RSC Pharmaceutics最新文献

{"title":"Recent advances in the technology of effervescent tablets: lessons learned and future perspectives","authors":"Paraskevi Chatzidopavlaki, Efstathia Triantafyllopoulou, Natassa Pippa, Georgia Valsami and Paraskevas P. Dallas","doi":"10.1039/D4PM00229F","DOIUrl":"https://doi.org/10.1039/D4PM00229F","url":null,"abstract":"<p >Effervescent tablets are solid pharmaceutical dosage forms that are widely accepted due to their advantages. The improvement in patient compliance results from a combination of factors related to both the extrinsic characteristics of the tablet and the effects it produces. An important reason is the possibility of avoiding swallowing whole tablets, as a large part of the population, such as the elderly, children, and dysphagic patients, find it difficult to swallow them. The aim of this investigation is to review the recent literature on the technology and application of effervescent tablets and investigate their added value towards upgrading of such dosage forms and in general of pharmaceutical technology. Special attention is given to the excipients that are used for the design and development of efficacious systems, as well as their added value for the drug release studies having in mind the patients’ unmet needs.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 8-18"},"PeriodicalIF":0.0,"publicationDate":"2024-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00229f?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994221","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":"Advances in liposomal nanotechnology: from concept to clinics","authors":"Reem M. Senjab, Nour AlSawaftah, Waad H. Abuwatfa and Ghaleb A. Husseini","doi":"10.1039/D4PM00176A","DOIUrl":"https://doi.org/10.1039/D4PM00176A","url":null,"abstract":"<p >Liposomes, spherical phospholipid vesicles with a unique morphology mimicking that of body cells, have emerged as versatile nanoparticles for drug delivery. Their biocompatibility, low cytotoxicity, targeted delivery, and hydrophobic and hydrophilic characteristics make them stand out over traditional drug delivery systems. Liposomes can be tailored in size, composition, lamellarity, and surface charge, offering a unique level of customization for various applications. Extensive research in liposome technology has led to the development of a wide range of liposomal formulations with enhanced functionalities, such as PEGylated liposomes, ligand-targeted liposomes, and stimuli-responsive liposomes. Beyond their crucial role in cancer treatment, liposomes play a significant role in influenza, COVID-19, cancer, and hepatitis A vaccines. They are also utilized in pain management, fungal treatment, brain targeting, and topical and ocular drug delivery. This review offers insight into the types of liposomes, their composition, preparation methods, characterization methods, and clinical applications. Additionally, it discusses challenges and highlights potential future directions in liposome-based drug delivery.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 928-948"},"PeriodicalIF":0.0,"publicationDate":"2024-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00176a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798232","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":"Optimized albendazole-loaded nanostructured lipid carrier gel: a redefined approach for localized skin cancer treatment†","authors":"Chinmayee Khot, Kaustubh Kolekar, Swati Dabhole, Akshay Mohite, Sameer Nadaf, Popat S. Kumbhar and John Disouza","doi":"10.1039/D4PM00207E","DOIUrl":"https://doi.org/10.1039/D4PM00207E","url":null,"abstract":"<p >The chief purpose of the current study is to fabricate nanostructured lipid carrier (NLC)-based gel for localized delivery of repurposed albendazole (ABZ) against skin cancer to reduce systemic and other organ-related side effects and enhance patient compliance. ABZ NLCs were constructed by the melt-emulsification ultrasonication method and optimized using Box-Behnken Design (BBD). The ABZ NLCs were analyzed for mean particle size, % entrapment efficiency (%EE), and zeta potential. Furthermore, an NLC-based gel was developed using optimized ABZ NLCs and the Carbopol-934 gelling agent and characterized for physical properties, viscosity, texture, <em>ex vivo</em> skin permeation, <em>in vitro</em> cytotoxicity, stability, <em>etc</em>. The optimized ABZ NLCs displayed a %EE of 89.85 ± 5.6% and a particle size of 176.5 ± 7.3 nm. The pH of the ABZ NLC-based gel developed using 1.0% w/v of Carbopol-934 was between 5.1 and 6.0. The viscosity of the optimized ABZ NLC-based gel was 6.64 ± 0.67 Pa s. Besides, the NLC-based gel exhibited better and controlled ABZ release at pH 5.5 and 6.8 than the conventional ABZ gel. The <em>ex vivo</em> permeation of ABZ from NLCs and the NLC-based gel was 5.1 and 4.5-fold higher, respectively, than from the conventional gel. Notably, the <em>in vitro</em> cytotoxicity against B16F10 cells of ABZ NLCs was 1.7-fold and 2.2-fold higher than those of pure ABZ and the ABZ NLC-based gel. A negligible cytotoxicity of the developed formulations was seen in normal HaCaT cells (human epidermal cells), signifying the compatibility of these formulations with healthy cells. Moreover, the ABZ-incorporated NLCs and NLC gel remained stable for twelve weeks at 4 ± 2 °C. Thus, the given research concludes that the NLC-loaded gel could be a harmless, efficient, and novel choice to treat skin cancer using repurposed ABZ.