Pharmaceutical Development and Technology最新文献

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Intranasal bilosomes in thermosensitive hydrogel: advancing desvenlafaxine succinate delivery for depression management. 热敏水凝胶中的鼻内双分子:推进琥珀酸去文拉法辛在抑郁症治疗中的应用
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-07-15 DOI: 10.1080/10837450.2024.2376067
Tayseer M El-Nawawy, Yomna A Adel, Mahmoud Teaima, Noha N Nassar, Asmaa Ashraf Nemr, Inas Al-Samadi, Mohamed A El-Nabarawi, Sammar F Elhabal
{"title":"Intranasal bilosomes in thermosensitive hydrogel: advancing desvenlafaxine succinate delivery for depression management.","authors":"Tayseer M El-Nawawy, Yomna A Adel, Mahmoud Teaima, Noha N Nassar, Asmaa Ashraf Nemr, Inas Al-Samadi, Mohamed A El-Nabarawi, Sammar F Elhabal","doi":"10.1080/10837450.2024.2376067","DOIUrl":"10.1080/10837450.2024.2376067","url":null,"abstract":"<p><p>Depression, the second biggest cause of disability worldwide, is widespread. Many antidepressant medications, including Desvenlafaxine Succinate (D.V.S.), function by elevating neurotransmitter levels at the synapse through the inhibition of reabsorption by neurons. However, the effectiveness of these treatments is often limited by their inability to reach the brain using conventional administration methods. Bilosome-stabilized nanovesicles containing bile salts have drawn much interest because of their adaptability and versatility in various applications. This study aimed to address this issue by formulating intranasal bilosomes incorporated into a mucoadhesive <i>in situ</i> gel to deliver D.V.S. directly to the brain for depression treatment. The desvenlafaxine-loaded bilosomes were developed using a thin film hydration method based on the l-optimal design. They were intended to provide a more convenient route of administration for antidepressants, enhancing bioavailability and brain targeting through intranasal delivery. The study assessed the optimized bilosomes for particle size (311.21 ± 0.42 nm), Zeta potential (-<u>37.35 ± 0.43</u>)and encapsulation efficiency (99.53 ± 0.41%) and further evaluated them in <i>ex vivo</i> and <i>in vivo</i> pharmacokinetics studies. Pharmacokinetic data reveal enhanced brain uptake compared to a free drug. A statistically optimized bilosome formulation was determined. The intranasal administration of mucoadhesive <i>in situ</i> gel containing desvenlafaxine succinate-loaded bilosomes facilitated direct nose-to-brain drug delivery, improving brain bioavailability.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"663-674"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141535064","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Highly functionalized pH-triggered supramolecular nanovalve for targeted cancer chemotherapy. 用于癌症靶向化疗的高功能化 pH 触发超分子纳米阀
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-08-20 DOI: 10.1080/10837450.2024.2392271
Muhammad Kawish, Samina Parveen, Nimra Naz Siddiqui, Humera Jahan, Abdelbari Elhissi, Saira Yasmeen, Muhammad Raza Shah
{"title":"Highly functionalized pH-triggered supramolecular nanovalve for targeted cancer chemotherapy.","authors":"Muhammad Kawish, Samina Parveen, Nimra Naz Siddiqui, Humera Jahan, Abdelbari Elhissi, Saira Yasmeen, Muhammad Raza Shah","doi":"10.1080/10837450.2024.2392271","DOIUrl":"10.1080/10837450.2024.2392271","url":null,"abstract":"<p><p>Chemotherapeutic drug delivery systems are commonly limited by their short half-lives, poor bioavailability, and unsuccessful targetability. Herein, pH-responsive hybrid NPs consist of benzimidazole-coated mesoporous silica nanoparticles (BZ-MSN) loaded with naturally occurring flavonoid quercetin (QUE-BZ-MSN). The NPs were further capped with beta-cyclodextrin (BCD) to obtain our desired BCD-QUE-BZMSN, with a zeta potential around 7.05 ± 2.37 mV and diameter about 115.2 ± 19.02 nm. The abundance of BZ onto the nanoparticles facilitates targeted quercetin chemotherapy against model lung and liver cancer cell lines. FTIR, EDX, and NMR analyses revealed evidence of possible surface functionalizations. Powder XRD analysis showed that our designed BCD-QUE-BZMSN formulation is amorphous in nature. The UV and SEM showed that our designed BCD-QUE-BZMSN has high