Journal of pharmaceutical sciences最新文献

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Computer modeling of bevacizumab drug distribution after intravitreal injection in rabbit and human eyes.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-16 DOI: 10.1016/j.xphs.2024.12.005
Jabia M Chowdhury, Eduardo A Chacin Ruiz, Matthew P Ohr, Katelyn E Swindle-Reilly, Ashlee N Ford Versypt
{"title":"Computer modeling of bevacizumab drug distribution after intravitreal injection in rabbit and human eyes.","authors":"Jabia M Chowdhury, Eduardo A Chacin Ruiz, Matthew P Ohr, Katelyn E Swindle-Reilly, Ashlee N Ford Versypt","doi":"10.1016/j.xphs.2024.12.005","DOIUrl":"10.1016/j.xphs.2024.12.005","url":null,"abstract":"<p><p>Age-related macular degeneration (AMD) is a progressive eye disease that causes loss of central vision and has no cure. Wet AMD is the late neovascular form treated with vascular endothelial growth factor (VEGF) inhibitors. VEGF is the critical driver of wet AMD. One common off-label anti-VEGF drug used in AMD treatment is bevacizumab. Experimental efforts have been made to investigate the pharmacokinetic (PK) behavior of bevacizumab in vitreous and aqueous humor. Still, the quantitative effect of elimination routes and drug concentration in the macula are not well understood. In this work, we developed two spatial models representing rabbit and human vitreous to better understand the PK behavior of bevacizumab. This study explores different cases of drug elimination and the effects of injection location on drug concentration profiles. The models are validated by comparing them with experimental data. Our results suggest that anterior elimination is dominant for bevacizumab clearance from rabbit vitreous, whereas both anterior and posterior elimination have similar importance in drug clearance from the human vitreous. Furthermore, results indicate that drug injections closer to the posterior segment of the vitreous help maintain relevant drug concentrations for longer, improving bevacizumab duration of action in the vitreous. The rabbit and human models predict bevacizumab concentration in the vitreous and fovea, enhancing knowledge and understanding of wet AMD treatment.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854459","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}
引用次数: 0
Photothermal therapeutic effect by gold nanostars/extracellular vesicles nanocomplex on melanoma cells.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-16 DOI: 10.1016/j.xphs.2024.12.014
Kazuki Sato, Koki Ogawa, Tatsuaki Tagami, Tetsuya Ozeki
{"title":"Photothermal therapeutic effect by gold nanostars/extracellular vesicles nanocomplex on melanoma cells.","authors":"Kazuki Sato, Koki Ogawa, Tatsuaki Tagami, Tetsuya Ozeki","doi":"10.1016/j.xphs.2024.12.014","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.12.014","url":null,"abstract":"<p><p>Photothermal therapy (PTT) is a method for treating cancer using the heat generated by light irradiation, often in combination with light-absorbing materials. Efficient PTT requires a drug delivery system to deliver light-absorbing materials to cancerous tissues. Gold nanostars (GNSs) enable efficient PTT through absorbing long-wavelength light. In this study, we established a platform for preparing GNS-loaded extracellular vesicles (EVs), that were expected to provide the combined biological functionality of EVs and photothermal conversion properties. By electrostatically binding cationic polyethylene glycol (PEG)-modified GNSs (PEG-GNSs) to naturally negatively charged EVs, EV/PEG-GNS nanocomplexes (EV-GNSs) were obtained by simply mixing the two components. The prepared EV-GNSs were approximately 200 nm in size and exhibited a negative surface charge. The surface protein marker of EVs, CD63, was detected using western blot, suggesting that the EVs were intact. In vitro evaluation showed that EV-GNSs exhibited better photothermal conversion properties than PEG-GNSs alone. When EV-GNSs were added to the cells, high laser-responsive cytotoxicity was observed following laser irradiation. Thus, EV-GNSs developed in this study may be suitable for PTT using gold-based nanoparticles.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854423","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}
