European Journal Of Pharmaceutics And Biopharmaceutics[JOURNAL]
Sun
200 papers
Factors affecting flash nanoprecipitation of Pharmaceuticals: Principles and applications.
Awuku W, Youan BC
Eur J Pharm Biopharm · 2026 Apr · PMID 41513154 · Publisher ↗
Flash nanoprecipitation (FNP) has emerged as a transformative technique in the preparation of nanoparticles for targeted drug delivery. Traditional drug delivery systems often struggle with challenges such as poor solubi...
Flash nanoprecipitation (FNP) has emerged as a transformative technique in the preparation of nanoparticles for targeted drug delivery. Traditional drug delivery systems often struggle with challenges such as poor solubility, limited bioavailability, and suboptimal targeting. FNP addresses these limitations through a one-step, scalable process that produces nanoparticles with tunable size, composition, morphology, and surface characteristics. This review explores the principles of FNP, focusing on its application in encapsulating bioactive agents, achieving controlled release, and enhancing bioavailability. Unlike conventional emulsification or antisolvent precipitation methods, FNP utilizes rapid mixing under kinetically controlled conditions to achieve high reproducibility and uniform particle distribution. The technique has been successfully employed for various pharmaceutical applications, including the delivery of small molecules, biologics, and nucleic acids. Beyond laboratory research, FNP has been adopted in industrial and clinical settings-for instance, in the scalable production of lipid nanoparticles (LNPs) for mRNA-based vaccines and other nucleic acid therapeutics-demonstrating its translational potential. Furthermore, its adaptability extends to theranostic and imaging applications. The review highlights critical formulation variables and process parameters, such as polymer type and its glass transition temperature, solvent selection, and Reynolds number, which influence key characteristics such as nanoparticle stability and performance. By synthesizing recent advances, this paper provides a comprehensive overview of how FNP is already transforming drug delivery, highlighting its current impact, and future research directions.
Novel drug-drug cocrystal form of Luteolin with Metformin: Improved solubility, bioavailability, and in vitro anticancer activity.
Wang N, Zhao J, Wang Y … +7 more , Chen X, Wu Y, Wang A, Chen Y, He D, Hou Y, Gan Y
Eur J Pharm Biopharm · 2026 Mar · PMID 41513153 · Publisher ↗
Due to the extremely low water solubility, poor oral bioavailability, and limited monotherapeutic efficacy of Luteolin (Lut), its clinical application is severely restricted. To overcome these limitations, this study suc...
Due to the extremely low water solubility, poor oral bioavailability, and limited monotherapeutic efficacy of Luteolin (Lut), its clinical application is severely restricted. To overcome these limitations, this study successfully synthesized and characterized the pharmaceutical cocrystal (Lut-Met) with a 1:1 M ratio of Luteolin and Metformin (Met) using the ethanol slow cooling recrystallization method. Single-crystal X-ray diffraction confirmed that cocrystal Lut-Met belongs to the monoclinic crystal system (space group P2), in which Lut and Met are stable through intramolecular hydrogen bonds, intermolecular hydrogen bonds (e.g., Met-N4-H4B…O2-Lut), and π-π stacking interactions. Physicochemical characterization demonstrated a reduced melting point and increased hygroscopicity for the Lut-Met compared to pure Lut. Its dissolution performance in 0.2% SDS and 3% ethanol solution increased by 7.6 times and 4.8 times, respectively. The pharmacokinetic evaluation in mice revealed a 3.13-fold improvement in the relative oral bioavailability of Lut (based on AUC, p < 0.0001) after administration of the cocrystal. In vitro CCK-8 assays demonstrated that the Lut-Met cocrystal exhibits enhanced anti-tumor activity against HeLa, A549, and HepG2 cancer cell lines, as evidenced by its significantly lower IC values compared to both individual drugs and their physical mixture. Furthermore, in vivo distribution studies showed enhanced accumulation of Lut in tumor-related organs, including the heart, liver, spleen, and kidney, following cocrystal treatment. This study confirms that cocrystallization with Met can simultaneously enhance the solubility, bioavailability, and anticancer efficacy of Lut, offering a promising strategy for its pharmaceutical development.
Tuning the in vivo transfection efficiency of mRNA-Loaded lipoplexes by PEG-Lipid structure and ratio.
Markov OV, Antropov DN, Shmendel EV … +10 more , Puchkov PA, Yakovlev OA, Kerbitskaya MD, Zhuravlev ES, Dome AS, Goncharova EP, Shcherbakov DN, Zenkova MA, Maslov MA, Stepanov GA
Eur J Pharm Biopharm · 2026 Mar · PMID 41490599 · Publisher ↗
The development of mRNA-based antiviral and antitumor therapeutics is progressing rapidly and shows considerable promise. Optimizing the composition of liposomal delivery vehicles is critical for enhancing mRNA vaccine e...
