International Journal of Pharmaceutics最新文献

{"title":"Methylcobalamin-loaded ultra-flexible liposomes: a nanocarrier approach for modulating melanocyte homeostasis and addressing pigmentation imbalances","authors":"Tülay Selin Erkut ,&nbsp;Sema Coşkun ,&nbsp;Menemşe Gümüşderelioğlu","doi":"10.1016/j.ijpharm.2025.125938","DOIUrl":"10.1016/j.ijpharm.2025.125938","url":null,"abstract":"<div><div>Although various therapeutic approaches have been developed for hyperpigmentation, the reliability and efficacy of these treatments remain controversial. This study investigates the effect of methylcobalamin encapsulated in ultra-flexible liposomes on melanocyte homeostasis and evaluates its antioxidant potential for treating pigmentation disorders. Ultra-flexible liposomes with a final lipid concentration of 10 mM were prepared using soy phosphatidylcholine and sodium cholate via the thin-film hydration method. The particle sizes of blank and methylcobalamin-loaded liposomes were 118 ± 9 nm and 124 ± 3 nm, respectively, demonstrating their suitability for <em>in vitro</em> drug release, permeability studies and biomedical applications. Dynamic Light Scattering analysis confirmed the formation of ultra-flexible liposomes with a negative surface charge, similar to cell membranes. Stability studies showed that both particle size and zeta potential remained stable for up to 4 weeks, indicating the structural integrity of the formulation. Approximately 70 % of the encapsulated methylcobalamin was released within 24 h, with an encapsulation efficiency of around 42 %. These liposomes, with a deformability index close to 1, penetrated deeper into the epidermis and dermis of porcine ear skin compared to the free drug. Cell culture studies demonstrated the biocompatibility of the liposomes, with no cytotoxic effects on human dermal fibroblasts and a high uptake rate by human dermal melanocytes. <em>In vitro</em> experiments on melanocyte cells showed a reduction in melanin content, tyrosinase activity, and reactive oxygen species levels, indicating the antioxidant potential of methylcobalamin. In conclusion, methylcobalamin-loaded ultra-flexible liposomes appear to be promising nanocarriers for the targeted treatment of pigmentation disorders.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125938"},"PeriodicalIF":5.3,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144583798","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":"A comparative study of cationic lipid-enriched LNPs for mRNA vaccine delivery","authors":"Burcu Binici ,&nbsp;Zahra Rattray ,&nbsp;Yvonne Perrie","doi":"10.1016/j.ijpharm.2025.125941","DOIUrl":"10.1016/j.ijpharm.2025.125941","url":null,"abstract":"<div><div>Lipid nanoparticles (LNPs) play a central role in mRNA vaccine delivery; however, intramuscular (IM) administration may lead to off-target hepatic expression. Here, we tested whether incorporating a cationic lipid (DOTAP) into ALC-0315-based LNPs could enhance local mRNA expression and immunogenicity. We used DODAP as a comparable ionisable lipid to DOTAP. LNPs were formulated by partially replacing their ionisable lipid (ALC-0315) with 5–50% DOTAP or 10–50% DODAP and evaluated for their physicochemical characteristics, <em>in vitro</em> transfection efficiency, <em>in vivo</em> expression and immunogenicity in mice. Substituting ALC-0315 with 10–25% DODAP had minimal impact on LNP physicochemical properties and expression both <em>in vitro</em> and <em>in vivo</em>. However, completely replacing ALC-0315 with DODAP reduced LNP potency <em>in vivo</em>. Incorporation of DOTAP into the LNPs shifted the zeta potential to positive values and altered morphology, with 5–25% DOTAP increasing <em>in vitro</em> transfection efficiency and enhancing local protein expression at the injection site. Notably, 10% DOTAP reduced hepatic expression, suggesting improved localised expression. Immunisation studies with OVA mRNA-LNPs demonstrated that 5% DOTAP enhanced total IgG responses after the prime dose, whereas higher DOTAP or DODAP levels produced minimal differences or reduced responses; these differences were not sustained after booster immunisation, providing no significant long-term benefits.