Journal of Drug Delivery Science and Technology最新文献

{"title":"Eggplant-derived Solamargin-Propolis nanoformulation as an efficacious chemotherapeutic agent for lung carcinoma A549 through mitochondrial dynamics dysregulation","authors":"Aeshah A. Awaji ,&nbsp;Khulud M. Alshehri","doi":"10.1016/j.jddst.2025.106687","DOIUrl":"10.1016/j.jddst.2025.106687","url":null,"abstract":"<div><div>Solamargine, derived from eggplant, has shown significant antitumor effects in preclinical studies, demonstrating its potential for cancer therapy. Its ability to modulate mitochondrial dynamics, induce apoptosis, and inhibit metastasis underscores its potential as an anticancer agent. The present study investigated the effectiveness of solamargine (Sm) extracted from eggplant and self-assembled with propolis nanoparticles (PNP) through an acid-base neutralization reaction to fabricate encapsulated Sm (Sm-PNP) for fighting lung cancer by disrupting mitochondrial fission/fusion dynamics. Spectral and microscopic analyses confirmed the formation of Sm-PNPs, wherein solamargine (Sm) was encapsulated within propolis nanoparticles (PNP). Solanine (SA) (31.5 ± 3.5), Sm (17.77 ± 2.3), and Sm-PNP (17.325 ± 3.62) showed significantly lower cytotoxic IC₅₀ concentrations against A549 lung carcinoma cells than PNP (99.825 ± 17.5) (P &lt; 0.0001). In contrast, these substances showed higher IC50 values in HeLa cells, without statistically significant differences, suggesting a preferential effect on cancer cells. Sm-PNP treatment progressively upregulated Drp1 and Fis1 (P &lt; 0.001) in A549 cells, whereas Mfn1 and 2 showed significant differences in inhibition across groups (P &lt; 0.01). This suggests the potential of encapsulated solamargine as an effective cancer therapy, providing insights into MFN1 and 2's roles and alternative treatments. Compared to untreated A549 cells and cisplatin (reference drug), Cyto C, Bax (P &lt; 0.01), and caspase 8 (P &lt; 0.001) gene expression was significantly upregulated, with varying values. Sm-PNP significantly inhibited the inflammatory cytokines TNFα (P &lt; 0.01) and IL10 (P &lt; 0.05) and enhanced apoptotic activity by upregulating P53 expression (P &lt; 0.0001) and inhibiting ATPase inhibitory factor 1 (P &lt; 0.001). Consequently, the encapsulated form of solamargine increased its bioavailability and could therefore serve as a promising approach for enhancing apoptosis in lung cancer by disrupting the balance of mitochondrial dynamics.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106687"},"PeriodicalIF":4.5,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143421483","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Regional brain distribution of PLGA nanoparticles functionalized with glutathione or phenylalanine dipeptide","authors":"Mario Alonso ,&nbsp;Emilia Barcia ,&nbsp;Sofía Negro ,&nbsp;Nicola Paccione ,&nbsp;Mahdieh Rahmani ,&nbsp;Consuelo Montejo ,&nbsp;Luis García-García ,&nbsp;Ana Fernández-Carballido","doi":"10.1016/j.jddst.2025.106680","DOIUrl":"10.1016/j.jddst.2025.106680","url":null,"abstract":"<div><div>Neurodegenerative diseases are chronic disorders affecting millions of people with their prevalence constantly increasing worldwide. The blood-brain barrier plays a key role in the design of successful treatments for these pathologies. Nanotechnology has the potential to improve treatment of CNS disorders and facilitate effective drug transfer. For this, biodegradable poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) are promising strategies as they can be surface-tailored with functionalized molecules for site-specific brain targeting. In our work PLGA NPs loaded with a fluorescent marker (rhodamine B) and functionalized with glutathione or phenylalanine dipeptide have been developed, characterized and analyzed for their passage across the BBB and distribution in different brain areas of Wistar rats.</div><div>Surface functionalization of the NPs with glutathione or phenylalanine (formulations NP-GSH-Rh and NP-PHE2-Rh) favoured their passage across the BBB process in which glutathione transporter and L-type amino acid transporter 1 (LAT-1) may be involved. One hour after their administration both functionalized formulations predominantly reached the hippocampus followed by the cortex and substantia nigra. Average values of intensity of fluorescence reached in the hippocampus showed statistically significant differences when compared to non-functionalized NPs and remained higher in this area 2 h after administration which allows us to highlight the potential importance of the results obtained as the presence of the NPs in the brain 2 h after their administration counteracts the efflux activity of the P-glycoprotein. In addition, none of the nanosystems caused tissue damage in the hippocampus, cortex or substantia nigra.