Pharmaceutical Development and Technology最新文献_第7页

Synergistic combination of quercetin and kaempferol via milk exosome-based emulsion for enhanced antioxidant and anti-skin aging efficacy. 槲皮素和山奈酚通过乳外泌体乳液协同结合，增强抗氧化和抗皮肤衰老功效。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-03-01 Epub Date: 2026-02-27 DOI: 10.1080/10837450.2026.2635734

Xuemei Gu, Jie Wang, Jing Chen, Zhiyang Lv, Shaohua Wu, Bowen Li, Guanyu Liu, Xiaohui Wang, Tianye Qian, Yuhang Wu

{"title":"Synergistic combination of quercetin and kaempferol via milk exosome-based emulsion for enhanced antioxidant and anti-skin aging efficacy.","authors":"Xuemei Gu, Jie Wang, Jing Chen, Zhiyang Lv, Shaohua Wu, Bowen Li, Guanyu Liu, Xiaohui Wang, Tianye Qian, Yuhang Wu","doi":"10.1080/10837450.2026.2635734","DOIUrl":"10.1080/10837450.2026.2635734","url":null,"abstract":"The natural flavonoids quercetin (Que) and kaempferol (Kae) show great potential for anti-aging applications but suffer from poor solubility and skin permeability. This study aimed to develop a synergistic topical emulsion system to overcome the poor bioavailability of the Que and Kae for enhanced efficacy. The optimal synergistic molar ratio (Que:Kae = 1:2) was first identified via 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and cellular assays. The drugs were then loaded into milk-derived exosomes (mExo) using a Box-Behnken design (BBD), achieving high encapsulation (>69%), a size of ∼120 nm, and a polydispersity index (PDI) of 0.180. This complex was incorporated into an oil-in-water emulsion, with its formulation also BBD-optimized for stability. In a D-galactose-induced skin aging mouse model, the final Que/Kae-mExo@Eml formulation significantly outperformed control groups (free drug mixture, blank exosome emulsion, and vitamin C). It most effectively reduced oxidative stress (malondialdehyde, MDA), enhanced antioxidant enzymes (superoxide dismutase, SOD and glutathione, GSH), suppressed matrix metalloproteinase-1 (MMP-1), promoted collagen I (Col I) synthesis, and improved skin histology, elasticity, and hydration. In conclusion, an optimized, stable emulsion leveraging a synergistic 1:2 drug ratio and an mExo delivery system was successfully developed, demonstrating superior comprehensive efficacy against skin aging.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"464-480"},"PeriodicalIF":2.9,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147271521","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Zoomlab™-guided co-crystal engineering of nilotinib for improved dissolution. Zoomlab™引导尼罗替尼共晶工程改善溶解。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-03-01 Epub Date: 2026-02-04 DOI: 10.1080/10837450.2026.2624727

Rahul Jha, Arzoo Sekhani, Nikita Panchal, Pranav Shah

{"title":"Zoomlab™-guided co-crystal engineering of nilotinib for improved dissolution.","authors":"Rahul Jha, Arzoo Sekhani, Nikita Panchal, Pranav Shah","doi":"10.1080/10837450.2026.2624727","DOIUrl":"10.1080/10837450.2026.2624727","url":null,"abstract":"Nilotinib (NH), a second-generation tyrosine kinase inhibitor for chronic myelogenous leukemia (CML), exhibits poor aqueous solubility and low intestinal permeability, classifying it as a Biopharmaceutics Classification System (BCS) Class IV drug. This study aimed to enhance NH solubility and dissolution through co-crystallization, guided by computational and experimental approaches. BASF's ZoomLab™ platform was utilized for rational coformer selection using the solubility parameter difference (Δδv) method. Validation with paracetamol and posaconazole datasets established 5 MPa0.5 as the optimal Δδv threshold. Pyroglutamic acid (PG) emerged as the most suitable coformer and was co-crystallized with NH via liquid-assisted grinding (LAG). Solid-state characterization (PXRD, DSC, FTIR, SEM) confirmed formation of Nilotinib-Pyroglutamic acid co-crystal (NH-PGCC). The co-crystal displayed significantly improved wettability and a 3.23-fold increase in solubility in 0.1 N HCl compared to pure NH. Although rapid phase transformation occurred within 3 min, PEG 6K stabilized the supersaturated state, improving dissolution. The optimized NH-PGCC capsule achieved 75% drug release in 15 min, significantly outperforming marketed formulations (Tasigna® and Nilotirel®) and reduction of crystallinity was less than 2% in 6 months, suggesting stability of co-crystal. This study successfully demonstrates the applicability of ZoomLab™ in coformer prediction and formulation development for solubility enhancement of poorly soluble drugs.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"395-412"},"PeriodicalIF":2.9,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146113776","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Galactosylated bilosomes for liver-targeted delivery of ledipasvir: optimization, conjugate synthesis, and cellular evaluation. 半乳糖化胆小体用于肝靶向递送来地帕韦：优化，偶联合成和细胞评价。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-14 DOI: 10.1080/10837450.2025.2611896