The development of mRNA-based antiviral and antitumor therapeutics is progressing rapidly and shows considerable promise. Optimizing the composition of liposomal delivery vehicles is critical for enhancing mRNA vaccine efficacy. Among their components, PEG-lipids require careful optimization to improve the colloidal stability of mRNA-liposome complexes, prolong their in vivo circulation time, and enhance mRNA delivery efficiency, thereby eliciting a robust immune response. Here, we report a structure-functional analysis of PEG-lipids incorporated into cationic liposomes based on the cationic lipid 2X3 and the helper lipid DOPE. The following parameters of PEG-lipids were varied: PEG chain length (800-2000 Da), PEG-lipid architecture (classical head-to-tail vs. gemini-like structures), hydrophobic anchor chain length (C14 octadecyl and C18 tetradecyl residues) and molar amount of PEG-lipid in formulations (0.5-4 mol%). We demonstrated that optimized liposomes contained 4 mol% of a PEG-lipid composed of linear PEG2000 conjugated to a C14-dialkylglycerol anchor via a carbamate linker. This formulation enabled efficient in vivo expression of luciferase-encoding mRNA and, upon delivery of influenza A/California//07/09 (H1N1pdm09) hemagglutinin-encoding mRNA, induced robust antigen-specific humoral and cellular immunity. Our findings underscore the critical importance of PEG-lipid optimization for advancing potent mRNA delivery platforms for antiviral and antitumor vaccines.
Humectant-plasticized poly(vinyl alcohol)-sericin hydrogels with improved dimensional stability and moisture retention for wound dressing applications.
Meetam T, Yamdech R, Chanvorachote P … +1 more , Aramwit P
Eur J Pharm Biopharm · 2026 Mar · PMID 41490598 · Publisher ↗
This study investigated the development of poly(vinyl alcohol) (PVA)/sericin hydrogels incorporating humectant-plasticizers glycerin, propylene glycol, and mannitol for wound dressing applications. Although PVA/sericin h...
This study investigated the development of poly(vinyl alcohol) (PVA)/sericin hydrogels incorporating humectant-plasticizers glycerin, propylene glycol, and mannitol for wound dressing applications. Although PVA/sericin hydrogels exhibit excellent cytocompatibility and promote fibroblast proliferation and collagen production, making them promising candidates for wound care, they suffer from rapid moisture loss and dimensional instability. To address these limitations, glycerin, propylene glycol, and/or mannitol were incorporated to enhance the properties of the hydrogels. The physicochemical and mechanical properties, together with the in vitro cytocompatibility of L929 fibroblasts, were evaluated. The results demonstrated that incorporating propylene glycol and/or mannitol improved dimensional stability, skin adhesion, moisture retention, exudate absorption, flexibility, and softness. Among all the formulations, the hydrogel containing 1 % v/v propylene glycol and 1 % w/v mannitol exhibited the most balanced performance, combining superior physicochemical and mechanical properties (time to initial upward bending: 2.83 h; time for complete upward bending of all four edges: 10.50 h; gel fraction: 60 %, highest absorption at 3 h: 34.41 %; tensile strength: 46.93 kPa, elastic modulus: 33.53 kPa, compressive strength: 19.94 kPa; compressive modulus: 15.58 kPa) with enhanced fibroblast viability (102 % cell viability) and sustained sericin release (∼90 % cumulative release at 168 h). In vitro assays confirmed the cytocompatibility of the optimized hydrogel. Taken together, these findings indicate its potential for effective management of moderately exudating wounds. This study introduces a simple and practical plasticization approach for PVA/sericin hydrogels, offering a promising candidate for wound dressing applications. Further clinical studies are warranted to evaluate its therapeutic efficacy and safety.
Corrigendum to "Nanogel therapy for chronic and post-surgical wounds: a bioengineered Lactoferrin-Acacia-Alginate system enhancing tissue regeneration and inflammatory resolution" [Eur. J. Pharm. Biopharm. 219 (2026) 114952].
Abdullah S, Thiab S, Altamimi AA … +4 more , Al-Masud AA, Al-Sharafa MM, AlKhatib HS, Hamadneh I
Eur J Pharm Biopharm · 2026 Mar · PMID 41456991 · Publisher ↗
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Co-administering clofazimine with infant formula enhances its oral bioavailability in rats and pigs.
Eason T, Ponsonby-Thomas E, Pham AC … +6 more , Huang S, Offersen SM, Thymann T, Zann V, Salim M, Boyd BJ
Eur J Pharm Biopharm · 2026 Mar · PMID 41448504 · Publisher ↗
Milk-based formulations have been proposed as enabling formulations for the delivery of poorly water-soluble drugs to children due to their safety, dose versatility and ability to improve drug solubilisation through the...
