AAPS PharmSciTech最新文献

{"title":"Hot Melt Extrusion Technology in Taste Masking.","authors":"Geetha Nayak, Usha Y Nayak","doi":"10.1208/s12249-025-03174-9","DOIUrl":"https://doi.org/10.1208/s12249-025-03174-9","url":null,"abstract":"<p><p>Hot melt extrusion (HME) is a widely used method of taste masking in medication formulations, notably for bitter Active Pharmaceutical Ingredients (APIs). This continuous, solvent-free technique successfully wraps APIs within a polymer matrix, forming a barrier that considerably decreases bitterness perception. These advantageous properties of HME in taste masking are especially important for pediatric, geriatric, and veterinary formulations, where palatability is critical. The technique entails melting a polymer matrix and combining it with the medicine, followed by extrusion to make granules or dosage forms. The efficacy of taste masking is dependent on selecting acceptable excipients and ensuring their compatibility with the medicine. Temperature, screw speed, and drug-to-polymer ratio are critical process parameters that must be tuned. Various screw configurations can influence the physical condition of the API during extrusion, increasing taste-masking efficacy. Future advances in HME technology are expected, with a focus on enhancing taste masking for a broader range of APIs. Innovations in the study of polymers and the combination of process analytical technology (PAT) will significantly enhance the effectiveness and reliability of flavor-masked formulations, resolving the important need for patient-friendly drugs that are taken orally.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 7","pages":"196"},"PeriodicalIF":3.4,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144688575","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring the Therapeutic Potential of Lipid Nanocarriers in Psoriasis Management: Advances and Applications.","authors":"Atif Husain, Poonam Kushwaha, Archita Kapoor, Priyanka Singh","doi":"10.1208/s12249-025-03188-3","DOIUrl":"https://doi.org/10.1208/s12249-025-03188-3","url":null,"abstract":"<p><p>Psoriasis is a chronic inflammatory skin disorder characterized by hyperproliferation of keratinocytes and immune dysregulation, leading to erythematous, scaly plaques. Conventional treatments, including corticosteroids, immunosuppressants, and biologics, often present challenges such as systemic side effects, poor skin penetration, and reduced patient compliance. Lipid nanocarriers (LNCs) have emerged as promising drug delivery systems for psoriasis management, offering enhanced drug stability, targeted delivery, improved skin penetration, and controlled drug release. This review explores the advancements in LNC-based formulations, including solid lipid nanoparticles, nanostructured lipid carriers, liposomes, and ethosomes, highlighting their advantages over traditional therapies. The physicochemical properties, mechanisms of skin penetration, and therapeutic efficacy of LNCs in psoriasis treatment are discussed, along with preclinical and clinical findings. The integration of lipid nanocarriers into psoriasis treatment regimens holds significant promise for improving patient outcomes by providing more effective and safer therapeutic alternatives.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 7","pages":"195"},"PeriodicalIF":3.4,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144681779","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Alternative Syringe and Needle Design for Clog-free Delivery of High-concentration Suspensions.","authors":"Kavin Kowsari, John Cline, Steven C Persak, Guangli Hu, Robert Berger, Jeffrey C Givand, Sahab Babaee","doi":"10.1208/s12249-025-03167-8","DOIUrl":"https://doi.org/10.1208/s12249-025-03167-8","url":null,"abstract":"<p><p>Needle clogging is one of the key challenges in delivery of suspension (i.e., multi-phase) formulations. It is a phenomenon by which the particles (i.e., solid phase) accumulate locally to occlude the flow, leading to injection failure. This work proposes alternative needle hub designs for suspension delivery systems, enabling enhanced injection process by reducing the risk of particle jamming. Rapid prototyping was harnessed to experimentally evaluate the injection behavior using our custom-built injection characterization set-up by monitoring plunger force throughout injection. Improved performance of several proposed designs was demonstrated compared to standard (unmodified) needles across a range of high-concentration suspension formulations. The proposed tapered contractions offer competitive advantage of enabling clog-free delivery of high-concentration suspension formulations that would otherwise exhibit failure using conventional syringe/needle systems, thereby potentially accelerating time to market.