Journal of pharmaceutical sciences最新文献

{"title":"The Crux of vehicle designations: The essence of topical dermatologic vehicles and their use","authors":"Christian Surber,&nbsp;Michael E. Herbig,&nbsp;Daphne Reinau-Häberlin","doi":"10.1016/j.xphs.2025.104109","DOIUrl":"10.1016/j.xphs.2025.104109","url":null,"abstract":"<div><div>Topical therapies are essential in dermatology, accounting for over half of all prescriptions. These treatments are invaluable for managing various skin conditions due to their localized effect, ease of access and application, and generally favourable safety profiles. However, the diversity in vehicle designations to describe the topical preparations has led to confusion among healthcare professionals, patients and consumers. The challenges surrounding vehicle designations stem from a lack of universally accepted classifications and terminology, leading to widespread misconceptions about topical products. This paper examines and clarifies the complexities associated with vehicle designations. Key concepts discussed include the evolution of vehicle classifications, the role of vehicle components in affecting the bioavailability of active pharmaceutical ingredients, and the vehicle metamorphosis/transformation phenomenon that alters the product's formulation upon skin application. It is crucial to prioritize clinically relevant properties over designations. Understanding the relationship between product characteristics and clinical efficacy can help in the selection of appropriate treatments. Pharmaceutical qualities of the preparation (polarity, spreadability) and clinical qualities (skin condition, treatment area) should be considered, with the focus on empirical evaluation of products rather than on the designation of the vehicle. This is the only way to find the appropriate product vehicle in dialogue with the patients. It also emphasizes the importance of shared decision making in topical dermato-pharmacotherapy.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104109"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145634965","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":"What happens after you apply it to the skin? Evaporative metamorphosis and the transformation of critical quality attributes in topical products","authors":"S. Narasimha Murthy","doi":"10.1016/j.xphs.2025.104069","DOIUrl":"10.1016/j.xphs.2025.104069","url":null,"abstract":"<div><div>Topical dermatological formulations undergo profound compositional, physicochemical, and microstructural transformations upon application to the skin. This process, termed evaporative metamorphosis, alters critical quality attributes (CQAs) such as drug concentration, pH, viscosity, interfacial properties, phase distribution, substantivity, globule size, particle size, and solid-state behavior. These shifts, driven primarily by solvent evaporation, consequently, affect the dermal absorption of active pharmaceutical ingredients (API). This review systematically examines the foundational role of critical quality attributes (CQAs) in topical drug delivery and explores how evaporative metamorphosis affects these attributes at the site of application. A comprehensive understanding of the dynamic processes involved in the formulation at the applied site is crucial for the rational development of robust topical formulations that can maintain therapeutic performance throughout the metamorphosis phase and beyond.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104069"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145573978","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 melt-cast microneedle patch for sustained drug release of islatravir","authors":"Mikayla L. Rahman,&nbsp;Sijia Tao,&nbsp;Camryn P. Mekal,&nbsp;Gulcin Arslan Azizoglu,&nbsp;Raymond F. Schinazi,&nbsp;Mark R. Prausnitz","doi":"10.1016/j.xphs.2026.104256","DOIUrl":"10.1016/j.xphs.2026.104256","url":null,"abstract":"<div><div>Low adherence to daily oral drug regimens is a significant obstacle in effectively managing chronic therapies like HIV treatment, pre-exposure prophylaxis (PrEP), and contraception. While long-acting injectables eliminate the need for daily compliance, they often require administration by healthcare professionals. To facilitate self-administration of long-acting treatments, we developed a microneedle patch (MNP) for the sustained release of islatravir or levonorgestrel, used for HIV treatment/PrEP or contraception, respectively. The MNPs were produced using a melt-casting technique to quickly create biodegradable polycaprolactone microneedles for continuous drug delivery. The low melting point of polycaprolactone and the high thermal stability of islatravir and levonorgestrel allowed melt casting at 65 °C. Incorporating centrifugation during fabrication improved the attachment of microneedles to the patch backing, making it easier to remove MNPs from the mold and ensuring effective microneedle insertion into skin. The MNPs demonstrated a sustained release of islatravir with roughly first-order release kinetics for ∼40 days in vitro. We conclude that MNPs made with a simple melt-casting process can enable prolonged drug release for HIV treatment/PrEP, contraception, and other therapeutic applications.