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125941"},"PeriodicalIF":5.3,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144583871","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":"Nanostructured lipid carriers-loaded dry powder inhaler for pulmonary delivery of amphotericin B in treatment of allergic bronchopulmonary aspergillosis","authors":"Florensia Dana Carla B. ,&nbsp;Ananda Fachriza ,&nbsp;Muh Thaufik Umar ,&nbsp;Johusua Entho Unawekla ,&nbsp;Waode Ainun Anggraini ,&nbsp;Maria Mir ,&nbsp;Ahmad R. Alsayed ,&nbsp;Andi Dian Permana","doi":"10.1016/j.ijpharm.2025.125926","DOIUrl":"10.1016/j.ijpharm.2025.125926","url":null,"abstract":"<div><div>Amphotericin B (AmB) is used to treat Allergic Bronchopulmonary Aspergillosis (ABPA) caused by <em>Aspergillus fumigatus</em>. AmB is available in oral and injectable forms but has limitations, resulting in low levels of AmB in the lungs. We formulated AmB using Nanostuctured Lipid Carriers (NLCs) and Dry Powder Inhaler (DPI) systems to improve the effectiveness of AmB delivery to the lungs. Oleic acid and Compritol® 888 ATO were used as liquid lipid and solid lipid materials for the preparation of NLCs. Characterization tests were conducted to determine the best formula, followed by in vivo pharmacokinetic studies. Characterization results of NLCs-AmB showed that AmB was encapsulated in NLCs in high amounts (21.37 %), with a particle size of 199.95 ± 18.97 nm. This value is better than NLCs-AmB 1 and NLCs-AmB 2. In vitro study showed the release of AmB from NLCs-AmB was 94.38 ± 5.68 %, while pure AmB was only 11.43 ± 1.83 %. Characterization of NLC-AmB-DPI showed good flow properties for NLCs-AmB-DPI 3, supporting delivery to the lungs. In vivo pharmacokinetic studies resulted in a high concentration in the lungs of 7.33 ± 0.56 µg/mL. Overall, this study offers proof-of-concept that the developed NLCs-AmB-DPI are good, safe, and can be used as an alternative for AmB delivery to the lungs, especially in the treatment of ABPA.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125926"},"PeriodicalIF":5.3,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144564782","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":"Silk fibroin microparticles as a candidate for wound healing applications: evaluating the role of adenosine","authors":"Beatriz G. Bernardes ,&nbsp;Rossella Laurano ,&nbsp;Clara López-Iglesias ,&nbsp;Rui Magalhães ,&nbsp;Raquel Costa ,&nbsp;Carlos A. García-González ,&nbsp;Ana Leite Oliveira","doi":"10.1016/j.ijpharm.2025.125930","DOIUrl":"10.1016/j.ijpharm.2025.125930","url":null,"abstract":"<div><div>In this study, silk fibroin (SF) aerogel microparticles were developed as a delivery system for adenosine (ADO) to exploit its anti-inflammatory and regenerative properties for wound healing. Supercritical CO₂ drying was used to prepare ADO-loaded SF aerogel microparticles with different SF concentrations (3 %, 5 %, 7 % w/v) and SF:ADO ratios (10:1, 5:1, 2:1). Characterization revealed high porosity (91–94 %), interconnected pores, high skeletal density (1.22–1.32 g/cm³) and significant surface area (191–306 m²/g). Notably, the 5 % SF with a 5:1 SF:ADO ratio emerged as the most promising formulation, exhibiting excellent morphological and biological properties (91 % porosity, 1.31 g/cm³ skeletal density, and 191 m²/g surface area). <em>In vitro</em> studies on human dermal fibroblasts (HDF), keratinocytes (HaCaT), and human dermal microvascular endothelial cells (HDMEC) demonstrated enhanced viability and proliferation in HDF and HaCaT cells. Specifically, the 5 % SF 5:1 and 5 % SF 2:1 formulations significantly boosted proliferation (over 100 % compared to control) for up to 7 days, highlighting their potential. While HDMECs showed sensitivity to higher ADO concentrations (observed with the 5 % SF 2:1 formulation), the 5 % SF 5:1 formulation achieved the most balanced cellular response across all cell types, underscoring the importance of precise dosage. These findings support the potential of ADO-loaded SF aerogel microparticles in tissue regeneration applications. Further <em>in vivo</em> studies are needed to validate therapeutic efficacy and benchmark against existing wound healing treatments.