Zeinab Hassan Gaafar, Suzan Fangary, Ahmed K B A W Farouk, Ahmed M Fatouh

{"title":"Galactosylated bilosomes for liver-targeted delivery of ledipasvir: optimization, conjugate synthesis, and cellular evaluation.","authors":"Zeinab Hassan Gaafar, Suzan Fangary, Ahmed K B A W Farouk, Ahmed M Fatouh","doi":"10.1080/10837450.2025.2611896","DOIUrl":"10.1080/10837450.2025.2611896","url":null,"abstract":"Ledipasvir is one of the direct-acting antiviral agents used for treating hepatitis C virus (HCV) infection. To achieve dose reduction and cost-effective therapy, this study aimed to enhance the interaction of ledipasvir with HCV-infected hepatocytes through the development of cationic bilosomes (CBs) and galactosylated bilosomes (GBs). These delivery systems were designed to promote hepatocellular targeting via the asialoglycoprotein receptors (ASGPRs). Eight bilosomal formulations were developed by the ethanol injection method following a 2³ full factorial design, and numerical optimization using Design Expert® software identified the optimized formulation. In parallel, galactosylated stearylamine (GSA) was synthesized through conjugation of stearylamine (SA) with lactobionic acid (LB). The successful synthesis of GSA was verified through FTIR and 1H NMR spectroscopic analyses. SA and GSA were subsequently incorporated into the optimized bilosomes to obtain CBs and GBs, respectively. The prepared systems were evaluated for particle size, polydispersity index, entrapment efficiency, and zeta potential, and their morphology was identified using transmission electron microscopy. Following 8-h incubation with HepG2 cells, CBs and GBs achieved significantly higher cumulative cellular uptake of ledipasvir (31.79% ± 3.11% and 20.62% ± 2.12%, respectively) compared to the ledipasvir free dispersion (11.02% ± 3.02%). These findings highlight CBs and GBs as promising nanocarriers for targeted delivery of ledipasvir to hepatocytes.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"199-210"},"PeriodicalIF":2.5,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145912624","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

In vitro antifungal and antibiofilm evaluation of reduction-responsive ketoconazole-loaded nanoparticles based on cystamine-modified poly (isobutene-alt-maleic anhydride) polymer. 基于半胺修饰的聚异丁烯-马来酸酐聚合物的负载还原响应酮康唑纳米颗粒的体外抗真菌和抗膜评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-12 DOI: 10.1080/10837450.2026.2615155

Fuyou Wang, Qingmin Liu, Wenhui Wu, Yuxiao Su, Zhimei Song, Runliang Feng

{"title":"In vitro antifungal and antibiofilm evaluation of reduction-responsive ketoconazole-loaded nanoparticles based on cystamine-modified poly (isobutene-alt-maleic anhydride) polymer.","authors":"Fuyou Wang, Qingmin Liu, Wenhui Wu, Yuxiao Su, Zhimei Song, Runliang Feng","doi":"10.1080/10837450.2026.2615155","DOIUrl":"10.1080/10837450.2026.2615155","url":null,"abstract":"Purpose: In order to develop reduction-responsive nano-drug delivery system for encapsulating antifungal drugs.Methods: Herein, with poly (isobutene-alt-maleic anhydride) as skeleton, we synthesized a polymer containing cross-linked disulfide bonds to prepare reduction-responsive ketoconazole-loaded nanoparticles (MPEG-P-KET). The in vitro reduction-responsive behavior and antifungal activity of MPEG-P-KET were investigated.Results: The MPEG-P-KET improved the dispersion and solubility of lipophilic KET. KET's imidazole group formed a salt with the free carboxyl groups in the polymer carrier, resulting in delayed drug release from MPEG-P-KET. However, MPEG-P-KET still exhibited reduction-sensitive drug release behavior, and showed comparable antifungal activity with KET in vitro. Interestingly, MPEG-P-KET demonstrated higher ability to inhibit biofilm formation and disrupt mature biofilms than KET.Conclusion: The polymeric nanoparticles with disulfide bonds could be used for the encapsulation and controlled delivery of antifungal drugs in the field of fungal infection treatment.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"253-266"},"PeriodicalIF":2.9,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145934347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Fabrication and evaluation of felodipine push-pull osmotic pump capsule. 非洛地平推拉式渗透泵胶囊的制备与评价。

