European Journal Of Pharmaceutics And Biopharmaceutics[JOURNAL]
Sun
200 papers
Impact of terminal groups on PLGA degradation rate and their role in sustained release of cyproterone acetate.
Zhao Q, Yang J, Liu J … +6 more , Zhang S, Zhao W, Jiang W, Zhou Y, Jiang L, Zhang J
Eur J Pharm Biopharm · 2026 Jan · PMID 41238007 · Publisher ↗
Poly(lactic-co-glycolic acid) (PLGA) is the most commonly used commercially available polymeric pharmaceutical excipient for developing injectable long-acting release products. Its degradation rate is influenced by facto...
Poly(lactic-co-glycolic acid) (PLGA) is the most commonly used commercially available polymeric pharmaceutical excipient for developing injectable long-acting release products. Its degradation rate is influenced by factors, such as molecular weight, the lactic/glycolic ratio (L/G ratio), and the nature of terminal groups. These variables impose challenges in achieving a precisely controlled release of loaded active compounds from finished PLGA-based formulations. This study investigated the impact of varying PLGA terminal groups on drug loading, encapsulation efficiencies, and drug release profiles in PLGA microspheres. We synthesized PLGA with four distinct terminal groups: carboxyl, n-hexyl, dodecyl, and hexadecyl, while keeping molecular weights and L/G ratios consistent to isolate the effects of the terminal groups on PLGA properties. Also, we examined how terminal groups influence the degradation behavior of PLGA microspheres and found that longer carbon chain lengths in the terminal groups resulted in a slower degradation rate. We have developed a novel method for analyzing terminal groups, enabling us to verify our synthesized products and to compare them against commercially available products. This method enhances the accuracy of our analyses and ensures the integrity of our product verification process. Additionally, we explored the underlying mechanism by which terminal groups affect the PLGA degradation. We then prepared four PLGA microspheres loaded with cyproterone acetate (CYA) through emulsification. The resulting microspheres exhibited consistent morphology, and a volume mean diameter of 9 to 11 µm,a drug loading rate of about 10% and an encapsulation efficiency of approximately 97%. The results of in vitro release experiments showed that CYA release from all microspheres could be sustained for up to two months with a recovery rate reaching 100%. Meanwhile, we investigated the mechanism of loaded drug release from PLGA microspheres with different terminal groups and elucidated how the degradation of PLGA influences the release profile of loaded drugs. The insights gained from this study will enhance the understanding of PLGA degradation and the mechanisms underlying the release of loaded actives from PLGA microspheres. Furthermore, the modification of terminal groups has the potential to support the development of advanced pharmaceutical excipients.
A strategy to prevent ciprofloxacin induced corneal toxicity.
Roy P, Kavanagh ON
Eur J Pharm Biopharm · 2026 Jan · PMID 41232849 · Publisher ↗
Every month thousands of patients are treated with ocular ciprofloxacin, yet crystalline deposits form on the surface of the cornea in one in ten patients. This occurs due to a pH shift when the formulation is instilled...
Every month thousands of patients are treated with ocular ciprofloxacin, yet crystalline deposits form on the surface of the cornea in one in ten patients. This occurs due to a pH shift when the formulation is instilled onto the eye, since ciprofloxacin formulations are buffered to pH 4.5 to keep the drug in solution, whereas the tear pH is around 7. We deconstruct the formulation and the chemical pathophysiology of this condition to enable the selection of inhibitors that can derisk corneal toxicity. Through in vitro and ex vivo models we show that some structurally similar fluoroquinolones (levofloxacin and ofloxacin) can successfully inhibit the nucleation of ciprofloxacin. In contrast, other fluoroquinolones like norfloxacin can promote the formation of a less soluble ciprofloxacin-norfloxacin complex, increasing the risk of corneal deposition. We further identify that mannitol, a common excipient in marketed ophthalmic formulations, accelerates nucleation and could promote the risk of crystallisation. These findings identify both beneficial and counterproductive formulation components and define a practical anticrystal engineering strategy to prevent ciprofloxacin-induced ocular precipitation. We anticipate that this study may inspire further work designing nucleation inhibitors for transient, high supersaturation conditions such as those seen regularly during drug delivery.
Oxygenated collagenase nanoliposomes for deep photodynamic therapy via remodelling the tumor extracellular matrix.
Xu X, Han J, Lou X … +2 more , Xu X, Du Y
Eur J Pharm Biopharm · 2026 Jan · PMID 41232848 · Publisher ↗
Melanoma is highly aggressive and remains difficult to treat. Traditional treatment options often result in damage to normal tissues and a high rate of recurrence. Conventional photodynamic therapy (PDT) is limited by po...