Milk-based formulations have been proposed as enabling formulations for the delivery of poorly water-soluble drugs to children due to their safety, dose versatility and ability to improve drug solubilisation through the digestion process. In this study the feasibility of using commercially available infant formula as an enabling formulation to enhance the solubilisation and oral bioavailability of clofazimine, a poorly soluble lipophilic drug, following oral administration was investigated. The solubilisation of crystalline clofazimine in digesting infant formula was assessed in vitro using synchrotron small-angle X-ray scattering. An in vivo pharmacokinetic study was then conducted to determine the oral bioavailability of a suspension of clofazimine in infant formula compared to a lipid-free aqueous suspension in both a rat and piglet animal model. Clofazimine administered in infant formula produced significantly higher plasma concentrations than the aqueous vehicle and resulted in comparable enhancements in relative oral bioavailability in both the piglet (235%) and rat animal models (256%). Results from this study demonstrated that infant formula was an effective enabling formulation, with a positive correlation between improved drug solubilisation during in vitro digestion of infant formula and enhanced in vivo drug exposure following oral administration. Infant formula therefore offers an inexpensive and scalable formulation approach for improving the bioavailability of paediatric drugs, like clofazimine, and enabling the treatment of infections in children.
Sulfasalazine-quercetin co-amorphous systems: Sustained release behaviors and enhanced pharmacokinetics.
Deng J, Li J, Peng Y … +5 more , Dai Q, Pang N, Wang Z, Zhang H, Chen X
Eur J Pharm Biopharm · 2026 Mar · PMID 41443395 · Publisher ↗
Sulfasalazine (SULF) is a well-established therapeutic agent for rheumatoid arthritis (RA) and inflammatory bowel disease (IBD), but its oral absorption is limited by efflux transporters, particularly MRP2 and BCRP. Cons...
Sulfasalazine (SULF) is a well-established therapeutic agent for rheumatoid arthritis (RA) and inflammatory bowel disease (IBD), but its oral absorption is limited by efflux transporters, particularly MRP2 and BCRP. Consequently, high daily doses (1-3 g) and frequent administration (three to four times daily) are required, increasing the risk of adverse effects during long-term therapy. To overcome these limitations, co-amorphous systems (CASs) of SULF with quercetin (QUE) were developed in this study. The CASs were systematically characterized using powder X-ray diffraction (PXRD), polarized light microscopy (PLM), scanning electron microscopy (SEM), and temperature-modulated differential scanning calorimetry (mDSC). The molecular-level formation mechanism was further elucidated via Fourier-transform infrared spectroscopy (FTIR) and molecular dynamics (MD) simulations. All SULF-QUE CASs exhibited glass transition temperatures around 113 °C and demonstrated sustained-release behavior, with markedly lower SULF dissolution (24.5-42.9 %) compared to the crystalline form (89.8 %) after 6 h. This reduction was attributed to the in situ formation of a dense "shell-like" recrystallized QUE surface structure resulting from its incongruent dissolution. Importantly, co-amorphous forms demonstrated enhanced oral bioavailability (1.52-2.80-fold) and prolonged T (1.84-5.52-fold) compared to crystalline SULF, fulfilling the original goal of their development. Moreover, these systems exhibited satisfactory physical stability over time. Overall, the SULF-QUE CASs present a promising strategy to optimize the clinical dosage of SULF, reduce side effects, and offer a synergistic therapeutic approach for RA and IBD.
Reflection paper on the APV workshop on in vitro performance testing of topically applied and topically acting substances.
Lunter D, Gorissen S, Herbig M … +2 more , Hukauf M, Eichner A
Eur J Pharm Biopharm · 2026 Mar · PMID 41435924 · Publisher ↗
With great anticipation, the European Medicines Agency (EMA) guideline titled "Quality and Equivalence of Locally Applied, Locally Acting Cutaneous Products" officially came into effect on April 2, 2025. This regulatory...
With great anticipation, the European Medicines Agency (EMA) guideline titled "Quality and Equivalence of Locally Applied, Locally Acting Cutaneous Products" officially came into effect on April 2, 2025. This regulatory document establishes the legal and scientific framework for the evaluation of generic topical medicinal products, particularly those for which systemic bioavailability is not a relevant endpoint. The guideline is designed to replace conventional clinical trials with scientifically justified alternative methodologies for demonstrating therapeutic equivalence to reference products in the context of generic marketing authorization. These methodologies include, most notably, in vitro release testing (IVRT), in vitro permeation testing (IVPT), stratum corneum sampling via tape stripping (TS), and the vasoconstriction assay for corticosteroids. Based on the draft guideline version released in 2018, preliminary experience has been gathered in recent years regarding the implementation and practical applicability of some testing parameters proposed. However, this early engagement also exposed several ambiguities and limitations in the draft guidance, prompting expectations that the finalized version would address these deficiencies and offer more comprehensive direction on the use of these methods. The present paper is intended to summarize these known limitations and critically examine selected aspects of the guideline. Thereby, it seeks to provide an informed perspective on the scope, robustness, and regulatory utility of the final guideline, and to facilitate a dialogue on its practical implementation in regulatory and industrial settings.