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104256"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147493582","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":"Relating plaque psoriasis barrier function changes with the underlying skin morphology and physiology","authors":"Sean E. Mangion,&nbsp;Joshua K. Dalton,&nbsp;James F. Clarke,&nbsp;Sebastian Polak,&nbsp;Eleftheria Tsakalozou,&nbsp;Karthika Natarajan,&nbsp;Shireen Sidhu,&nbsp;Warren Weightman,&nbsp;Lorraine Mackenzie,&nbsp;Michael S. Roberts","doi":"10.1016/j.xphs.2026.104320","DOIUrl":"10.1016/j.xphs.2026.104320","url":null,"abstract":"<div><div>The relationship between skin barrier function and the underlying morphological and physiological changes in disease states remains incompletely characterised. Improved understanding of these relationships is important for informing topical drug development, as disease-driven alterations may directly influence drug delivery at or near the site of action. This study characterised biophysical and structural properties of psoriatic skin in 28 patients with mild-to-severe psoriasis and compared these with measurements from 28 healthy participants. Assessed parameters included transepidermal water loss (TEWL), dermal blood flow, stratum corneum (SC) thickness, viable epidermal thickness, lower SC cell width, skin hydration, temperature, pH, and hair follicle density. Findings were subsequently contextualised against existing literature on skin structure and physiology in psoriasis. TEWL, a key indicator of barrier function, was significantly elevated in psoriatic lesions compared with healthy skin (12.84 vs. 7.14 g/m²/h, <em>P</em> = 0.0011). Lesional skin also demonstrated increased dermal blood flow (123.3 vs. 32.2 perfusion units, <em>P</em> &lt; 0.0001), SC thickness (3.5-fold), viable epidermal thickness (2.2-fold), and lower SC cell width (<em>P</em> &lt; 0.0001). In contrast, skin hydration was significantly reduced (16.7 vs. 102.0 µS, <em>P</em> &lt; 0.001), while elasticity, temperature, pH, and hair follicle density were not significantly different. Non-lesional skin largely resembled healthy skin across measured parameters. These results suggest that blood flow, viable epidermal thickness and SC dimensions are determinants of healthy and psoriatic skin TEWL driving potential differences in drug transport between psoriatic and healthy skin. The robust and comprehensive characterization of the skin barrier in healthy and diseased (lesional and non-lesional psoriatic skin) populations presented here is in agreement with existing literature providing insights on drug absorption and clinical effects in patients with psoriasis.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104320"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147930708","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":"A formal thank-you to my postdoctoral advisor, Richard H. Guy","authors":"Audra L. Stinchcomb","doi":"10.1016/j.xphs.2026.104339","DOIUrl":"10.1016/j.xphs.2026.104339","url":null,"abstract":"<div><div>This issue of the Journal of Pharmaceutical Sciences honors Richard H. Guy, Professor at the University of Bath. It is easy to look up his more than 400 peer-reviewed publications, research grants from multiple institutes and companies, patents for noninvasive biosensing, and many other scientific achievments. This commentary focuses on his mentorship, which has helped so many scientists continue to grow in their chosen career paths. He instilled entrepreneurial spirit, encouraged academic and industrial professional trajectories, and fostered an appreciation for the critical role of evidence-based regulatory science.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104339"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147988109","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 and evaluation of sorafenib and curcumin co-loaded microemulsion gel for the management of breast cancer","authors":"Md. Abul Barkat,&nbsp;Afaf F. Almuqati,&nbsp;Harshita Barkat,&nbsp;Abdulkareem Ali Alanezi,&nbsp;Faisal Shwaikh Alanazi,&nbsp;Lokesh Kaushik,&nbsp;Mahesh Kumar Sharma,&nbsp;Kaisar Raza","doi":"10.1016/j.xphs.2026.104310","DOIUrl":"10.1016/j.xphs.2026.104310","url":null,"abstract":"<div><div>In this study, sorafenib (an established anticancer drug) and curcumin (a polyphenolic compound), both with numerous challenges like solubility, permeation, bioavailability, and dose-dependent toxicity, were co‑loaded in a microemulsion-based hydrogel for breast cancer management by the topical route. Based on the solubility studies, Capmul MCM was selected as the oil, and the surfactant mixture was selected as Labrasol and Tween‑80. A total of three pseudoternary phase diagrams were explored to select the optimum composition. Out of three studied compositions, the selected one exhibited a globule size of 100.7 ± 6.83 nm with a polydispersity index value of 0.239, zeta potential of -8.14 ± 1.61 mV, and pH of 5.7 ± 0.2. The developed Carbopol-based hydrogel offered shear‑thinning rheology with appreciable spreadability, higher drug content, and skin-compatible pH. MCF‑7 cell-based cytotoxicity studies not only established the substantial decrease in the IC₅₀ values for both sorafenib and curcumin when co‑delivered but also offered a combination index &lt; 1, indicating synergism. Rodent skin permeation studies offered a higher release flux and drug retention for both the drugs <em>vis-à-vis</em> the conventional gel, and the dermatokinetics proved the skin delivery potential of the developed system with elevated C_max, permeation rates, and AUC, and also slower elimination for sorafenib. The studies established the synergism of both drugs and provided a proof of concept for enhanced topical delivery with substantial <em>in vitro</em> anticancer effect that can be further explored in the <em>in vivo</em> models.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 7","pages":"Article 104310"},"PeriodicalIF":3.