RSC Pharmaceutics最新文献

{"title":"Comparative analysis of the inhibitory effects of aloin on tyrosinase supported by Fe3O4@rGO: investigation of interaction mechanisms, inhibitory activity, and conformational changes†","authors":"Zhu Wang, Lu Chen, Jing Yuan, Qiulan Zhang and Yongnian Ni","doi":"10.1039/D5PM00067J","DOIUrl":"https://doi.org/10.1039/D5PM00067J","url":null,"abstract":"<p >Tyrosinase is a key enzyme that regulates the rate of melanin synthesis, thereby modulating both food browning and skin pigmentation. It has been found that aloin is an effective inhibitor of tyrosinase activity and Fe<small>₃</small>O<small>₄</small>@rGO has remarkable drug-loading capability. In this study, enzyme inhibition kinetics and multispectral techniques were employed to investigate the enzyme inhibitory effect of Fe<small>₃</small>O<small>₄</small>@rGO-aloin nanocomposites and evaluate their anti-browning effect and safety. The binding ability of tyrosinase and aloin was further enhanced by the addition of Fe<small>₃</small>O<small>₄</small>@rGO. The IC<small>₅₀</small> value of Fe<small>₃</small>O<small>₄</small>@rGO-aloin against tyrosinase was determined to be 2.26 ± 0.15 × 10<small>⁻⁵</small> mol L<small>⁻¹</small> with a typical anticompetitive inhibition. The findings suggest that Fe<small>₃</small>O<small>₄</small>@rGO-aloin exhibits a more potent inhibitory effect on tyrosinase compared to aloin. Furthermore, three-dimensional fluorescence, Fourier transform infrared and circular dichroism experiments demonstrated that aloin-loaded Fe<small>₃</small>O<small>₄</small>@rGO nanoparticles induce alterations in the secondary structure and conformation of tyrosinase. This indicates the potential of Fe<small>₃</small>O<small>₄</small>@rGO nanocomposites as candidates for the development of novel tyrosinase inhibitors for the treatment of hyperpigmentation disorders.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 1110-1124"},"PeriodicalIF":0.0,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d5pm00067j?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145073544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Glivec to generic imatinib switch: in vitro comparative dissolution assessment, bioequivalence, safety, and tolerability of 400 mg imatinib tablets in healthy volunteers","authors":"Samir Das, Saurav Sarkar, Ranabir Sahu, Tarun Kumar Dua, Paramita Paul and Gouranga Nandi","doi":"10.1039/D5PM00099H","DOIUrl":"https://doi.org/10.1039/D5PM00099H","url":null,"abstract":"&lt;p &gt;Imatinib is currently considered the “gold standard” pharmacotherapy for chronic myelogenous leukemia (CML) at all stages and is most commonly used in the form of tablets taken orally. The aim of the present study was to perform a quality assessment, bioequivalence study, and safety and tolerability assessment of an investigational test product, imatinib tablets (400 mg), and its comparability with a reference product (Glivec tablets, 400 mg). &lt;em&gt;In vitro&lt;/em&gt; dissolution studies of the test and reference products were conducted in three different buffer media (pH 1.2, pH 4.5, and pH 6.8) using Apparatus II (paddle), and the results were compared. The similarity (&lt;em&gt;f&lt;/em&gt;&lt;small&gt;&lt;sub&gt;2&lt;/sub&gt;&lt;/small&gt;) factor was calculated to assess &lt;em&gt;in vitro&lt;/em&gt; bioequivalence requirements. An open-label, balanced, randomized, two-treatment, two-sequence, two-period, single oral dose, crossover, bioequivalence study was conducted in normal, healthy, adult human subjects under fed conditions. The pharmacokinetic parameters &lt;em&gt;T&lt;/em&gt;&lt;small&gt;&lt;sub&gt;max&lt;/sub&gt;&lt;/small&gt;, &lt;em&gt;C&lt;/em&gt;&lt;small&gt;&lt;sub&gt;max&lt;/sub&gt;&lt;/small&gt;, AUC&lt;small&gt;&lt;sub&gt;0–&lt;em&gt;t&lt;/em&gt;&lt;/sub&gt;&lt;/small&gt;, and AUC&lt;small&gt;&lt;sub&gt;0–∞&lt;/sub&gt;&lt;/small&gt; were calculated through a non-compartmental model using Phoenix WinNonlin Version 8.3 (Certara L.P.) software. Statistical evaluation and comparison of the two formulations were carried out using PROC GLM in SAS version 9.4 (SAS Institute Inc., USA). The safety profile of the investigational product was monitored during the study by applying a clinical process for recording observed untoward effects post-administration of the investigational product. The investigational test product met USP and BP pharmacopoeial quality standards for &lt;em&gt;in vitro&lt;/em&gt; dissolution. Very rapid dissolution (&gt;85% release in 15 minutes) was obtained for the reference and test products in all three buffered dissolution media (pH 1.2, pH 4.5, and pH 6.8) in &lt;em&gt;in vitro&lt;/em&gt; dissolution