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"105 ","pages":"Article 106680"},"PeriodicalIF":4.5,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143350180","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A detailed insight into the role of nanosized drug carriers for the management of diabetic wounds","authors":"Abhinab Goswami ,&nbsp;Pratap Kalita ,&nbsp;Bedanta Bhattacharjee ,&nbsp;Sandhanam K ,&nbsp;Partha Pratim Dutta","doi":"10.1016/j.jddst.2025.106688","DOIUrl":"10.1016/j.jddst.2025.106688","url":null,"abstract":"<div><div>The chronic hyperglycaemic condition in diabetes patients leads to nerve and blood vessel damage, which causes neuropathy and peripheral vascular diseases. Furthermore, these pathological conditions severely affect the wound-healing process in diabetic patients. Compared to normal wounds, diabetic wounds display augmented infection, excessive free radicals, elevated inflammations, diminished collagen production, and reduced growth factor formation. Although several promising therapeutics exist, such as standard drugs, growth factors, cell therapy, etc., none ensures long-term efficacy. Therefore, it is essential to emphasize the need for developing novel therapeutics based on the pathophysiology of diabetic wounds. The literature was performed by using Google Scholar, PubMed and Scopus to construct a detailed review. Compared to other therapeutics modalities, nanosized drug carriers display an accelerated diabetic wound healing rate owing to their unique physicochemical and biological properties. These unique carriers can permeate deeper wound sites, stabilize the loaded drug against the surrounding harsh environment, and modulate the drug release pattern to achieve effective and faster healing. The nanosized drug carriers can deliver therapeutic drugs/biologicals for stimulating angiogenesis, accelerating wound-healing associated protein expression, treating infections, scavenging free radicals, and reducing inflammation. Furthermore, nanosized drug carriers can intrinsically act on the wound to elevate healing. In this review, an attempt has been made to comprehensively report the usage of different nanosized drug carriers for managing diabetic wounds.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"105 ","pages":"Article 106688"},"PeriodicalIF":4.5,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143377855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"MPPD modeling based differential lung dosimetry of rifabutin loaded β-glucan dry powder microparticles in adult mice and various human age groups","authors":"Anshita ,&nbsp;Vyas Kumar ,&nbsp;Firoz Ahmad ,&nbsp;Mohd Khubaib ,&nbsp;Rolee Sharma ,&nbsp;Jyotsna Singh","doi":"10.1016/j.jddst.2025.106686","DOIUrl":"10.1016/j.jddst.2025.106686","url":null,"abstract":"<div><div>Rifabutin β-glucan dry powder inhalable microparticles (DYDGP) prepared by alkaline acidic extraction method, spray-dried and, analyzed for <em>in vitro</em> aerodynamic particle size distribution using a handheld powder disperser and micro-orifice uniform deposit impactor (MOUDI), a 10-stage cascade impactor connected through induction port revealed mass median aerodynamic diameter (MMAD) and geometric standard deviation (GSD) of 1.58 μm, 1.43 respectively. The assessment of adult mice (nose only) and child, adult, elderly human (oral) airways particle dosimetry (regional, tissue, lobular particle deposition and clearance) under chronic breathing scenario was performed using Multiple Path Particle Dosimetry (MPPD 3.04). The MPPD data obtained was normalized for interspecies comparison. The deposition fraction was higher in pulmonary and head region in humans and mice, respectively. A higher deposition fraction was observed in children followed by adolescent, adults and elderly for regional (pulmonary), tissue (peripheral, upper and lower), lobular, and airway generations. Tracheobronchial (TB) and alveolar clearance were maximum in initial hours and highest in adults and lowest in children. Differential deposition observed in male and females were mostly related to their breathing physiology inputs. Differential mass and particle number deposition per alveolar macrophage was observed. The mass retained for humans at 400 mg/m³ with 30 min exposure (7 day/week for 26 weeks) was close to mass retained in mice at 1500 mg/m³ with 30 min exposure (5 days/week for 26 weeks) or at 400 mg/m³ with 4 h exposure (5 days/week for 26 weeks). Data generated may be useful in <em>in vivo</em> result interpretation (in future) and <em>in vitro</em> to <em>in vivo</em> and interspecies dose extrapolation for clinical applications. In future. integration of dosimetry data with DPI drug kinetic modelling/studies may be useful in establishment of better human chronic dose for inhalable antituberculosis therapeutics.