the di-gradient copolymer nanoparticles.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114635"},"PeriodicalIF":4.4,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143037654","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Haja Muhamad , Abdul Basit Bashir , James Charlton-Harrison , Rand Abdulhussain , Nihad Mawla , Krishan Patel , James Williamson , Liam Blunt , Karl Walton , Barbara Conway , Kofi Asare-Addo
{"title":"Hot-melt extruded-FDM 3D-printed polyethylene oxide tablets: Dissolution imaging analysis of swelling and drug release","authors":"Haja Muhamad , Abdul Basit Bashir , James Charlton-Harrison , Rand Abdulhussain , Nihad Mawla , Krishan Patel , James Williamson , Liam Blunt , Karl Walton , Barbara Conway , Kofi Asare-Addo","doi":"10.1016/j.ejpb.2025.114636","DOIUrl":"10.1016/j.ejpb.2025.114636","url":null,"abstract":"<div><div>Recent developments in pharmacogenetics have emphasised the importance of customised medication, driving interest in technologies like FDM 3D-printing for tailored drug delivery. FDM 3D-printing is a promising technique for the on-demand manufacturing of customised oral dosage forms, providing flexibility in terms of shape and size, dose and drug release profiles. This study investigates the fabrication and characterisation of 3D-printed oral dosage forms using PEO as the primary polymer and PEG 6 K as a plasticiser. Firstly, the printability of the PEO filaments with different propranolol hydrochloride concentrations was explored using the hot-melt extrusion technology. The influence of the propranolol hydrochloride concentrations on the mechanical properties of the filaments was examined was then examined after which surface characteristics, including roughness and wettability, were evaluated. Dissolution imaging was used to visualise the effects of drug content on the swelling and dissolution characteristics of the PEO-based 3D-printed tablets. Results showed a reduction in the flexural stress of the filaments with increasing drug load. It was also observed that increasing the drug load led to higher surface roughness and lower contact angles of the 3D-printed PEO tablets, implying increased surface hydrophilicity. The swelling behaviour of the tablets increased with higher drug concentrations, resulting in a larger gel layer formation. When comparing the drug release percentages, the release rate was higher in the 10 mg propranolol tablets, suggesting that a lower drug content led to a faster release. The greater gel layer of the 40 mg PPN tablets hindered the drug release by acting as a diffusion barrier, while the 10 mg PPN tablets, with less swelling and gel formation, experienced a faster drug release. These findings show the importance of drug content in modifying the surface properties, swelling behaviour, and drug release profiles of 3D-printed PEO tablets. The study also demonstrates the novel use of dissolution imaging for 3D-printed dosage forms, providing valuable quantitative and qualitative insights into swelling dynamics and channel formation to optimise 3D-printed tablets for drug delivery systems.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114636"},"PeriodicalIF":4.4,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143037667","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}
S. İrem Güler , Cem Levent Altan , E. Esma Demircioglu , Nihan Verimli , Beyza Abisoglu , Cigdem Bayraktaroglu , Mustafa Caglar Beker , S. Sibel Erdem
{"title":"Glow in the dark tumor: Enhanced near-IR visualization and destruction of cancer with a self-quenched theranostic","authors":"S. İrem Güler , Cem Levent Altan , E. Esma Demircioglu , Nihan Verimli , Beyza Abisoglu , Cigdem Bayraktaroglu , Mustafa Caglar Beker , S. Sibel Erdem","doi":"10.1016/j.ejpb.2025.114632","DOIUrl":"10.1016/j.ejpb.2025.114632","url":null,"abstract":"<div><div>Late diagnosis is one of the major obstacles for the treatment of breast cancer which can be overcome with a system offering sensitive imaging and selective therapeutic effect. In this study, we developed a “dark-bright” multifunctional drug delivery system bringing real-time imaging and non-invasive therapy together. Theranostic ability of the system was delivered by Verteporfin (VP), serving as a fluorescence probe and a photosensitizer. To create a “dark state” system via self-quenching ability of VP, it was immobilized onto the superparamagnetic iron oxide nanoparticle (SPION) surface. Upon cellular uptake of the “dark