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 7","pages":"193"},"PeriodicalIF":3.4,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144648225","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploration of Predictive Potential of AI-enabled Portable System in Anticancer Drug Delivery: A Comparative Study with Modified Gompertz like Biphasic Response Model.","authors":"Subeel Shah, Kapil Saraswat, Charu Misra, Poonam Negi, Kaisar Raza","doi":"10.1208/s12249-025-03193-6","DOIUrl":"https://doi.org/10.1208/s12249-025-03193-6","url":null,"abstract":"<p><p>Mathematical models are conventionally used to understand the of tumor behaviors, but they generally lack in precisely correlating drug efficacy with tumor response. Artificial intelligence (AI) has forged a new avenue in cancer management, but requires complex and heavy computing resources. In this paper, we have presented an AI enabled single board computer (SBC) and proposed a modified Gompertz like biphasic response model (MGBRM) for the prediction of anti-tumor activity of docetaxel-palmitate and its solid lipid nano-particles on breast cancer. Linear regression algorithm using C +  + library utilizing in-vivo experimental data over the span of 20 days was employed. A MGBRM was validated for no treatment, treatment with DTX-PL and DTX-PL-SLN using in-vivo data and compared with the AI model. The actual tumor volumes versus the numerically calculated tumor volumes from the modified Gompertz model exhibited good correlation coefficient with r² value of 0.999 for no treatment, 0.986 for DTX-PL and 0.998 for DTX-PL-SLN. In addition to that, the presented AI enabled SBC system also demonstrated good correlation with tumor volumes obtained through in-vivo experiment over a time. The r² for actual tumor volumes versus AI predicted tumor volumes for the studies conditions were close to 1. Both models were compared for biphasic response that can be useful to understand the numerical system parameters and black-box (AI) prediction for the tumor specific treatment. However, the modified MGBRM model is a leveraging step in predicting the tumor volumes in animals receiving treatment that was not feasible with the conventional model.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 7","pages":"194"},"PeriodicalIF":3.4,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144648226","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanotechnology in Uveal Melanoma: Cutting-Edge Advances to Halt Progression and Metastasis.","authors":"Rohit Bhawale, Omar Khan, Ravindra Vasave, Rati Yadav, Neelesh Kumar Mehra","doi":"10.1208/s12249-025-03184-7","DOIUrl":"https://doi.org/10.1208/s12249-025-03184-7","url":null,"abstract":"<p><p>Uveal melanoma (UM) represents the most prevalent primary intraocular malignancy in adults, distinguished by its aggressive progression and significant propensity for metastasis, predominantly to the liver and lungs. Despite advances in diagnostic tools and therapeutic approaches, the prognosis for metastatic UM remains dismal, underlining the critical need for novel treatment regimens. Nanotechnology is an exciting new area in the treatment of UM that offers creative ways to get around the problems with current medicines. Nanocarrier systems, including albumin-based nanoparticles, PEGylated nanostructured lipid carriers, nanostructured lipid carriers, and gold nanoparticles, facilitate targeted drug delivery, enhance bioavailability, and allow for controlled release. These advancements contribute to improved therapeutic outcomes while simultaneously reducing off-target effects. Recent advancements in nanotechnology have demonstrated considerable promise in the prevention of metastasis by facilitating early intervention and enabling the targeted delivery of chemotherapeutic agents or immune modulators directly to the tumor microenvironment. Furthermore, nanotechnology-based systems are being investigated for the delivery of RNA therapies and gene-editing tools, offering a fresh approach to tackling the genetic foundations of UM. Preclinical and clinical investigations have shown encouraging results, with nanotechnology-enhanced medicines demonstrating higher effectiveness, lower toxicity, and increased patient compliance. Recently, new ideas have been talked about in this study, like theranostic systems and stimuli-responsive nanocarriers, which can do both diagnostic and medicinal work. This makes personalized medicine possible in UM treatment. To summarize, nanotechnology has enormous potential for revolutionizing the therapeutic landscape for UM, especially in terms of medication delivery and metastasis prevention. Further research and practical translation of these technologies are required to enhance UM patients' survival rates and quality of life.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"191"},"PeriodicalIF":3.4,"publicationDate":"2025-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144635893","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phospholipid-Drug Conjugates in Cancer Therapy: Emerging Paradigms and Future Directions.","authors":"Kiran Dudhat, Harsh Pirojiya, Krupali Bhalala, Dhaval Mori, Bhupendra Prajapati","doi":"10.1208/s12249-025-03175-8","DOIUrl":"10.1208/s12249-025-03175-8","url":null,"abstract":"<p><p>Phospholipid-drug conjugates (PDCs) represent a novel advancement in cancer therapy, combining the therapeutic potential of active drug molecules with the biocompatibility and targeting benefits of phospholipids. Conventional cancer treatments face limitations such as drug resistance, off-target toxicity, and poor solubility. PDCs address these issues by enhancing drug stability, bioavailability, and targeted delivery, reducing systemic toxicity. Their amphiphilic nature enables self-assembly into nanocarriers, allowing controlled and site-specific drug release. PDCs utilize both passive