Alice Parkes, Enrico Spoletti, John O'Reilly, Matteo Lusi, Ahmad Ziaee and Emmet O'Reilly
{"title":"Controlled isolation of a novel polymorphic form of chlorothiazide by spray drying†","authors":"Alice Parkes, Enrico Spoletti, John O'Reilly, Matteo Lusi, Ahmad Ziaee and Emmet O'Reilly","doi":"10.1039/D4PM00286E","DOIUrl":"https://doi.org/10.1039/D4PM00286E","url":null,"abstract":"<p >This study outlines a route to producing a novel polymorphic form of chlorothiazide (CTZ). CTZ was spray dried using three different atomising gas flowrate settings to determine whether it has any effect on the solid-state of CTZ. At a lower atomising gas flowrate, a new form of CTZ, CTZ form IV, was obtained in pure form, whereas at the highest atomising gas flowrate, a mixture of CTZ form I and CTZ form IV was obtained. The morphology of CTZ form I was prism-shaped, and the new form, CTZ form IV, consisted of spherical clusters, some of which were porous and some non-porous. As a result of the rapid drying process, acetone was trapped within the porous clusters and could be released by milling. CTZ form IV has been shown to be stable at room temperature and below 40% relative humidity (RH); however, after 1 week of stability under accelerated conditions of 40 °C/75% RH, CTZ form IV converted to CTZ form I. Also, at high temperatures between 150 °C and 175 °C, CTZ form IV converted to form I, with the simultaneous release of acetone upon its morphology change. This study demonstrates how spray drying can be useful to discover new forms of APIs by a controlled drying process.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 398-412"},"PeriodicalIF":0.0,"publicationDate":"2025-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00286e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638125","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}
Tomoko Ito, Takayuki Yoshimoto, Izuru Mizoguchi and Yoshiyuki Koyama
{"title":"Tumor immunotherapy by plasmid DNAs encoding adenovirus virus-associated RNA†","authors":"Tomoko Ito, Takayuki Yoshimoto, Izuru Mizoguchi and Yoshiyuki Koyama","doi":"10.1039/D4PM00219A","DOIUrl":"https://doi.org/10.1039/D4PM00219A","url":null,"abstract":"<p >Immunotherapy has become a most promising weapon for cancer treatment; however, tumor antigens generally exhibit low immunogenicity, limiting its effectiveness. In contrast, viral infections efficiently trigger innate and adaptive immunity. This is attributed to the high immunogenicity of microbial antigens and also to the activation of pattern recognition receptors such as retinoic acid-inducible gene-I (RIG-I). Upon recognizing viral RNA, RIG-I induces secretion of type-I interferons (IFNs). Type I IFNs not only invite antiviral effects but also plays an effective role in cancer immunotherapy. Therefore, activation of RIG-I by the ligands has gained attention as a novel cancer immunotherapy in recent years. Virus-associated RNAs (VA-RNA I and VA-RNA II) are non-coding small RNAs generated from the adenovirus genome. VA-RNA I strongly activates RIG-I, leading to type-I IFN production. In this study, plasmid DNAs encoding both VA-RNA I and II [pDNA(I,II)] or only VA-RNA I [pDNA(I)] were prepared, and their IFN inducing and anti-tumor effects were investigated. In culture cells, introduction of pDNA(I,II) or pDNA(I) effectively induced both IFN-α and IFN-β production. Both plasmids significantly inhibited tumor growth in mice. pDNA(I) exhibited superior IFN-inducing and anti-tumor effects compared to pDNA(I,II). VA-RNA I gene administration holds promise as a novel anti-tumor immunotherapy strategy.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 257-263"},"PeriodicalIF":0.0,"publicationDate":"2025-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00219a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638118","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}
Elizabeth J. Legge, Ryan T. Coones, William A. Lee, Yiwen Pei, Natalie A. Belsey and Caterina Minelli