Melanoma is highly aggressive and remains difficult to treat. Traditional treatment options often result in damage to normal tissues and a high rate of recurrence. Conventional photodynamic therapy (PDT) is limited by poor light penetration, oxygen depletion, and extracellular matrix (ECM) barriers. In this study, we developed an acid-responsive liposome system that co-loads indocyanine green (ICG, a photosensitizer) and 1-bromoperfluorooctane (PFOB) modified with collagenase (Col-LIP-(ICG + PFOB)) to facilitate the degradation of the tumor extracellular matrix and enable near-infrared (NIR)-triggered PDT. Our findings demonstrated that Col-LIP-(ICG + PFOB) effectively degrades the tumor extracellular matrix via collagenase, resulting in increased accumulation of the formulation within the tumor. Upon NIR irradiation, ICG produced reactive oxygen species and heat, while PFOB provided supplemental oxygen and collagenase degraded the extracellular matrix, together contributing to enhanced antitumor efficacy. In melanoma models, this system significantly inhibited tumor growth and reduced HIF-1α levels. In conclusion, this study offers a novel strategy to increase the efficacy of PDT in the treatment of melanoma.
Corrigendum to "Combination of magnetic targeting with synergistic inhibition of NF-κB and glutathione via micellar drug nanomedicine enhances its anti-tumor efficacy." [Eur. J. Pharm. Biopharm. 155 (2020) 162-176].
Elhasany KA, Khattab SN, Bekhit AA … +8 more , Ragab DM, Abdulkader MA, Zaky A, Helmy MW, Ashour HMA, Teleb M, Haiba NS, Elzoghby AO
Eur J Pharm Biopharm · 2026 Jan · PMID 41224543 · Publisher ↗
Abstract loading — click title to view on PubMed.
Review of design strategies for active targeted drug delivery systems for pancreatic cancer.
Rahmatulla A, Bi X, Wang P … +5 more , Wang X, Li S, Zhang X, Qiao X, Chen Y
Eur J Pharm Biopharm · 2026 Jan · PMID 41218726 · Publisher ↗
Pancreatic cancer (PC) is frequently referred to as the "king of cancers" due to its high mortality rate and poor prognosis. Chemotherapy drugs of a traditional nature are confronted with a multitude of challenges, inclu...
Pancreatic cancer (PC) is frequently referred to as the "king of cancers" due to its high mortality rate and poor prognosis. Chemotherapy drugs of a traditional nature are confronted with a multitude of challenges, including poor water solubility, low bioavailability, significant toxic side effects, and poor patient tolerance. This article provides a comprehensive review of the epidemiological and pathophysiological features of PC. The review also highlights the key antigens and receptors that are overexpressed in PC cells, including antigens such as TROP2, MSLN, MUC, and CA19-9. Furthermore, the article covers receptors like EGFR, TfR, integrins, GPCRs, IGF, GPC1, TF, and MET. The text introduces current pancreatic cancer treatment drugs, including gemcitabine, tegafur, and albumin-bound paclitaxel. The text also discusses targeted drug delivery carriers for PC, including liposomes, carbon nanotubes, exosome, polymer micelles, nanoparticles, nanocrystals, and hydrogel-encapsulated nanoparticles. The review offers a concise overview of the antibodies and ligands employed in active targeted drug delivery systems for PC, including hRS7, αTROP2, MF-T, TAB004, HzMUC1, as well as ligands such as EGF, GE11 peptide, Tf, tTR14, XQ-2d, cNGQ, α5β1-targeted peptide, IGF1, and SDC1. The therapeutic effects and prospects of combining active targeting strategies with photothermal therapy, immunotherapy, and gene editing technology are discussed in this paper.
A bedside-savior for insomnia and anxiety disorders: melatonin/buspirone hydrochloride compound oral fast-dissolving film.
Liu X, Chu C, Lu Q … +8 more , Song X, Wu M, Gou J, He H, Yin T, Tang X, Jiang X, Zhang Y
Eur J Pharm Biopharm · 2026 Jan · PMID 41218725 · Publisher ↗
Insomnia and anxiety disorders are highly prevalent conditions that significantly impair daily functioning. Notably, a bidirectional relationship exists between these two disorders: heightened cortical excitability secon...
Insomnia and anxiety disorders are highly prevalent conditions that significantly impair daily functioning. Notably, a bidirectional relationship exists between these two disorders: heightened cortical excitability secondary to anxiety disrupts sleep onset mechanisms, while prolonged sleep insufficiency impairs prefrontal cortical regulation of emotional processing, thereby exacerbating anxiety symptoms. This creates a vicious cycle that worsens both conditions. To address this clinical challenge, we developed a combination therapy using two pharmacological agents with complementary mechanisms of action. Given the potential adverse neurological effects associated with conventional anxiolytics and hypnotics, we specifically selected two short-acting drugs with favorable safety profiles: melatonin and buspirone hydrochloride. To address insomnia accompanied by anxiety, we have designed and prepared a Bedside-savior:a compound oral fast-dissolving film containing melatonin and buspirone hydrochloride. Unlike traditional tablets or capsules, this immediate-release film offers distinct advantages for our target patients. Since it requires no water for administration, it prevents sleep disruption caused by nighttime drinking. Its ease of use makes it ideal for children, elderly individuals, and those with swallowing difficulties. Furthermore, the medication is rapidly absorbed through the sublingual venous plexus, enabling quick onset of action to simultaneously ease anxiety and promote faster sleep initiation-all without the need to get out of bed.