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 1042-1054"},"PeriodicalIF":0.0,"publicationDate":"2024-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00207e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798216","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":"Multilamellar nanovectors composed of microbial glycolipid–polylysine complexes for drug encapsulation†","authors":"Silvia Alonso-de-Castro, Sergio Oliveira Formoso, Chloé Seyrig, Korin Ozkaya, Julien Dumont, Luisa Riancho, Javier Perez, Christophe Hélary and Niki Baccile","doi":"10.1039/D4PM00163J","DOIUrl":"https://doi.org/10.1039/D4PM00163J","url":null,"abstract":"<p >This study addresses the potential use of single-glucose microbial amphiphiles as pohospholipid-free drug carriers. Microbial amphiphiles, also known as biosurfactants, are molecules obtained from the fermentation of bacteria, fungi or yeast and are largely studied for their antimicrobial, cleaning or anti-pollution potential. However, recent understanding of their self-assembly properties combined with their interactions with macromolecules suggests broader potential applications, one being the phospholipid-free formulation of drugs. In this study, we demonstrate that this class of bio-based molecules can be directly used to design colloidally-stable vesicular carriers for hydrophobic drugs, without employing phospholipid supports, and that the actives can be delivered to human cells. In this study, multilamellar wall vesicles (MLWVs) have been synthesised using a microbial glycolipid amphiphile and poly-L-lysine, held together by electrostatic attractive interactions. Curcumin, a highly lipophilic molecule, was used as a natural drug model to evaluate the present colloidal system as a potential nanocarrier. The cell uptake of the curcumin-loaded nanocarriers was significantly higher for HeLa cells (50%) compared to normal human dermal fibroblasts (35%) and THP-1-derived macrophages (20%). The cytotoxic effect of delivered curcumin or other pharmaceuticals (doxorubicin, docetaxel, paclitaxel) was higher in HeLa cells as the cell viability was reduced by 50%.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 1008-1020"},"PeriodicalIF":0.0,"publicationDate":"2024-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00163j?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798213","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 lipid nanoparticle dimensions through manufacturing processes†","authors":"Caitlin McMillan, Amy Druschitz, Stephen Rumbelow, Ankita Borah, Burcu Binici, Zahra Rattray and Yvonne Perrie","doi":"10.1039/D4PM00128A","DOIUrl":"10.1039/D4PM00128A","url":null,"abstract":"<p >Lipid nanoparticles (LNPs), most commonly recognised for their role in COVID-19 mRNA vaccines, are important delivery vehicles for nucleic acid (mRNA, siRNA) therapies. The physicochemical attributes, such as size, nucleic acid encapsulation and electric charge, may have a significant impact on the efficacy of these medicines. In this study, adjustments to aqueous to lipid phase ratios were assessed for their impact on LNP size and other critical quality attributes (CQAs). It was observed that minor adjustments of aqueous-to-organic lipid phase ratios can be used to precisely control the size of ALC-0315-formulated LNPs. This was then used to evaluate the impact of phase ratio and corresponding size ranges on the <em>in vitro</em> and <em>in vivo</em> expression of these LNPs. In HEK293 cells, larger LNPs led to higher expression of the mRNA cargo within the LNPs, with a linear correlation between size and expression. In THP-1 cells this preference for larger LNPs was observed up to 120 d.nm after which there was a fall in expression. In BALB/c mice, however, LNPs at the lowest phase ratio tested, &gt;120 d.nm, showed reduced expression compared to those of range 60–120 d.nm, within which there was no significant difference between sizes. These results suggest a robustness of LNP expression up to 120 d.nm, larger than those &lt;100 d.nm conventionally used in medicine.