IF 2.5 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-18 DOI: 10.1080/10837450.2025.2608713

Chaowalit Monton, Poj Kulvanich

{"title":"Fabrication and evaluation of felodipine push-pull osmotic pump capsule.","authors":"Chaowalit Monton, Poj Kulvanich","doi":"10.1080/10837450.2025.2608713","DOIUrl":"10.1080/10837450.2025.2608713","url":null,"abstract":"Felodipine is traditionally delivered as extended-release tablets, but a push-pull osmotic pump (PPOP) capsule represents a promising alternative platform for controlled-release delivery. This work sought to characterize properties of the felodipine drug substance and crosslinked hard gelatin capsules (HGCs) for the preparation of the PPOP capsule. Additionally, drug release profiles of felodipine PPOP capsules under various formulation and medium conditions were investigated. Felodipine drug substances and crosslinked HGCs were evaluated for their physicochemical properties. Moreover, the type of release medium, number of Corelease CA coating rounds, amounts of Polyox WSR N80 and Polyox WSR Coagulant, sodium chloride content, and source of the drug substance were studied. Results showed that the physicochemical properties of felodipine drug substances exhibited statistically significant but minor variations between the two sources. Crosslinked HGCs remained insoluble in all tested media and exhibited spectral changes consistent with formaldehyde-induced crosslinking. Drug release approached Higuchi's kinetics when the formulation comprised 10 mg felodipine from a specific manufacturer, 120 mg of Polyox WSR N80, 35 mg of Polyox WSR Coagulant, and 20 mg of sodium chloride, with 10 coating rounds of Corelease CA and 1% sodium lauryl sulfate as the release medium. In conclusion, these findings highlight the significant influence of formulation parameters on drug-release behavior and provide a basis for developing PPOP capsules with consistent and predictable performance.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"183-198"},"PeriodicalIF":2.5,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145820394","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Hydrogel nanoparticles of retinol acetate via modified rapid expansion of supercritical solution: design, optimization, and anticancer evaluation. 超临界溶液快速膨胀法制备醋酸视黄醇纳米水凝胶：设计、优化和抗癌评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-12 DOI: 10.1080/10837450.2026.2614360

Milind Velhal, Jyotiram Sawale

{"title":"Hydrogel nanoparticles of retinol acetate via modified rapid expansion of supercritical solution: design, optimization, and anticancer evaluation.","authors":"Milind Velhal, Jyotiram Sawale","doi":"10.1080/10837450.2026.2614360","DOIUrl":"10.1080/10837450.2026.2614360","url":null,"abstract":"Polymeric nanoparticles are promising drug carriers due to their biocompatibility, sustained release, and improved therapeutic efficacy; however, conventional fabrication methods often suffer from broad size distribution, low encapsulation efficiency, and instability. To address these limitations, Sonication Assisted Particle Production using Supercritical Solution (SAPSS®), a modified RESS technique integrating ultrasonication and mechanical mixing, was developed to prepare and optimize HPMC K-100M hydrogel nanoparticles encapsulating retinol acetate using DOE, RSM, and ANOVA. The optimized formulation (retinol acetate: HPMC K-100M, 1:1 w/w) produced at 290 bar and 75 °C for 45 min with 1% Tween 80 yielded nanoparticles of 138.6 ± 1 nm, PDI 0.583 ± 0.03, zeta potential -14.9 ± 2.0 mV, encapsulation efficiency 99.02 ± 0.2%, and yield 66.4 ± 0.3%. FTIR, DSC, and XRD confirmed amorphous encapsulation and drug-polymer interactions, while SEM demonstrated spherical, discrete morphology. In vitro release studies revealed sustained drug release across physiological pH, with mucoadhesive strength supporting gastrointestinal retention. Cytotoxicity assays on COLO-205 cells, doxorubicin showed >90% cytotoxicity, free retinol acetate caused only 10-25% cell death, while HPMC-encapsulated retinol acetate nanoparticles produced enhanced, dose-dependent cytotoxicity of 25%, 35%, and 55% at 100, 200, and 300 µg/mL, respectively, with negligible toxicity from blank HPMC. Overall, SAPSS® provides a green, scalable approach for fabricating stable therapeutic nanoparticles.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"233-252"},"PeriodicalIF":2.9,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145948940","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Clobetasol propionate loaded nanostructured lipid carrier gel: formulation strategy and in vitro performance evaluation. 负载丙酸氯倍他索纳米结构脂质载体凝胶的制备策略及体外性能评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-21 DOI: 10.1080/10837450.2026.2615158