Exploration of a dual-mimetic mucus inert nanocomplex for enhanced oral insulin delivery.
Zhai Q, Guo S, Cui Z … +4 more , Qin L, Guan J, Zhang X, Mao S
Eur J Pharm Biopharm · 2026 Mar · PMID 41429219 · Publisher ↗
The development of oral insulin delivery systems has advanced significantly, with polyelectrolyte nanocomplexes (PEC) showing promise due to their solvent-free synthesis. However, their efficacy is limited by poor mucus...
The development of oral insulin delivery systems has advanced significantly, with polyelectrolyte nanocomplexes (PEC) showing promise due to their solvent-free synthesis. However, their efficacy is limited by poor mucus penetration and intestinal absorption. Inspired by the nature of mucin, chitosan (CS) modified with proline, threonine and serine to mimic the mucin's PTS sequence were synthesized to enhance mucus permeability of the PEC. To further improve the mucus permeability and the trans-epithelial transport of the PEC, muco-penetrating nanocomplexes were fabricated by utilizing hyaluronic acid (HA), thus forming a surface with high-density positive and negative charges to mimic the surface charge properties of viruses. The nanocomplexes were self-assembled using modified CS and insulin, followed by HA coating. It was demonstrated that the nanocomplexes exhibited good physical stability, enhanced protection against enzymatic degradation, and increased penetration efficiency across the mucus layer and small intestine compared to unmodified counterparts. Furthermore, the in vivo hypoglycemic study further revealed a 2.16-fold increase in relative pharmacological availability for the nanocomplexes over the CS/Ins PEC Collectively, these findings reveal the potential of (PTS-CS/Ins)/HA, a dual-mimicking muco-penetrating nanocomplex based on the nature of mucin and virus, as a promising platform for oral insulin delivery.
Novel PLA-based shape-memory formulation: Design, preparation, and evaluation for gastro-retentive delivery of 5-fluorouracil to enhance oral bioavailability.
Liu F, Yu X, Wu Y … +5 more , Zhu T, Chen N, Chen H, Shen W, Zheng W
Eur J Pharm Biopharm · 2026 Mar · PMID 41422985 · Publisher ↗
5-fluorouracil (5-FU) is one of the most effective chemotherapeutic drugs for various solid tumors. However, its low water solubility and limited absorption rates in the stomach are crucial limitations that prevent it fr...
5-fluorouracil (5-FU) is one of the most effective chemotherapeutic drugs for various solid tumors. However, its low water solubility and limited absorption rates in the stomach are crucial limitations that prevent it from being effectively applied in clinical practice. To address these issues, we first encapsulated 5-FU in β-cyclodextrin (5-FU-β-CD) to enhance its solubility, and the resulting 5-FU-β-CD was then loaded into a PLA film to prepare a novel gastro-retentive drug delivery system (GRDDS) based on shape-memory properties. The excipients, such as tributyl citrate (TBC), hydroxyethyl cellulose (HEC), citric acid (CA), and sodium bicarbonate (NaHCO), were incorporated into the PLA matrix at an optimized ratio. This was done to enhance the performance of PLA as an ideal matrix material in GRDDS, including improvements in drug release, floating behavior, shape recovery, gastric retention, and in vivo anti-tumor activity. The results suggested that the solubility of the 5-FU-β-CD inclusion complex was significantly enhanced, which was 1.88-fold higher than that of pure 5-FU. The optimal shape-memory drug delivery formulation, 5-FU-β-CD-PLA/TBC (86/14), prepared in this study consists of PLA/TBC (86/14) incorporating 3 % HEC, 3 % NaHCO, 1 % CA, and 3 % 5-FU. Its gastric retention time was notably prolonged to approximately 8 h following oral administration in mice, whereas the residual amount of 5-FU-β-CD at this time point was much lower than the initial loading. The oral bioavailability of the 5-FU-β-CD-PLA/TBC (86/14) was 269 % higher than that of pure 5-FU. Additionally, the mean tumor size and weight in the mouse model of gastric carcinoma administered with 5-FU-β-CD-PLA/TBC (86/14) were 215.3 mm and 241.4 mg respectively, significantly smaller than those in the 5-FU group. This indicates that the novel PLA-based drug delivery system has significantly enhanced anti-tumor effects. Its excellent therapeutic effects were further confirmed through HE, Ki67, and TUNEL staining. Taken together, 5-FU-β-CD-PLA/TBC (86/14) can be retained in the stomach to improve relative bioavailability. This system represents a promising carrier not only for 5-FU but also for other poorly soluble drugs that require prolonged retention in the stomach.