{"title":"Non-invasive quantitative chemical measurements of liposomal formulations using Raman spectroscopy†","authors":"Elizabeth J. Legge, Ryan T. Coones, William A. Lee, Yiwen Pei, Natalie A. Belsey and Caterina Minelli","doi":"10.1039/D4PM00238E","DOIUrl":"https://doi.org/10.1039/D4PM00238E","url":null,"abstract":"<p >With a growing interest towards low batch-volume personalised medicines and continuous manufacturing of pharmaceuticals, the need for robust non-invasive quality control analytical methods is becoming increasingly important. Current methods for the quantification of total and encapsulated drug in a liposomal formulation include reversed-phase high-performance liquid chromatography with ultraviolet or fluorescence spectroscopy, which requires sample consumption after procedures such as ultrafiltration to separate the free drug from the encapsulated drug. We have developed and tested a method to perform non-invasive Raman spectroscopy measurements on liposomal doxorubicin. Raman spectroscopy provides chemically specific, potentially quantitative information, with measurements able to be performed on the contents of a sealed glass vial. We developed and validated the method by using a model system of polystyrene (PS) nanospheres and produced calibration curves for the concentration of PS at sizes of 40 nm, 125 nm and 200 nm. We then applied the same method to a liposomal doxorubicin formulation to measure the concentration of lipidic and drug components, and differences in the percentage of encapsulated drug. Our results show that by this method we can measure differences in doxorubicin concentration of 0.25 mg ml<small><sup>−1</sup></small> and distinguish between free and encapsulated doxorubicin down to a minimal relative concentration of 2.3%.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 279-291"},"PeriodicalIF":0.0,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00238e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638120","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}
Haja Muhamad, Nihad Mawla, Saedah Dereiah, Adam Ward, James Williamson and Kofi Asare-Addo
{"title":"Comparative analysis of drug release kinetics in polyethylene oxide and xanthan gum matrices with various excipients","authors":"Haja Muhamad, Nihad Mawla, Saedah Dereiah, Adam Ward, James Williamson and Kofi Asare-Addo","doi":"10.1039/D4PM00296B","DOIUrl":"https://doi.org/10.1039/D4PM00296B","url":null,"abstract":"<p >This study aimed to investigate the effect of various pharmaceutical excipients on the drug release kinetics of extended-release formulations composed of polyethylene oxide (PEO) and xanthan gum (XG), using propranolol hydrochloride (PPN) as the model drug. The formulations contained different ratios (1 : 3, 1 : 1, and 3 : 1 w/w) of PEO or XG to either lactose, dibasic calcium phosphate (DCP), or microcrystalline cellulose (MCC). Compaction analysis revealed that formulations that contain higher excipient content exhibit increased porosity and decreased hardness values. Contact angle measurements indicated that formulations with higher excipient content, particularly with lactose, displayed lower contact angles, which is indicative of increased hydrophilicity. After the <em>in vitro</em> dissolution studies were conducted, the dissolution efficiency (DE), mean dissolution time (MDT), mean dissolution rate (MDR), and similarity factors (<em>f</em><small><sub>2</sub></small>) were analysed. The findings showed that a higher amount of lactose in both PEO and XG formulations resulted in faster drug release, with the PEO : lactose 1 : 3 ratio achieving the highest DE (64 ± 8%) and the shortest MDT (77 ± 10 min). Similarly, the XG : lactose 1 : 3 ratio exhibited the highest DE (61 ± 2%) and fastest MDR (0.20 ± 0.01% min<small><sup>−1</sup></small>), although the effect was less pronounced compared to PEO formulations. The kinetic analysis showed that most PEO formulations followed the Peppas model, indicating non-Fickian transport driven by both diffusion and polymer erosion mechanisms. However, most of the XG formulations followed the Higuchi model. The similarity factors (<em>f</em><small><sub>2</sub></small>) revealed the influence of excipient type and ratio on the dissolution profiles. Formulations containing a higher amount of MCC displayed higher similarity with the pure polymer profiles. These results give important insights into how excipients can be used to optimise polymeric matrices to regulate drug release in extended-release formulations.