{"title":"Biotechnological Phytocomplex of <i>Zanthoxylum piperitum</i> (L.) DC. Enhances Collagen Biosynthesis In Vitro and Improves Skin Elasticity In Vivo.","authors":"Giovanna Rigillo, Giovanna Pressi, Oriana Bertaiola, Chiara Guarnerio, Matilde Merlin, Roberto Zambonin, Stefano Pandolfo, Angela Golosio, Francesca Masin, Fabio Tascedda, Marco Biagi, Giulia Baini","doi":"10.3390/pharmaceutics17010138","DOIUrl":"10.3390/pharmaceutics17010138","url":null,"abstract":"<p><p><b>Background:</b><i>Zanthoxylum piperitum</i> (L.) DC., commonly known as Japanese pepper, is a deciduous shrub native to East Asia. Its berries are widely used as a spice, known for imparting a distinctive, tingly numbing sensation. Biologically, <i>Z. piperitum</i> has antimicrobial, antioxidant, and anti-inflammatory properties, and it is studied for its potential benefits in pain relief and digestive health. This study proposed a novel biotechnological <i>Z. piperitum</i> phytocomplex (ZPP) obtained by plant cell culture for skin health, specifically targeting collagen synthesis, extracellular matrix stability, and resilience against cellular stress. Given the bioactivity of <i>Z. piperitum</i>, we aimed to analyze its efficacy as a sustainable alternative for skin-supportive applications in cosmetics and supplements. <b>Methods:</b> ZPP was produced through stable plant cell cultures, yielding a lignan-rich (3.02% <i>w</i>/<i>w</i>) phytocomplex. Human fibroblasts (HFFs) were treated with varying ZPP concentrations to assess cellular viability, collagen metabolism, and ECM-related enzyme activities, both under normal and cell stress conditions. The in vivo assessment was performed by measuring biophysical skin parameters such as hydration, elasticity, and roughness in female volunteers for a period of six weeks. <b>Results:</b> In vitro, ZPP exhibited non-cytotoxicity at all concentrations tested. Under hyperosmotic stress, ZPP reduced cellular damage, suggesting enhanced resilience. ZPP upregulated lysyl oxidase (LOX) protein levels, critical for collagen cross-linking and ECM stability, with protective effects observed under oxidative/inflammatory conditions. Additionally, ZPP selectively inhibited collagenase, attenuating collagen breakdown, though antioxidant activity was modest. In vivo evaluation highlighted improved skin hydration, elasticity, and roughness. <b>Conclusions</b>: ZPP shows promise as a biotechnological agent for skin health, particularly in supporting collagen integrity, ECM stabilization, and cellular resilience under stress. While further studies are needed to explore its full efficacy, especially for aging and environmentally stressed skin, these findings highlight ZPP's potential as a new ingredient for cosmetic formulations aimed at skin care and the treatment of alterations caused by aging or environmental conditions.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768096/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040279","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-20DOI: 10.3390/pharmaceutics17010137
Carlos O Amorim
{"title":"A Compendium of Magnetic Nanoparticle Essentials: A Comprehensive Guide for Beginners and Experts.","authors":"Carlos O Amorim","doi":"10.3390/pharmaceutics17010137","DOIUrl":"10.3390/pharmaceutics17010137","url":null,"abstract":"<p><p>Magnetic nanoparticles (MNPs) are advanced materials that combine the unique properties of magnetic materials and nanoscale dimensions, enabling a wide range of applications in biomedicine, environmental science, and information technology. This review provides a comprehensive yet accessible introduction to the fundamental principles, characterization techniques, and diverse applications of MNPs, with a focus on their nanoscale magnetic properties, such as superparamagnetism, single-domain behavior, and surface effects. It also delves into their classification and the critical role of parameters like magnetic anisotropy and blocking temperature. Emphasis is placed on routine characterization methods, including X-ray diffraction, electron microscopy, and magnetometry, as well as advanced concepts like magnetic hyperthermia and self-regulated heating. Designed for newcomers and experts alike, this review serves as both an educational guide and a quick-reference resource, ensuring clarity while maintaining scientific rigor.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768579/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040989","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-19DOI: 10.3390/pharmaceutics17010136