drug entrapment efficiency and a nearly spherical morphology. <i>In vitro,</i> drug release assessments show controlled pH-dependent release profiles that could enhance the targeted chemotherapeutic response against mildly acidic regions in cancer cell lines. The obtained BCD-QUE-BZMSN nanovalve achieved significantly higher cytotoxic efficacy as compared to QUE alone, which was evaluated by <i>in vitro</i> cellular uptake against liver and lung cancer cell lines, and the cellular morphological ablation was further confirmed <i>via</i> inverted microscopy. The outcomes of the study imply that our designed BCD-QUE-BZMSN nanovalve is a potential carrier for cancer chemotherapeutics.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"751-761"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141976336","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Transdermal drug delivery of rizatriptan using microneedles array patch: preparation, characterization and ex-vivo/in-vivo study. 使用微针阵列贴片透皮给药利扎曲普坦:制备、表征和体内外研究
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-08-24 DOI: 10.1080/10837450.2024.2393218
Suhair S Al-Nimry, Ahlam Z Alkilani, Nareman A Alda'ajeh
{"title":"Transdermal drug delivery of rizatriptan using microneedles array patch: preparation, characterization and ex-vivo/in-vivo study.","authors":"Suhair S Al-Nimry, Ahlam Z Alkilani, Nareman A Alda'ajeh","doi":"10.1080/10837450.2024.2393218","DOIUrl":"10.1080/10837450.2024.2393218","url":null,"abstract":"<p><p>Given the extensive first pass metabolism of rizatriptan in oral administration and its delayed absorption during a migraine attack as a result of gastric stasis, focus has been on transdermal delivery. The main purpose of this study is to prepare and assess transdermal formulation of rizatriptan, loaded on hydrogel microneedles delivery system, to avoid first pass metabolism and also improve its percutaneous permeation rate. Rizatriptan hydrogel microneedles were prepared using micromolding method and evaluated in terms of mechanical strength, encapsulation efficiency, permeation and in-vivo skin absorption. Different formulations of rizatriptan microneedles (F1-F5) were successfully prepared using different concentrations of carboxymethyl cellulose and gelatin type A. Rizatriptan hydrogel microneedles demonstrated favorable mechanical properties, including withstanding insertion forces, thereby enhancing its skin insertion ability. In permeation study, the percent cumulative drug released after 24 h ranged between 93.1-100% which means that microneedles were able to deliver the drug effectively. For in-vivo study, F3 formulation was selected due to its superior characteristics over other formulations as it exhibited the highest swelling capacity, and demonstrated favorable mechanical properties. Furthermore, F3 showcased the most controlled drug release over a 24-hour period. Relative bioavailability of F3 microneedles was 179.59% compared to oral administration based on the AUC<sub>0-24</sub>. The observed AUC<sub>0-24</sub> in F3 microneedles was statistically significant and 1.80 times greater than that in oral administration. The higher rizatriptan level in the microneedle demonstrated adequate drug permeability through the rat skin, suggesting the potential of microneedles for enhanced therapeutic effectiveness.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"776-789"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142004952","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Intravenous delivery of furosemide using lipid-based versus polymer-based nanocapsules: in vitro and in vivo studies. 使用脂质纳米胶囊和聚合物纳米胶囊静脉注射呋塞米:体外和体内研究。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-08-14 DOI: 10.1080/10837450.2024.2389855
Yasmine N Kamel, Eman M El-Marakby, Heba A Gad
