Molecular Pharmaceutics最新文献_第9页

Dry Powder Inhalation of Nintedanib in Dibasic Calcium Phosphate for Targeting the Lungs in Pulmonary Fibrosis

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-04 DOI: 10.1021/acs.molpharmaceut.4c0119010.1021/acs.molpharmaceut.4c01190

Sanjay Singh, Frinto Francis, Mohit Barsain, Naresh Kothuri, Sonia Verma, Himanshu Bansode, Chakradhar J. V. U. S., Chunna Yadav, Ashok Kumar Sharma, Baisakhi Moharana, Gautam Panda and Amit Misra*,

{"title":"Dry Powder Inhalation of Nintedanib in Dibasic Calcium Phosphate for Targeting the Lungs in Pulmonary Fibrosis","authors":"Sanjay Singh, Frinto Francis, Mohit Barsain, Naresh Kothuri, Sonia Verma, Himanshu Bansode, Chakradhar J. V. U. S., Chunna Yadav, Ashok Kumar Sharma, Baisakhi Moharana, Gautam Panda and Amit Misra*, ","doi":"10.1021/acs.molpharmaceut.4c0119010.1021/acs.molpharmaceut.4c01190","DOIUrl":"https://doi.org/10.1021/acs.molpharmaceut.4c01190https://doi.org/10.1021/acs.molpharmaceut.4c01190","url":null,"abstract":"We prepared three variants of nintedanib dry powder inhalations (DPIs), one with dibasic calcium phosphate dihydrate (CaHPO4·2H2O) and two with lactose monohydrate as the carrier. CaHPO4 is not reported as a DPI excipient. We compared nintedanib pharmacokinetics and efficacy of the CaHPO4 formulation against bleomycin-induced pulmonary fibrosis following oral (3.875 mg/q12h) and DPI (200 μg/12 h) dosing in rats. Blood plasma Cmax, Tmax, and AUC resulting from oral dosing and DPI were 780 versus 147.5 μg/mL, 2.47 versus 2.22 h, and 5562 versus 1094 μg/mL·h, respectively. Drug remaining in the lungs and airways at the end of 12 h of dosing with the DPI (2.41 ± 0.37 μg/g of tissue) was double the amount found after oral dosing (1.25 ± 0.56 μg/g). Lung fibrosis induced in rats using bleomycin was resolved equally well by the two interventions administered q12h for 14 days. We submit that the reduction in systemic exposure to nintedanib and enhanced exposure to target tissue could offer significant therapeutic and safety advantages, and CaHPO4 can be easily developed as an excipient for DPIs.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":"22 3","pages":"1471–1479 1471–1479"},"PeriodicalIF":4.5,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143528435","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanosystems at Nexus: Navigating Nose-to-Brain Delivery for Glioblastoma Treatment. 纳米系统在Nexus：导航鼻部到脑部的胶质母细胞瘤治疗。

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 Epub Date: 2025-01-02 DOI: 10.1021/acs.molpharmaceut.4c00703

Tejas Girish Agnihotri, Akanksha Dahifale, Shyam Sudhakar Gomte, Biswajit Rout, Vasu Peddinti, Aakanchha Jain

{"title":"Nanosystems at Nexus: Navigating Nose-to-Brain Delivery for Glioblastoma Treatment.","authors":"Tejas Girish Agnihotri, Akanksha Dahifale, Shyam Sudhakar Gomte, Biswajit Rout, Vasu Peddinti, Aakanchha Jain","doi":"10.1021/acs.molpharmaceut.4c00703","DOIUrl":"10.1021/acs.molpharmaceut.4c00703","url":null,"abstract":"Glioblastoma multiforme (GBM) is considered to be one of the most devastating brain tumors with a shorter life expectancy. Several factors contribute to the dismal prognosis of GBM patients including the complicated nature of GBM, the ability of tumor cells to resist treatment, and the difficulty of delivering drugs to the brain because of barriers like the blood-brain barrier (BBB) and blood-tumor barrier (BTB). The unique challenges posed by the BBB in delivering therapeutic agents to the brain have led to the development of innovative nanotechnology-based approaches. By exploiting the olfactory/trigeminal pathway, nanosystems offer a promising strategy for targeted drug delivery to the brain, glioblastoma tumors in particular. This review contemplates varied nanocarriers, including polymeric nanoparticles, lipid-based nanosystems, in situ gel formulations, peptide, and stem cell-based nanoformulations, signifying their utility in brain targeting with minimal systemic side effects. Emerging trends in gene therapy and immunotherapy in the context of GBM treatment have also been discussed. Since safety is a paramount aspect for any drug product to get approved, this review also delves into toxicological considerations associated with intranasal delivery of nanosystems. Regulatory aspects and critical factors for the successful development of intranasal products are also explored in this review. Overall, this review underscores the significant advancements in nanotechnology for nose-to-brain delivery and its potential impact on GBM management.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":"599-619"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142918680","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Macrophage Membrane-Cloaked ROS-Responsive Albumin Nanoplatforms for Targeted Delivery of Curcumin to Alleviate Acute Liver Injury. 巨噬细胞膜覆盖ros响应白蛋白纳米平台靶向递送姜黄素以减轻急性肝损伤。