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125930"},"PeriodicalIF":5.3,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144564783","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":"Sustained delivery of 4-phenylbutyric acid via chitosan nanoparticles in foam for decontamination and treatment of lewisite-mediated skin injury","authors":"Meheli Ghosh ,&nbsp;Nethra Viswaroopan ,&nbsp;Sharvari M. Kshirsagar ,&nbsp;Jasim Khan ,&nbsp;Suha Mohiuddin ,&nbsp;Ritesh K. Srivastava ,&nbsp;Mohammad Athar ,&nbsp;Ajay K. Banga","doi":"10.1016/j.ijpharm.2025.125928","DOIUrl":"10.1016/j.ijpharm.2025.125928","url":null,"abstract":"<div><div>Lewisite, a chemical warfare agent, induces severe skin injury by oxidative stress and endoplasmic reticulum (ER) dysfunction, necessitating innovative antidote strategies. This study developed chitosan nanoparticle-loaded foam formulations for rapid skin decontamination and sustained topical delivery of 4-phenylbutyric acid (4-PBA), an ER stress-reducing chaperone. Nanoparticles were synthesized via ionic gelation using low (LMW) and medium molecular weight (MMW) chitosan. The optimized formulations, N31 (LMW) and N35 (MMW), achieved drug loadings of 5.04 % and 10.09 % w/w, particle sizes of 141.88 ± 26.31 nm and 176.10 ± 36.97 nm, monodisperse distributions (PDI &lt; 0.3), high entrapment efficiency (&gt;93 %) and good stability with zeta potential of −16.67 mV and −19.37 mV, respectively. Incorporation into foam enabled both effective decontamination (&gt;70 % efficiency) and sustained 4-PBA delivery. In vitro release studies demonstrated sustained drug release over 24 h. Permeation studies using dermatomed human skin revealed that nanoparticle formulations significantly reduced 4-PBA delivery: N35 decreased permeation by 38.4 % (214.35 ± 16.6 µg/cm² vs. 348.10 ± 5.37 µg/cm² for free 4-PBA), while N31 reduced it by 81.35 % (64.90 ± 6.89 µg/cm²). Both formulations retained efficacy in PAO challenged skin, with N35 delivering 158.54 ± 53.93 µg/cm² and N31 138.25 ± 14.72 µg/cm² over 24 h.</div><div>Furthermore, in vivo studies showed that the optimized formulation with N35 chitosan (4-PBA N35 + N-acetyl cysteine (NAC)) significantly protects against PAO-induced skin injury and inflammatory cytokine production in Ptch1+/−/SKH-1 hairless mice. Thus, the translational feasibility and effective treatment by the foam formulated 4-PBA N35 + NAC against arsenical-induced skin injury is demonstrated.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125928"},"PeriodicalIF":5.3,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144563229","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":"Smart nano exosomes as precision drug carriers: a new frontier in targeted treatment of oral cancer","authors":"Seyyed Mojtaba Mousavi ,&nbsp;Mitra Abbasifard ,&nbsp;Roshanak Abbasi ,&nbsp;Shadi Tivay ,&nbsp;Hasti Hosseini ,&nbsp;Mobina Taghipoor ,&nbsp;Masoomeh Yari Kalashgrani ,&nbsp;Mahmood D. Aljabri ,&nbsp;Mohammed Muzibur Rahman ,&nbsp;Wei-Hung Chiang ,&nbsp;Yasamin Ghahramani","doi":"10.1016/j.ijpharm.2025.125923","DOIUrl":"10.1016/j.ijpharm.2025.125923","url":null,"abstract":"<div><div>Oral cancer remains a major global health concern due to its high morbidity and mortality rates. Traditional therapies, including surgery, radiation, and chemotherapy, often come with significant side effects and limited effectiveness, especially in advanced stages. Recent advancements in nanotechnology have opened new avenues for targeted drug delivery and personalized treatment approaches. Among these innovations, exosome-based nanocarriers have emerged as promising candidates for the efficient treatment of oral cancer. Exosomes, naturally occurring extracellular vesicles, are involved in intercellular communication and are capable of encapsulating a wide range of therapeutic agents, including drugs, nucleic acids, and proteins. The inherent biocompatibility, low immunogenicity, and ability to cross biological barriers make exosomes an ideal platform for drug delivery. Moreover, the use of “smart” modifications, such as targeting ligands, stimuli-responsive materials, and surface engineering, has further enhanced their specificity and therapeutic efficacy for oral cancer. This review highlights recent progress in the development of smart nano-exosomes for oral cancer therapy, focusing on their design strategies, and clinical potential. It also discusses the challenges and future directions of this promising approach in the fight against oral cancer.