Journal of pharmaceutical sciences最新文献

{"title":"Response to the comment on \"Intranasal mucoadhesive chitosan microspheres of ranolazine: Formulation, design, and pharmacokinetic evaluation\".","authors":"Gyati Shilakari Asthana, Shilpa V, B Geethika Reddy, Abhay Asthana, Sri Rupa Bhoomika Satti","doi":"10.1016/j.xphs.2026.104446","DOIUrl":"10.1016/j.xphs.2026.104446","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104446"},"PeriodicalIF":3.9,"publicationDate":"2026-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148648563","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":"Comment on \"Intranasal Mucoadhesive Chitosan Microspheres of Ranolazine: Formulation, Design, and Pharmacokinetic Evaluation\".","authors":"Sagar Nanasaheb Kharde, Prasad Laxman Gorde, Sandip Gangadhar Laware","doi":"10.1016/j.xphs.2026.104445","DOIUrl":"https://doi.org/10.1016/j.xphs.2026.104445","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104445"},"PeriodicalIF":3.9,"publicationDate":"2026-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148648628","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":"Design of poly(jasmine lactone) micelles for enhanced delivery of remdesivir as a substitute for β-cyclodextrin formulations.","authors":"Jyoti Verma, Fanny Frejborg, Pekka Kolehmainen, Vishal Kumar, Carl-Eric Wilén, Kuldeep K Bansal, Jessica M Rosenholm","doi":"10.1016/j.xphs.2026.104431","DOIUrl":"10.1016/j.xphs.2026.104431","url":null,"abstract":"<p><p>Remdesivir (REM), a nucleoside analogue that has been approved for SARS-CoV-2 treatment, is poorly soluble in water and is currently administered intravenously formulated with sulfobutylether-β-cyclodextrin (SBECD) to facilitate solubilization. The major drawback associated with SBECD in the clinical setting is its high excipient load in the formulation leading to potential risk of renal accumulation, especially in patients with pre-existing impaired renal function and need of specialized staff trained in IV administration. The objective of this study was to investigate acid-functionalized poly(jasmine lactone) (PJL) based copolymers as potential alternatives to β-cyclodextrin based formulations for subcutaneous delivery of REM. PJL was selected because of its hydrophobic backbone and tunable functional group, making it more suited for hydrophobic interaction with REM. REM loaded PJL micelles were prepared utilizing nanoprecipitation technique and characterized for drug content, particle size, stability, in vitro release of REM, antiviral efficacy against human coronavirus HCoV-229E, pharmacokinetic profile and biodistribution in CD-1 mice. The thus prepared REM micelles exhibited a uniform nanoparticulate size with high loading efficiency of 96%, significant physicochemical stability at 4 °C up to 12 months and sustained REM release at pH 6.8 (≈ 100% in 24 h). The micelles demonstrated ≈ 100% inhibition against human coronavirus HCoV-229E, equivalent to the marketed formulation Jubi-R™ used for benchmarking. In vivo studies indicate increased systemic exposure and peak concentration of 217 ng/mL compared to 134 ng/mL after subcutaneous administration compared to marketed IV administration of micelles. The in vivo results also indicated an accumulation of the REM metabolite (GS-441524) in the lungs, demonstrating more targeted tissue distribution and production of active metabolites in vivo. Overall, these results provide evidence that PJL mediated micellar delivery of REM resulted in successful solubilization and delivery through a less invasive means of administration representing a promising biocompatible platform for delivering antiviral drug with improved systemic exposure.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104431"},"PeriodicalIF":3.9,"publicationDate":"2026-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148584642","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":"Elucidation of intermolecular interaction patterns in quaternary solid dispersion complexes of enzalutamide.","authors":"Shun Matsuzawa, Tatsuya Fukuta, Naoki Yoshihara, Mayumi Ikeda-Imafuku, Kazunori Kadota","doi":"10.1016/j.xphs.2026.104425","DOIUrl":"10.1016/j.xphs.2026.104425","url":null,"abstract":"<p><p>Enzalutamide (ENZ) is commercially formulated as an amorphous solid dispersion (ASD) using a single polymer. This study investigated an alternative multicomponent ASD for ENZ to expand formulation options beyond single-polymer systems. While individual polymers showed limited efficacy, a binary polymer system composed of amino alkyl methacrylate copolymer E (Eudragit E [EUD-E]) and hydroxypropyl cellulose (HPC) enhanced supersaturation. To further improve performance, saccharin (SAC), which is known to form a co-amorphous system with ENZ, was incorporated. Dissolution testing of the quaternary ASD prepared by hot-melt extrusion showed that adding SAC markedly improved supersaturation. Spectroscopic