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 Epub Date: 2025-01-09 DOI: 10.1021/acs.molpharmaceut.4c00808

Dandan Hu, Zhenqiu Huang, Wenlong Li, Lianhai Shan, Ming-Yu Wu, Shun Feng, Yu Wan

{"title":"Macrophage Membrane-Cloaked ROS-Responsive Albumin Nanoplatforms for Targeted Delivery of Curcumin to Alleviate Acute Liver Injury.","authors":"Dandan Hu, Zhenqiu Huang, Wenlong Li, Lianhai Shan, Ming-Yu Wu, Shun Feng, Yu Wan","doi":"10.1021/acs.molpharmaceut.4c00808","DOIUrl":"10.1021/acs.molpharmaceut.4c00808","url":null,"abstract":"Developing low-toxicity, high-efficacy, and fast-acting strategies to manage acute liver injury (ALI) is critical due to its rapid progression and potential for severe outcomes. Curcumin (CUR) has shown promise in ALI therapy due to its ability to modulate the inflammatory microenvironment by scavenging reactive oxygen species (ROS). Nevertheless, CUR is highly hydrophobic limiting its bioavailability and effective in vivo transport, which hinders its further application. In this study, we developed an inflammatory microenvironment-targeted drug delivery system by covalently coupling human serum albumin (HSA) with ROS-sensitive thioketal linkers and loading it with CUR to form nanoparticles (HSA-TK/CUR). These nanoparticles were then coated with a macrophage membrane (CM@HSA-TK/CUR), resulting in negatively charged spherical particles (≈ -23.26 mV) with an average particle size of around 165 nm. ROS responsiveness was confirmed through drug release assays and enhanced ROS depletion was further demonstrated by Diacetyldichlorofluorescein (DCFH-DA) ROS detection experiments. CM@HSA-TK/CUR treatment resulted in a 94.7% reduction in ROS levels in inflammatory cells. In addition, cellular uptake and in vivo distribution experiments demonstrated that camouflaging HSA-TK/CUR with macrophage membranes significantly enhanced its targeting of the inflammatory microenvironment. The findings revealed that CM@HSA-TK/CUR rapidly accumulated in the injured liver within 6 h, inhibited the production of pro-inflammatory factors (IL-1β, IL-6, and TNF-α), shifted macrophage polarization from M1 to M2 in vivo, and protected hepatocytes from oxidative stress-associated cell death, significantly attenuating the inflammatory response in ALI mice. In conclusion, CM@HSA-TK/CUR has excellent potential in treating mice with ALI.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":"771-786"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142941498","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

MRI-Based Multifunctional Nanoliposomes for Enhanced HCC Therapy and Diagnosis. 基于mri的多功能纳米脂质体增强HCC治疗和诊断。

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 Epub Date: 2025-01-14 DOI: 10.1021/acs.molpharmaceut.4c00917

