Pharmaceutics最新文献

{"title":"An Insight to Nanoliposomes as Smart Radiopharmaceutical Delivery Tools for Imaging Atherosclerotic Plaques: Positron Emission Tomography Applications.","authors":"Reabetswe Sebatana, Kahwenga D Kudzai, Allan Magura, Amanda Mdlophane, Jan Rijn Zeevaart, Mike Sathekge, Maryke Kahts, Sipho Mdanda, Bwalya Angel Witika","doi":"10.3390/pharmaceutics17020240","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020240","url":null,"abstract":"<p><p>Atherosclerosis is a chronic progressive disease which is known to cause acute cardiovascular events as well as cerebrovascular events with high mortality. Unlike many other diseases, atherosclerosis is often diagnosed only after an acute or fatal event. At present, the clinical problems of atherosclerosis mainly involve the difficulty in confirming the plaques or identifying the stability of the plaques in the early phase. In recent years, the development of nanotechnology has come with various advantages including non-invasive imaging enhancement, which can be studied for the imaging of atherosclerosis. For targeted imaging and atherosclerosis treatment, nanoliposomes provide enhanced stability, drug administration, extended circulation, and less toxicity. This review discusses the current advances in the development of tailored liposomal nano-radiopharmaceutical-based techniques and their applications to atherosclerotic plaque diagnosis. This review further highlights liposomal nano-radiopharmaceutical localisation and biodistribution-key processes in the pathophysiology of atherosclerosis. Finally, this review discusses the direction and future of liposomal nano-radiopharmaceuticals as a potential clinical tool for the assessment and diagnosis of atherosclerotic plaque.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503291","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Tailored Intranasal Albumin Caged Selegiline-α Synuclein siRNA Liposome with Improved Efficiency in Parkinson's Model.","authors":"Ahmed A Katamesh, Hend Mohamed Abdel-Bar, Mohammed Khaled Bin Break, Shimaa M Hassoun, Gehad Mohammed Subaiea, Amr Radwan, Hadel A Abo El-Enin","doi":"10.3390/pharmaceutics17020243","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020243","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Parkinson's disease (PD) is a progressive neuro-degenerative disorder characterized by α-synuclein aggregation, which promotes neuronal death and accelerates neurodegeneration. Small interfering RNA (siRNA) can reduce α-synuclein levels, but its therapeutic potential is limited by poor stability and delivery challenges. Similarly, Selegiline (Sel), a monoamine oxidase-B (MAO-B) inhibitor, has low bioavailability, restricting its effectiveness. This study aims to develop an intranasal (IN) albumin-coated liposomal system (C-Lip_Sel-siSNCA2) for the co-delivery of Sel and α-synuclein-targeting siRNA (siSNCA2) to enhance brain targeting and therapeutic efficacy. <b>Methods:</b> Liposomes were prepared using the ethanol injection method and optimized via D-optimal design for size, charge, and encapsulation efficiency (EE%). The optimized formulation was coated with human serum albumin (HSA) and characterized for stability, cellular uptake, and gene silencing. In vivo pharmacokinetics and pharmacodynamics were assessed in a rotenone-induced PD rat model to evaluate the motor function, biochemical markers, and brain-targeting efficiency. <b>Results:</b> Optimized liposomes had a particle size of 113.5 ± 6.8 nm, zeta potential of 6.2 ± 0.8 mV, and high EE% (Sel: 92.35%; siRNA: 78.66%). Albumin coating increased size to 136.5 ± 10.3 nm and shifted zeta potential to -13.5 ± 1.4 mV, enhancing stability and targeting. IN administration achieved a 3-fold increase in brain area under the concentration-time curve (AUC) versus intravenous delivery. In PD rats, C-Lip_Sel-siSNCA2 improved motor and non-motor functions, restored dopamine levels, enhanced catalase activity, and reduced MAO-B levels, mitigating dopamine degradation and α-synuclein aggregation. <b>Conclusions:</b> This non-invasive, dual-action nanoplatform offers a targeted therapy for PD, combining siRNA gene silencing and MAO-B inhibition, with the potential for clinical translation in neurodegenerative diseases.