Development of piperine/HPβCD-loaded PVA-coated iron oxide nanoparticles in in situ gel for enhanced retinal delivery and anti-VEGF activity.
Jansook P, Soe HMSH, Tun T … +11 more , Hnin HM, Chamni S, Asasutjarit R, Lapmanee S, Bhummaphan N, Puttipanyalears C, Bhubhanil S, Inchan A, Charoenphon N, Lu Y, Wu W
Eur J Pharm Biopharm · 2026 Jan · PMID 41213343 · Publisher ↗
Piperine (PIP) is a potential therapeutic agent for retinal diseases; however, its poor aqueous solubility limits its ocular bioavailability. To overcome this limitation, a novel nanocarrier system was fabricated through...
Piperine (PIP) is a potential therapeutic agent for retinal diseases; however, its poor aqueous solubility limits its ocular bioavailability. To overcome this limitation, a novel nanocarrier system was fabricated through the adsorption of PIP/hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complexes onto the surface of polymer-stabilized iron oxide nanoparticles (IONs), which were then incorporated into an in situ gelling formulation. Three hydrophilic polymers, i.e., polyethylene glycol, poloxamer 407, and polyvinyl alcohol (PVA) were used as surface coatings. Among these, PIP/HPβCD/PVA-IONs exhibited the highest percent entrapment efficiency (77.38 ± 2.17 %) and superior mucoadhesive properties. Ocular safety was evaluated using the hen's egg test on chorioallantoic membrane (HET-CAM), which indicated no irritation. To further enhance ocular retention and retinal delivery, the PIP/HPβCD/PVA-IONs were incorporated into an in situ gel. Upon contact with simulated tear fluid, the formulation underwent a sol-to-gel transition with excellent gelling capacity and improved ex vivo permeation across excised porcine cornea (0.85 ± 0.07 × 10 cm⋅s) and sclera (3.16 ± 0.29 × 10 cm⋅s). In vitro studies on ARPE-19 retinal cells demonstrated the formulation was non-toxic at concentrations up to 50 µg/mL (>70 % cell viability). Furthermore, in vitro and in vivo evaluations revealed that the formulation effectively suppressed vascular endothelial growth factor A at both the protein and mRNA levels. It also exhibited significant anti-inflammatory and anti-angiogenic effects. These findings suggest that the PIP/HPβCD-loaded IONs incorporated in in situ gel system offers a promising nanocarrier platform for targeted ocular drug delivery in the treatment of retinal diseases.
Pharmacomagnetography of floating gastroretentive systems in vivo in different prandial states evaluated by AC biosusceptometry.
Rodrigues GS, Buranello LP, Barboza JM … +5 more , Abílio Almeida MJ, Stoppa EG, Ferrari PC, Soares GA, de Arruda Miranda JR
Eur J Pharm Biopharm · 2026 Jan · PMID 41207573 · Publisher ↗
In recent decades, the development of effective therapies with minimal adverse effects has become a major challenge in the pharmaceutical field. Despite its popularity, oral administration faces limitations related to th...