studies. The dissolution profile of the investigational test product (imatinib tablets, 400 mg) was comparable to that of the reference product (Glivec tablets, 400 mg). Furthermore, pharmacokinetic values (&lt;em&gt;C&lt;/em&gt;&lt;small&gt;&lt;sub&gt;max&lt;/sub&gt;&lt;/small&gt;, &lt;em&gt;T&lt;/em&gt;&lt;small&gt;&lt;sub&gt;max&lt;/sub&gt;&lt;/small&gt;, and AUC) of the test and reference forms of imatinib were similar. Geometric mean ratios (test/reference) for the AUC&lt;small&gt;&lt;sub&gt;0–∞&lt;/sub&gt;&lt;/small&gt;, AUC&lt;small&gt;&lt;sub&gt;0–&lt;em&gt;t&lt;/em&gt;&lt;/sub&gt;&lt;/small&gt;, and &lt;em&gt;C&lt;/em&gt;&lt;small&gt;&lt;sub&gt;max&lt;/sub&gt;&lt;/small&gt; were 95.2, 0.95.2, and 98.4, respectively. Confidence limits for each of these parameters were in the interval (80.00, 125.00), as were the unadjusted confidence limits. The test and reference formulations of imatinib met the criteria for bioequivalence based on the rate and extent of absorption. Based on the findings of this study, it can be concluded that the test product is bioequivalent and safe, thus suggesting the clinical application of the test product as an alternative to Glivec 400 mg film-c","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 807-813"},"PeriodicalIF":0.0,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d5pm00099h?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144624154","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and preliminary evaluation of cardiac imaging with [68Ga]Ga-NOTA-CTP in normal and infarcted CD1 mice†","authors":"Surendra Reddy Gundam, Manasa Kethamreddy, Andy González Rivera, Aditya Bansal, Viktoria Krol, Daniella A. Sahagun, Joanna E. Kusmirek, Derek R. Johnson, Maliha Zahid, Val J. Lowe and Mukesh K. Pandey","doi":"10.1039/D5PM00047E","DOIUrl":"https://doi.org/10.1039/D5PM00047E","url":null,"abstract":"<p >Cell-penetrating peptide-based probes for positron emission tomography (PET) are currently being developed for cardiac imaging. Herein, we have conjugated a synthetic 12 amino acids (NH<small>₂</small>-APWHLSSQYSRT-COOH) cardiac targeting peptide (CTP) with a NOTA chelator for <small>⁶⁸</small>Ga labeling. The [<small>⁶⁸</small>Ga]Ga-NOTA-CTP was synthesized with a decay-corrected radiochemical yield of 68.9 ± 12.8% (<em>n</em> = 13) and molar activity (<em>A</em><small>_m</small>) of 1.3 ± 0.5 GBq per μmol (<em>n</em> = 13). The tracer was evaluated in healthy and diseased CD1 mice with myocardial infarction following ligation of the left anterior descending artery. PET/CT imaging and <em>ex vivo</em> biodistribution revealed rapid (within 30 min) clearance of [<small>⁶⁸</small>Ga]Ga-NOTA-CTP from the blood through renal and hepatobiliary excretion pathways in both healthy and infarcted animals. The uptake of [<small>⁶⁸</small>Ga]Ga-NOTA-CTP in the heart of healthy and infarcted animals did not show any statistically significant difference for up to 120 min post-injection, but regional differences within healthy and infarcted hearts were detected with [<small>⁶⁸</small>Ga]Ga-NOTA-CTP by PET/CT imaging at early time points post-injection. Within a healthy heart, the left ventricle standardized uptake value (SUV) was lower than the right ventricle SUV at 10–30 min post-injection. This regional difference between the left and right ventricles was absent in the infarcted heart, likely due to post-ligation changes.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 691-702"},"PeriodicalIF":0.0,"publicationDate":"2025-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d5pm00047e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144624142","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Outstanding Reviewers for RSC Pharmaceutics in 2024","authors":"","doi":"10.1039/D5PM90008E","DOIUrl":"https://doi.org/10.1039/D5PM90008E","url":null,"abstract":"<p >We would like to take this opportunity to thank all of <em>RSC Pharmaceutics</em>’ reviewers for helping to preserve quality and integrity in pharmaceutics literature. We would also like to highlight the Outstanding Reviewers for <em>RSC Pharmaceutics</em> in 2024.