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Quantifying Heart Rate Changes After Delta-9-Tetrahydrocannabinol Administration Using a PBPK-PD Model in Healthy Adults.","authors":"Lixuan Qian, Zhu Zhou","doi":"10.3390/pharmaceutics17020237","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020237","url":null,"abstract":"<p><p><b>Background</b>: As cannabis becomes legal in several U.S. states, the risk of THC-induced tachycardia increases. This study aimed to develop and verify a physiologically based pharmacokinetic-pharmacodynamic (PBPK-PD) model to assess the impact of THC and its active metabolite, 11-hydroxy-THC (11-OH-THC), on the heart rate of healthy adults. <b>Methods</b>: A PBPK-PD model for intravenous (IV) 11-OH-THC administration was first developed. Secondly, a PBPK-PD model for IV THC, combined with the metabolized 11-OH-THC, was established, verified, and validated. Direct PD models driven by the plasma, brain, and heart concentrations of THC and 11-OH-THC predicted using our previously verified PBPK model were tested for model development. Finally, the risks of tachycardia at a rest condition from various doses of oral and inhaled THC were simulated for 500 individuals aged 18-65 years, with a sex ratio of 1:1 and a baseline heart rate of 70 beats per minute. <b>Results</b>: The PD model was best described by a direct nonlinear E_max model driven by the sum of the total THC and 11-OH-THC concentrations in their effect compartments linked to their heart compartments. In 42 simulated dosing regimens with THC doses ranging from 2 to 69.4 mg, 97% of the observed heart rates or heart rate changes following THC administration fell within the 5th to 95th percentiles of the model-predicted values. Similarly, for two simulated 11-OH-THC IV doses, 93% of the observations fell within this range. Simulations indicated that half of the simulated population would experience tachycardia at doses of 60 mg and 15 mg of THC for oral and inhaled administration, respectively. The simulated risks of tachycardia based on specific conditions should be interpreted with caution. <b>Conclusions</b>: Our verified PBPK-PD model successfully describes the heart rate changes in healthy adults after IV, oral, and inhaled THC administration. This model provides a tool to predict the effects of THC and its primary metabolite on heart rates, offering valuable insights for assessing the risk of tachycardia in both clinical and recreational cannabis use.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development, Safety, and Therapeutic Evaluation of Voriconazole-Loaded Zein-Pectin-Hyaluronic Acid Nanoparticles Using Alternative In Vivo Models for Efficacy and Toxicity.","authors":"Margani Taise Fin, Kelvin Sousa Dos Santos, Marcos William de Lima Gualque, Rafaela Cristine Dos Santos, Natália Cristina Morici Aoki, Marcos Ereno Auler, Ana Marisa Fusco-Almeida, Maria José Soares Mendes-Gianinni, Rubiana Mara Mainardes","doi":"10.3390/pharmaceutics17020231","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020231","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Fungal infections caused by <i>Candida</i> species remain a significant clinical challenge, exacerbated by limitations in current antifungal therapies, including toxicity and poor bioavailability. This study aimed to develop and evaluate voriconazole-loaded zein-pectin-hyaluronic acid nanoparticles (ZPHA-VRC NPs) as a novel drug delivery system to enhance efficacy and reduce toxicity. Alternative in vitro and in vivo models were utilized to assess the safety and therapeutic potential of the nanoparticles. <b>Methods</b>: ZPHA-VRC NPs were prepared using a nanoprecipitation method and characterized for particle size, polydispersity index, zeta potential, and encapsulation efficiency. Antifungal activity was assessed via MIC assays against <i>Candida albicans</i>, <i>C. krusei</i>, and <i>C. parapsilosis</i>. Cytotoxicity was evaluated on Vero cells, while in vivo toxicity and efficacy were assessed using <i>Galleria mellonella</i> and <i>Caenorhabditis elegans</i> models. The therapeutic efficacy was further evaluated in an infected <i>Caenorhabditis elegans</i> model using survival and health scores. <b>Results</b>: ZPHA-VRC nanoparticles exhibited favorable physicochemical properties, including a particle size of approximately 192 nm, a polydispersity index of 0.079, a zeta potential of -24 mV, and an