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125923"},"PeriodicalIF":5.3,"publicationDate":"2025-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144563228","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":"Ranking of apparent drug affinity to mesoporous silica utilizing a chromatographic screening method and a tree-based prediction model","authors":"Andreas Niederquell ,&nbsp;Barbora Vraníková ,&nbsp;Martin Kuentz","doi":"10.1016/j.ijpharm.2025.125918","DOIUrl":"10.1016/j.ijpharm.2025.125918","url":null,"abstract":"<div><div>Mesoporous silica has emerged as a promising component in bio-enabling formulation strategy. However, there is currently a lack of predictive tools for assessing drug-silica interactions in a preformulation phase, when formulators only have minimal material to guide them. This study proposes a solution: a chromatographic method to rank apparent drug-silica affinity for mesoporous formulations. Using a dataset of 52 drugs, a hydrophilic liquid interaction chromatography (HILIC) screening method was developed, with a stationary silica phase to simulate the drug carrier. Molecular descriptors were calculated for various compounds to analyze HILIC retention times using a tree-based machine learning algorithm. For silica affinity, the distribution coefficient (LogD), the molecular shape descriptor Kappa1, and the number of conjugated bonds (NCB) were identified as possible critical parameters. Additionally, an amine-modified HILIC column was evaluated to simulate a surface-modified silica carrier. The classification tree analysis revealed that Abraham’s hydrogen bonding acidity, the NCB and the pKa were determinants for a qualitative assessment of drug affinity to the modified silica. The classification into low, moderate, and high affinity to the stationary phase appeared to be useful in understanding drug release from mesoporous silica formulations, highlighting its potential for future research.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125918"},"PeriodicalIF":5.3,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144560144","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":"Spray drying strategies for the construction of drug-loaded particles: Insights into design principles and pharmaceutical applications","authors":"Na Chen ,&nbsp;Siqi Huang ,&nbsp;Ting Nie,&nbsp;Liang Luo,&nbsp;Tianqi Chen,&nbsp;Kexian Chen,&nbsp;Zeneng Cheng,&nbsp;Wenjie Liu","doi":"10.1016/j.ijpharm.2025.125917","DOIUrl":"10.1016/j.ijpharm.2025.125917","url":null,"abstract":"<div><div>The design and preparation of particulate drug delivery systems are crucial for enhancing drug efficacy and reducing adverse effects. Spray drying has emerged as a versatile technique for tailoring the particle size, morphology, encapsulation efficiency and release kinetics of drug-loaded particles. This review provides a comprehensive overview of spray drying processes used in the design and fabrication of particulate drug delivery systems. It offers an in-depth analysis of spray drying for modulating the physicochemical properties and performance of drug-loaded particles, as well as its updated applications in various pharmaceutical formulations. Furthermore, the review discusses the different processing parameters of this technique and their effects on drug-loaded particles properties, along with emerging applications in the delivery of biologics and advancements in equipment technology. The objective of this review is to provide researchers with a valuable resource and guide for the recent development and evaluation of spray dried drug-loaded particles.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125917"},"PeriodicalIF":5.3,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144553473","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":"Formulation optimization, in vitro and in vivo correlation, and long-acting analgesic efficacy of dezocine-loaded microspheres overcoming the “quick sand” phenomenon","authors":"Xue-Cheng Li ,&nbsp;Ming-Wei Huo ,&nbsp;Xiang-Xiang Huang ,&nbsp;Ling-Zhi Shi ,&nbsp;Le-Yan Gu ,&nbsp;Ye-Chao Zhang ,&nbsp;Jing-Yi Liu ,&nbsp;Renyu Huang ,&nbsp;Qing-Ri Cao","doi":"10.1016/j.ijpharm.2025.125916","DOIUrl":"10.1016/j.ijpharm.2025.125916","url":null,"abstract":"<div><div>Polymeric acids and their copolymer-based microspheres constitute a critical platform for extended and controlled-release drug delivery systems. However, the precipitated drug crystals (commonly termed “quick sand” phenomenon) during microsphere fabrication significantly limits their application for specific drug molecules, leading to suboptimal drug loading (DL) and encapsulation efficiency (EE) in final products. In this study, dezocine-loaded microspheres (Dez-Ms) were fabricated using microfluidic reactor technology. The formulation and process parameters were systematically optimized through single-factor screening and orthogonal experimental design. Three distinct formulations