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106686"},"PeriodicalIF":4.5,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143378028","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Neat amorphous form and amorphous solid dispersions of apalutamide: A comparative study","authors":"Rekha Sapkal ,&nbsp;Pawan Devangan ,&nbsp;Jitender Madan ,&nbsp;Amol G. Dikundwar","doi":"10.1016/j.jddst.2025.106678","DOIUrl":"10.1016/j.jddst.2025.106678","url":null,"abstract":"<div><div>Amorphous form and Amorphous solid dispersions (ASDs) of an anticancer drug Apalutamide (APA) with four polymers of different categories namely, PVPK30, HPMCAS, Soluplus and Eudragit L100-55 are investigated. The drug loads were screened based on an <em>in situ</em> drug polymer miscibility study using differential scanning calorimetry. Amorphous form of the API and ASDs prepared for each of the polymers at two different drug loads (20 % w/w and 50 % w/w) were characterized using Powder XRD, DSC and ATR-FTIR. Comparative analysis with regards to <em>in vitro</em> drug release profiles of the ASDs and their physical and chemical stability is provided. The observed trends were evaluated based on the measurements of solubility enhancement ability and nucleation inhibition potential of the polymers. Also, role of surfactant in dissolution media in effecting the drug release is described in relation to the drug load of the ASDs and compared with that of the neat amorphous form. Assessment of dissolution of the polymer alone in the dissolution media provided clear indication of importance of right amphiphilicity of the polymer in achieving maximal drug release. This study reinforces the critical balance of multiple parameters while making the choice of an amorphous phase of the drug for delivering the oral solid dosage form and provides insights into drug-specific requirement of the polymer, balancing product stability and drug release.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106678"},"PeriodicalIF":4.5,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143395770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Sustained release studies on 3-hydroxyflavone-loaded eudragit nanofibers to combat inflammatory conditions","authors":"Kakunje Shreevani ,&nbsp;Badiadka Narayana ,&nbsp;Balladka Kunhanna Sarojini ,&nbsp;Bikrodi Sesappa Dayananda ,&nbsp;Aroor Ganesha ,&nbsp;Punchappady Devasya Rekha ,&nbsp;Raifa Abdul Aziz ,&nbsp;Shamprasad Varija Raghu","doi":"10.1016/j.jddst.2025.106677","DOIUrl":"10.1016/j.jddst.2025.106677","url":null,"abstract":"<div><div>The strategy for this study is the fabrication of biocompatible eudragit (RS100) nanofiber carrying a newly synthesized 3-hydroxyflavone with potential anti-inflammatory property for sustained delivery in the periodontal pocket. As this compound is proved to be biocompatible and exhibiting promising biological activities, it is taken as a molecule of choice. The polymer solution with bioactive compound was electrospun to yield nanofiber scaffolds which were characterized using FESEM, PXRD, FTIR, UV spectroscopy and TGA. The developed nanofibers exhibited bead-free and randomly arranged structures with a diameter range of 261 nm–285 nm. The amorphous nature of the polymer is depicted by its low degree of crystallinity whereas the values increased profusely for compound loaded samples indicating the semicrystalline nature. The evaluation of surface wettability by the apparent contact angle measurement showed a hydrophilic nature of the mat with θ = 82.8° upon increasing the concentration. This is followed by an increase in swelling ability which is conducive to increased proliferation and the cell attachment characteristics required by the periodontal barrier membrane. Furthermore, upon dissolution, nanofibers showed a release of 49.26 % of the encapsulated drug for approximately 32 h in an <em>in-vitro</em> model with R² (0.9863) fitting to Korsmeyer Peppas model suggesting a diffusion mechanism. In addition, cell viability greater than 90 % was obtained from <em>in-vitro</em> study. Concomitantly, <em>in-vivo</em> biocompatibility studied using <em>Drosophila melanogaster</em> model depicted 82 % of the survival rate. The drug also showed an astonishing effect again albumin denaturation (&gt;80 %). All the results were compared with standard drug diclofenac diethylamine at the same concentration. The results thus revealed the suitability of the fabricated nanofiber mat with potential application in combating periodontal infections.