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839378","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 \"Industry guidance on container closure integrity strategies for difficult-to-test parenteral products (DTPs)\".","authors":"Shweta Sharma, Talha Jawaid, Konda V V S Krishna","doi":"10.1016/j.xphs.2026.104340","DOIUrl":"https://doi.org/10.1016/j.xphs.2026.104340","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104340"},"PeriodicalIF":3.8,"publicationDate":"2026-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148005595","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":"Evaluating hemicellulose-API miscibility using melting point depression.","authors":"Tuomas Kilpeläinen, Riikka Laitinen","doi":"10.1016/j.xphs.2026.104329","DOIUrl":"10.1016/j.xphs.2026.104329","url":null,"abstract":"<p><p>To improve the solubility of poorly soluble APIs, amorphous solid dispersions (ASDs) are commonly employed. For an ASD to remain stable and effective, sufficient miscibility between the API and the polymeric carrier is essential. Although hemicelluloses possess several favourable attributes compared with commonly used synthetic polymers, they are not yet widely applied in pharmaceutical formulation research due to limited understanding of their behavior in pharmaceutical mixtures. In this study, we demonstrate that Flory-Huggins theory combined with melting point depression measurements can be used to estimate the miscibility between hemicelluloses and APIs. Based on these analyses, all three model APIs were found to be immiscible with both hemicelluloses. The resulting phase diagrams indicate that, at room temperature, only ASDs containing minimal API fractions would remain stable. This suggests that hemicelluloses may have a limited ability to form thermodynamically stable mixtures with lipophilic drugs. However, they may still be able to stabilize APIs in amorphous form and enhance dissolution properties through other mechanisms.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104329"},"PeriodicalIF":3.8,"publicationDate":"2026-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147960014","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":"Resolving drug release mechanisms of amorphous solid dispersions using optical coherence tomography.","authors":"Daniel Powell, Ecaterina Bordos, John Robertson, Jukka Rantanen, Daniel Markl","doi":"10.1016/j.xphs.2026.104300","DOIUrl":"10.1016/j.xphs.2026.104300","url":null,"abstract":"<p><p>This study presents an integrated approach utilising optical coherence tomography (OCT) to investigate the drug release mechanisms of hot-melt extruded (HME) amorphous solid dispersions (ASDs) of ritonavir and Soluplus®. Ritonavir-Soluplus® extrudates were prepared via HME using a twin-screw extruder and characterized during dissolution using a custom-designed 3D-printed flow cell, which enabled in-situ OCT imaging and continuous UV-vis monitoring of drug release. OCT provided high-resolution, time resolved visualization of structural transformations within the dissolving extrudates, while UV-vis spectroscopy quantified active pharmaceutical ingredient (API) release kinetics. Results revealed a multiphase dissolution mechanism involving sequential surface film formation, polymer swelling, delamination, and erosion. Increasing drug loading (10-30% w/w) produced marked effects on dissolution behaviour: formulations above 14% exhibited delayed release onset, extended swelling phases, and reduced overall release efficiency. OCT data showed that drug loadings above 14% led to slower erosion rates, greater swelling, and prolonged structural integrity, correlating with delayed UV-vis release profiles. Image processing using a machine learning segmentation model enabled quantitative extraction of sample cross-sectional area, confirming load-dependent swelling and erosion dynamics. Together, these findings establish a mechanistic link between structural evolution and release kinetics in HME ASDs and demonstrate the capability of OCT to provide real-time, non-destructive insight into solid dosage form dissolution. This methodology offers a powerful framework for optimizing ASD formulations and enhancing the predictive understanding of drug release mechanisms.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104300"},"PeriodicalIF":3.8,"publicationDate":"2026-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147816602","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":"Sericin and alginate loaded nanocomposite hydrogels for encapsulation and oral administration of insulin","authors":"Sania Faiz,&nbsp;Hafiz Muhammad Tahir,&nbsp;Rida Mahnoor,&nbsp;Aamir Ali,&nbsp;Ayesha Muzamil,&nbsp;Fariha Munir,&nbsp;Sidra Arshad,&nbsp;Fatima Ijaz,&nbsp;Ayesha Afzal,&nbsp;Farwa Shafique","doi":"10.1016/j.xphs.2026.104175","DOIUrl":"10.1016/j.xphs.2026.104175","url":null,"abstract":"<div><div>Diabetes mellitus is a major global health concern, with limited progress in the development of efficient oral insulin formulations. The current study was designed to assess the physicochemical, biochemical, and therapeutic efficiency of alginate and sericin loaded nanocomposites, which were developed as a protective oral delivery route for insulin. Ionic gelation was used to create the nanocomposites, which demonstrated excellent stability, controlled release, and high encapsulation efficiency in gastrointestinal simulations. Mice with alloxan induced diabetes were used for in-vivo evaluations. Insulin-loaded sericin-alginate nanocomposites administered orally for 21 days preserved body weight and significantly decreased fasting blood glucose levels as compared to the negative control. Blood glucose levels in the NC group increased gradually, from about 210 mg/dL to about 348 mg/dL, while 60 UI INS/60 kg reduced fasting blood glucose level from 220 mg/dL to 115 mg/dL. Significant improvements in liver and kidney function were evident by biochemical study, coupled with restored lipid profiles that showed higher HDL and lower levels of LDL, triglycerides, and cholesterol. Histological analysis revealed normal architecture of pancreatic and liver tissue in treatment groups similar to positive control. It can be concluded from the study that the sericin–alginate nanocomposites are safe, natural, and efficient oral insulin delivery method that can replace traditional subcutaneous injections.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 4","pages":"Article 104175"},"PeriodicalIF":3.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146086154","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}