Shery Jacob, Fathima Sheik Kather, Sai H S Boddu, Mahesh Attimarad, Anroop B Nair
{"title":"Nanosuspension Innovations: Expanding Horizons in Drug Delivery Techniques.","authors":"Shery Jacob, Fathima Sheik Kather, Sai H S Boddu, Mahesh Attimarad, Anroop B Nair","doi":"10.3390/pharmaceutics17010136","DOIUrl":"10.3390/pharmaceutics17010136","url":null,"abstract":"<p><p>Nanosuspensions (NS), with their submicron particle sizes and unique physicochemical properties, provide a versatile solution for enhancing the administration of medications that are not highly soluble in water or lipids. This review highlights recent advancements, future prospects, and challenges in NS-based drug delivery, particularly for oral, ocular, transdermal, pulmonary, and parenteral routes. The conversion of oral NS into powders, pellets, granules, tablets, and capsules, and their incorporation into film dosage forms to address stability concerns is thoroughly reviewed. This article summarizes key stabilizers, polymers, surfactants, and excipients used in NS formulations, along with ongoing clinical trials and recent patents. Furthermore, a comprehensive analysis of various methods for NS preparation is provided. This article also explores various in vitro and in vivo characterization techniques, as well as scale-down technologies and bottom-up methods for NS preparation. Selected examples of commercial NS drug products are discussed. Rapid advances in the field of NS could resolve issues related to permeability-limited absorption and hepatic first-pass metabolism, offering promise for medications based on proteins and peptides. The evolution of novel stabilizers is essential to overcome the current limitations in NS formulations, enhancing their stability, bioavailability, targeting ability, and safety profile, which ultimately accelerates their clinical application and commercialization.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768797/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040853","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-19DOI: 10.3390/pharmaceutics17010134
Lyubomira Radeva, Krassimira Yoncheva
{"title":"Resveratrol-A Promising Therapeutic Agent with Problematic Properties.","authors":"Lyubomira Radeva, Krassimira Yoncheva","doi":"10.3390/pharmaceutics17010134","DOIUrl":"10.3390/pharmaceutics17010134","url":null,"abstract":"<p><p>Resveratrol is a natural polyphenol (stilbenoid), which can be found in grape skin, red wine, blueberries, peanuts and others. The biological properties of resveratrol, in particular antioxidant, anti-inflammatory, anticancer, estrogenic, vasorelaxant and cardioprotective activity, are the main reason for its importance in medicine and pharmacy. Despite all of its advantages, however, there are many problems related to this polyphenolic substance, such as low stability, water insolubility, poor bioavailability and fast metabolism. For this reason, scientists are currently searching for different approaches to dealing with these problematic properties and improving the therapeutic usage of resveratrol. This review summarizes the mechanisms of the biological effects of resveratrol, determined in vitro and in vivo, and the main limitations of the drug. The article emphasizes new approaches for the improvement of resveratrol delivery, in particular nanoencapsulation, formation of nanocrystals, prodrugs and structure analogues.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768323/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-19DOI: 10.3390/pharmaceutics17010135
Charissa Wijnands, Peter G A Karel, Jolein Gloerich, Gad Armony, Anastasia Tzasta, Corrie M de Kat Angelino, Luciano Di Stefano, Vincent Bonifay, Theo M Luider, Martijn M VanDuijn, Sandra J Croockewit, Elizabeth A de Kort, Daan A R Castelijn, Claudia A M Stege, Hans J C T Wessels, Alain J van Gool, Niels W C J van de Donk, Joannes F M Jacobs