Mine Diril, Esra Karataş, H Yeşim Karasulu

{"title":"Clobetasol propionate loaded nanostructured lipid carrier gel: formulation strategy and in vitro performance evaluation.","authors":"Mine Diril, Esra Karataş, H Yeşim Karasulu","doi":"10.1080/10837450.2026.2615158","DOIUrl":"10.1080/10837450.2026.2615158","url":null,"abstract":"Clobetasol propionate (CP) is a potent Class I corticosteroid widely used to treat dermatological conditions; however, its poor aqueous solubility limits bioavailability. In this study, a nanostructured lipid carrier (NLC)-based gel was developed via the microemulsion method to improve the topical delivery of CP. The formulation was optimized using stearic acid (solid lipid), Captex 300 (liquid lipid), Tween 20 and Span 80 (surfactants), and propylene glycol (co-surfactant), based on solubility and thermodynamic stability assessments. Vitamin E acetate was incorporated as an antioxidant to inhibit lipid oxidation and enhance formulation stability. The optimized CP-NLC (F5) formulation had a particle size of 75.96 ± 4.87 nm, a zeta potential of -23.88 ± 4.10 mV, and a polydispersity index (PDI) of 0.27 ± 0.11. Encapsulation efficiency was 93.72 ± 0.26%, and drug loading reached 100.69 ± 0.62%. Transmission electron microscopy (TEM) confirmed spherical morphology. The gel (CP-NLC-F5-G) prepared with Carbopol 934 demonstrated a pH of 5.58 ± 0.68 and drug content uniformity of 99.03 ± 1.18%. In vitro release studies using Franz diffusion cells revealed sustained CP release compared to a commercial product. Stability studies indicated long-term encapsulation retention, attributed to the antioxidant effect of Vitamin E acetate. These findings suggest the potential of CP-NLC systems for effective, sustained corticosteroid delivery with enhanced dermal retention.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"267-281"},"PeriodicalIF":2.9,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146011688","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanostructured lipid nanoparticles delivering berberine with Se coating: a new nanotherapeutic approach against cryptosporidiosis. 纳米结构脂质纳米颗粒递送带有Se涂层的小檗碱：一种新的治疗隐孢子虫病的纳米方法。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-27 DOI: 10.1080/10837450.2026.2620476

Areej Eskandrani, Sara H Akl, Yahya H Shahin, Bassma H Elwakil, Keshav Raj Paudel, Amira Abd-Elfattah Darwish, Esraa A Moneer

{"title":"Nanostructured lipid nanoparticles delivering berberine with Se coating: a new nanotherapeutic approach against cryptosporidiosis.","authors":"Areej Eskandrani, Sara H Akl, Yahya H Shahin, Bassma H Elwakil, Keshav Raj Paudel, Amira Abd-Elfattah Darwish, Esraa A Moneer","doi":"10.1080/10837450.2026.2620476","DOIUrl":"10.1080/10837450.2026.2620476","url":null,"abstract":"Berberine (BBR) exhibits broad antimicrobial and metabolic activities but suffers from limited bioavailability. Nanostructured lipid carriers (NLCs) can enhance oral delivery, while selenium (Se) coating may synergistically improve hypoglycemic and antiparasitic effects. This study aimed to design and evaluate the selenium-doped, berberine-loaded nanostructured lipid carriers (BBR-SeNLCs) for enhanced absorption, tissue diffusion, and antiparasitic efficacy against Cryptosporidium parvum in an immunosuppressed mouse model. BBR-SeNLCs were prepared via hot-melt dispersion/homogenization, followed by in situ reduction to deposit elemental selenium on the nanoparticle surface. A Cryptosporidium murine infection model was established. Parasitological burden (oocyst shedding), biochemical markers (ALT and AST), immunological parameters (IFN-γ, TNF-α, IL-6, and IL-10), and TEM ultrastructure of intestinal tissues were assessed. BBR-SeNLCs demonstrated successful berberine encapsulation. Among treatments, BBR-SeNLCs achieved comparable antiparasitic effects, with a notable reduction in oocyst shedding relative to infected controls. Biochemical assays indicate formulation-dependent hepatoprotective trends, particularly in BBR-SeNLCs formulations. Immunologically, Se-containing groups (Se alone and BBR-SeNLCs) displayed a shift toward moderated inflammatory responses (reduced IFN-γ, TNF-α, IL-6) with preserved or enhanced anti-inflammatory IL-10, suggesting balanced host immunity. Parasitological and ultrastructural analyses corroborated these findings, with BBR-SeNLCs showing preserved intestinal architecture and reduced parasite burden in treated groups.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"324-337"},"PeriodicalIF":2.9,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146019027","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A critical comparative insight on nanocarrier-based intranasal delivery of statins for neuroprotective applications. 基于纳米载体的他汀类药物鼻内递送用于神经保护应用的关键比较见解。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-23 DOI: 10.1080/10837450.2026.2614071