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 303-317"},"PeriodicalIF":0.0,"publicationDate":"2024-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00296b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638122","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":"Strategies for beating the bitter taste of pharmaceutical formulations towards better therapeutic outcomes","authors":"Lohare Rahul Sanjay, Makka Krupali Ashokbhai, Shubham Ghatole, Subhadeep Roy, Kardile Punam Kashinath and Santanu Kaity","doi":"10.1039/D4PM00191E","DOIUrl":"https://doi.org/10.1039/D4PM00191E","url":null,"abstract":"<p >Oral drug delivery remains the most favored method of administration due to its convenience and patient compliance. However, the unpleasant taste of certain medications often leads to poor acceptance, particularly among pediatric and geriatric patients. To address this issue, taste-masking (TM) technologies have emerged as effective solutions for improving the palatability of oral drugs. This review provides an overview of the key features of TM technologies, including the properties of materials used, their mechanisms, and applications in drug delivery. Typically, TM materials work by complexing or encapsulating drug molecules to prevent direct interaction with taste receptors, thus mitigating unpleasant flavors and enhancing the overall sensory experience. The review explores a range of materials—both synthetic and natural—and various TM technologies designed to mask bitter taste. Additionally, it discusses the latest methods for assessing the effectiveness of TM and the current regulatory landscape surrounding the use of these technologies in drug delivery.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 59-81"},"PeriodicalIF":0.0,"publicationDate":"2024-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00191e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994220","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":"Injectable sustained-release hydrogel for high-concentration antibody delivery†","authors":"Talia Zheng and Patrick S. Doyle","doi":"10.1039/D4PM00290C","DOIUrl":"https://doi.org/10.1039/D4PM00290C","url":null,"abstract":"<p >There is an increasing interest in subcutaneous (SC) delivery as an alternative to the traditional intravenous (IV) for immunotherapies and other advanced therapies. High-concentration formulations of antibodies are needed to meet the limited-volume requirements of subcutaneous SC delivery. Despite this need, there remain challenges in delivering stable and injectable antibodies in these high concentrations. Hydrogel encapsulation of amorphous solid antibodies has been proven to improve the stability and injectability of high-concentration antibody formulations. However, the antibody is quickly released from the hydrogel due to the material's porosity, leading to rapid, uncontrolled drug release kinetics undesirable for the drug's efficacy and safety. In this paper, we propose a dual-network composite hydrogel which leverages interactions between the two polymer networks to achieve controlled release of the antibody. We load the solid form of the antibody at high concentrations within alginate hydrogel microparticles which are then suspended in thermogelling methylcellulose solution to formulate the <em>in situ</em> gelling composite hydrogel. By facile chemical modification of the alginate to tune the microparticles’ gel properties and alginate–methylcellulose interactions, we demonstrate how the composite system can delay release of the drug in a tunable manner and achieve a near-zero order release profile for improved therapeutic efficacy. We show acceptable injectability properties of the composite hydrogel at high antibody concentrations, highlighting the functionalities of dualnetwork encapsulation. We imagine this composite system to be applicable for the sustained delivery of various therapeutic protein forms, especially for high-loading SC formulations.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 186-196"},"PeriodicalIF":0.0,"publicationDate":"2024-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00290c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994217","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}
Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla
{"title":"Design and evaluation of solid self-nanoemulsifying drug delivery systems of cyclosporine developed with a superior adsorbent base†","authors":"Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla","doi":"10.1039/D4PM00198B","DOIUrl":"https://doi.org/10.1039/D4PM00198B","url":null,"abstract":"<p >Cyclosporine (CYC) is a drug that belongs to the BCS class II category. This study was designed to develop novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) for cyclosporine (CYC), using chitosan–EDTA microparticles. Such microparticles are known to exhibit superior adsorbent characteristics and were prepared by two different methods <em>viz</em>. spray drying (SD-CHEM) and solvent evaporation (SE-CHEM). Capmul® GMS-50K, Labrafac, and PEG 400 were chosen as the oil, surfactant, and co-surfactant, respectively. The cyclosporine liquid self-nanoemulsifying drug delivery system (CYC-L-SNEDDS) was developed with an optimal oil to <em>S</em><small><sub>mix</sub></small> (surfactant : co-surfactant) ratio of 40 : 60, determined through a pseudo ternary phase diagram. The novel S-SNEDDS were developed by adsorbing CYC-L-SNEDDS onto the chitosan–EDTA microparticles, resulting in CYC-SD-S-SNEDDS and CYC-SE-S-SNEDDS. Both formulations exhibited favorable drug loading, with 81.184 ± 4.191% for CYC-SD-S-SNEDDS and 56.426 ± 5.471% for CYC-SE-S-SNEDDS. XRD and DSC confirmed drug amorphization, while SEM revealed a smooth, well-distributed adsorbate on the adsorbent surfaces, with particle sizes of 5–8 μm for CYC-SD-S-SNEDDS and 10–12 μm for CYC-SE-S-SNEDDS. When tested for stability, the developed formulations exhibited excellent physical and thermodynamic stability. The globule size for CYC-SD-S-SNEDDS was 138.7 ± 4.14 nm, with a PDI of 0.613 ± 0.004, while CYC-SE-S-SNEDDS had a globule size of 166.9 ± 4.04 nm and a PDI of 0.579 ± 0.003. The results of <em>in vitro</em> dissolution studies revealed that there was a fourfold increase in drug dissolution for CYC-SD-S-SNEDDS (80.03%) and CYC-SE-S-SNEDDS (72.26%) when compared to the pure cyclosporine (19.8%). A similar pattern was observed in <em>ex vivo</em> permeation studies where CYC-SD-S-SNEDDS showed 39.34% release and CYC-SE-S-SNEDDS exhibited 28.31% release as compared to CYC-L-SNEDDS (41.46%). Furthermore, CYC-SD-S-SNEDDS outperformed CYC-SE-S-SNEDDS, indicating the superiority of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These findings suggest enhanced dissolution and permeation for cyclosporine in S-SNEDDS.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 318-332"},"PeriodicalIF":0.0,"publicationDate":"2024-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00198b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638123","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}
Sucheta Sarkar, Arijit Prosad Roy, Sanchita Mitra, Gouranga Nandi, Ranabir Sahu, Tarun Kumar Dua and Paramita Paul
{"title":"Preparation and characterization of efavirenz cocrystal-encapsulated pronanoliposomes for antiretroviral therapy with improved bioavailability†","authors":"Sucheta Sarkar, Arijit Prosad Roy, Sanchita Mitra, Gouranga Nandi, Ranabir Sahu, Tarun Kumar Dua and Paramita Paul","doi":"10.1039/D4PM00215F","DOIUrl":"https://doi.org/10.1039/D4PM00215F","url":null,"abstract":"<p >The present research work aims to improve the bioavailability of the antiretroviral drug efavirenz (EFV) using pharmaceutical cocrystallization technique. EFV is a potential antiretroviral drug that exhibits extremely poor water solubility and poor oral bioavailability and falls under the BCS-II category. EFV and <small>L</small>-proline were selected in a 1 : 1 equimolar ratio to formulate efavirenz proline co-crystals, and a facile method was adopted to prepare co-crystals of EFV. The formation of a new solid phase was confirmed through advanced techniques such as Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and powder X-ray diffraction (pXRD) analysis, and solubility study was conducted utilising UV visible spectroscopy. Proliposomal vesicles containing EFV or EFV cocrystals were prepared using thin film hydration methods with few modifications. The vesicle size in dispersion, zeta potential, surface morphology, drug loading and <em>in vitro</em> drug release were assessed. Co-crystallization increased the solubility of EFV up to 3 fold, and the liposomes were found to release the drug in a sustained manner. The optimized formulation was found to have a substantial amount of EFV loading (32.70%) and entrapment efficiency (99.28%) with a narrow range of size distribution. The liposomes containing the pure drug showed 72% release of the drug in 72 h, whereas the liposomes containing co-crystals showed 99.98% release of the drug in 72 h. This was due to the presence of <small>L</small>-proline in association with EFV, which led to an enhancement in the polarity of hydrophobic EFV, thus increasing its dissolution in drug release media. The present work reports a cost-effective method for the enhancement of drug solubility, providing sustained drug release from liposome and thereby improving the oral bioavailability of the antiviral agent EFV.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 342-352"},"PeriodicalIF":0.0,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00215f?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638126","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}