Understanding peroxide formation in Tween® 80 using RapidOxy®: Implications for pharmaceutical nanoemulsions.
Fedorko A, Tetyczka C, Afonso Urich JA
Eur J Pharm Biopharm · 2026 Feb · PMID 41407213 · Publisher ↗
The oxidation stability of Tween® 80, a widely used surfactant in pharmaceutical formulations, was analyzed in-depth to predict its shelf life under pharmaceutical stability conditions. This study aimed to determine the...
The oxidation stability of Tween® 80, a widely used surfactant in pharmaceutical formulations, was analyzed in-depth to predict its shelf life under pharmaceutical stability conditions. This study aimed to determine the influence of oxidative degradation on the stability of nanoemulsions (NEs) by assessing peroxide formation as a marker of oxidation. By correlating the amount of oxygen absorbed with the oxidation level, a novel mathematical approach was proposed to estimate real-time shelf-life predictions, specifically determining the time required to reach a peroxide value of 10 (mEq O)·kg. Furthermore, nanoemulsions prepared with Tween® 80 at varying levels of oxidative degradation were analyzed. While no significant differences were observed in the overall properties (droplet size, polydispersity index) of these formulations compared to the control, a slight increase in zeta potential and partial degradation of the active pharmaceutical ingredient (API) were detected when oxidized Tween® 80 was used. These findings suggest a potential impact on system stability, emphasizing the need for further long-term investigations to fully understand the implications of oxidative degradation on pharmaceutical nanoemulsions.
Development of spray-dried phage-aztreonam microparticles for inhalation therapy of Pseudomonas aeruginosa lung infections.
Hübl A, Most J, Hauß C … +2 more , Planz V, Windbergs M
Eur J Pharm Biopharm · 2026 Feb · PMID 41407212 · Publisher ↗
Despite considerable efforts in antibiotic therapy, pulmonary infections caused by Pseudomonas aeruginosa remain a major challenge, particularly in diseases such as cystic fibrosis. Bacteriophage-antibiotic combinations...
Despite considerable efforts in antibiotic therapy, pulmonary infections caused by Pseudomonas aeruginosa remain a major challenge, particularly in diseases such as cystic fibrosis. Bacteriophage-antibiotic combinations have recently emerged as a potential alternative due to synergistic effects and the ability to overcome resistance. However, phage instability and sensitivity continue to hinder clinical translation. In this study, we developed an inhalable spray-dried microparticle formulation co-encapsulating bacteriophages against P. aeruginosa and the β-lactam antibiotic aztreonam using mannitol, leucine, and trehalose as excipients. The particles exhibited favorable aerosol properties for deep lung delivery (geometric diameter: 1.39 ± 0.11 µm, mass median aerodynamic diameter: 2.42 ± 0.14 µm) and a burst release profile enabling immediate antimicrobial activity. Aztreonam was efficiently encapsulated (97.87 ± 0.91 %), while phage viability could be maintained through processing, remaining stable for 28 days at 4 and -20 °C. Therapeutic efficacy was confirmed by treatment of P. aeruginosa biofilms. A reduction in bacterial load by 99.90 % was achieved within 24 h. Microparticle biocompatibility was demonstrated in vitro using human lung epithelial cells. The spray-dried phage-aztreonam microparticles enabled phage viability and stability in a formulation and highlight the feasibility of phage-antibiotic co-delivery through dry powder inhalation therapy for treating pulmonary P. aeruginosa infections.
3D-printing of lipid formulations: Going slow in a fast-paced field.
Abdelhamid M, Kumar D, Spoerk M … +1 more , Salar-Behzadi S
Eur J Pharm Biopharm · 2026 Feb · PMID 41407211 · Publisher ↗
Lipid-based excipients (LBE) are a crucial class of functional excipients with significant potential for pharmaceutical formulation and product development. The wide variety of molecules in this class provides opportunit...
Lipid-based excipients (LBE) are a crucial class of functional excipients with significant potential for pharmaceutical formulation and product development. The wide variety of molecules in this class provides opportunities for designing novel dosage forms. However, the utilization of LBEs for 3D-printing applications is currently limited, thereby hindering the full potential of lipids and impeding the advancement of 3D-printing technologies. Notably, only a few publications report the 3D-printing of lipid-based formulations. This review provides a detailed discussion and analysis of these publications. It elucidates the revolutionary capabilities of 3D-printing and presents the potential of LBEs as functional pharmaceutical excipients, with a particular focus on 3D-printing applications. Additionally, the review provides an overview of the current challenges from material perspectives and suggests potential future research topics related to LBEs for 3D-printing of personalized medicine.