state” system, release of VP led to fluorescence regain, switching the system to “bright state” after which photodynamic therapy (PDT) was initiated to lead to cell death. Theranostic feature of the system was evaluated in MCF-7 and MDA-MB-231 cell lines. Following internalization, fluorescence signal was increased up to ∼56-fold in MCF-7 cells. The IC<sub>50</sub> value decreased ∼20-fold and ∼117-fold in MCF-7 and MDA-MB-231 cell lines, respectively. Moreover, the system significantly inhibited migration in the highly aggressive MDA-MB-231 cell line and induced apoptosis by caspase-3 activation. The developed “dark-bright” system is a promising multifunctional drug delivery vehicle with extraordinary theranostic features for the detection and destruction of micro tumors.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114632"},"PeriodicalIF":4.4,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002680","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Excipients in drug delivery systems: A comprehensive review of approved inactive ingredients for human ophthalmic formulations","authors":"Raquel Gregorio Arribada , Daniela Rodrigues-Braz , Armando Silva-Cunha , Francine Behar-Cohen","doi":"10.1016/j.ejpb.2025.114637","DOIUrl":"10.1016/j.ejpb.2025.114637","url":null,"abstract":"<div><div>Pharmaceutical excipients, commonly known as inactive ingredients, encompass any substance aside from the active ingredient that fulfills a distinct and vital role in a formulation. Their purpose is to enhance specific characteristics, whether associated with the performance of the formulation or aspects related to patient comfort, safety, and acceptability. Because of the limited toxicity studies provided, and the several allergic and toxic side effects that have been reported throughout the years, it is not trivial for the regulatory agencies to approve inactive ingredients for human use. In general, excipients are approved within good manufacturing practices (GMPs) when they undergo analysis of the formulation as a whole, not the standalone substance. However, there is a lack of updated information regarding this subject, given that only the American Food and Drug Administration (FDA) provides a complete list describing the inactive ingredients that are currently approved in drug products for human use. Here, we aimed to provide an overview of key excipients approved by the FDA for ophthalmic use in humans, focusing on their functional roles in ophthalmic formulations, particularly eye drops, and the regulatory requirements involved in these ingredients approval.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114637"},"PeriodicalIF":4.4,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002655","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}
Raul Edison Luna Lazo , Fernando Miguel Stelmach Alves , Eric Luiz Domingos , Alexandre de Fatima Cobre , Paulo Vitor Farago , Letícia Cruz , Tiana Tasca , Roberto Pontarolo , Luana Mota Ferreira
{"title":"Advances in soft nanoparticle-based platforms for human and veterinary trichomoniasis therapy: A scoping review","authors":"Raul Edison Luna Lazo , Fernando Miguel Stelmach Alves , Eric Luiz Domingos , Alexandre de Fatima Cobre , Paulo Vitor Farago , Letícia Cruz , Tiana Tasca , Roberto Pontarolo , Luana Mota Ferreira","doi":"10.1016/j.ejpb.2025.114638","DOIUrl":"10.1016/j.ejpb.2025.114638","url":null,"abstract":"<div><div>This scoping review focuses on drug delivery systems based on soft materials designed for the administration of drugs with anti-<em>Trichomonas vaginalis</em> activity. It primarily examines their use in addressing human trichomoniasis, exploring their physicochemical characteristics, <em>in vitro</em> and <em>in vivo</em> evaluation and identifying existing challenges and gaps. Given the economic burden and the One Health approach, formulations developed aiming at treating animal infections − cattle and poultry − were also discussed. The review involved searching electronic databases, such as PubMed, Scopus, and Web of Science, to find studies published until May 2024; out of the 103 articles retrieved, 18 fulfilled the eligibility criteria. This study investigated soft-nanoparticle formulations, including polymeric<!--> <!