{"title":"Intravenous delivery of furosemide using lipid-based versus polymer-based nanocapsules: <i>in vitro</i> and <i>in vivo</i> studies.","authors":"Yasmine N Kamel, Eman M El-Marakby, Heba A Gad","doi":"10.1080/10837450.2024.2389855","DOIUrl":"10.1080/10837450.2024.2389855","url":null,"abstract":"<p><strong>Objectives: </strong>Furosemide (FSM), a potent loop diuretic, is used to treat edema due to hypertension, congestive heart failure, and liver and renal failures. FSM applications are limited by its low bioavailability. Our aim is to use different nanoencapsulation strategies to control the release of FSM and enhance its pharmacokinetic properties.</p><p><strong>Methods: </strong>Two types of FSM-loaded nanocapsules, namely FSM-loaded lipid nanocapsules (LNCs) and polymeric nanocapsules (PNCs), were developed, physicochemically characterized, and subjected to pharmacokinetic and pharmacodynamic studies. Lipid nanocapsules were prepared by the simple phase inversion method using Labrafac<sup>TM</sup> lipid, while the polymeric nanocapsules were prepared by nanoprecipitation method using polycaprolactone polymer.</p><p><strong>Results: </strong>Transmission electron microscopy ascertains spherical structures, corroborating the nanometric diameter of both types of nanocapsules. The particle size of the optimized FSM-loaded LNCs and FSM-loaded PNCs was 32.19 ± 0.72 nm and 230.7 ± 5.13 nm, respectively. The percent entrapment efficiency was 63.56 ± 1.40% of FSM for the optimized PNCs. The <i>in vitro</i> release study indicated prolonged drug release compared to drug solutions. The two loaded nanocapsules systems succeeded in enhancing the pharmacokinetic parameters in comparison to the marketed FSM solution with superior diuretic activity (<i>p</i> < 0.05). The results of the stability study and the terminal sterilization by autoclave indicated the superiority of LNCs over PNCs in maintaining the physical parameters under storage conditions and the drastic conditions of sterilization.</p><p><strong>Conclusions: </strong>LNCs and PNCs are considered promising nanosysems for improving the diuretic effect of FSM.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"738-750"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141894089","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Experimental and numerical characterization of screw elements used in twin-screw extrusion. 双螺杆挤压工艺中所用螺杆元件的实验和数值特性分析
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-07-16 DOI: 10.1080/10837450.2024.2378323
Vanessa Düphans, Vincent Kimmel, Lukas Messing, Gerhard Schaldach, Markus Thommes
{"title":"Experimental and numerical characterization of screw elements used in twin-screw extrusion.","authors":"Vanessa Düphans, Vincent Kimmel, Lukas Messing, Gerhard Schaldach, Markus Thommes","doi":"10.1080/10837450.2024.2378323","DOIUrl":"10.1080/10837450.2024.2378323","url":null,"abstract":"<p><p>Hot melt extrusion by a co-rotating twin screw extruder is an important process in the pharmaceutical industry. Especially for quality by design aspects, a comprehensive process understanding is indispensable. The performance of conveying elements was determined as critical process parameter, and therefore an experimental and numerical framework was developed to analyze and compare variations. A test rig capable of measuring volume flow, pressure and torque with high accuracy and precision was designed and built. The 3D simulation was performed using computational fluid dynamics (CFD). A stationary model with impulse transmission and an apparent motion of the screws was applied. The experimental data were fitted to the model of Pawlowski, and parameters for the pressure (A<sub>1</sub>, A<sub>2</sub>) and power characteristics (B<sub>1</sub>, B<sub>2</sub>) were determined. Good agreement between experimental data and the model was observed. The simulation was significantly faster compared to common methods, and the results were consistent with the literature. Systematic investigations of a native and worn screw were performed with CFD resulting in a transport capacity increase and a pressure build up decrease for all tested screw elements. An experimental and simulation setup was generated to assess the performance of co-rotating twin screw elements. The experiments provided high-quality data, and the simulations exhibited high flexibility with low computational effort.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"675-683"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141559387","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dwell time on tableting: dwell time according to force versus geometric dwell time. 台模的停留时间:根据力计算的停留时间与几何停留时间。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-08-01 DOI: 10.1080/10837450.2024.2384446