A biomimetic nano-suspension based on orthoester designed for the inhibition of postoperative tumor recurrence.
Hu R, Zhang X, Shao W … +3 more , Li N, Kang L, Wang X
Eur J Pharm Biopharm · 2026 Feb · PMID 41407210 · Publisher ↗
Tumor recurrence after surgery remains a major challenge. Herein, an orthoester (OE) compound was synthesized as a liquid pharmaceutical excipient. Next, an injectable suspension loaded with biomimetic nanoparticles and...
Tumor recurrence after surgery remains a major challenge. Herein, an orthoester (OE) compound was synthesized as a liquid pharmaceutical excipient. Next, an injectable suspension loaded with biomimetic nanoparticles and photothermal agents was constructed based on OE to inhibit tumor recurrence. The synthesized OE has the characteristics of simple structure, acid-sensitivity, clear degradation mechanism in vivo. More importantly, as a liquid excipient, OE can dissolve or disperse a variety of drugs, biomacromolecules or nanoparticles to form a stable suspension at extremely high concentrations. Thus, dasatinib (DAS) and sunitinib (SUN) were self-assembled to form nanoparticles, and cancer cell membrane vesicles were coated to obtain biomimetic nanoparticles (HCM@NPs). The self-assembly of DAS and SUN induces molecular aggregation, resulting in an aggregation-induced emission (AIE) effect, which facilitates the tracking of intracellular drug delivery. HCM@NPs and photothermal agent IR820 were co-dispersed in OE to obtain a synergistic therapeutic suspension (OE/IR/HCM@NPs). The suspension can be injected around the tumor or applied directly to the surgical bed to cover any suspicious areas. OE significantly improves the photothermal conversion efficiency of IR820 through its exceptionally low specific heat capacity (1.8 J/(g·℃)), which is markedly lower than that of water (4.2 J/(g·℃). In vitro and in vivo data demonstrated that the OE-based suspension directly inhibited tumor growth and prevented tumor recurrence. All mice receiving chemotherapy alone succumbed within 26 days due to tumor recurrence, whereas 66 % of those treated with the OE nano-suspension exhibited complete suppression of tumor recurrence over the observation period. This paper provides a new idea for the development of suspensions based on OE.
Co-delivery of dolutegravir and carbon-nanoparticles using niosomal platform for enhanced anti-HIV and pharmacokinetic activity.
Ash K, Harshithkumar R, Chandane-Tak M … +5 more , Mukherjee A, Pattnaik A, Mohanty S, Dwivedi M, Dev A
Eur J Pharm Biopharm · 2026 Feb · PMID 41391814 · Publisher ↗
The present study investigates the comparative evaluation of DTG-P, DTG-N and C-Np-DTG-N against HIV-1 infection. C-Np were synthesized from Buchanania lanzan leaves using a microwave-assisted method. The DTG-N formulati...
The present study investigates the comparative evaluation of DTG-P, DTG-N and C-Np-DTG-N against HIV-1 infection. C-Np were synthesized from Buchanania lanzan leaves using a microwave-assisted method. The DTG-N formulation was optimized using central composite design and exhibited particle size, %EE and zeta potential of 124 nm, 80 %, and -32.7 mV respectively. The C-Np-DTG-N exhibited particle size and zeta potential of 134 nm and -37.5 mV respectively. Additionally, cytotoxicity studies were carried out in TZM-bl cells and human PBMCs where C-Np-DTG-N demonstrated greater efficacy against two different subtypes of HIV-1 strains (EC = 0.0032 µg/mL for HIV-1 and 0.0036 µg/mL for HIV-1) than DTG-P (EC = 0.0125 µg/mL for HIV-1 and 0.0155 for HIV-1). The confirmatory analysis using PBMCs validated the enhanced efficacy of C-Np-DTG-N. C-Np-DTG-N demonstrated highest inhibitory effect on HIV-1 integrase (89 %) compared to DTG-P (68.16 %). Furthermore, the pharmacokinetic and fluorescence spectroscopy studies were performed on adult, white New Zealand rabbits. C-Np-DTG-N exhibited a lower C and a longer half-life (114.8 ng/mL and 34.3 h respectively) than DTG-N (144.82 ng/mL and 28.5 h) and DTG-P solution (157.4 ng/mL and 23.2 h respectively). AUC and AUC of C-Np-DTG-N were greater (1109.8 ng/h/mL and 1370.2 ng/h/mL respectively) than DTG-N (1023.4 ng/h/mL and 1293.6 ng/h/mL) and DTG-P solution (942.7 ng/h/mL and 1205.1 ng/h/mL). Moreover, the T of C-Np-DTG-N was longer (2 h) compared to DTG-N &DTG-P solution (1 h). Additionally, the fluorescence intensity of C-Np-DTG-N was higher (4721282 RFU) than C-Np alone (1035558 RFU after 48 h). This research suggests that C-Np-DTG-N offers an improved HIV therapy, providing enhanced anti-HIV activity and bioavailability compared to DTG & C-Np.