Haritha Kirla, Juliana Hamzah, Zhong-Tao Jiang and David J. Henry
{"title":"Dual-action antimicrobial surface coatings: methylene blue and quaternary ammonium cation conjugated silica nanoparticles†","authors":"Haritha Kirla, Juliana Hamzah, Zhong-Tao Jiang and David J. Henry","doi":"10.1039/D4PM00278D","DOIUrl":"https://doi.org/10.1039/D4PM00278D","url":null,"abstract":"<p >The increasing prevalence of healthcare-associated infections from multidrug-resistant bacteria presents a growing challenge due to their high transmissibility, and resistance to traditional antimicrobial strategies. In this study, we introduce an innovative dual-mode antibacterial strategy through the development of novel surface coatings on glass substrates, offering a proof-of-concept solution for enhanced infection control. Our approach uniquely combines the light-active methylene blue silane (MBS1) dye with the potent antimicrobial compound dimethyloctadecyl[3-(trimethoxysilyl)propyl] ammonium chloride (QAS) into silica nanoparticles (SNPs) to create multifunctional antibacterial surface coatings. The distinct use of silane-functionalized MB and QA enables strong covalent bonding with silica nanoparticles, while the robust silane chemistry ensures durable adhesion of SNPs to the glass substrates. While MBS1–SNP coatings generated highly hydrophilic (CA = 28°), light-active surfaces, combination of QAS (QA–MBS1–SNP) coating enhanced surface hydrophobicity (CA = 90°) without compromising photokilling efficiency. The antibacterial efficacy of these coatings was rigorously tested against the Gram-negative bacterium <em>Escherichia coli</em>. The synergistic action of MB and QA demonstrated exceptional photokilling performance achieving >99.999% (>5-log reduction) bactericidal activity under white light (∼500 lux, ∼0.0732 mW cm<small><sup>−2</sup></small>) and effectively inhibited biofilm formation by up to 80%. The demonstrated efficacy of these coatings highlights their potential for transformative applications in healthcare settings, providing a robust, multifaceted approach to infection control.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 163-177"},"PeriodicalIF":0.0,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00278d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994215","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}
Tianyi Xiang, Sichen Song, Ronald A. Siegel and Changquan Calvin Sun
{"title":"Efficient development of high drug loaded posaconazole tablets enabled by amorphous solid dispersion","authors":"Tianyi Xiang, Sichen Song, Ronald A. Siegel and Changquan Calvin Sun","doi":"10.1039/D4PM00301B","DOIUrl":"https://doi.org/10.1039/D4PM00301B","url":null,"abstract":"<p >Determining the upper limits of drug loading in amorphous solid dispersion (ASD) with sufficient physical stability and release performance is critical for developing ASD-enabled tablets for poorly soluble drugs. Recent studies have highlighted the utility of the polymer overlap concentration, <em>c</em>*, in maintaining the physical stability of ASD formulations. The present work demonstrates the feasibility of effectively developing high drug loaded ASD tablets using the <em>c</em>* concept as a guide, with posaconazole as the model drug. By incorporating various material sparing formulation technologies, a record high 50% POS loaded tablet with adequate manufacturability and satisfactory dissolution performance was developed using 1.5 g of POS within 14 days. Physical stabilities of the ASD and tablet were maintained for at least 6 months under ambient conditions and 1 month at 40 °C.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 178-185"},"PeriodicalIF":0.0,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00301b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994216","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}