引用次数: 0
The Impact of Volume of Dissolution Medium for Biopredictive Dissolution/Permeation Studies of Enabling Formulations: A Comparison of Two Brands of Telmisartan / Amlodipine Tablets.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-16 DOI: 10.1016/j.xphs.2024.12.010
Jonas Borregaard Eriksen, Johanna Milsmann, Martin Brandl, Annette Bauer-Brandl
{"title":"The Impact of Volume of Dissolution Medium for Biopredictive Dissolution/Permeation Studies of Enabling Formulations: A Comparison of Two Brands of Telmisartan / Amlodipine Tablets.","authors":"Jonas Borregaard Eriksen, Johanna Milsmann, Martin Brandl, Annette Bauer-Brandl","doi":"10.1016/j.xphs.2024.12.010","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.12.010","url":null,"abstract":"<p><p>For compendial dissolution testing of solid dosage forms, media volumes of 500 to 900 mL are used in apparatus I and II to ensure sink conditions. However, these volumes are considerably larger than those in the gastrointestinal tract. Thus, the experiments are not biomimetic and possibly not suitable for biopredictive dissolution testing. The present study investigates the influence of volumes of dissolution media in non-compendial dissolution/permeation settings. Dissolution/permeation studies of two commercial bilayer tablets (Twynsta® and Arrow) containing the active pharmaceutical ingredients telmisartan (40 mg) and amlodipine (10 mg) were evaluated using the MacroFlux tool with various biomimetic media mimicking fasted and fed states as well as biological variability (\"biorelevant\"). Particularly, the two-stage dissolution process of telmisartan from the tablets is interesting because the compound has a pH-dependent solubility, and 2-stage dissolution leads to supersaturation and precipitation upon pH shift. For telmisartan, lower dissolution volumes significantly induced precipitation, leading to lower permeation, while no precipitation was observed in the larger volume. The permeation of telmisartan was overly sensitive to both pH and micelle concentrations in the biomimetic media. Amlodipine showed complete dissolution under any conditions, which correlates with its known complete absorption in vivo. In conclusion, volumes of dissolution media (and their compositions) are key parameters and play a significant role for designing relevant biomimetic experiments used to predict the bioavailability of supersaturating systems.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854445","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}
引用次数: 0
Bioequivalence study of voriconazole for intravenous infusion in healthy Chinese subjects under fasting conditions.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-16 DOI: 10.1016/j.xphs.2024.12.012
Zhangqiang Xiang, Mupeng Li, Shaoting Cui, Chunyan Gan, Fangfang Liu, Qian Huang, Gang Mai, Lianlian Fan
{"title":"Bioequivalence study of voriconazole for intravenous infusion in healthy Chinese subjects under fasting conditions.","authors":"Zhangqiang Xiang, Mupeng Li, Shaoting Cui, Chunyan Gan, Fangfang Liu, Qian Huang, Gang Mai, Lianlian Fan","doi":"10.1016/j.xphs.2024.12.012","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.12.012","url":null,"abstract":"<p><strong>Objective: </strong>Voriconazole, a second-generation triazole, is used to prevent and treat invasive fungal infections. This study aimed to assess the bioequivalence and safety of test and reference voriconazole intravenous infusion under the fasting conditions.</p><p><strong>Methods: </strong>The study employed a randomized, open-label, single-dose, two-period, crossover trial design. Eligible subjects randomly assigned for screening, receiving either the test or reference voriconazole for intravenous infusion during the first period, with alternative products administered during the second period. The washout period lasted 7 days. The single administration dosage was fixed at 6mg/kg. Nineteen blood samples were collected at pre-dose and up to 46 h post-dose for each subject. The validated LC-MS/MS method was used to determine the concentration of voriconazole in plasma.