-->and lipid-based systems, and their incorporation into suitable formulations for topical application, including hydrogels and polymeric films. Additionally, the discussion covered toxicology and highlighted the knowledge gaps related to the potential use of these formulations in humans. Anti-trichomonas soft nano-based formulations emerge as promising candidates for treating gynecological and animal infections. In conclusion, further preclinical testing is necessary, as none of the formulations have progressed to human clinical trials and have only been evaluated in animal models.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114638"},"PeriodicalIF":4.4,"publicationDate":"2025-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002645","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Control of biomedical nanoparticle distribution and drug release in vivo by complex particle design strategies","authors":"Melanie Bresinsky, Achim Goepferich","doi":"10.1016/j.ejpb.2025.114634","DOIUrl":"10.1016/j.ejpb.2025.114634","url":null,"abstract":"<div><div>The utilization of targeted nanoparticles as a selective drug delivery system is a powerful tool to increase the amount of active substance reaching the target site. This can increase therapeutic efficacy while reducing adverse drug effects. However, nanoparticles face several challenges: upon injection, the immediate adhesion of plasma proteins may mask targeting ligands, thereby diminishing the target cell selectivity. In addition, opsonization can lead to premature clearance and the widespread presence of receptors or enzymes limits the accuracy of target cell recognition. Nanoparticles may also suffer from endosomal entrapment, and controlled drug release can be hindered by premature burst release or insufficient particle retention at the target site. Various strategies have been developed to address these adverse events, such as the implementation of switchable particle properties, regulating the composition of the formed protein corona, or using click-chemistry based targeting approaches. This has resulted in increasingly complex particle designs, raising the question of whether this development actually improves the therapeutic efficacy in vivo. This review provides an overview of the challenges in targeted drug delivery and explores potential solutions described in the literature. Subsequently, appropriate strategies for the development of nanoparticular drug delivery concepts are discussed.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114634"},"PeriodicalIF":4.4,"publicationDate":"2025-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002646","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}
Jessica M. Sampieri-Morán , Diego A. Bravo-Alfaro , Esmeralda Uribe-Lam , Gabriel Luna-Barcenas , Mara Montiel-Sánchez , Luz del C. Velasco-Rodríguez , Andrés A. Acosta-Osorio , Mercedes Ferrer , Hugo S. García
{"title":"Delivery of Magnolia bark extract in nanoemulsions formed by high and low energy methods improves the bioavailability of Honokiol and Magnolol","authors":"Jessica M. Sampieri-Morán , Diego A. Bravo-Alfaro , Esmeralda Uribe-Lam , Gabriel Luna-Barcenas , Mara Montiel-Sánchez , Luz del C. Velasco-Rodríguez , Andrés A. Acosta-Osorio , Mercedes Ferrer , Hugo S. García","doi":"10.1016/j.ejpb.2025.114627","DOIUrl":"10.1016/j.ejpb.2025.114627","url":null,"abstract":"<div><div>Honokiol (HK) and Magnolol (MG), isomers found in <em>Magnolia officinalis</em> bark extract (MBE), possess bioactive properties attributed to their biphenolic structure. However, their low polarity results in poor oral absorption, limiting their bioavailability. To enhance their systemic absorption after passing through the digestive tract, efficient carrier systems are essential. Nanoemulsions (NE) have been suggested to enhance their solubility in the oily core and enable passive diffusion through absorptive cells. Surfactants ensure stability by reducing surface tension between hydrophobic and hydrophilic compounds. In this study we report the preparation of NE containing HK and MG using high and low-energy methods (SNEDDS); we aimed to improve their absorption after oral administration. Results demonstrated that NE enhanced their bioavailability significantly. Compared to the free forms, HK bioavailability increased by 3.47 times, and MG by 3.03 times. SNEDDS further increased HK bioavailability by 3.98 times and MG by 7.97 times compared to their free forms.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"208 ","pages":"Article 114627"},"PeriodicalIF":4.4,"publicationDate":"2025-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143170649","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}