In recent decades, the development of effective therapies with minimal adverse effects has become a major challenge in the pharmaceutical field. Despite its popularity, oral administration faces limitations related to the physiological variability of the gastrointestinal tract (GIT), such as gastric emptying time, absorption window, and site of drug release. In this context, modified-release systems-especially gastroretentive drug delivery systems (GRDDS)-have gained prominence. GRDDS aim to prolong gastric retention time (GRT), facilitating controlled and localized drug release, particularly beneficial for drugs with limited absorption windows or instability in alkaline pH. This study evaluated the in vivo performance of a magnetic floating drug delivery system (MFDDS) containing metronidazole using pharmacomagnetography based on alternating current biosusceptometry (ACB) in healthy volunteers (n = 12, aged 19-21 years) under fasted and fed conditions. Results demonstrated that the prandial state significantly influenced MFDDS behavior, with food intake prolonging both the floating lag time (FLT) (105-120 min fed vs. 45-60 min fasted) and gastric retention time (GRT) (165.0±32.2 min fed vs. 118.3±35.3 min fasted, p < 0.0001). The orocecal transit time (OCTT) was similar between groups (271.7±32.0 min fed vs. 254.2±44.9 min fasted, p > 0.05), while small intestine transit time (SITT) was shorter in the fed state (111.7±22.3 min) compared to the fasted state (140.0±47.7 min), though not statistically significant. Pharmacokinetic parameters showed significant differences, with the fed state resulting in delayed time to maximum concentration (Tmax) (252.0±52.9 min fed vs. 174.0±60.0 min fasted, p < 0.05) but substantially higher maximum plasma concentrations (Cmax) (11.0±5.7 µg/mL fed vs. 4.7±2.2 µg/mL fasted, p < 0.05) and area under the curve (AUC360) (2606.1±1825.5 µg·h/mL fed vs. 969.3±638.3 µg·h/mL fasted, p < 0.05). The time lag before detectable plasma concentration (Tlag) was similar between groups (67.5±21.8 min fed vs. 86.7±31.4 min fasted, p > 0.05). The increased viscosity of gastric contents in the fed state delayed the initial tablet flotation by forming a hydrophobic barrier around the tablet, restricting gastric fluid diffusion into the polymeric matrix. This extended gastric retention in the fed state resulted in more complete and sustained metronidazole absorption, confirming the effectiveness of the gastroretentive system in optimizing drug bioavailability, particularly when administered after meals.
Synergistic co-processing of heat-moisture treated resistant rice starch with HPMC and Eudragit® S100: A novel multifunctional excipient for direct compression and colon-targeted delivery.
Trisopon K, Saokham P, Kittipongpatana N … +2 more , Chomchoei N, Kittipongpatana OS
Eur J Pharm Biopharm · 2026 Jan · PMID 41197883 · Publisher ↗
A novel multifunctional excipient was developed based on co-processed resistant rice starch (RRS) for direct compression (DC) tablet and targeted colonic drug delivery. While rice starch (RS) is biodegradable and exhibit...
A novel multifunctional excipient was developed based on co-processed resistant rice starch (RRS) for direct compression (DC) tablet and targeted colonic drug delivery. While rice starch (RS) is biodegradable and exhibits good compressibility for DC, its poor flowability and low resistant starch content limit its applicability in both DC and controlled-release formulations. To address these limitations, RS was modified using heat-moisture treatment (HMT) with optimal process parameters (moisture content, temperature, and treatment time) were determined through a design of experiments (DoE) approach. The optimized HMT conditions successfully increased resistant starch content by approximately fourfold compared with native RS, and enhanced the plastic deformation properties of RRS, improving its compressibility. To achieve targeted colonic release, a pH-sensitive and enzyme-degradable polymer system was incorporated. The optimized RRS was co-processed with high-viscosity HPMC and Eudragit® S100 through wet granulation to obtain a co-processed excipient (CRRS). The resulting CRRS demonstrated enhanced flowability, packing efficiency, and plastic deformation characteristics, meeting all SeDeM expert system criteria for DC suitability. The corrective excipient proportion (CP, %) indicated a high dilution capacity, supporting drug loading of up to 55 %. Tablets containing 30 % w/w 5-aminosalicylic acid (5-ASA) as a model drug, prepared by DC using CRRS, exhibited acceptable uniformity of dosage units, friability, and drug content. In vitro dissolution studies revealed a controlled-release pattern, achieving approximately 80 % cumulative release within 12 h. The dense matrix formed by resistant starch and functional polymers effectively restricted water penetration and enzymatic access, promoting gradual and site-specific release under colonic conditions compared with tablets lacking RRS. Release kinetics followed the Higuchi model, with n values suggesting an anomalous transport mechanism involving both diffusion and erosion. Overall, CRRS represents a promising multifunctional excipient combining excellent DC performance with controlled, site-specific colonic drug delivery potential, supporting the development of advanced oral dosage forms.
Analysis of discrepancy in SNEDDS performance for a "brick dust" mebendazole between in-vitro and in-vivo estimation.
Maehara S, Nishiyama S, Maruyama M … +1 more , Higaki K
Eur J Pharm Biopharm · 2026 Jan · PMID 41183581 · Publisher ↗
Oral absorption of mebendazole (MBZ), a brick dust, was successfully improved 10 times by dosing 2% HPMCP-50 SNEDDS of MBZ co-amorphized with (+)-10-camphorsulufonic acid (CSA) (MBZ-CSA), compared with crystal powders in...