Jingxin Sun, Zhehao Jin, Yong Jin, Haidan Yuan, Guangyu Jin, Jishan Quan

{"title":"MRI-Based Multifunctional Nanoliposomes for Enhanced HCC Therapy and Diagnosis.","authors":"Jingxin Sun, Zhehao Jin, Yong Jin, Haidan Yuan, Guangyu Jin, Jishan Quan","doi":"10.1021/acs.molpharmaceut.4c00917","DOIUrl":"10.1021/acs.molpharmaceut.4c00917","url":null,"abstract":"The morbidity and mortality rates of hepatocellular carcinoma (HCC) are high and continue to increase. The antitumor effects of single therapies are limited because of tumor heterogeneity and drug resistance, and the lack of real-time monitoring of tumor progression during the treatment process leads to poor therapeutic outcomes. Therefore, novel nanodelivery platforms combining tumor therapy and diagnosis have garnered extensive attention. In this study, we developed a multifunctional nanodelivery vector, LPSD-DOX/siRNA, which was loaded with oleic acid-modified superparamagnetic iron oxide nanoparticles (OA-SPION) and the antitumor drug doxorubicin (DOX), further modified by DOTAP to carry small interfering RNA targeting phosphatidylinositol proteoglycan-3 (Glypican-3, GPC3) (siRNA-GPC3). These components were utilized for the combined treatment of HCC and tumor monitoring with magnetic resonance imaging. LPSD-DOX/siRNA exhibited high drug loading, high gene transfection efficiency, and low toxicity. Pharmacokinetic and in vivo distribution experiments showed that LPSD-DOX/siRNA significantly prolonged the circulation time of DOX and enhanced drug accumulation at the tumor site. Magnetic resonance imaging demonstrated that LPSD-DOX/siRNA can serve as a T2 imaging contrast agent to enhance the imaging contrast between the tumor site and other tissues and facilitate the imaging monitoring of tumor tissues. Antitumor experiments revealed that the effects of DOX were promoted by inhibiting the expression of GPC3 protein in HepG2 cell-transplanted tumors, with increased tumor apoptosis. In conclusion, LPSD-DOX/siRNA serves as a promising strategy for combination therapy and monitoring of HCC, with significant potential in antitumor therapy.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":"787-807"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142981974","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enhancement of Transdermal Drug Delivery: Integrating Microneedles with Biodegradable Microparticles. 增强经皮给药：整合微针与可生物降解微粒。

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 Epub Date: 2025-01-17 DOI: 10.1021/acs.molpharmaceut.4c01202

Hiep X Nguyen, Thomas Kipping, Ajay K Banga

{"title":"Enhancement of Transdermal Drug Delivery: Integrating Microneedles with Biodegradable Microparticles.","authors":"Hiep X Nguyen, Thomas Kipping, Ajay K Banga","doi":"10.1021/acs.molpharmaceut.4c01202","DOIUrl":"10.1021/acs.molpharmaceut.4c01202","url":null,"abstract":"This investigation aimed to enhance transdermal methotrexate delivery through human skin by employing Dr. Pen microneedles and poly(d,l-lactide-co-glycolide) acid microparticles formulated from eight polymer grades (Expansorb DLG 95-4A, DLG 75-5A, DLG 50-2A, DLG 50-5A, DLG 50-8A, DLG 50-6P, DLG 50-7P, and DLL 10-15A). A comprehensive characterization of the microparticles was performed, encompassing various parameters such as size, charge, morphology, microencapsulation efficiency, yield, release kinetics, and chemical composition. The efficacy of microneedles in disrupting skin integrity was demonstrated by scanning electron microscopy, dye binding, histological examination, confocal laser microscopy, and pore size analysis. Microneedle-mediated skin microporation led to a substantial reduction in skin electrical resistance and a concomitant increase in transepidermal water loss. In vitro permeation experiments using human skin delivered microparticles into microporated skin and demonstrated a considerable difference in methotrexate delivery among the polymer groups. Microneedle treatment significantly amplified cumulative drug delivery, steady-state flux, diffusion coefficient, permeability coefficient, and drug concentration within skin layers while concurrently diminishing lag time (p < 0.05). Furthermore, a robust correlation was established between microparticle properties (cumulative release, release rate, encapsulation efficiency) and drug deposition in the skin. In conclusion, the synergistic combination of Dr. Pen microneedles and PLGA microparticles facilitated enhanced and regulated transdermal methotrexate delivery.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":"984-1009"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142996293","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Biocompatibility of Phosphorus Dendrimers and Their Antibacterial Properties as Potential Agents for Supporting Wound Healing. 磷树状大分子的生物相容性及其抗菌性能作为支持伤口愈合的潜在药物。

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 Epub Date: 2025-01-11 DOI: 10.1021/acs.molpharmaceut.4c01156

Beata Bielska, Natalia Wrońska, Joanna Kołodziejczyk-Czepas, Serge Mignani, Jean-Pierre Majoral, Iveta Waczulikova, Katarzyna Lisowska, Maria Bryszewska, Katarzyna Miłowska