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 666-666"},"PeriodicalIF":0.0,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d5pm90008e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144624141","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Artificial intelligence in smart drug delivery systems: a step toward personalized medicine","authors":"Mitali Panchpuri, Ritu Painuli and Chetan Kumar","doi":"10.1039/D5PM00089K","DOIUrl":"https://doi.org/10.1039/D5PM00089K","url":null,"abstract":"<p >One of the most interesting applications of artificial intelligence is in the design of drug delivery systems. Smart drug delivery systems can transfer drugs to specific tissues and cells, enhancing therapeutic effects while reducing undesirable side effects. Attention is focused on the main concepts and techniques of AI such as machine learning, deep learning, and genetic algorithms. In addition to this, genetic algorithms can be used for the selection of the best numerical models, which are able to predict biological processes or optimize the activity of new drugs. Besides the powerful impact of AI on drug design, its combination with new biotechnologies for personalized medicine, sometimes called theragnostics, brings novel diagnostic tools together with targeted therapy, which could ensure quality and effectiveness during clinical research on new drugs. Artificial intelligence (AI) techniques are finding their application in almost all disciplines, with particular success in healthcare. AI-based algorithms can solve complex problems related to diagnosis, prediction, control, and prevention of diseases that are beyond the scope of human abilities. At the same time, the Internet of Things (IoT) revolution has added value to the healthcare sector. The resulting combination of IoT and AI platforms presents a promising fusion to provide healthcare delivery innovations like digital drug delivery, online healthcare consultancy platforms, and virtual healthcare assistants. Personalized medicine is well-suited, regardless of potential disadvantages, to creating drug delivery systems that can respond to the exact needs and other special requirements of patients. The development of smart drug delivery systems is a potential response to the unimodal properties of drugs and the discordance between patient requirements and patient outcomes achieved by currently prescribed medications. The potential and actual positive economic and health-related impacts of advanced drug delivery technologies have created strong demand for new advanced delivery forms.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 882-914"},"PeriodicalIF":0.0,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d5pm00089k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145073488","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimizing mesoporous silica synthesis procedures to enhance their potential as nanoplatforms in therapeutic applications†","authors":"Olia Alijanpourtolouti, Gamini Senanayake, Sulev Koks and David J. Henry","doi":"10.1039/D5PM00066A","DOIUrl":"https://doi.org/10.1039/D5PM00066A","url":null,"abstract":"<p >PARK7 mRNA encodes the DJ-1 protein, which functions as a protective agent against oxidative stress and cell damage within brain cells. Mutations in the mRNA can lead to reduced production of DJ-1 and initiate brain diseases such as Parkinson's disease. Transport of appropriate mRNA to damaged brain cells may provide a suitable treatment. Mesoporous silica nanoparticles (MSNPs), particularly pore-expanded and dye-labeled varieties, are regarded as potential carriers for large therapeutic agents such as mRNA. This study explored the influence of alterations in reaction conditions on the structural characteristics of MSNPs to produce nanoparticles with favorable characteristics for delivering large therapeutic agents to target sites. One-stage and two-stage procedures were compared for the introduction of 3-aminopropyltriethoxysilane (APTES) and an APTES−dye adduct, in conjunction with two different surfactants, cetyltrimethylammonium bromide (CTAB) and cetyltrimethylammonium chloride (CTAC). Analysis of the MSNPs shows that the two-stage method using CTAB as a surfactant produced amine-functionalized, dye-labelled particles with smaller overall size and better uniformity than the one-stage approach. However, due to their small pore size (&lt;10 nm), these particles were unable to encapsulate the PARK7 mRNA (926 nucleotides). The one-stage method <em>via</em> CTAC produced MSNPs with a large pore size (150 nm), broad pore distribution (10–20 nm), and high aggregation, limiting their suitability for brain-targeted gene delivery. In comparison, the two-stage method using CTAC yielded well-ordered MSNPs with an optimal size (80 nm) and pore diameters (15–20 nm), enabling effective encapsulation of the large PARK7 mRNA and offering strong potential for future brain gene therapy studies.