Nanogel therapy for chronic and post-surgical wounds: a bioengineered Lactoferrin-Acacia-Alginate system enhancing tissue regeneration and inflammatory resolution.
Abdullah S, Thiab S, Altamimi AA … +4 more , Al-Masud AA, Al-Sharafa MM, AlKhatib HS, Hamadneh I
Eur J Pharm Biopharm · 2026 Feb · PMID 41389993 · Publisher ↗
Chronic and post-surgical wounds often exhibit poor angiogenesis, persistent inflammation, and delayed tissue remodeling. Lactoferrin (LAC), a multifunctional glycoprotein with immunomodulatory and healing properties, fa...
Chronic and post-surgical wounds often exhibit poor angiogenesis, persistent inflammation, and delayed tissue remodeling. Lactoferrin (LAC), a multifunctional glycoprotein with immunomodulatory and healing properties, faces challenges like low solubility and enzymatic degradation that limit its therapeutic use. This study developed a topical nanogel system incorporating LAC, acacia gum (ACC), and sodium alginate (SA) to improve stability, local delivery, and wound healing efficacy. A LAC-ACC complex was formed through adsorption and embedded into SA-based nanogels (Formulations A-C), with Formulation B (2.5 % SA) optimized based on physicochemical and rheological properties. Characterisation techniques included particle size analysis (DLS), thermal profiling (DSC), molecular interaction (FT-IR), crystallinity evaluation (XRD), morphological analysis (TEM), and viscoelastic property determination (rheology). The optimized nanogel exhibited nanoscale size (120.2 nm), low PDI (0.18), and improved solubility (∼2.9-fold). It sustained LAC release up to 82.5 % over 24 h and remained stable for 12 months. In vivo, the LAC-ACC-SA nanogel achieved 95.3 % wound closure by day 14 in rats, significantly outperforming LAC-SA gel, blank gel, and untreated control. The nanogel formulation enhanced VEGF, TGF-β1, and Collagen I expression while reducing IL-6 levels, collectively supporting accelerated tissue regeneration. This nanogel system demonstrates strong potential for managing chronic and post-operative wounds through improved protein delivery and modulation of wound healing pathways.
Utilizing the dynamic gastrointestinal model (DGM) to evaluate the gastric integrity of Capsugel® Enprotect® capsules in fasted and fed states.
Knopp MM, Jannin V, Gonzalez V … +1 more , Müllertz A
Eur J Pharm Biopharm · 2026 Feb · PMID 41386382 · Publisher ↗
This study aimed to evaluate if the Dynamic Gastrointestinal Model (DGM) is able to simulate the gastro-resistant behavior of Capsugel® Enprotect® capsules under physiologically relevant fasted and fed states. Enprotect®...
This study aimed to evaluate if the Dynamic Gastrointestinal Model (DGM) is able to simulate the gastro-resistant behavior of Capsugel® Enprotect® capsules under physiologically relevant fasted and fed states. Enprotect® capsules were filled with a caffeine powder blend and tested under three conditions: fasted state, a light meal (∼500 kcal), and a high-fat meal (∼900 kcal). Results showed that the capsules remained intact in the stomach across all conditions and released their contents only after intestinal entry. Dissolution and pharmacokinetic predictions closely aligned with published clinical data for the fasted state and light meal. The extended gastric residence and elevated pH of the high-fat meal did not compromise capsule integrity possibly due to a combination of capsule floating and acid pocket formation on the top of the digesting meal. These findings confirm the robustness of Enprotect® capsules and demonstrate the utility of the DGM in predicting oral dosage form behavior and performance under physiologically relevant gastrointestinal conditions.
Mucoadhesive bilayer nanomicelles-in-nanofibers nasal insert for sustained treatment of dry eye disease.
Refaat AA, Yahia S, El-Sherbiny IM
Eur J Pharm Biopharm · 2026 Feb · PMID 41380806 · Publisher ↗
Dry eye disease (DED) is a common medical condition that affects quality of life and limits work productivity. Conventional eye drops remain the most common treatment but are limited by low bioavailability and the need f...