</p><p><strong>Results: </strong>Twenty-four subjects were enrolled in the study, comprising 20 males and 4 females. The primary pharmacokinetic parameters (mean ± SD) were as follows: C<sub>max</sub> was 4631.20±744.80 and 5008.09±1020.77 ng/mL, AUC<sub>0-t</sub> was 27121.07±12658.03 and 28674.08±13118.05 ng*h/mL, and AUC<sub>0-∞</sub> was 28056.10±14428.76 and 29616.29±14783.70 ng*h/mL for the test and reference formulations, respectively. The 90% confidence intervals of geometric mean ratios for C<sub>max</sub>, AUC<sub>0-t</sub>, and AUC<sub>0-∞</sub> fell within the range of 80.00% to 125.00%. Both products were well tolerated and no serious adverse event was observed.</p><p><strong>Conclusion: </strong>The test and reference voriconazole intravenous infusion demonstrated bioequivalence and good tolerability.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854449","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}
引用次数: 0
Call for manuscript submissions to the Richard H. Guy dedicated issue.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-09 DOI: 10.1016/j.xphs.2024.11.012
Kenneth L Audus
{"title":"Call for manuscript submissions to the Richard H. Guy dedicated issue.","authors":"Kenneth L Audus","doi":"10.1016/j.xphs.2024.11.012","DOIUrl":"10.1016/j.xphs.2024.11.012","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142785307","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}
引用次数: 0
Attribute ranging as a coordinated strategy between drug substance and drug product to accelerate commercial process nomination.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-05 DOI: 10.1016/j.xphs.2024.11.008
Clara Hartmanshenn, Alexander Bechtold, Thomas Kwok, Jeff Mora, Nathan Contrella, Alex Confer, Rachel Bade, Teresa Andreani, Jonathan M E Hughes, Billy Chen, Eric Sirota, Lorenzo Codan, David J Lamberto, Yingju Xu, Nastaran Salehi, Stephen Crowley
{"title":"Attribute ranging as a coordinated strategy between drug substance and drug product to accelerate commercial process nomination.","authors":"Clara Hartmanshenn, Alexander Bechtold, Thomas Kwok, Jeff Mora, Nathan Contrella, Alex Confer, Rachel Bade, Teresa Andreani, Jonathan M E Hughes, Billy Chen, Eric Sirota, Lorenzo Codan, David J Lamberto, Yingju Xu, Nastaran Salehi, Stephen Crowley","doi":"10.1016/j.xphs.2024.11.008","DOIUrl":"10.1016/j.xphs.2024.11.008","url":null,"abstract":"<p><p>To make investigational drug candidates available to patients sooner, timelines for drug development are becoming shorter. Synthesis route scouting for active pharmaceutical ingredients (API) and drug product development often must occur simultaneously, requiring formulators to make decisions regarding drug product process selection before commercial API route finalization. Alternatively, the formulation strategy may be locked, thereby constraining drug substance processes with strict API attribute requirements. Critical quality attributes of the drug product can depend heavily on the API, yet final physical attributes may not be known early on in development. Furthermore, the desire to reduce pill burden means higher drug loading in formulations, leaving little room for excipients to compensate for suboptimal API performance. The opposing challenges of API synthetic route and drug product formulation development typically lead to elongated development timelines requiring an iterative approach. In this work, a coordinated strategy was designed and implemented to deliberately range API attributes via crystallization and milling techniques to enable robust assessment of downstream manufacturing and significantly reduce the time for final process selection. The study presented was conducted on a protease inhibitor targeted for treatment of Covid-19. Given the emergent need for treatment options, this dramatically accelerated approach was crucial for potential emergency use authorization (EUA).</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142791838","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}
引用次数: 0