{"title":"Biocompatibility of Phosphorus Dendrimers and Their Antibacterial Properties as Potential Agents for Supporting Wound Healing.","authors":"Beata Bielska, Natalia Wrońska, Joanna Kołodziejczyk-Czepas, Serge Mignani, Jean-Pierre Majoral, Iveta Waczulikova, Katarzyna Lisowska, Maria Bryszewska, Katarzyna Miłowska","doi":"10.1021/acs.molpharmaceut.4c01156","DOIUrl":"10.1021/acs.molpharmaceut.4c01156","url":null,"abstract":"Dendrimers are a wide range of nanoparticles with desirable properties that can be used in many areas of medicine. However, little is known about their potential use in wound healing. This study examined the properties of phosphorus dendrimers that were built on a cyclotriphosphazene core and pyrrolidinium (DPP) or piperidinium (DPH) terminated groups, to be used as potential factors that support wound healing (in vitro). Therefore, the degree of toxicity of the tested compounds for human erythrocytes and the human fibroblast cell line (BJ) was determined, and it was found that at low concentrations, the tested compounds are compatible with blood. The influence of phosphorus dendrimers on plasma proteins (human serum albumin (HSA) and fibrinogen) was examined, with a lack of conformational changes in the structure of these proteins, suggesting that their physiological function was not disturbed. The effects on plasma coagulation cascade and fibrinolysis were also assessed, and it was found that phosphorus dendrimers in low concentrations are blood compatible and interfere neither with coagulation processes nor in clot breakdown. Skin injuries, especially chronic wounds, are also susceptible to infection; therefore, the antimicrobial potential of dendrimers was tested, and it was found that these dendrimers had antibacterial activity against both Gram-negative and Gram-positive bacteria. The highest activity of the tested compounds was found for higher applied concentrations.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":"927-939"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11795522/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142963351","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

New Trends in Brain Shuttle Peptides

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 DOI: 10.1021/acs.molpharmaceut.4c0132710.1021/acs.molpharmaceut.4c01327

Roger Prades, Meritxell Teixidó and Benjamí Oller-Salvia*,

引用次数: 0

In Vitro Drug Release and Ex Vivo Dermal Drug Permeation Studies of Selected Commercial Benzoyl Peroxide Topical Formulations: Correlation Between Human and Porcine Skin Models.

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 DOI: 10.1021/acs.molpharmaceut.4c01058

Murilo de Souza Brighenti, Lilian Rosário da Silva Montanheri, Marcelo Dutra Duque, Newton Andreo-Filho, Patricia Santos Lopes, Maria Teresa Junqueira Garcia, Lorraine Mackenzie, Vânia Rodrigues Leite-Silva

{"title":"In Vitro Drug Release and Ex Vivo Dermal Drug Permeation Studies of Selected Commercial Benzoyl Peroxide Topical Formulations: Correlation Between Human and Porcine Skin Models.","authors":"Murilo de Souza Brighenti, Lilian Rosário da Silva Montanheri, Marcelo Dutra Duque, Newton Andreo-Filho, Patricia Santos Lopes, Maria Teresa Junqueira Garcia, Lorraine Mackenzie, Vânia Rodrigues Leite-Silva","doi":"10.1021/acs.molpharmaceut.4c01058","DOIUrl":"https://doi.org/10.1021/acs.molpharmaceut.4c01058","url":null,"abstract":"In vitro release testing (IVRT) serves as a crucial tool to assess the quality, physicochemical behavior, and performance of semisolid formulations already available on the market. In vitro skin permeation studies (IVPT) are widely used to evaluate the safety and efficacy profiles of topical drugs, utilizing biological membranes prepared from ex vivo human and porcine skin tissues. This study aimed to develop and validate a discriminative IVRT method to evaluate various marketed topical benzoyl peroxide formulations. Additionally, IVPT was employed to assess skin permeation and retention profiles of these formulations, comparing porcine skin results with those obtained by using ex vivo human skin tissues. Physicochemical differences among the evaluated benzoyl peroxide formulations were identified, with the poloxamer-based formulation exhibiting a higher release rate. IVPT using both porcine and human skin differentiated retention and skin permeation profiles, with the poloxamer-based formulation demonstrating greater skin retention capacity compared to the other formulations evaluated. Similar conclusions on benzoyl peroxide retention and cutaneous permeation were drawn from both porcine and human skin IVPT tests, confirming the correlation between the two models.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143121785","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

End Plate Chondrocyte-Derived Exosomal miR-133a-3p Alleviates Intervertebral Disc Degeneration by Targeting the NF-κB Signaling Pathway through the miR-133a-3p/MAML1 Axis.