{"title":"Monitoring M-Protein, Therapeutic Antibodies, and Polyclonal Antibodies in a Multiparametric Mass Spectrometry Assay Provides Insight into Therapy Response Kinetics in Patients with Multiple Myeloma.","authors":"Charissa Wijnands, Peter G A Karel, Jolein Gloerich, Gad Armony, Anastasia Tzasta, Corrie M de Kat Angelino, Luciano Di Stefano, Vincent Bonifay, Theo M Luider, Martijn M VanDuijn, Sandra J Croockewit, Elizabeth A de Kort, Daan A R Castelijn, Claudia A M Stege, Hans J C T Wessels, Alain J van Gool, Niels W C J van de Donk, Joannes F M Jacobs","doi":"10.3390/pharmaceutics17010135","DOIUrl":"10.3390/pharmaceutics17010135","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Multiple Myeloma (MM) is a hematologic malignancy caused by clonally expanded plasma cells that produce a monoclonal immunoglobulin (M-protein), a personalized biomarker. Recently, we developed an ultra-sensitive mass spectrometry method to quantify minimal residual disease (MS-MRD) by targeting unique M-protein peptides. Therapeutic antibodies (t-Abs), key in MM treatment, often lead to deep and long-lasting responses. However, t-Abs can significantly decrease the total polyclonal immunoglobulin (Ig) levels which require supplemental IgG infusion. Here, we demonstrate the simultaneous monitoring of M-proteins, t-Abs, and polyclonal Ig-titers using an untargeted mass spectrometry assay, offering a comprehensive view of therapy response. <b>Methods:</b> Sera collected between 2013 and 2024 from four patients and cerebrospinal fluid (CSF) from one patient who received various t-Abs were analyzed with MS-MRD. M-protein sequences were obtained with a multi-enzyme de novo protein sequencing approach. Unique peptides for M-proteins and t-Abs were selected based on linearity, sensitivity, and slope coefficient in serial dilutions. Ig constant regions were monitored using isotype-specific peptides. <b>Results:</b> The MS-MRD multiplex analysis provided detailed information on drug concentrations and therapy response kinetics. For example, in two patients with refractory disease over five lines of therapy, the MS-MRD analysis showed that the deepest responses were achieved with bispecific t-Ab (teclistamab) treatment. M-protein and t-Ab were also detectable in the CSF of one patient with MS-MRD. <b>Conclusions:</b> This proof-of-concept study shows that the multiplex monitoring of the M-protein, any t-Ab combination, and all Ig-isotypes within one mass spectrometry run is feasible and provides unique insight into therapy response kinetics.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11769374/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040807","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-19DOI: 10.3390/pharmaceutics17010133
Marcus Flowers, Alex Paulsen, Claire R W Kaiser, Adam B Tuma, Hubert H Lim, Brenda M Ogle, Chun Wang
{"title":"Alginate Hydrogel Beads with a Leakproof Gold Shell for Ultrasound-Triggered Release.","authors":"Marcus Flowers, Alex Paulsen, Claire R W Kaiser, Adam B Tuma, Hubert H Lim, Brenda M Ogle, Chun Wang","doi":"10.3390/pharmaceutics17010133","DOIUrl":"10.3390/pharmaceutics17010133","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Focused ultrasound has advantages as an external stimulus for drug delivery as it is non-invasive, has high precision and can penetrate deep into tissues. Here, we report a gold-plated alginate (ALG) hydrogel system that retains highly water-soluble small-molecule fluorescein for sharp off/on release after ultrasound exposure. <b>Methods:</b> The ALG is crosslinked into beads with calcium chloride and layered with a polycation to adjust the surface charge for the adsorption of catalytic platinum nanoparticles (Pt NPs). The coated bead is subject to electroless plating, forming a gold shell. Ultrasound is applied to the gold-plated ALG beads and the release of fluorescein with or without ultrasound stimulation is quantified. <b>Results:</b> Polyethylenimine (PEI), not poly-L-lysine (PLL), is able to facilitate Pt NP adsorption. Gold shell thickness is proportional to the duration of electroless plating and can be controlled. Gold-plated ALG beads are impermeable to the fluorescein cargo and have nearly zero leakage. Exposure to focused ultrasound initiated the release of fluorescein with full release achieved after 72 h. <b>Conclusions:</b> The gold-plated ALG hydrogel is a new material platform that can retain highly water-soluble molecules with a sharp off/on release initiated by focused ultrasound.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768098/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143041012","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Chitosan Nanoparticles for Enhanced Immune Response and Delivery of Multi-Epitope <i>Helicobacter pylori</i> Vaccines in a BALB/c Mouse Model.","authors":"Rita Amaral, Tomás Concha, Jorge Vítor, António J Almeida, Cecília Calado, Lídia M Gonçalves","doi":"10.3390/pharmaceutics17010132","DOIUrl":"10.3390/pharmaceutics17010132","url":null,"abstract":"<p><p><b>Background/Objectives</b>: <i>Helicobacter pylori</i> is the leading cause of chronic gastritis, peptic ulcer, gastric adenocarcinoma, and mucosal-associated lymphoma. Due to the emerging problems with antibiotic