Development of a thermal stabilizer formulation optimized by response surface methodology for Senecavirus A antigen.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-04 DOI: 10.1016/j.xphs.2024.11.013
Zhenru Hu, Jiankun Huang, Simiao Zhao, Huiying Zhou, Shiqi Sun, Xiaobo Wen, Xuhua Ran
{"title":"Development of a thermal stabilizer formulation optimized by response surface methodology for Senecavirus A antigen.","authors":"Zhenru Hu, Jiankun Huang, Simiao Zhao, Huiying Zhou, Shiqi Sun, Xiaobo Wen, Xuhua Ran","doi":"10.1016/j.xphs.2024.11.013","DOIUrl":"10.1016/j.xphs.2024.11.013","url":null,"abstract":"<p><p>Numerous members of the family Picornaviridae, such as the Senecavirus A (SVA) and foot-and-mouth disease virus (FMDV), exhibit thermal instability, resulting in the dissociation of viral particles, which affects the insufficient potency of the vaccine. Based on this characteristic, this study aimed to maintain the thermal stability of SVA by supplementing it with a stabilizer. Excipients, such as sucrose, mannitol, sorbitol, polyethylene glycol (PEG), L-arginine (L-Arg), glutamic acid (Glu), polyvinyl pyrrolidone (PVP), bovine serum albumin (BSA), and potassium chloride (KCl) dissolved in Tris-HCl buffer solution, retained the infectivity of SVA in the thermostability assay. Thermal stability formulations were developed by combining different excipients in disaccharide polyol systems and optimizing formulations using the Box-Behnken experimental design (BBD) combined with response surface methodology (RSM). Three significant factors were studied: sucrose 9.9%, sorbitol 9.9%, and L-Arg 0.06 mol/L against virus titer of thermal-resistance of SVA as a response. The formulation improved the stability of SVA, whose viral infectivity titer decreased by 10<sup>1.0</sup> TCID<sub>50</sub>/mL at 4°C, 25°C, and 37°C, respectively, until it decreased by 10<sup>1.21</sup> TCID<sub>50</sub>/mL at 7 d of incubation at 42°C. The combinational thermal stabilizer generated in this study enabled the stabilization of the SVA, which might contribute to storage and transportation when the cold chain is unavailable, especially in rural areas. Therefore, the thermal stabilizer is an efficient candidate stabilizer for picornavirus formulations, which keep picornavirus infectivity at various temperatures. Further optimization of this approach will provide new opportunities for the generation of stabilizer formulation from different stabilizers.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142791841","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}
引用次数: 0
Corrigendum to "Co-Delivery of Daunorubicin and Homoharringtonine in Folic Acid Modified-Liposomes for Enhancing Therapeutic Effect on Acute Myeloid Leukemia" [Journal of Pharmaceutical Sciences Volume 112 (2023) 123-131].
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-03 DOI: 10.1016/j.xphs.2024.11.026
Qi Liu, Lijun Luo, Xiaofeng Gao, Di Zhang, Xinqian Feng, Peng Yang, Hui Li, Shengjun Mao
{"title":"Corrigendum to \"Co-Delivery of Daunorubicin and Homoharringtonine in Folic Acid Modified-Liposomes for Enhancing Therapeutic Effect on Acute Myeloid Leukemia\" [Journal of Pharmaceutical Sciences Volume 112 (2023) 123-131].","authors":"Qi Liu, Lijun Luo, Xiaofeng Gao, Di Zhang, Xinqian Feng, Peng Yang, Hui Li, Shengjun Mao","doi":"10.1016/j.xphs.2024.11.026","DOIUrl":"10.1016/j.xphs.2024.11.026","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142785413","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}
引用次数: 0
In vitro model of reconstructed human corneal epithelium for the evaluation of ocular surface desiccation and protection with vitamin A enriched ophthalmic ointment.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-03 DOI: 10.1016/j.xphs.2024.11.022
Ignacio Alcalde, Cristina Sánchez-Fernández, Ángel Azpeitia, Natalia Vázquez, Manuel Chacón, Carla Martín, Jesús Merayo-Lloves