analyses suggested the formation of an organized quaternary interaction network rather than isolated pairwise interactions. HPC disrupted characteristic π-π stacking of ENZ molecules by steric hindrance. EUD-E, which forms ionic interactions with SAC, established additional hydrogen bonds with the amide moieties of ENZ. These sequential and synergistic interactions promoted the formation of a robust quaternary complex. Furthermore, we indicated that SAC relaxes the globular structure of EUD-E, thereby facilitating drug release in solution-state. Since the amide groups and aromatic π-electrons of ENZ are common in many pharmaceutical compounds, this multicomponent strategy offers a promising approach for improving the bioavailability of diverse poorly water-soluble drugs.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104425"},"PeriodicalIF":3.9,"publicationDate":"2026-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148471314","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":"Step-by-step optimization of a colchicine-loaded nanoemulgel for superior topical therapy of acute gouty arthritis.","authors":"Jian Zhang, Xiaqian Xu, Anqi Zhu, Jie He, Guangrui Liu, Ting Cui, Yanna Lin, Yijing Wang, Guisen Zhang, Chao Hao","doi":"10.1016/j.xphs.2026.104415","DOIUrl":"https://doi.org/10.1016/j.xphs.2026.104415","url":null,"abstract":"<p><p>A colchicine-loaded nanoemulgel (COL-nEMG) was developed for rapid and potent topical therapy of acute gouty arthritis (AGA). An O/W COL-loaded nanoemulsion (COL-nEMS, 14.20 ± 1.73 nm) was first prepared and optimized step by step, including excipient screening, pseudo-ternary phase diagram, in vitro transdermal delivery and D-optimal design. The optimized COL-nEMS containing 10% isosorbide dimethyl ether (DMI) was then dispersed into a gel matrix to produce the final COL-loaded nanoemulgel (COL-nEMG-DMI10). COL-nEMG-DMI10 exhibited a homogeneous appearance, favorable rheological properties, stable three-dimensional porous structure, and good storage stability with a steady-state transdermal flux of 54.6 ± 3.7 µg/cm²/h and 8 h cumulative permeation amount of 425.6 ± 28.3 µg/cm². In an AGA mouse model, COL-nEMG-DMI10 demonstrated rapid therapeutic effects with joint swelling inhibition rate (JSIR) of 37.0 ± 3.4% and maximum possible effect of 37.5 ± 5.3% at 1 h post-administration. In addition, COL-nEMG-DMI10 significantly suppressed the levels of local inflammatory cytokines, including TNF-α and IL-1β, in the ankle joints of AGA animals. This COL-nEMG-DMI10 topical formulation provides a promising treatment strategy for AGA with rapid and pronounced therapeutic efficacy.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104415"},"PeriodicalIF":3.9,"publicationDate":"2026-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148430618","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":"Editorial Advisory Board","authors":"","doi":"10.1016/S0022-3549(26)00231-5","DOIUrl":"10.1016/S0022-3549(26)00231-5","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104382"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148693991","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":"Enhancing transdermal drug delivery with dissolving microneedles: A review of optimization strategies and challenges","authors":"Zixuan Zhang,&nbsp;Yongbing Sun,&nbsp;Haocheng Li,&nbsp;Jianfang Feng,&nbsp;Meng Cheng,&nbsp;Liangxing Tu","doi":"10.1016/j.xphs.2026.104189","DOIUrl":"10.1016/j.xphs.2026.104189","url":null,"abstract":"<div><div>Microneedles represent a novel transdermal drug delivery technology that relies on micron-sized needle structures. This approach effectively penetrates the stratum corneum to achieve localized or systemic therapeutic effects, addressing the pain associated with traditional injections and the low bioavailability issues of oral administration. It addresses the pain associated with traditional injections and the low bioavailability of oral administration. Dissolving microneedles have emerged as a research hotspot in microneedle technology due to their distinctive advantages, including dissolvability, ease of operation, and absence of sharp waste. They have garnered widespread attention and application in the pharmaceutical field as an efficient means to enhance transdermal drug absorption. However, many drugs (particularly poorly soluble ones) require higher transdermal absorption enhancement factors, which traditional dissolving microneedles struggle to meet. In light of this, this paper will compare dissolving microneedles with other types of microneedles, propose optimization strategies for dissolving microneedle technology, discuss existing challenges, and outline future research directions, aiming to provide valuable references for the further development of dissolving microneedles.