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106677"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143378087","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Inorganic biomaterials for ocular drug delivery: A comprehensive review","authors":"Rudra Narayan Sahoo ,&nbsp;Sagar Rout ,&nbsp;Ankita Parmanik ,&nbsp;Bhabani Sankar Satapathy ,&nbsp;Snigdha Pattnaik ,&nbsp;Laxmidhar Maharana ,&nbsp;Amit Kumar Nayak","doi":"10.1016/j.jddst.2025.106667","DOIUrl":"10.1016/j.jddst.2025.106667","url":null,"abstract":"<div><div>Since last few decades, a wide range of biomaterials have been employed for ocular drug delivery applications, including natural and synthetic polymers, proteins and peptides, inorganic biomaterials, engineered biomaterials, <em>etc</em>. Amongst these, inorganic biomaterials have already been demonstrated to control biological responses, including cell-matrix interaction. Metals (like gold, silver, titanium, <em>etc</em>.), metal oxides like silicon dioxide (SiO₂), magnetic iron oxide (Fe₃O₄), titanium dioxide (TiO₂), zinc oxide (ZnO₂), <em>etc</em>., ceramics, mesoporous silica nanoparticles (MSNs), carbon-based inorganics, <em>etc</em>., are some of the most often used inorganic biomaterials for ocular drug delivery applications. This review article outlines different inorganic biomaterials, their classification, properties, and applications in ocular drug delivery. The ocular toxicity of inorganic biomaterials has also been comprehensively reviewed. Several metals and metal oxides have shown their antioxidant with high chemical stability in ocular drug delivery therapeutics. Different carbon-based inorganics like carbon dots (CDs), carbon nanotubes (CNTs), graphene, <em>etc</em>., with their bioinert, biocompatibility, and biomimicking activity have also demonstrated a promising usefulness in ocular therapeutics. The unique physicochemical, chemical, mechanical, optical, and magnetic properties of inorganic biomaterials make them highly efficient for drug targeting. The therapeutic capabilities of inorganic biomaterials can be modified using attachment of ligands to enrich their attraction towards the molecules at the target site, which makes them more appealing for efficient target-specific drug delivery with bioimaging (diagnostic) applications.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106667"},"PeriodicalIF":4.5,"publicationDate":"2025-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143386603","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of a novel Cissus quadrangularis extract loaded sodium alginate/chitosan based 3D printed scaffold for regeneration of cancellous alveolar bone","authors":"Samapti Padhihary,&nbsp;Krishna Pramanik","doi":"10.1016/j.jddst.2024.106440","DOIUrl":"10.1016/j.jddst.2024.106440","url":null,"abstract":"<div><div>Development of a polymeric based scaffold with phytomolecules is important to enhance osteo-active property of polymeric bone substitute, decrease use of synthetic drugs and sustained release of phytomolecules. The present study highlights the fabrication and characterizations of a novel <em>Cissus quadrangularis</em> (CQ) extract impregnated sodium alginate (SA) and chitosan (CH) based 3D printed scaffolds for regenerative therapy of cancellous alveolar bone. Addition of CQ extract in SA/CH scaffold changed the wettability and degradation rate of the scaffolds. Protein adsorption, bioactivity and free radical scavenging properties of the scaffolds were enhanced remarkably by CQ extract, but exhibiting biphasic dose response. Impregnation of CQ extract up to a certain dose, such as 0.125 % and 0.25 % (w/v), in SA/CH scaffold, represented as SA/CH/CQ_0.125 and SA/CH/CQ_0.25 scaffold respectively, significantly enhanced the cell viability of human osteoblast like Saos-2 cell line. However, viability of cells significantly declined after this point, as evidenced in SA/CH/CQ_0.5 and SA/CH/CQ_1.0 scaffolds. SEM and confocal micrographs demonstrated that SA/CH/CQ_0.25 3D construct exhibited a greater number of inter-connected living cells with elongated actin filaments compared to other constructs. The osteogenic studies demonstrated that SA/CH/CQ_0.25 construct followed by SA/CH/CQ_0.125 shown higher bone mineral deposition and bone marker ALP gene expression than the SA/CH construct, while SA/CH/CQ_0.5 and SA/CH/CQ_1.0 constructs displayed significantly reduced expressions of these markers. The results indicated that the CQ extract exhibited a biphasic hormetic response <em>i.e.</em> the extract increased the osteogenic properties of the SA/CH scaffold when used in an appropriate dose, but thereafter impeded the proliferation of bone cells. Among all the scaffolds, SA/CH/CQ_0.25 displayed better osteogenic performances and thus can act as a promising bone substitute for the regeneration of cancellous alveolar bone.