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 DOI: 10.1021/acs.molpharmaceut.4c00962

Qiuwei Li, Ruocheng Guo, Chenhao Zhao, Xuewu Chen, Hong Wang, Cailiang Shen

{"title":"End Plate Chondrocyte-Derived Exosomal miR-133a-3p Alleviates Intervertebral Disc Degeneration by Targeting the NF-κB Signaling Pathway through the miR-133a-3p/MAML1 Axis.","authors":"Qiuwei Li, Ruocheng Guo, Chenhao Zhao, Xuewu Chen, Hong Wang, Cailiang Shen","doi":"10.1021/acs.molpharmaceut.4c00962","DOIUrl":"https://doi.org/10.1021/acs.molpharmaceut.4c00962","url":null,"abstract":"Chondrocyte-derived exosomes have shown efficacy in differentiating osteoarthritis-affected cartilage. Intervertebral disc degeneration (IVDD) and osteoarthritis often affect facet joints of the spine and show common epidemiological and pathophysiological characteristics. However, the potential of chondrocyte-derived exosomes for treating IVDD remains unclear. The present study aimed to confirm the effect of end plate chondrocyte-derived exosomes (EPC-Exo) on IVDD and elucidate the underlying mechanism. EPC-Exos were isolated and identified by ultracentrifugation, Western blotting, electron microscopy, and nanoparticle tracking analysis. In the in vitro, EPC-Exo uptake by nucleus pulposus (NP) cells reduced cell death by blocking the nuclear factor-κB (NF-κB) signaling pathway. In the in vivo study, EPC-Exos injected into rat intervertebral discs mitigated lipopolysaccharide-induced IVDD, as revealed by a decreased loss of disc height and improved magnetic resonance imaging findings and histological scores. Bioinformatics and sequencing analyses indicated that EPC-Exos alleviated IVDD through the miR-133a-3p/MAML1 axis. The present study suggests that EPC-Exos reduced IVDD incidence via the miR-133a-3p/MAML1 axis-mediated suppression of NF-κB signaling, which prevented the pyroptosis of NP cells.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143077958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

In Vitro Drug Release and Ex Vivo Dermal Drug Permeation Studies of Selected Commercial Benzoyl Peroxide Topical Formulations: Correlation Between Human and Porcine Skin Models

IF 4.5 2区医学

Molecular Pharmaceutics Pub Date : 2025-02-03 DOI: 10.1021/acs.molpharmaceut.4c0105810.1021/acs.molpharmaceut.4c01058

Murilo de Souza Brighenti, Lilian Rosário da Silva Montanheri, Marcelo Dutra Duque, Newton Andreo-Filho, Patricia Santos Lopes, Maria Teresa Junqueira Garcia, Lorraine Mackenzie and Vânia Rodrigues Leite-Silva*,

{"title":"In Vitro Drug Release and Ex Vivo Dermal Drug Permeation Studies of Selected Commercial Benzoyl Peroxide Topical Formulations: Correlation Between Human and Porcine Skin Models","authors":"Murilo de Souza Brighenti, Lilian Rosário da Silva Montanheri, Marcelo Dutra Duque, Newton Andreo-Filho, Patricia Santos Lopes, Maria Teresa Junqueira Garcia, Lorraine Mackenzie and Vânia Rodrigues Leite-Silva*, ","doi":"10.1021/acs.molpharmaceut.4c0105810.1021/acs.molpharmaceut.4c01058","DOIUrl":"https://doi.org/10.1021/acs.molpharmaceut.4c01058https://doi.org/10.1021/acs.molpharmaceut.4c01058","url":null,"abstract":"In vitro release testing (IVRT) serves as a crucial tool to assess the quality, physicochemical behavior, and performance of semisolid formulations already available on the market. In vitro skin permeation studies (IVPT) are widely used to evaluate the safety and efficacy profiles of topical drugs, utilizing biological membranes prepared from ex vivo human and porcine skin tissues. This study aimed to develop and validate a discriminative IVRT method to evaluate various marketed topical benzoyl peroxide formulations. Additionally, IVPT was employed to assess skin permeation and retention profiles of these formulations, comparing porcine skin results with those obtained by using ex vivo human skin tissues. Physicochemical differences among the evaluated benzoyl peroxide formulations were identified, with the poloxamer-based formulation exhibiting a higher release rate. IVPT using both porcine and human skin differentiated retention and skin permeation profiles, with the poloxamer-based formulation demonstrating greater skin retention capacity compared to the other formulations evaluated. Similar conclusions on benzoyl peroxide retention and cutaneous permeation were drawn from both porcine and human skin IVPT tests, confirming the correlation between the two models.","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":"22 3","pages":"1365–1372 1365–1372"},"PeriodicalIF":4.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/epdf/10.1021/acs.molpharmaceut.4c01058","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143528432","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0