encapsulation efficiency of 34%. The nanoparticles retained antifungal activity comparable to free voriconazole while significantly reducing cytotoxicity. In vivo studies using <i>G. mellonella</i> and <i>C. elegans</i> demonstrated that ZPHA-VRC NPs markedly improved survival rates, reduced fungal burden, and enhanced health scores in infected models, outperforming the free drug. Additionally, the nanoparticles exhibited a superior safety profile, minimizing systemic toxicity while maintaining therapeutic efficacy. <b>Conclusions</b>: ZPHA-VRC NPs offer a safer and more effective delivery system for VRC, addressing the limitations of conventional formulations. The integration of alternative efficacy and safety models highlights their value in preclinical research.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Toxicity, Half-Life and Antitumor Activity of Phenyl 4-(2-Oxo-3-alkylimidazolidin-1-yl)benzenesulfonates as Novel Antimitotic CYP1A1-Targeted Prodrugs in Female Mouse Models.","authors":"Atziri Corin Chavez Alvarez, Chahrazed Bouzriba, Vincent Ouellette, Mathieu Gagné-Boulet, Alexandre Patenaude, Sylvie Pilote, René C-Gaudreault, Chantale Simard, Sébastien Fortin","doi":"10.3390/pharmaceutics17020233","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020233","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Chemoresistance of breast cancers (BCs) is a major impediment to current chemotherapeutics that urges the development of new drugs and new therapeutic approaches. To that end, phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates (PAIB-SOs) were recently prepared to fulfill some of the unmet needs with classic chemotherapeutics. PAIB-SOs are prodrugs bioactivated into potent antimitotics by the cytochrome P450 1A1 (CYP1A1), which is a frequent enzyme in resistant BC cells, but mostly missing in normal cells. Our screening program studies of PAIB-SO chemolibraries selected three prototypical PAIB-SOs as antimitotic prodrugs amenable for studies using BC animal models. <b>Methods</b>: Healthy female CD1^® IGS mice were treated with three prototypical PAIB-SOs, namely CEU-835, -934, and -938, for the determination of their toxicity and half-lives. Moreover, MCF7 tumor-bearing CD1-<i>Foxn1^nu</i> Nude female mice were treated with the three prototypical PAIB-SOs for the determination of their antitumor activity. <b>Results</b>: Herein, we show that multi-intravenous administrations of CEU-835, -934, and -938 at their maximal solubilities are well tolerated in healthy female CD1^® IGS mice, as depicted by the evaluation of distress behaviors, organ necropsy, total blood cell count, and histology. Moreover, the half-life of CEU-835, -934, and -938 administered intravenously in healthy CD1^® IGS female mice were 8.1, 23.2, and 21.5 h, respectively. Finally, their intravenous administrations of CEU-934 and -938 decreased MCF7 tumor growth as efficiently as paclitaxel in MCF7 tumor-bearing CD1-<i>Foxn1^nu</i> Nude mouse model. <b>Conclusions:</b> overall, our study demonstrated for the first time that pentyl-bearing PAIB-SOs are new CYP1A1-dependent prodrugs efficiently decrease breast cancer tumor growth, and show no side effects at their pharmacological concentration in mouse models.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503018","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Intravenous Nanoemulsions Loaded with Phospholipid Complex of a Novel Pyrazoloquinolinone Ligand for Enhanced Brain Delivery.","authors":"Tijana Stanković, Tanja Ilić, Branka Divović Matović, Milos Petkovic, Vladimir Dobričić, Ivan Jančić, Biljana Bufan, Kristina Jezdić, Jelena Đoković, Ivana Pantelić, Danijela Randjelović, Dishary Sharmin, James M Cook, Miroslav M Savić, Snežana Savić","doi":"10.3390/pharmaceutics17020232","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020232","url":null,"abstract":"<p><p><b>Background/Objectives</b>: The novel pyrazoloquinolinone ligand CW-02-79 shows a unique profile of selective binding to σ2 receptors, but its poor solubility in both water and lipids makes its research and development a burdensome task. We aimed to develop a phospholipid-complex-based nanoemulsion formulation containing CW-02-79 suitable for intravenous administration in preclinical research. <b>Methods</b>: The decorated and undecorated nanoemulsions were formulated and subjected