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 792-806"},"PeriodicalIF":0.0,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d5pm00066a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144624153","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comprehensive physicochemical, biophysical, and in vitro characterization of lung surfactant SP-A peptidomimetics","authors":"David Encinas-Basurto, Priya Muralidharan, M. D. Saiful Islam, Ernest L. Vallorz, Stephen M. Black, Monica Kraft, Julie G. Ledford and Heidi M. Mansour","doi":"10.1039/D4PM00265B","DOIUrl":"10.1039/D4PM00265B","url":null,"abstract":"<p >Surfactant protein-A (SP-A) is an endogenous and essential lung surfactant-specific protein that is integral to pulmonary immunity, including inhibition of asthma exacerbations. This study aims to comprehensively characterize two peptides (10-AA and 20-AA) of SP-A which confer activity similar to the full-length oligomeric SP-A protein. Spectroscopic and chromatographic analyses revealed that the phosphate (PS) and acetate (AC) salts exhibited distinct solubility and log <em>P</em> partitioning behavior, impacting their physicochemical properties. MD simulations and circular dichroism showed that SP-A 10-AA initially adopts an α-helical structure but loses helicity over time, while SP-A 20-AA remains disordered. Differential scanning calorimetry confirmed variations in thermal stability between salt forms and zeta potential measurements showed that PS salts had a more negative surface charge, potentially influencing membrane interactions. <em>In vitro</em> studies showed high cell viability (&gt;90%) and stable TEER values at the air–liquid interface, confirming biocompatibility and potential epithelial permeability. These findings provide crucial insights into the structural and functional properties of SP-A peptides, supporting their potential as therapeutic agents for pulmonary diseases.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 731-748"},"PeriodicalIF":0.0,"publicationDate":"2025-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12053052/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144034200","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Calcium phosphate reinforced chitosan–carrageenan scaffolds: characterization and in vitro assessment for wound healing†","authors":"Vinita Patole, Gaurav Kavitkar, Ganesh Ingavle, Isha Behere, Ravindra Wavhale, Abhishek Jha, Sanjeevani Deshkar, Avinash Sanap and Pramod Sakpal","doi":"10.1039/D4PM00284A","DOIUrl":"https://doi.org/10.1039/D4PM00284A","url":null,"abstract":"<p >Wound healing is a multifaceted and dynamic biological process, which traditional wound dressings often fail to adequately support, leading to prolonged healing times. It would be highly beneficial to develop wound dressings with the ability to support biological processes such as cell proliferation and angiogenesis and deliver the active agents required to restore intracellular activities to promote wound healing. The current work aimed at developing a polyelectrolyte complex of chitosan (CH) and an anionic polymer, condensed with calcium phosphate (CaP) powder to attain antibacterial and angiogenic potential, cell proliferation, appropriate swelling index, and enhanced wound healing. Polyelectrolyte complexes (PECs) were formulated using chitosan (CH), as a cationic polymer and pectin (PE), sodium alginate (SA), and carrageenan (CA), respectively, as an anionic polymer through a lyophilization process. PEC formation was confirmed by FTIR, XRD, and DSC by observing the changes in their vibrational frequencies, structures, and thermal properties. SEM revealed the porous structure of the scaffolds. From the prepared PEC scaffolds, chitosan–carrageenan (CH-CA) was selected for further studies based on the swelling index, porosity, and degradation studies. Following the production of CaP powder using a microwave-assisted synthesis method, the powder was characterized by FTIR, SEM, XRD, and energy dispersive X-ray (EDX) techniques before being loaded onto CH-CA scaffolds. The results demonstrated approximately 60.75% release of calcium ions (Ca<small>⁺⁺</small>) from the CH-CA scaffolds in PBS, pH 5.5, as analysed by atomic absorption spectroscopy (AAS) over 24 h. The scaffolds demonstrated a higher swelling index and exhibited antimicrobial activity against <em>E. coli</em> and <em>S. aureus</em>. The scaffolds were found to be hemocompatible and demonstrated angiogenic potential, evidenced by stimulating new blood vessel development in a chick yolk sac membrane assay. Cell proliferation studies demonstrated the cytocompatibility of the scaffolds, and improvement in the cell density of the L929 mouse fibroblast cell line was observed in a live/dead assay. In conclusion, the calcium-loaded CH-CA scaffolds demonstrated antimicrobial properties, increased angiogenesis, blood compatibility, and cell proliferation, indicating their potential as an appropriate wound dressing material.