treatment against <i>H. pylori</i> in clinical practice, <i>H. pylori</i> vaccination has gained more interest. Oral immunization is considered a promising approach for preventing initial colonization of this bacterium in the gastrointestinal tract, establishing a first line of defense at gastric mucosal surfaces. Chitosan nanoparticles can be exploited effectively for oral vaccine delivery due to their stability, simplicity of target accessibility, and beneficial mucoadhesive and immunogenic properties. <b>Methods</b>: In this study, new multi-epitope pDNA- and recombinant protein-based vaccines incorporating multiple <i>H. pylori</i> antigens were produced and encapsulated in chitosan nanoparticles for oral and intramuscular administration. The induced immune response was assessed through the levels of antigen-specific IgGs, secreted mucosal SIgA, and cytokines (IL-2, IL-10, and IFN-γ) in immunized BALB/C mice. <b>Results</b>: Intramuscular administration of both pDNA and recombinant protein-based vaccines efficiently stimulated the production of specific IgG2a and IgG1, which was supported by cytokines levels. Oral immunizations with either pDNA or recombinant protein vaccines revealed high SIgA levels, suggesting effective gastric mucosal immunization, contrasting with intramuscular immunizations, which did not induce SIgA. <b>Conclusions</b>: These findings indicate that both pDNA and recombinant protein vaccines encapsulated into chitosan nanoparticles are promising candidates for eradicating <i>H. pylori</i> and mitigating associated gastric diseases in humans.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768296/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040679","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-17DOI: 10.3390/pharmaceutics17010131
Yue Lv, Jiaoqin Xue, Pengfei Cui, Lin Qiu
{"title":"Spermine Significantly Increases the Transfection Efficiency of Cationic Polymeric Gene Vectors.","authors":"Yue Lv, Jiaoqin Xue, Pengfei Cui, Lin Qiu","doi":"10.3390/pharmaceutics17010131","DOIUrl":"10.3390/pharmaceutics17010131","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Non-viral vectors have gained recognition for their ability to enhance the safety of gene delivery processes. Among these, polyethyleneimine (PEI) stands out as the most widely utilized cationic polymer due to its accessibility. Traditional methods of modifying PEI, such as ligand conjugation, chemical derivatization, and cross-linking, are associated with intricate preparation procedures, limited transfection efficiency, and suboptimal biocompatibility. <b>Methods:</b> In this investigation, enhanced transfection efficiency was achieved through the straightforward physical blending of PEI carriers with spermine. <b>Results:</b> Transfection assays explored the maximal enhancement potential conferred by spermine, alongside further methodological refinements aimed at optimizing transfection efficacy, showcasing a potential increase of up to 40.7%. Through the comparison of different addition sequences of spermine, the optimal complex PEI/Spermine/DNA for transfection efficiency was selected. Characterization of PEI/Spermine/DNA revealed that, compared to PEI/DNA, its particle size increased to approximately 150 nm. Molecular dynamics simulation results revealed that spermine can enhance the interaction between PEI and DNA, thereby forming a system with lower energy and greater stability. Mechanistic inquiries studies also disclosed that spermine augments the endosomal escape capability of PEI carriers without altering pathways involved in the cellular uptake of gene nanoparticles, thereby facilitating heightened gene expression. <b>Conclusions:</b> PEI-Sper emerges as a promising non-viral vector for gene delivery, distinguished by its simplicity in preparation, cost-effectiveness, and superior transfection efficiency.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768368/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143041065","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-17DOI: 10.3390/pharmaceutics17010123
Toka T Elebyary, Amal A Sultan, Sally E Abu-Risha, Gamal M El Maghraby, Manna Amin