to detailed physiochemical characterization. The delivery and exposure to CW-02-79 from selected nanoemulsions were examined in the in vitro blood-brain barrier model based on human-induced pluripotent stem-cell-derived microvascular endothelial cells, astrocytes, and pericytes, and in vivo neuropharmacokinetic study in rats, respectively. <b>Results</b>: The developed biocompatible nanoemulsions loaded with a CW-02-79-phospholipid complex at a mass ratio of 1:10 exhibited a small droplet size and narrow size distribution, with satisfactory physicochemical stability during steam sterilization and short-term storage at 25 °C. The analysis of protein binding interactions revealed that the PEGylated nanoemulsions had fewer observable interactions compared to the undecorated nanoemulsions, especially when 0.2% DSPE-PEG2000 and 0.1% DSPE-PEG2000-mannose were combined. An in vitro BBB study demonstrated that a substantial part of CW-02-79 present in the applied nanoemulsion is able to permeate the barrier. The quantification of CW-02-79 in plasma/brain homogenate and calculated pharmacokinetic parameters confirmed good systemic and brain availability after intravenous administration. There were subtle differences in the pharmacokinetic parameters in favor of a dual surface-functionalized nanoemulson containing the glucose transporter-1-targeting ligand (mannose). <b>Conclusions</b>: The developed and characterized nanoemulsions enable substantial brain exposure to CW-02-79 as a prerequisite for a pharmacologically and clinically relevant selective modulation of σ2 receptors.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Drug Delivery Systems Based on Metal-Organic Frameworks for Tumor Immunotherapy.","authors":"Ning Yang, Zongyan He, Tianqun Lang","doi":"10.3390/pharmaceutics17020225","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020225","url":null,"abstract":"<p><p>Metal-organic frameworks (MOFs) are a class of inorganic-organic hybrid nanoparticles formed by the coordination of metal ions/clusters and organic ligands. Due to their high porosities, large surface areas, adjustable structures, and responsiveness to light/sound, etc., MOFs have shown great clinical potential in the field of tumor therapy. Tumor immunotherapy exerts antitumor effects through reshaping tumor immune microenvironment, showing significant preclinical and clinical advantages. Based on the mechanisms of immunity activation, the tumor immunotherapy agents can be divided into chemotherapeutic agents, immunomodulators, enzymes, tumor vaccines and oligonucleotide drugs, etc. Herein, we review the MOFs-based drug delivery systems for tumor immunotherapy. The classification of MOFs, followed by their antitumor immunity activation mechanisms, are first introduced. Drug delivery systems based on MOFs with different immunotherapy agents are also summarized, especially the synergetic immunity activation mechanisms triggered by MOFs and their loadings. Furthermore, the merits and drawbacks of MOFs and the potential strategies for MOFs to promote their clinical applications are discussed.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bioadhesive Nanoparticles in Topical Drug Delivery: Advances, Applications, and Potential for Skin Disorder Treatments.","authors":"Rashed M Almuqbil, Bandar Aldhubiab","doi":"10.3390/pharmaceutics17020229","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020229","url":null,"abstract":"<p><p>Skin disorders are the fourth most common cause of all diseases, which affect nearly one-third of the world's population. Topical drug delivery can be effective in treating a range of skin disorders, including microbial infections, skin cancer, dermatitis, burn injury, wounds, and psoriasis. Bioadhesive nanoparticles (BNPs) can serve as an efficient topical drug delivery system as they can serve dual purposes as bioadhesives and nanocarriers, which can mediate targeted drug delivery, prolong retention time, and deepen drug penetration through skin layers. There is an increasing demand for BNP-based applications in medicine because of their various advantages, including biodegradability, flexibility, biocompatibility, and enhanced adhesive strength. A number of BNPs have already been developed and evaluated as potential topical drug delivery systems. In addition, a range of studies have already been carried out to evaluate the potential of BNPs in the treatment of various skin disorders, including atopic dermatitis, irritant contact dermatitis, skin cancer, psoriasis, microbial infections, wounds, and severe burn injuries. This review article is timely and unique, because it provides an extensive and unique summary of the recent advances of BNPs in the treatment of wide-ranging skin disorders. Moreover, this review also provides a useful discussion on the bioadhesion mechanism and various biopolymers that can be used to prepare BNPs.