and active targeting mechanisms, with the enhanced permeability and retention (EPR) effect facilitating tumor accumulation and ligand-receptor interactions enhancing active targeting. Stimuli-responsive PDCs further improve specificity by releasing drugs in response to tumor microenvironment factors such as acidity and enzymatic activity. Recent advances in PDC synthesis, including covalent bonding strategies, modular designs, and bio-inspired approaches, have broadened their therapeutic potential. Their integration with nanotechnology and gene-based therapies presents new possibilities for precision medicine and personalized treatment. Despite these benefits, challenges such as scalability, regulatory hurdles, and multidrug resistance (MDR) remain. Research is addressing these issues through AI-driven optimization, bioprinting-based formulations, and sustainable green chemistry. Future applications extend beyond oncology, with potential uses in neurodegenerative, infectious, and cardiovascular diseases. Overall, PDCs hold tremendous promise in transforming cancer treatment, offering safer, more effective, and highly targeted therapies that could revolutionize patient outcomes and therapeutic precision.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"190"},"PeriodicalIF":3.4,"publicationDate":"2025-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144635894","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Integration of Design of Experiments for the Development and Evaluation of Sulfasalazine Loaded Hybrid Albumin Chitosan Based Polymeric Nanocarriers.","authors":"Sushrut Marathe, Rohit Joshi, Rongbing Yang, Gauri Shadambikar, André S Bachmann, Mahavir Bhupal Chougule","doi":"10.1208/s12249-025-03190-9","DOIUrl":"https://doi.org/10.1208/s12249-025-03190-9","url":null,"abstract":"<p><p>Sulfasalazine is a sepiapterin reductase and System x - c inhibitor with anti-neuroblastoma activity. The objective was to develop cellular redox glutathione stimuli-responsive Sulfasalazine-loaded albumin-chitosan hybrid nanocarriers with a target profile of < 100 nm, polydispersity index (PDI) of < 0.3, charge of 3 to 10 mV, and drug load of > 8% w/w. Taguchi orthogonal array experimental design was utilized in the formulation of cellular redox glutathione stimuli-responsive albumin-chitosan-based hybrid nanocarriers using the nano-precipitation method. Chitosan was coated on the Albumin nanocarriers, followed by PEGylation. Nanocarriers were characterized in terms of size, zeta potential, polydispersity index (PDI), entrapment efficiency, and drug release. The uptake of chitosan-coated sulfasalazine-loaded albumin nanocarriers was investigated using SK-N-Be(2)c neuroblastoma cells. Taguchi orthogonal array results revealed that the acetone concentration and organic phase to aqueous phase ratio were the significant variables in formulating stable monodispersed nanocarriers with mean particle size of 80.55 ± 3.30 nm, polydispersity index (PDI) of 0.120 ± 0.037, zeta potential of 6.60 ± 1.95 mV, entrapment efficiency of 96.42 ± 1.38%, and 10% w/w drug load. The concentration of acetone had a significant impact on the size and PDI of Albumin nanocarriers. The cellular redox glutathione stimuli-responsive nanocarriers exhibited an extended drug release of 30 ± 1% at 10 mM, an intracellular concentration, and 25 ± 1% at 20 mM glutathione, an extracellular systemic concentration in PBS-based release media. PEGylation of nanocarriers confers stability in ionic environments. Sulfasalazine-loaded albumin-chitosan nanocarriers showed significantly higher SK-N-BE (2)c cellular uptake than Albumin nanocarriers (p < 0.001). The Taguchi orthogonal array design was successfully applied in the development of cellular redox glutathione stimuli-responsive sulfasalazine-loaded extended-release albumin-chitosan hybrid nanocarriers, which met the target profile of < 100 nm, a polydispersity index (PDI) of < 0.3, a charge of 3 to 10 mV, and a drug load of > 8% w/w against neuroblastoma.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"192"},"PeriodicalIF":3.4,"publicationDate":"2025-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144635892","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring Protein Aggregation in Biological Products: From Mechanistic Understanding to Practical Solutions.","authors":"Satish Rojekar, Amol D Gholap, Krishna Jadhav, Ganesh Shevalkar, Vrashabh V Sugandhi, Rohan Pai, Kinjal Parikh, Mahendra Kumar Prajapati, Nimeet Desai, Lalitkumar K Vora, Rahul G Ingle, Keshav Raj Paudel","doi":"10.1208/s12249-025-03189-2","DOIUrl":"https://doi.org/10.1208/s12249-025-03189-2","url":null,"abstract":"<p><p>Proteins are vital for the regulation of several cellular functions, including the synthesis of structural components. The change in environmental conditions will impact conformational stability and result in aggregation. Protein aggregation involves different states of proteins, like nonnative, unfolded, and native states, which make them complex processes. The proper understanding of protein aggregation pathways involving the role of thermodynamically unfavoured lag phase, soluble protofibrils triggered polymerization through an exponential phase, and depleted free monomers owing to the saturation phase resulted in the leveling off of the polymerization process. The aggregated