Ravi Paruparla, Manisha Lalan, Pranav Shah, Nupur Vasdev

{"title":"A critical comparative insight on nanocarrier-based intranasal delivery of statins for neuroprotective applications.","authors":"Ravi Paruparla, Manisha Lalan, Pranav Shah, Nupur Vasdev","doi":"10.1080/10837450.2026.2614071","DOIUrl":"10.1080/10837450.2026.2614071","url":null,"abstract":"The incidence of central nervous system (CNS) disorders is rising globally, particularly as the prevalence of neurodegenerative diseases increases. The primary challenge in such cases is limited transport of therapeutics through the blood-brain barrier (BBB). Statins, widely used for hypercholesterolemia, exhibit pleiotropic neuroprotective effects; however, their therapeutic potential in CNS disorders is restricted by poor brain bioavailability with conventional routes. Intranasal (IN) delivery has long been recognized as a plausible pathway for brain targeting. This narrative review critically examines preclinical literature on IN nanocarrier-based delivery systems developed specifically for statins, with emphasis on nose-to-brain transport, formulation strategies, pharmacokinetics (PK), and neuroprotective outcomes. This work uniquely integrates a formulation-centric comparison of IN nanocarriers for statins. It highlights the potential of IN delivery, discussing the influence of carrier type, physicochemical properties, and delivery strategy on brain targeting efficiency and therapeutic relevance across different neurological indications. IN nanocarrier systems display potential to enhance statin brain delivery by bypassing the BBB and first-pass metabolism. Nevertheless, current evidence is predominantly preclinical, with significant variability in study design, pharmacokinetic reporting, and safety evaluation. Translation to clinics will require standardized nose-to-brain metrics, long-term safety studies, scalable manufacturing processes, and early regulatory alignment.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"211-232"},"PeriodicalIF":2.9,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145960068","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Morin-loaded water-soluble nanomicelles as a novel anti-alcohol intoxication medication. 一种新型抗酒精中毒药物-含桑酸水溶性纳米胶束。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-02-01 Epub Date: 2026-01-16 DOI: 10.1080/10837450.2026.2617346

Chuanxu Luo, Linlin Zhao, Yu Chen, Xiaoyuan Liu, Jiamin Mao, Jing Ye, Lie Zhang, Yucheng Xiang, Xiaohong Xu, Xi Fu, Quan Zhang

{"title":"Morin-loaded water-soluble nanomicelles as a novel anti-alcohol intoxication medication.","authors":"Chuanxu Luo, Linlin Zhao, Yu Chen, Xiaoyuan Liu, Jiamin Mao, Jing Ye, Lie Zhang, Yucheng Xiang, Xiaohong Xu, Xi Fu, Quan Zhang","doi":"10.1080/10837450.2026.2617346","DOIUrl":"10.1080/10837450.2026.2617346","url":null,"abstract":"Acute alcohol intoxication (AAI) poses serious health risks. Currently, no approved therapy effectively treats both CNS depression and tissue damage in AAI. Standard care, including supportive measures and off-label naloxone, manages respiratory depression but fails to prevent oxidative organ injury. We identified morin (MOR) as a promising candidate for addressing these challenges. Given that MOR is limited by poor water solubility and low oral bioavailability, we developed water-soluble nano-micelle formulations (MOR-Ms) using Kolliphor HS15 (HS15) as a surfactant for intravenous administration. The resulting MOR-Ms exhibited a uniform size of 13.84 ± 0.23 nm and a zeta potential of -9.99 ± 0.21 mV. In vivo, MOR-Ms accelerated alcohol metabolism by enhancing hepatic enzyme activity. In an AAI mouse model induced by intraperitoneal injection of 50% alcohol (10 ml/kg), MOR-Ms (3 mg/kg) significantly shortened the duration of loss of righting reflex (LORR) by 58.01%, which was comparable to the 67.83% reduction achieved by naloxone (1 mg/kg). Furthermore, MOR-Ms markedly lessened tissue damage by decreasing malondialdehyde (MDA) levels (by 32.01% in liver and 53.75% in brain compared to the model group) and boosting antioxidant enzyme activity. These results highlight the potential of MOR-Ms as a promising therapeutic approach for AAI.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"282-293"},"PeriodicalIF":2.9,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145966300","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0