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 772-791"},"PeriodicalIF":0.0,"publicationDate":"2025-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00284a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144624152","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Understanding the impact of vitamin D supplement formulation, quality and provision to older adults in UK residential care homes†","authors":"N. Rombel, C. Lim, A. Majeed, S. Abdul-Jabbar, G. R. McClelland and S. A. Jones","doi":"10.1039/D5PM00003C","DOIUrl":"10.1039/D5PM00003C","url":null,"abstract":"<p >Supplying vitamin D supplements to all older adults is beneficial and cost-effective. However, operationalising this supply to residents in long-term care is problematic. This study aimed to understand the challenges of vitamin D supplement provision by auditing the extent of supplementation, measuring the quality of the supplements and investigating the attitudes towards supplement provision in UK care homes. This case study investigated the supply of vitamin D supplement formulations in four UK care homes and analysed the vitamin D content of nine formulation types. It employed semi-structured interviews with care home stakeholders to understand attitudes toward vitamin D supply. Across the nine analysed products, there was &gt;50% variability in their quality (75–137% of the label), but 44% of supplements were of medicinal grade. One tablet from a food-grade product contained 167% vitamin D, and one medicinal-grade tablet only contained 70% vitamin D. Interviews with care home staff highlighted four challenges to providing supplements: the perceived responsibility of healthcare professionals to supplement, difficulties obtaining prescription medications, the absence of national/local strategies, and the financial burden. This study demonstrated sub-optimal vitamin D supplement supply to care home residents, with staff unclear about who was responsible for choosing the correct type of vitamin D supplement, who paid for it, and who was to supply it. This study suggests a new approach to delivering vitamin D supplements to older adults is needed.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 683-690"},"PeriodicalIF":0.0,"publicationDate":"2025-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12090889/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144129955","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Tailoring bromelain-loaded lipid–polymer hybrid nanoparticles for asthma management: fabrication and preclinical evaluation†","authors":"Manu Sharma and Namita Gupta","doi":"10.1039/D4PM00327F","DOIUrl":"https://doi.org/10.1039/D4PM00327F","url":null,"abstract":"<p >Poor response and associated side effects of available drugs in clinics have limited successful asthma management. Traditionally, bromelain has been found effective in asthma management; however, its use is limited by the need for high oral doses and poor bioavailability. Therefore, the present investigation was tailored to prepare bromelain-loaded lipid–polymer hybrid nanoparticles (Br-LPHNs) to enhance the oral bioavailability and therapeutic efficacy of bromelain in the management of allergic asthma. Br-LPHNs, consisting of a lipid core encapsulated in a biomimetic polymethylmethacrylate coating, were prepared utilizing the double emulsion solvent evaporation method. The drug release behavior, mucolytic potential and stability of the optimized formulation were evaluated. Pharmacokinetic and pharmacodynamic studies were executed in an allergen-induced asthma model. The optimized Br-LPHNs exhibited a nanosize (190.91 ± 29.48 nm) and high entrapment efficiency (89.94 ± 3.98%), along with gastro-resistant and sustained drug release behavior for up to 24 h. Using LPHNs as a carrier improved shelf life (∼6.99-fold) and bioavailability (6.89-fold) compared to pure bromelain. The optimized formulation significantly suppressed bronchial hyperresponsiveness, delayed the onset of bronchospasm and reduced its severity. Moreover, oxidative and immunological markers were significantly (<em>p</em> &lt; 0.05) reduced, accompanied by the restoration of antioxidant enzyme levels to normal. Histopathological investigations also confirmed reduced tissue injury. Thus, the development of Br-LPHNs not only ensured <em>in vitro</em> and <em>in vivo</em> stability of bromelain but also offered a promising approach for asthma management.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 749-760"},"PeriodicalIF":0.0,"publicationDate":"2025-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00327f?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144624150","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}