therapeutic proteins can induce deleterious immune responses in patients, and control of the aggregation is essential for better therapeutic protein stability and targeting with the help of stable protein structures and function. Protein-protein interactions (PPIs) are important for protein stability, aggregation rate, and solubility, while advanced computational and biophysical methods have been developed to characterize therapeutic protein aggregation better. Hence, an effective strategy for controlling, monitoring, and reproducing protein aggregation propensities of the polypeptide chains is required. An in-depth understanding of protein aggregation mechanisms, characterization, and combat strategies will counter the issues of protein aggregation. It will also reduce the cost of the product, time constraints, stable & effective product availability, and potential immunogenicity.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"189"},"PeriodicalIF":3.4,"publicationDate":"2025-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144590210","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Solid Lipid Nanoparticles: An Innovative Drug Delivery System for Enhanced Bioavailability and Targeted Therapy.","authors":"Kaushal Aggarwal, Sachin Joshi, Priya Jindal, Preeti Patel, Balak Das Kurmi","doi":"10.1208/s12249-025-03185-6","DOIUrl":"https://doi.org/10.1208/s12249-025-03185-6","url":null,"abstract":"<p><p>Since the 1990s, solid lipid nanoparticles have been developed as a novel drug delivery system and utilized for delivering various drugs. These nanoparticles can be composed of different solid lipids, such as waxes, fatty acids, and glycerides, which can be stabilized using various surfactants. Solid lipid nanoparticles have attracted considerable interest from researchers due to their innovative and adaptable properties. Furthermore, this delivery strategy offers many benefits over standard colloidal carriers such as polymeric nanoparticles, emulsions, and liposomes. Solid lipid nanoparticles are one of the technologies developed to address challenges related to drug bioavailability and targeting delivery. In this review paper, we have compiled all the essential information concerning solid lipid nanoparticles, including a general introduction, multiple techniques of preparation, and the numerous excipients related to the formulation. Various features of drug inclusion and manufacturing models, as well as their applications, are thoroughly covered. They can improve pharmacokinetics and modulate drug release. The prospect of surface modification, increased penetration across multiple biological barriers, chemical resistance, and the capacity to encapsulate two or more therapeutic substances simultaneously leads to widespread interest in solid lipid nanoparticles.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"186"},"PeriodicalIF":3.4,"publicationDate":"2025-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144590213","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Innovative Microneedle-based Therapies for the Treatment of Diabetic Wound Healing.","authors":"Sunny Rathee, Richa Dayaramani","doi":"10.1208/s12249-025-03187-4","DOIUrl":"https://doi.org/10.1208/s12249-025-03187-4","url":null,"abstract":"<p><p>Microneedle-based medical devices have gained significant attention as innovative tools for addressing challenges in wound healing, particularly in diabetic wound management. These devices offer a minimally invasive, patient-compliant platform for drug delivery, tissue regeneration, and real-time monitoring. This review provides a comprehensive overview of their design and applications, focusing on their role in modulating biological pathways and enzymatic markers essential for wound repair. Key biological pathways such as VEGF (Vascular Endothelial Growth Factor)-mediated angiogenesis, matrix metalloproteinase (MMP)-driven tissue remodeling, and inflammatory response regulation are discussed to elucidate the mechanisms underlying wound healing. The utility of biochemical markers, including oxidative stress indicators and growth factors, in evaluating wound progression is highlighted. Additionally, microneedles demonstrate unique advantages, such as enhanced bioavailability, precise drug delivery, and integration with biosensors for real-time feedback, making them ideal for chronic wound management. In the context of diabetic wounds, microneedle-based devices address specific challenges like impaired angiogenesis, prolonged inflammation, and delayed healing by facilitating localized delivery of therapeutic agents and monitoring critical biomarkers. Advanced material innovations and emerging technologies further enhance their performance and scalability. This review also examines the regulatory landscape and commercialization prospects of microneedle systems while outlining future directions, including novel materials and synergistic therapies. By bridging technological advancements with clinical needs, microneedle-based devices hold the potential to revolutionize wound care and improve outcomes in diabetic and other chronic wound conditions.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"187"},"PeriodicalIF":3.4,"publicationDate":"2025-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144590211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}