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 841-853"},"PeriodicalIF":0.0,"publicationDate":"2024-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11417672/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142335937","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":"Nano-steps in altered opioid pharmacokinetics: a perspective on potential drug delivery post-bariatric surgery applications","authors":"A. E. Avanu, A. M. Ciubotariu, A. M. Ciornei, A. D. Cozmîncă and G. Dodi","doi":"10.1039/D4PM00187G","DOIUrl":"https://doi.org/10.1039/D4PM00187G","url":null,"abstract":"<p >Despite being a transformative intervention in treating obesity, bariatric surgery, encompassing procedures like Roux-en-Y gastric bypass and vertical sleeve gastrectomy, presents unique challenges in postoperative pain management due to altered pharmacokinetics in both adult and pediatric populations. Opioid medication, while being effective, poses risks of addiction and life-threatening side effects, thus, inviting alternative therapeutic approaches. Nanotechnology holds promise as it provides targeted solutions <em>via</em> nano-drug delivery systems, thereby reducing adverse effects and enhancing efficacy in an altered gastrointestinal system. Different methods, including subcutaneous and nasal delivery systems, prolong drug release, offer potential alternatives for patients with modified drug absorption and metabolism, as demonstrated by <em>in vivo</em> and <em>in vitro</em> studies investigating tramadol, ketamine, fentanyl, buprenorphine and others. Currently, safety issues associated with nanocarriers hinder their clinical deployment. This review prompts a new perspective on nano-controlled release methods and their applications in opioid analgesia, indicating that nanotechnology could address the pharmacokinetic challenges in pain management post-bariatric surgery. Alternative strategies, including the use of endogenous neuropeptides, are discussed for mitigating opioid-related complications and improving pain management outcomes.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 864-878"},"PeriodicalIF":0.0,"publicationDate":"2024-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00187g?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798229","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":"Prodrug nanotherapy demonstrates in vivo anticryptosporidial efficacy in a mouse model of chronic Cryptosporidium infection†","authors":"Amalendu P. Ranjan, Daniel J. Czyzyk, Griselle Martinez-Traverso, Aygul Sadiqova, Margarita Valhondo, Deborah A. Schaefer, Krasimir A. Spasov, William L. Jorgensen, Jamboor K. Vishwanatha, Michael W. Riggs, Alejandro Castellanos-Gonzalez and Karen S. Anderson","doi":"10.1039/D4PM00093E","DOIUrl":"10.1039/D4PM00093E","url":null,"abstract":"<p >The gastrointestinal disease cryptosporidiosis, caused by the genus <em>Cryptosporidium</em>, is a common cause of diarrheal diseases in children, particularly in developing countries and frequently fatal in immunocompromised individuals. <em>Cryptosporidium hominis</em> (<em>Ch</em>)-specific bifunctional dihydrofolate reductase-thymidylate synthase (DHFR-TS) has been a molecular target for inhibitor design. (<em>Note that this bifunctional enzyme has also been referred to as TS-DHFR in previous literature since the functional biochemical reaction first involves the conversion of methylene tetrahydrofolate to dihydrofolate at the TS site</em>.) While nanomolar inhibitors of <em>Ch</em> DHFR-TS have been identified at the biochemical level, effective delivery of these compounds to achieve anticryptosporidial activity in cell culture and <em>in vivo</em> models of parasite infection remains a major challenge in developing new therapies. Previous studies, using a nanotherapy approach, have shown a promising <em>Ch</em> DHFR-TS inhibitor, 906, that can successfully target <em>Cryptosporidium</em> parasites in cell culture with nanomolar anticryptosporidial activity. This formulation utilized poly(lactic-<em>co</em>-glycolic acid) (PLGA) nanoparticles (NPs) loaded with 906 (NP-906) and conjugated with a <em>Cryptosporidium</em> monoclonal antibody (MAb) on the nanoparticle surface to specifically target the glycoprotein GP25–200 in excysting oocysts. However, a limitation for <em>in vivo</em> use is antibody susceptibility to gastric acidity. To address this gap, a prodrug diethyl ester form of 906 (MAb-NP-Prodrug) was synthesized that allowed higher compound loading in the MAb-coated PLGA nanoparticles. An oral formulation was prepared by loading lyophilized MAb-NP-Prodrug into gelatin capsules with an enteric coating for gastric stability. Proof-of-concept studies with this oral formulation demonstrated antiparasitic activity in a chronic mouse model of <em>Cryptosporidium</em> infection. Efficacy was observed after a low daily dose of 2 × 8 mg kg<small>⁻¹</small> for 5 days, when examined 6 and 20 days postinfection, offering a new avenue of drug delivery to be further explored.