Dry eye disease (DED) is a common medical condition that affects quality of life and limits work productivity. Conventional eye drops remain the most common treatment but are limited by low bioavailability and the need for frequent application to sustain therapeutic effect. The current study involves the development of innovative non-invasive single-dose mucoadhesive varenicline (VAR)-loaded biodegradable and biocompatible nanomicelles-in-nanofibers (NFs) nasal insert for DED treatment. The insert has a bilayer structure: the first layer is coaxial NFs and is composed of free VAR-loaded polyethylene oxide (PEO) core and a shell of 1:9 (w/w) polycaprolactone (PCL) and cellulose acetate (CA). Hydrophilic CA was incorporated into the hydrophobic PCL shell to act as exit channels allowing sustained VAR release from the NFs core towards prolonged therapeutic activity. The second layer is to improve mucoadhesiveness and stimulate fast-term drug release to impede inflammation promptly. This second layer is made of electrospun chitosan (CS)/PEO NFs incorporating both VAR-loaded pluronic-F127 nanomicelles (VAR-NPs) and free VAR. The fabricated VAR-NPs and VAR-NPs-in-NFs nasal inserts were characterized using DLS, FTIR, tensile strength, porosity, hydrophilicity, swelling, degradation %, SEM, TEM, and fluorescent micrographs. VAR loading capacity and entrapment efficiency in VAR-NPs were 23.7 and 95 %, respectively. In-vitro VAR release from VAR-NPs and nasal insert was determined after 8 and 16 days, respectively. Cell viability % investigation of human oral epithelial cells (OECs) proves the safety of the developed formulations. In-vivo evaluation including analysis of histological micrographs of the corneal structure, revealed clear signs of structure improvement. The newly developed VAR-NPs-in-NFs nasal inserts can serve as an effective alternative to conventional eye drops for treating DED and offer a progressive strategy with considerable potential for broader application across various ocular diseases beyond DED.
Pediatric orally disintegrating tablets: Overlook the future from multiple aspects.
Yin Z, Lin X, Hong Y … +2 more , Shen L, Zhao L
Eur J Pharm Biopharm · 2026 Feb · PMID 41365425 · Publisher ↗
Orally disintegrating tablets (ODTs) have been a popular dosage form in recent years known for easy administration and fast action. In the case of the global shortage of pediatric-specific medicines and the limited marke...
Orally disintegrating tablets (ODTs) have been a popular dosage form in recent years known for easy administration and fast action. In the case of the global shortage of pediatric-specific medicines and the limited market scale, which are prevalent issues that require urgent attention and resolution, ODTs have great potential to improve medication compliance and expand patient coverage for pediatric population. Through analysing information on manufacturing technologies, excipients, and quality control difficulties of pediatric ODTs from the unique aspects of pediatric patients in this review, the implementation of quality controls, trends of future development and application with possible challenges of pediatric ODTs are prospected. Under the core principle of Quality by Design (QbD) and the development trend of personalized drug delivery, the quality control of pediatric ODTs would continuously optimize in a cycle involving four perspectives: research and development, manufacture, market, and clinical practice. The future application of pediatric ODTs would mainly focus on acute diseases, mental disorders, oral health care, and respiratory diseases in children. It is hoped that through the multi-faceted analysis and future outlook of pediatric ODTs in this review, a reference can be provided for the development of pediatric ODTs.
One-step formation of plasmid DNA-loaded lipid-inorganic salt nanoparticles optimized via two-step design of experiments.
Kato R, Fumoto S, Muttil P … +6 more , Okami K, Yamashita M, Koyanagi H, Miyamoto H, Kawakami S, Nishida K
Eur J Pharm Biopharm · 2026 Feb · PMID 41354109 · Publisher ↗
For successful gene delivery, researchers need to consider multiple processes, such as the endosomal escape of cargos. The preparation of highly functional systems is complicated. Here, we developed a simplified preparat...
For successful gene delivery, researchers need to consider multiple processes, such as the endosomal escape of cargos. The preparation of highly functional systems is complicated. Here, we developed a simplified preparation method for plasmid DNA-loaded galactosylated lipid-inorganic salt nanoparticles, which adopts a one-step alcohol injection method for the formation of lipid nanoparticles. The nanoparticles were designed to have a core of plasmid DNA with inorganic salts consisting of calcium carbonate and phosphate for endosomal escape and a lipid shell for the stable formation of nanoparticles. The formulation and process parameters were optimized using a two-step design of experiments, that is, a definitive screening design followed by a central composite design. We successfully established uniform nanoparticles of 120 nm in size based on micropipette mixing. Transfection efficiency of the nanoparticles prepared via micropipette mixing was equivalent to that of a commercially available transfection reagent in human hepatocellular carcinoma HepG2 cells. Using a microfluidic device, the nanoparticle size was decreased to 70 nm, while a high transfection efficiency was maintained in HepG2 cells. Moreover, the effect of inorganic salts on the nanoparticle transfection efficiency was evaluated. Notably, the formation of a calcium carbonate core was crucial for achieving an effective endosomal escape and a high transfection efficiency. Overall, this study provides valuable information for the design and simplified preparation of lipid-inorganic salt nanoparticles for efficient gene delivery.
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