{"title":"Bilosomal Co-Encapsulated Tamoxifen and Propranolol for Potentiated Anti-Breast Cancer Efficacy: In Vitro and In Vivo Investigation.","authors":"Toka T Elebyary, Amal A Sultan, Sally E Abu-Risha, Gamal M El Maghraby, Manna Amin","doi":"10.3390/pharmaceutics17010123","DOIUrl":"10.3390/pharmaceutics17010123","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Tamoxifen (TAM) is an anti-breast cancer drug suffering from acquired resistance development, prompting cancer relapse. Propranolol (PRO)'s repurposing for cancer therapy has gained interest. This work aimed to investigate combined TAM/PRO therapy for potentiating the anti-breast cancer activity of TAM. The work probed bilosomes versus standard noisome for simultaneous oral and intratumor delivery of TAM and PRO. <b>Methods</b>: Bilosomes comprising Span60, cholesterol, and increasing concentrations of bile salts were prepared together with bile salts containing free standard niosomes. The vesicular size and morphology were characterized. The entrapment and release efficiencies of TAM and PRO from the tailored vesicles were determined. The in vivo investigations of anti-tumor activity of TAM with or without PRO employed the solid Ehrlich carcinoma model. <b>Results:</b> The vesicles of all fabricated dispersions were spherical and negatively charged, with a size ranging from 104 to 182 nm. The entrapment efficiency depended on the nature of the drug, recording values ranging from 87.5% to 97.8% for TAM and from 31.0% to 46.8% for PRO. Incorporation of bile salts into vesicles increased TAM and PRO release compared to standard niosomes. Oral administration of combined TAM/PRO bilosomes showed a significant reduction in tumor growth volume compared to that recorded following naked drug administration. Histopathological investigations reflected a significant decline in tumor giant cells and mitotic figures, implying the in vivo capability of the TAM/PRO combination to interfere with cancer cell proliferation and persistence. <b>Conclusions</b>: The overall results demonstrated the impact of repurposed PRO to enhance the anti-breast cancer activity of TAM when both were co-encapsulated into bilosomes.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768151/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040038","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaceuticsPub Date : 2025-01-17DOI: 10.3390/pharmaceutics17010122
Shradha Dattani, Xiaoling Li, Charina Lampa, Amanda Barriscale, Behzad Damadzadeh, David Lechuga-Ballesteros, Bhaskara R Jasti
{"title":"Development of Spray-Dried Micelles, Liposomes, and Solid Lipid Nanoparticles for Enhanced Stability.","authors":"Shradha Dattani, Xiaoling Li, Charina Lampa, Amanda Barriscale, Behzad Damadzadeh, David Lechuga-Ballesteros, Bhaskara R Jasti","doi":"10.3390/pharmaceutics17010122","DOIUrl":"10.3390/pharmaceutics17010122","url":null,"abstract":"<p><p><b>Objectives:</b> Micelles, liposomes, and solid lipid nanoparticles (SLNs) are promising drug delivery vehicles; however, poor aqueous stability requires post-processing drying methods for maintaining long-term stability. The objective of this study was to compare the potential of lipid-based micelles, liposomes, and SLNs for producing stable re-dispersible spray-dried powders with trehalose or a combination of trehalose and L-leucine. This study provides novel insights into the implementation of spray drying as a technique to enhance long-term stability for these lipid-based nanocarriers. <b>Methods:</b> Aqueous dispersions of LDV-targeted micelles, liposomes, and SLNs loaded with paclitaxel (PTX) were converted into re-dispersible powders using spray drying. The physicochemical properties of the nanocarriers were determined via scanning electron microscopy (SEM), Karl Fischer titration, differential scanning calorimetry (DSC), and dynamic light scattering (DLS). Short-term stability of all nanocarrier formulations was compared by measuring particle size, polydispersity index (PDI), and paclitaxel retention over 7 days at room temperature and at 4 °C. <b>Results:</b> Paclitaxel-loaded micelles, liposomes, and SLN formulations were successfully converted into well-dispersed spray-dried powders with acceptable yields (71.5 to 83.5%), low moisture content (<2%), and high transition temperatures (95.1 to 100.8 °C). SEM images revealed differences in morphology, where nanocarriers spray-dried with trehalose or a combination of trehalose and L-leucine produced smooth or corrugated particle surfaces, respectively. Reconstituted spray-dried nanocarriers maintained their nanosize and paclitaxel content over 7 days at 4 °C. <b>Conclusions:</b> The results of this study demonstrate the potential for the development of spray-dried lipid-based nanocarriers for long-term stability.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11768165/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040874","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}