with high, medium, and low release profiles (designated as Dez-Ms-H, Dez-Ms-M, and Dez-Ms-L) were characterized for mean particle size, DL, and EE. The optimized formulations exhibited mean particle sizes of 55.99 ± 0.02 μm, 62.42 ± 0.01 μm, and 52.93 ± 0.16 μm, DL values of 25.96 ± 0.14 %, 25.02 ± 0.23 %, and 23.12 ± 0.52 %, and EE values of 86.65 ± 0.28 %, 86.33 ± 0.66 %, and 79.72 ± 2.00 %, respectively. Physicochemical characterization via X-ray powder diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy revealed alterations in the drug’s melting point, crystalline form, and infrared absorption peaks post-encapsulation, suggesting intermolecular interactions between the polymeric carrier and the drug within the microspheres. Pharmacokinetic analysis demonstrated that, compared to the dezocine solution group (Dez-Sol), the microsphere groups (Dez-Ms-H, Dez-Ms-M, and Dez-Ms-L) exhibited significantly elevated maximum drug concentrations (C<em>_max</em>) and clearance rates (CL), alongside prolonged time to peak concentration (T<em>_max</em>), elimination half-life (T<em>_1/2</em>), and mean residence time (MRT) (p &lt; 0.05), confirming sustained <em>in vivo</em> release kinetics. An internally validated <em>in vitro</em>-<em>in vivo</em> correlation (<em>IVIVC</em>) model demonstrated robust predictive capability for the microspheres’ pharmacokinetic behavior, establishing a foundation for achieving Level A <em>IVIVC</em> compliance. Additionally, a significant delay in pain response latency (p &lt; 0.05) was observed in the Dez-Ms groups compared to Dez-Sol, indicating sustained analgesic efficacy. Preliminary stability studies further identified optimal storage conditions for Dez-Ms as hermetically sealed containers under dry, low-temperature, and light-protected environments. In conclusion, this study successfully optimized Dez-Ms formulations to overcome the “quick sand” limitation, achieving high EE, validated <em>IVIVC</em>, and prolonged analgesic activity. These findings advance the development of polymeric microsphere systems for controlled drug delivery applications.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125916"},"PeriodicalIF":5.3,"publicationDate":"2025-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144534395","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":"From nature to medicine: snail slime-based functional excipients for oral dosage forms","authors":"Marta Cabibbo,&nbsp;Cinzia Scialabba,&nbsp;Salvatore Emanuele Drago,&nbsp;Emanuela Fabiola Craparo,&nbsp;Gennara Cavallaro","doi":"10.1016/j.ijpharm.2025.125914","DOIUrl":"10.1016/j.ijpharm.2025.125914","url":null,"abstract":"<div><div>Snail slime, well-known for its outstanding benefits in wound healing and skin disorders, is just beginning to be investigated for its potential in treating gastrointestinal inflammatory diseases.</div><div>This study presents novel microparticle-based powders as functional excipients for oral dosage forms, produced via spray-drying (SD) of <em>Helix Aspersa Muller</em> snail mucus combined with pectin and starch. Two formulations were developed: SS_SD_40 (40 wt% slime, 60 wt% pectin/starch 1:1) and SS_SD_20 (20 wt% slime, 80 wt% pectin/starch 1:1). Pure slime showed low yield (17.4 % w/w) and high stickiness, whereas blending with pectin and starch improved yields up to 50 %. The resulting powders had well-defined microparticles with diameters of 9.70  μm and 7.56  μm. HPLC analysis confirmed allantoin preservation (&gt;94 % recovery). SS_SD_40 and SS_SD_20 displayed acceptable flowability as a pharmaceutical grade powder, low water content, and mucoadhesiveness under simulated GI conditions. Antioxidant tests revealed dose-dependent radical scavenging, with SS_SD_20 achieving up to 60 % higher activity and lowest IC₅₀ than the other investigated samples. Anti-inflammatory effects, assessed by BSA denaturation, were strongest for SS_SD_40 (∼90 % inhibition at 2.5 mg/ml and lowest IC₅₀ that the other samples). Both samples showed no cytotoxicity towards Caco-2 cells and reduced IL-6 and IL-8 secretion. The synergistic combination of snail slime, pectin, and starch produced multifunctional, biocompatible powders suitable as new functional excipients for oral formulations.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125914"},"PeriodicalIF":5.3,"publicationDate":"2025-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144517288","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}