Oral absorption of mebendazole (MBZ), a brick dust, was successfully improved 10 times by dosing 2% HPMCP-50 SNEDDS of MBZ co-amorphized with (+)-10-camphorsulufonic acid (CSA) (MBZ-CSA), compared with crystal powders in our previous study. However, an in-vitro non-sink dissolution study with pH3.9 acetate buffer or FaSSIF (conventional method) revealed that 2% HPMCP-50 SNEDDS of MBZ-CSA improved the dissolution of MBZ over 440 times compared to the crystal. In the current study, we assessed the reason for the large discrepancy in SNEDDS performance between in-vitro and in-vivo estimations using several novel in-vitro methods. The Sequential Gastro-Intestinal Exposure (SGIE) method, reflecting the transit from the stomach to the small intestine (GI-transit), revealed MBZ precipitation higher than that in the conventional method using FaSSIF. The Egg phosphatidylcholine-Monolayer-CHCl Partition (EMCP) method, reflecting the absorption process, also indicated MBZ precipitation at early time periods greater than the conventional method. The SGIE-EMCP method, reflecting both GI-transit and subsequent absorption processes, indicated the highest precipitation of MBZ and MBZ transfer to the CHCl phase less than the EMCP method. The SGIE-EMCP method also indicated that 2% HPMCP-50 SNEDDS transferred MBZ to the CHCl phase significantly larger than SNEDDS without the polymer, which coincided with the in-vivo tendency.
Nanoparticle-based oral rinses for plaque control: A systematic review of efficacy and safety.
Ahmed B, Ahmed F, Kumar A … +3 more , Imran M, Iqubal MK, Al-Lami HA
Eur J Pharm Biopharm · 2026 Jan · PMID 41176187 · Publisher ↗
This systematic review analyzes clinical, preclinical, and patent literature on nano-enabled mouthwashes for plaque control. Searches were conducted across PubMed, Embase, Scopus, Web of Science, and three patent databas...
This systematic review analyzes clinical, preclinical, and patent literature on nano-enabled mouthwashes for plaque control. Searches were conducted across PubMed, Embase, Scopus, Web of Science, and three patent databases (Google Patents, Lens, and Espacenet) for English-language records published from January 2018 to June 2025. Eligible studies included randomized controlled trials (RCTs), other human investigations, and in vitro, ex vivo, or animal studies evaluating nanoparticle-based mouthrinses. Two reviewers independently extracted data, assessed bias risk using the RoB-2 tool, and rated evidence certainty with the GRADE approach. Findings were narratively summarized due to methodological differences. A total of 38 records met the inclusion criteria: 25 primary research studies (10 RCTs; 15 in vitro/animal) and 13 patents on nano-enabled mouthwashes. Silver nanoparticles were the most studied, followed by zinc oxide, titanium dioxide, calcium phosphate, and herbal nanoemulsions. Nano-enabled mouthwashes reduced plaque index by a pooled mean difference of 0.32(95 % CI: 0.25 to 0.39; I = 45 %) and gingival index by a pooled mean difference of 0.27(95 % CI: 0.21 to 0.33; I = 50 %) units, respectively, comparable to 0.12 % chlorhexidine (CHX), with fewer reports of staining or taste changes. Nanosilver rinses decreased white-spot lesions in orthodontic patients by 66 %, and titanium dioxide-based rinses halved dentine hypersensitivity scores. Preclinical studies showed ≥2-log reductions in biofilm viability, pH-triggered mineral release, and nanozyme-like catalytic activity. Thirteen patents (2003-2024) described stable nanoformulations, odour-neutralizing systems, mucoadhesive carriers, and theranostic technologies, indicating significant commercial interest. Evidence certainty was moderate for short-term plaque and gingival control but low for caries prevention and long-term safety. Nano-enabled mouthwashes show promise as alternatives to CHX, but large, long-term RCTs are needed to confirm efficacy, monitor safety, and support clinical use.
Optimization of intranasal trifluoperazine/SPION-leciplex thermosensitive organogel for depression therapy: Pharmacodynamic and pharmacokinetic comparison of magnet placement effects on brain versus nose.
Elsalhy S, Refai H, Osman DA … +2 more , Sayed NE, Khalifa MKA
Eur J Pharm Biopharm · 2025 Dec · PMID 41167290 · Publisher ↗
Trifluoperazine (TFP), an antipsychotic used in depression management, suffers from extensive first-pass metabolism and poor oral bioavailability. Intranasal delivery offers a promising non-invasive route for direct nose...