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"104 ","pages":"Article 106440"},"PeriodicalIF":4.5,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143100547","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Rizatriptan loaded bilosomes for nose to brain delivery: Fabrication, statistical optimization, and biological evaluation","authors":"Nabil K. Alruwaili ,&nbsp;Omar Awad Alsaidan ,&nbsp;Ameeduzzafar Zafar ,&nbsp;Hassan H. Alhassan ,&nbsp;Eyad Abdulrazaq Alburaykan ,&nbsp;Aseel Awad Alsaidan ,&nbsp;Mohd Yasir ,&nbsp;Lubhan Singh ,&nbsp;Mohammad Khalid","doi":"10.1016/j.jddst.2024.106489","DOIUrl":"10.1016/j.jddst.2024.106489","url":null,"abstract":"<div><div>Rizatriptan (RTP) is an anti-migraine drug and after oral administration, it exhibits low bioavailability (45 %) due to high first-pass hepatic metabolism. Therefore, to resolve this issue, RTP-loaded bilosomes (BLSs) for brain delivery through the intranasal route were developed. RTP-BLSs were prepared by the thin-film hydration technique and optimized by the L9 Taguchi model. Bile salt (sodium glycocholate, mg), surfactant (Span 40, mg), and edge activator (Cremophor RH 40, mg) were selected as independent factors and their influence was observed on vesicle size (nm) and entrapment efficiency (%). Selected optimized RTP-BLSs (F5) formulation exhibited low vesicle size (204.70 ± 5.8 nm) and polydispersity index (0.260 ± 0.022), good entrapment efficiency (78.32 ± 3.1 %), and high zeta potential (−27.6 ± 1.67 mV). The optimized RTP-BLSs formulation exhibited more sustained released profile (96.41 ± 4.48 % in 24 h) than RTP-Sol (98.65 ± 3.46 % RTP released in 4 h). The flux and apparent permeability coefficient for optimized RTP-BLSs were found to be 1.069 ± 0.026 μg cm⁻² h¹ and 10.690 × 10⁻⁴ ± 0.262 × 10⁻⁴ cm h⁻¹, respectively which were significantly (P &lt; 0.05) better than the flux (0.548 ± 0.148 μg cm⁻² h⁻¹) and apparent permeability coefficient (5.481 × 10⁻⁴ ± 1.476 × 10⁻⁴ cm h⁻¹) of RTP-Sol. The relative bioavailability of RTP formulated within the optimized RTP-BLSs administered intranasally was 2.94 ± 0.78-fold higher than the one obtained with RTP-Sol. The optimized RTP-BLSs showed 1.91 ± 0.15-fold higher absolute bioavailability as compared to intravenous administration RTP-BLSs. The optimized RTP-BLSs showed 64.18 ± 2.34 % nose-to-brain drug transport, while RTP-Sol exhibited 20.72 ± 1.46 % after intranasal administration. The optimized RTP-BLSs showed a significantly higher brain drug targeting efficiency (279.16 ± 6.37 %) as compared to RTP-Sol (126.15 ± 4.79 %) given intranasally. From the findings, it can be concluded that the developed BLSs are novel alternative RTP carriers for direct nose-to-brain delivery for the improvement of brain drug targeting.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"104 ","pages":"Article 106489"},"PeriodicalIF":4.5,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143104830","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mucoadhesive gellan gum/poly(2-ethyl-2-oxazoline) films for ocular delivery of pilocarpine hydrochloride","authors":"Guzel K. Abilova ,&nbsp;Shamil F. Nasibullin ,&nbsp;Kuanysh Ilyassov ,&nbsp;Aslan N. Adilov ,&nbsp;Marzhan K. Akhmetova ,&nbsp;Rouslan I. Moustafine ,&nbsp;Yesset T. Muratov ,&nbsp;Sarkyt E. Kudaibergenov ,&nbsp;Vitaliy V. Khutoryanskiy","doi":"10.1016/j.jddst.2024.106492","DOIUrl":"10.1016/j.jddst.2024.106492","url":null,"abstract":"<div><div>The study aims to develop new prolonged delivery systems of pilocarpine hydrochloride (pilocarpine⸱HCl) for the therapy of glaucoma. Polymer films based on gellan gum (GG) and its mixtures with poly(2-ethyl-2-oxazoline) (POZ) at different ratios were prepared by casting. The films were found to be homogeneous, transparent, and sufficiently flexible. The GG:POZ mixtures were examined using spectroscopic, thermal and microscopic methods. Additionally, the mechanical and mucoadhesive properties of GG and GG:POZ films were studied. It was found that the greater content of gellan gum in the mixture enhances the mechanical strength and mucoadhesive properties of GG:POZ films. In <em>vivo</em> experiments in rabbits were conducted to evaluate the practical application of these films loaded with pilocarpine hydrochloride. The results demonstrate the effectiveness of the polymeric films compared to traditional eye drops in terms of prolonged release of the miotic drug and extended therapeutic effect duration.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"104 ","pages":"Article 106492"},"PeriodicalIF":4.5,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143104832","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}