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143502919","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fundamental and Targeted Approaches in Pulmonary Arterial Hypertension Treatment.","authors":"Ji Su Park, Yong Hwan Choi, Ji-Young Min, Jaeseong Lee, Gayong Shim","doi":"10.3390/pharmaceutics17020224","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020224","url":null,"abstract":"<p><p>Pulmonary arterial hypertension (PAH) is a chronic and progressive disease marked by vascular remodeling, inflammation, and smooth muscle cell proliferation, with limited treatment options focused primarily on symptom management. The multifactorial nature of PAH, encompassing genetic, autoimmune, and connective tissue contributions, complicates its treatment, while irreversible vascular changes, such as fibrosis, remain unaddressed by current therapies. Fundamental research on molecular pathways and targeted delivery systems has paved the way for advanced therapeutic strategies that aim to modify disease progression rather than merely manage symptoms. Nanoparticle-based drug delivery systems, leveraging controlled release and pulmonary targeting, offer a promising avenue to overcome these challenges. Such systems enable precise localization to pulmonary vasculature, minimize systemic side effects, and support emerging approaches like gene therapy and combination treatments. Future research should focus on refining nanoparticle formulations for personalized medicine, optimizing inhalation delivery systems, and integrating multi-target approaches to achieve curative outcomes in PAH. This review explores pathophysiology of PAH, current pharmacological strategies, and innovative nanoparticle-based therapies, emphasizing their potential to transform PAH treatment and address its underlying mechanisms.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503139","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"pH-Dependent Drug Delivery Systems for Ulcerative Colitis Treatment.","authors":"Yana Gvozdeva, Radiana Staynova","doi":"10.3390/pharmaceutics17020226","DOIUrl":"https://doi.org/10.3390/pharmaceutics17020226","url":null,"abstract":"<p><p>Inflammatory bowel diseases (IBDs), such as ulcerative colitis (UC) or Crohn's disease, are becoming a growing global problem due to the limitations of current treatments, which fail to address the needs of patients effectively. UC is characterized by the widespread inflammation of the mucosal lining, affecting both the rectum and the entire length of the colon. Over the past forty years, traditional treatments for IBDs have primarily relied on anti-inflammatory drugs and immunosuppressive medications. Treatment could be more effective if drugs could be specifically targeted to act directly on the colon. Conventional drug delivery systems for IBDs encounter numerous challenges on their way to the colon, such as physiological barriers and disease severity. To address these issues, pH-dependent carriers have emerged as a promising advancement, offering a more effective and tolerable treatment for UC. These carriers enable localized, targeted action, reducing side effects and preventing the premature clearance of drugs from inflamed colon tissues. pH-responsive systems are a leading approach for targeted drug release in colitis treatment as they take advantage of the varying pH levels throughout the gastrointestinal tract (GIT). By incorporating pH-sensitive polymers, they ensure drug protection and controlled release in the lower GIT. This review will discuss the advantages and limitations of pH-dependent drug delivery systems for colon-targeted drug delivery.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 2","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503302","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}