Trifluoperazine (TFP), an antipsychotic used in depression management, suffers from extensive first-pass metabolism and poor oral bioavailability. Intranasal delivery offers a promising non-invasive route for direct nose-to-brain targeting, while magnetic nanoparticles can further enhance drug localization and absorption. This study aimed to optimize and evaluate a superparamagnetic iron oxide nanoparticle (SPION)-loaded leciplex organogel for intranasal delivery of TFP, with emphasis on the effect of external magnet location. The study compared magnet application on the brain to promote olfactory targeting versus on the nose to enhance systemic absorption. TFP/SPION-leciplex nanoparticles were optimized and incorporated into a thermosensitive mucoadhesive organogel. Pharmacodynamic efficacy was assessed via the forced swimming test, and pharmacokinetics were determined in plasma and brain across four groups: no magnet, magnet on nose, magnet on brain, and oral marketed product. The optimized formulation (266.20 nm, +50.9 mV, 5.90 emu/g, IC 393.92 μg/ml) showed safety and favorable characteristics. Both magnet-assisted groups significantly reduced immobility time versus the non-magnet and oral controls, with no significant difference between the two strategies. However, the "magnet on nose" group achieved the highest plasma levels, favoring systemic absorption, while the "magnet on brain" group achieved the highest brain levels, favoring olfactory targeting. The SPION-loaded leciplex organogel significantly improved intranasal TFP delivery, enabling dose reduction and superior efficacy compared with oral therapy. Magnet placement was profound in directing drug distribution toward systemic circulation or brain, suggesting that the two approaches may be clinically tailored-"magnet on nose" for systemic delivery and "magnet on brain" for CNS targeting.
Development of Trastuzumab-coupled, siRNA encapsulating mPolyplexes targeting HER2 overexpressing cancer cells.
Müller JT, Caruso S, Nguyen A … +5 more , Jürgens DC, Kromer APE, Sheshachala S, Adams NBP, Merkel OM
Eur J Pharm Biopharm · 2025 Dec · PMID 41167289 · Publisher ↗
Over the past decades, significant advancements have been made in various medical fields; however, ovarian cancer (OC) remains inadequately addressed, predominantly relying on relatively toxic cytostatic treatments. In t...
Over the past decades, significant advancements have been made in various medical fields; however, ovarian cancer (OC) remains inadequately addressed, predominantly relying on relatively toxic cytostatic treatments. In this study, we applied newly developed poly(β-amino) esters (PBAEs) for siRNA delivery. As recent literature has shown, the introduction of a hydrophobic, unsaturated fatty acid together with polycationic spermines as the PBAE side chains are leading to a favourable transfection efficiency, and the resulting materials form a unique class of micelleplexes, termed micelle-embedded polyplexes (mPolyplexes). Here, such mPolyplexes were modified post-particle formation with the approved monoclonal antibody Trastuzumab for HER2 targeting, as supported by a receptor binding analysis through fluorescence shift assay. Physicochemical analysis revealed suitable hydrodynamic diameters of modified mPolyplexes, as determined by dynamic light scattering. Improved cellular uptake when targeted with Trastuzumab was optimized by applying Design of Experiment (DoE). We demonstrated superior gene silencing efficiency of EGFR as well as PLK1, both involved in OC progression, with knockdown values exceeding 82% and 70%, respectively. These findings were corroborated by a relevant cell migration assay. The macroscopic impact after PLK1 silencing on epithelial-mesenchymal transition (EMT) was visualized using confocal microscopy. This work addresses critical questions in the field of ovarian cancer therapy and confirms the suitability of siRNA encapsulating PBAE nanocarriers as promising non-viral vectors.
Development of media simulating the properties of human peritoneal fluid and verification of its bio-relevance.
Abdelquader MM, Li S, Andrews GP … +1 more , Jones DS
Eur J Pharm Biopharm · 2025 Dec · PMID 41161499 · Publisher ↗
Intraperitoneal drug delivery offers a promising strategy for localized treatment of peritoneal tumours and post-surgical wound care. To control drug release profiles, drugs are often embedded within peritoneal implants...
Intraperitoneal drug delivery offers a promising strategy for localized treatment of peritoneal tumours and post-surgical wound care. To control drug release profiles, drugs are often embedded within peritoneal implants or delivery devices. Typically, release studies from these devices are performed in phosphate-buffered saline (PBS), which underestimates in vivo release due to its lower drug solubility compared to human peritoneal fluid (hPF). Adding surfactants or albumin alone does not replicate the complexity of hPF, and few studies have addressed the development of a simulated peritoneal fluid (sPF). Accordingly, this study aimed to develop a biorelevant sPF based on hPF composition and to evaluate its ability to mimic hPF. The developed formulation contained salts, glucose, albumin, phosphatidylcholine stabilized by cholesterol and surfactants. The physicochemical properties (pH, buffering capacity, osmolality, wettability, and flow) of the formed fluid were assessed alongside conducting solubility studies of five model drugs with diverse ionization status (acids, bases, and neutral species) in sPF, hPF, and PBS. The results demonstrated that PBS underperformed relative to hPF, while sPF closely matched hPF in buffering capacity, osmolality, flow behaviour, solubilization of the model drugs, and wetting ability. These findings support the use of sPF as a biorelevant medium for solubility and release studies of intraperitoneal drug delivery systems.
Mucus-penetrating archaeolipid nanocarriers delivering Thymus vulgaris essential oil and tobramycin: A multifunctional approach against Pseudomonas aeruginosa biofilms and inflammation.