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104189"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146132002","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":"Mechanistic dermal patch modelling for fentanyl: Linking in vitro release and permeation data to a physiologically based pharmacokinetic approach","authors":"Daniel Paterson,&nbsp;Yanling Zhang,&nbsp;Sebastian Polak,&nbsp;James F. Clarke","doi":"10.1016/j.xphs.2026.104217","DOIUrl":"10.1016/j.xphs.2026.104217","url":null,"abstract":"<div><div>Dermal physiologically based pharmacokinetic (PBPK) models can be informed by various types of data. <em>In vitro</em> permeation testing (IVPT) experiments aid parameterisation of skin permeation independent of the complexities of systemic uptake. <em>In vitro</em> release testing (IVRT) studies isolate the formulation parameters by utilising a synthetic membrane. Leveraging this data in dermal PBPK model development, via an IVRT - IVPT - <em>in vivo</em> (IVIVIV) workflow, can reduce identifiability issues arising from concurrent parameterisation of formulation and skin permeation, or fitting directly to clinical data. In this work, three fentanyl matrix patch formulations were modelled with this approach using the Simcyp MPML MechDermA simulator. Mechanistic patch models were developed for each of the three different formulations, using IVRT data to parameterise formulation differences. These formulation models were coupled to a fentanyl skin absorption model in Simcyp’s IVPT Module to simulate IVPT data. The resulting model each formulation was used to extrapolate and predict <em>in vivo</em> application, with validation against clinical data. A virtual bioequivalence study was conducted to investigate bioequivalence given differing geometries and characteristics. A validated fentanyl patch model was used to predicted plasma profiles for patches that suffered manufacturing defects, as a risk assessment exemplifying PBPK model utilisation.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104217"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147307052","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":"Richard H. Guy—He has skin in the game","authors":"Russell O. Potts","doi":"10.1016/j.xphs.2025.104130","DOIUrl":"10.1016/j.xphs.2025.104130","url":null,"abstract":"<div><div>This article provides a review of the Potts-Guy equation and its impact on transdermal drug delivery. The equation has been widely cited and used over the past 30 years to predict delivery of a variety of molecules into the skin.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104130"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145756739","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":"Role of saturation dynamics in driving skin permeation from topical gel formulations","authors":"Srinath Rangappa,&nbsp;Srinivasa Ajjarapu,&nbsp;Vijay Kumar Shankar,&nbsp;Bharathi Avula,&nbsp;Anandavalli Varadarajan,&nbsp;Santanu Kundu,&nbsp;S. Narasimha Murthy","doi":"10.1016/j.xphs.2026.104349","DOIUrl":"10.1016/j.xphs.2026.104349","url":null,"abstract":"<div><div>The thermodynamic activity of an active pharmaceutical ingredient (API) is a key driver of permeation performance in topical formulations. This study investigated how solvent composition and evaporation impact the degree of saturation (DS) and skin permeation of three representative APIs: diclofenac sodium, metronidazole, and lidocaine. Model hydroxyethyl cellulose gels containing 1%, 10%, or 20% w/w Polyethylene Glycol (PEG-200) were prepared and characterized for solubility, pH, viscosity, and drying behavior. The solubility of all APIs increased with increasing PEG-200 concentration, whereas the DS varied correspondingly at a given drug load. Polystyrene substrate drying studies demonstrated that higher PEG-200 levels slowed solvent loss. The <em>in situ</em> drying studies on human cadaver skin using Franz cells enabled dynamic tracking of PEG-200 content and API saturation. Diclofenac sodium and lidocaine gels formulated with 1% PEG-200 showed progressively increasing DS over time and correspondingly higher permeation fluxes in in vitro permeation studies. In contrast, metronidazole gels showed little discrimination in DS and flux across PEG-200 concentrations, consistent with their hydrophilic nature and distinct solubility dynamics. The cumulative absorption confirmed a strong concordance between DS and permeation for diclofenac sodium and lidocaine, but not for metronidazole. Overall, the findings highlight that thermodynamic activity, modulated by solvent evaporation and shifts in solubility, governs the performance of topical formulations. These results underscore the value of monitoring DS profiles as predictive markers of drug delivery efficiency in topical product design.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104349"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148163633","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}