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 963-975"},"PeriodicalIF":0.0,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11447440/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142383175","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":"Insight into central nervous system targeted nanostructured lipid carriers via the nose to brain pathway","authors":"Mridusmita Das, Anupam Sarma, Himakshi Baruah and Debojeet Basak","doi":"10.1039/D4PM00057A","DOIUrl":"https://doi.org/10.1039/D4PM00057A","url":null,"abstract":"<p >In nanomedicine, targeting the central nervous system (CNS) is one of the biggest challenges. The presence of the blood–brain barrier (BBB) leads to the failure of drugs to reach the brain; hence, CNS-related diseases are challenging to treat. Various invasive and noninvasive methods have been established to overcome the difficulty of passing through the BBB. Delivery of drugs by using nanoparticles through the nasal route is one of the noninvasive methods developed to treat CNS disorders. The nose to brain pathway allows direct transport to the brain without crossing the BBB. Among the nanocarriers designed to target the CNS, nanostructured lipid carriers (NLC) are the focus of this review. NLCs appeared as a newer generation of solid lipid nanoparticles (SLN) developed to get over SLN's limitations. They are novel pharmaceutical preparations made of lipids, surfactants and co-surfactants that are physiologic and biocompatible. Liquid lipids (oil) are added to the solid lipid to create a matrix which results in structural flaws in the solid lipids and creates a less ordered crystalline framework that prevents leakage of the drug and provides high drug loading. The imperfection in the internal arrangement of NLCs aids more drug accommodation. A systematic search was performed across the main databases like PubMed, Springer, Scopus, Taylor and Francis, Google Scholar and Wiley. The search applied terms and keywords related to nose to brain delivery, nanostructured lipid carriers and neurodegenerative diseases. This review discusses the anatomy of the nose, associated pathways, advantages and limitations of NLCs, and preparation techniques and recent developments of NLCs delivered <em>via</em> the nose to brain route. The reported records demonstrated the feasibility and potential of NLCs for innovative uses for treatment in the future <em>via</em> the nose to brain route.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 904-927"},"PeriodicalIF":0.0,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00057a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798231","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":"A comprehensive investigation of the biophysical approach for aptamer functionalized nanoparticles in cancer therapy: a review","authors":"Alanthatta Govindan Navaneeth and Subramani Karthikeyan","doi":"10.1039/D3PM00027C","DOIUrl":"https://doi.org/10.1039/D3PM00027C","url":null,"abstract":"<p >Aptamers stand out for their remarkable specificity and versatility, making them an invaluable tool in cancer therapy. When combined with nanoparticles, they form a dynamic platform for targeted drug delivery and diagnostics, leveraging enhanced cellular take up and the enhanced permeability and retention effect. This review explores both experimental and computational studies that probe the intricate interactions between aptamers and nanoparticles. By combining theoretical insights with empirical studies, this approach deepens our understanding of aptamer–nanoparticle conjugation, opening new avenues to enhance therapeutic efficacy and reduce off-target effects. Recent advancements in the field are critically analysed, spotlighting transformative studies that highlight the potential of this approach. Offering a comprehensive overview of current achievements and future prospects, this article aims to establish the pivotal role of aptamer-functionalized nanoparticles in personalized cancer treatment strategies.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 879-903"},"PeriodicalIF":0.0,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d3pm00027c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798230","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":"Reconceptualising mucoadhesion for future medicines†","authors":"Michael T. Cook and David Shorthouse","doi":"10.1039/D4PM00149D","DOIUrl":"https://doi.org/10.1039/D4PM00149D","url":null,"abstract":"<p >The field of mucoadhesion has grown from a niche interest to a central consideration for the optimisation of mucosal medicines. As new therapies progress through development pipelines there are constantly emerging conditions which would benefit from the ability to target prolonged residence at mucosal sites. As such, there continues to be expansive investigation into mucoadhesion and the design of novel mucoadhesive materials for dosage form design. In this perspective piece, we give consideration to the recent progress in the field of mucoadhesive materials and make suggestion for reconsideration of current focus. Opinion on risks around current approaches to the development of mucoadhesive materials are described. Furthermore, challenges with translation are discussed, focussing on sensitisation and incompatibilities. Finally, the state of data in this field is critically assessed with a focus to <em>in vitro</em>–<em>in vivo</em> correlation and the formulation state space. It is intended that this manuscript challenges some important areas currently under investigation in the field.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 949-957"},"PeriodicalIF":0.0,"publicationDate":"2024-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00149d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798233","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}