Perez N, Velurtas M, Rivas Rojas PC … +3 more , Morilla MJ, Romero EL, Perez AP
Eur J Pharm Biopharm · 2025 Dec · PMID 41151657 · Publisher ↗
Cystic fibrosis (CF) is characterized by thick mucus obstruction, persistent Pseudomonas aeruginosa biofilms, and chronic airway inflammation, leading to progressive lung damage. Inhaled tobramycin (TB) is the standard a...
Cystic fibrosis (CF) is characterized by thick mucus obstruction, persistent Pseudomonas aeruginosa biofilms, and chronic airway inflammation, leading to progressive lung damage. Inhaled tobramycin (TB) is the standard antibiotic therapy but has limited efficacy due to poor biofilm penetration and bacterial tolerance, while Thymus vulgaris essential oil (EOT) provides antioxidant and anti-inflammatory effects but is hindered by low solubility and instability. In this study, a comprehensive in vitro evaluation was conducted on EOT and TB co-loaded into nanostructured archaeolipid carriers (NAL-EOT/TB), composed of a compritol-miglyol lipid matrix with a surface coating of Tween 80 and archaeolipids from the archaea Halorubrum tebenquichense. NAL-EOT/TB interacted minimally with mucins and diffused efficiently through artificial mucus. Under mucus-covered conditions, macrophage uptake was higher for NAL-EOT/TB than for non-archaeolipid nanocarriers (NLC-EOT/TB), likely due to improved mucus permeation and scavenger receptor recognition. In epithelial cell-biofilm co-cultures, NAL-EOT/TB significantly decreased epithelial cell damage compared to both free EOT/TB and NLC-EOT/TB. Moreover, NAL-EOT/TB lowered ROS in neutrophil-like cells and achieved greater IL-8 reduction than dexamethasone. These findings support NAL-EOT/TB as a multifunctional nanotherapeutic platform to address mucus penetration, biofilm disruption, and airway inflammation in CF.
Self-assembled rapamycin prodrug nanoparticles for posterior segment targeting and effective treatment of experimental uveitis.
Liang F, Wang Y, Li N … +6 more , Liu Y, Gao Y, Song Y, Zhao Z, Wang Y, Liu H
Eur J Pharm Biopharm · 2025 Dec · PMID 41110639 · Publisher ↗
The treatment of posterior uveitis remains challenging due to the need for long-term medication and the limited efficacy of current therapies. In this study, we developed an injectable rapamycin-based nanoparticle formul...
The treatment of posterior uveitis remains challenging due to the need for long-term medication and the limited efficacy of current therapies. In this study, we developed an injectable rapamycin-based nanoparticle formulation designed to extend intraocular residence time and enhance retinal penetration, thereby improving therapeutic outcomes. The nanoparticles were formed via self-assembly of rapamycin conjugated with a hydrophobic alkyl chain, yielding uniformly spherical particles with an average diameter of approximately 90 nm. In vitro experiments confirmed that the formulation exhibited minimal cytotoxicity, potent anti-inflammatory effects, inhibition of endothelial cell migration, and efficient uptake by retinal pigment epithelial (RPE) cells. In vivo imaging demonstrated that the nanoparticles rapidly localized to the RPE layer of the posterior segment following intravitreal injection, in contrast to the free drug. Moreover, experimental autoimmune uveoretinitis (EAU) rats treated with nanoparticles exhibited a substantial alleviation of ocular inflammation and a concomitant reduction in the expression of inflammatory markers, including CD45, CD68, IBA-1, and IL-17.
Corrigendum to "Dissolving microneedle patches for delivery of amniotic mesenchymal stem cell metabolite products for skin regeneration in UV-aging induced mice" [Eur. J. Pharm. Biopharm. 204 (2024) 114482].
Miatmoko A, Hariawan BS, Cahyani DM … +9 more , Anjani QK, Annuryanti F, Octavia RT, Legowo D, Purwantari KE, Rosita N, Purwati, Donnelly RF, Hariyadi DM
Eur J Pharm Biopharm · 2025 Dec · PMID 41109819 · Publisher ↗
Abstract loading — click title to view on PubMed.
Gas-based therapies in chronic wounds: A scoping review of preclinical and clinical data.
Kasha S, Hanning SM, Mugisho OO … +1 more , Thakur SS
Eur J Pharm Biopharm · 2025 Dec · PMID 41106558 · Publisher ↗
INTRODUCTION: Chronic wounds are injuries that persist beyond expected healing timeframes. Although they have varying aetiologies abnormal development, prolonged inflammation and evident hypoxia are common features in al...