{"title":"In vitro model of reconstructed human corneal epithelium for the evaluation of ocular surface desiccation and protection with vitamin A enriched ophthalmic ointment.","authors":"Ignacio Alcalde, Cristina Sánchez-Fernández, Ángel Azpeitia, Natalia Vázquez, Manuel Chacón, Carla Martín, Jesús Merayo-Lloves","doi":"10.1016/j.xphs.2024.11.022","DOIUrl":"10.1016/j.xphs.2024.11.022","url":null,"abstract":"<p><p>The aim of this study was to evaluate the efficacy of a paraffin ointment enriched with vitamin A in the protection against severe desiccation using 2D and 3D corneal epithelial in vitro models. We used immortalized human corneal epithelial cell cultures to evaluate the efficacy of four compounds -a paraffin ointment enriched with vitamin A (vA-PFF) and its vehicle; an aqueous gel containing hydroxypropyl guar (HPG); and an aqueous gel containing sodium carboxymethylcellulose (CMC)- to preserve cell viability in an in vitro model of desiccation. WST-1 and Live/Dead assays were used to study cell viability. Protection against cell damage was evaluated using a tridimensional reconstructed human corneal epithelial stem cell model (QobuR-RhCE). Compared to CMC, the paraffin ointment produced a significant prosurvival effect and it was similar to hydroxypropyl guar (HPG). The effect of vA-PFF in the protection against cell damage in QobuR-RhCE was significantly higher than CMC and HPG. Our results suggested that reconstructed 3D human corneal epithelia are sensitive tools to evaluate the efficacy of topical formulations against chemical damage and severe desiccation, indicating that would be an alternative method to animal experimentation, valid to use in ocular drug screening. vA-PFF caused no toxicity to cells in culture and was effective against extreme desiccation and cell damage in vitro 2 D and 3D models.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142785508","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}
引用次数: 0
Optimization and preparation of doxycycline-loaded chitosan nanoparticles using Box-Behnken design for better diabetic wound healing.
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2024-12-02 DOI: 10.1016/j.xphs.2024.11.014
Harish Bhardwaj, Ram Kumar Sahu, Rajendra Kumar Jangde
{"title":"Optimization and preparation of doxycycline-loaded chitosan nanoparticles using Box-Behnken design for better diabetic wound healing.","authors":"Harish Bhardwaj, Ram Kumar Sahu, Rajendra Kumar Jangde","doi":"10.1016/j.xphs.2024.11.014","DOIUrl":"10.1016/j.xphs.2024.11.014","url":null,"abstract":"<p><p>A diabetic wound is one of the most devastating difficulties associated with diabetes and leads to significant death and morbidity. Hence, the aim was to make Doxycycline-loaded chitosan nanoparticles (DOX-CNPs) using ionic gelation with a cross-linking technique. In the Box-Behnken design, the DOX-CNPs were optimized by considering the effects of the following 3 variables independently, namely chitosan, sodium tripolyphosphate in volume ratio, strength of chitosan and sodium tripolyphosphate, among several response variables related to nanoparticle properties. The Fourier transform infrared, transmission electron microscopy, differential scanning calorimeter, X-ray diffraction, particle size, entrapment efficiency, and drug release in-vitro were used to characterized the nanoparticles. Additionally, DPPH scavenging activity and activity against Escherichia coli and Staphylococcus aureus bacteria and in vivo characterization were carried out to optimize DOX-CNPs. Then effective delivery of DOX-CNPs is incorporated in chitosan hydrogel for diabetic wounds. The findings of this study indicate that DOX-CNPs exhibit free radical scavenging properties, demonstrate significant antibacterial activity, and enhance cell viability and migration in an in vitro wound healing assay using the L929 fibroblast cell line, and in vivo demonstrate increased blood vessels, collagen deposition epithelization. Chitosan could be used as a drug carrier in a DOX-chitosan-NP system to help develop procedures that can be used in the lab and to treat diabetic wounds.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":""},"PeriodicalIF":3.7,"publicationDate":"2024-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142780486","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}
引用次数: 0
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