INTRODUCTION: Chronic wounds are injuries that persist beyond expected healing timeframes. Although they have varying aetiologies abnormal development, prolonged inflammation and evident hypoxia are common features in all chronic wounds. Innovative treatments are sought and gas-based therapies in particular have shown promise in supporting conventional treatment strategies. This scoping review aims to identify and compare the range of formulations that are used for gas-based therapy and evaluate their effectiveness in treating chronic wounds. METHODS: A scoping review was conducted with articles identified from the Medline, Embase and Scopus databases. Articles exploring gas-based therapies in chronic wound healing were identified after screening all the search results against inclusion and exclusion criteria. RESULTS AND DISCUSSION: There were 54 clinical studies and 45 preclinical studies eligible for analysis. Gas-based therapies were delivered by various modalities. Hyperbaric oxygen therapy and topical gas therapies demonstrated some clinical utilisation, though adoption into standard care protocols was limited by costs and variable treatment outcomes. Novel formulations were of significant interest within the preclinical space, with micro- and nanoparticle systems and hydrogel scaffolds demonstrating an ability to effectively deliver various therapeutic gases and improve chronic injury outcomes in cell and animal-based models. However, the wound healing capacities of established and exploratory approaches have rarely been compared to each other. CONCLUSIONS: Hyperbaric oxygen therapy and topical gas therapy are clinically used in chronic wound management, although they have not been adopted as part of standard wound care. A variety of recently developed gas-loaded formulations have demonstrated preclinical potential and are poised to soon migrate into the clinical trial domain.
Effects of Co-Processed and conventional excipients on content uniformity.
Stewart S, Reinhard J, Carpanzano A … +2 more , Ciurczak E, Warnke G
Eur J Pharm Biopharm · 2025 Dec · PMID 41101516 · Publisher ↗
Silicification of microcrystalline cellulose (MCC) has previously been shown to have positive effects on the powder's flowability and tabletability compared to plain MCC or physical blends of colloidal silicon dioxide (C...
Silicification of microcrystalline cellulose (MCC) has previously been shown to have positive effects on the powder's flowability and tabletability compared to plain MCC or physical blends of colloidal silicon dioxide (CSD) and MCC [1]. A further characteristic of silicified MCC (SMCC) is its specific surface area, which is approximately five times larger than that of plain MCC [1]. It was hypothesized, therefore, that SMCC might have beneficial effects in terms of blend and content uniformity via effects of interactive blending. This study was designed to compare the blending efficacy of silicified microcrystalline cellulose and a co-processed SMCC-based multifunctional excipient to that of physical blends comprising the same nominal components. Near infrared spectroscopy (NIRS) was used to probe blend uniformity during the blending process of the excipients and a model active pharmaceutical ingredient (API), caffeine, presenting morphological and electrostatic challenges with regard to content uniformity. In addition to NIRS, both particle size analysis and scanning electron microscopy (SEM) were used to investigate the resulting blends. Content uniformity on the tableted blends, obtained by caffeine dissolution, was used to investigate the effects of differing blend uniformity on a final oral solid dosage form. For this non-optimized formulation with a challenging API, use of SMCC and a co-processed SMCC-based multifunctional excipient yielded formulations with significant benefits over using standard MCC, or MCC blended with colloidal silicon dioxide (CSD). These benefits included a faster blend uniformity, prevention of particle attrition, and a reduced impact of blender type and materials. Additionally, use of silicified microcrystalline cellulose yielded formulations with increased tablet hardness and reduced ejection forces.
Improving prefilled syringe injectability: influences of critical component attributes and human factors.
Wang Y, Li H, Wu L … +3 more , Zhao Z, Chen Q, Guo J
Eur J Pharm Biopharm · 2025 Dec · PMID 41093078 · Publisher ↗
Prefilled syringes (PFSs) have emerged as a predominant primary packaging format for subcutaneous biopharmaceutical drug products. Subcutaneous administration typically requires low injection volumes and high drug concen...
Prefilled syringes (PFSs) have emerged as a predominant primary packaging format for subcutaneous biopharmaceutical drug products. Subcutaneous administration typically requires low injection volumes and high drug concentrations, which frequently leads to a nonlinear increase in viscosity; that can impair injectability and feasibility for patient self-administration, potentially affecting drug safety and efficacy. This research investigates critical PFS design elements (including silicone oil coating, barrel diameter, plunger stopper contact length, needle length and inner diameter) that can be optimized to further mitigate injection resistance and enhance injectability. Transitioning from 29-gauge to 27-gauge needles reduced glide force by 59 % (32 N → 13 N) during administration of 1 mL 20-centipoise viscous fluid (10 s injection), demonstrating enhanced injectability of high-viscosity formulations. Furthermore, a simulated human factors study with a diverse cohort (n = 12) evaluated the usability of the optimized device. A reduction in glide force correlates with an improvement in user perception and usability. Collectively, these combined studies provide practical, patient-centric design strategies to advance PFS injectability, linking technical optimization with real-world usability requirements.
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