Valentyn Mohylyuk
{"title":"Dwell time on tableting: dwell time according to force versus geometric dwell time.","authors":"Valentyn Mohylyuk","doi":"10.1080/10837450.2024.2384446","DOIUrl":"10.1080/10837450.2024.2384446","url":null,"abstract":"<p><p>Dwell time is an important parameter responsible for the material deformation and the mechanical and biopharmaceutical properties of the tablet. Thus, it is widely used for scale-up purposes. The geometric dwell time (GDT) can be assumed based on the shape of the punch head and the diameter and speed of the turret. This research is aimed to compare compaction simulator-recorded dwell time according to force (DTF) and the GDT calculated for the simulated rotary tablet press using the microcrystalline cellulose and calcium phosphate mixtures (CEOLUS™ UF-711 and DI-CAFOS<sup>®</sup> A60) in different proportions. Tablets were prepared, and DTF was analyzed with a compaction simulator (STYL'One Nano and Alix software) upon simulating a small rotary press at 70 rpm and a compression pressure of 10-50 kN (100-500 MPa). While GDT comprised of 14.4 ms, DTF was compression force and formulation dependent. The differences between the DTF values of the formulations decreased as the compression force increased, which was most pronounced at compression forces of 10 and 15 kN.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"719-726"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141752371","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Extracellular vesicle-based formulation of doxorubicin: drug loading optimization, characterization, and cytotoxicity evaluation in tumor spheroids. 基于细胞外囊泡的多柔比星制剂:在肿瘤球体内的药物负载优化、表征和细胞毒性评估。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-08-06 DOI: 10.1080/10837450.2024.2384448
Fatemeh Mehryab, Marzieh Ebrahimi, Hossein Baharvand, Azadeh Haeri, Faezeh Shekari
{"title":"Extracellular vesicle-based formulation of doxorubicin: drug loading optimization, characterization, and cytotoxicity evaluation in tumor spheroids.","authors":"Fatemeh Mehryab, Marzieh Ebrahimi, Hossein Baharvand, Azadeh Haeri, Faezeh Shekari","doi":"10.1080/10837450.2024.2384448","DOIUrl":"10.1080/10837450.2024.2384448","url":null,"abstract":"<p><p>Doxorubicin (DOX) is a chemotherapeutic with considerable efficacy, but its application is limited due to cardiotoxicity. Nanoparticles can improve DOX efficacy and prevent its adverse effects. Herein, DOX-loaded extracellular vesicles (DOX-EVs) were prepared using different loading methods including incubation, electroporation, and sonication in different hydration buffers to permeabilize nanostructures or desalinize DOX for improved entrapment. Different protein:drug (µg:µg) ratios of 1:10, 1:5, and 1:2, and incubation parameters were also investigated. The optimal formulation was characterized by western blotting, electron microscopy, Zetasizer, infrared spectroscopy, and release study. The cellular uptake and efficacy were investigated in MCF-7 spheroids <i>via</i> MTS assay, spheroid formation assay (SFA), confocal microscopy, and flow cytometry. The percentage of entrapment efficiency (EE) of formulations was improved from 1.0 ± 0.1 to 22.0 ± 1.4 using a protein:drug ratio of 1:2 and sonication in Tween 80 (0.1%w/v) containing buffer. Characterization studies verified the vesicles' identity, spherical morphology, and controlled drug release properties. Cellular studies revealed the accumulation and cytotoxicity of DOX-EVs in the spheroids, and SFA and confocal microscopy confirmed the efficacy and cellular localization. Flow cytometry results revealed a comparable and amplified efficacy for DOX-EV formulations with different cell origins. Overall, the EV formulation of DOX can be applied as a promising alternative with potential advantages.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"727-737"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141788844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Impact of surfactant raw material variability on extrudate clarity appearance (transparency) in HME continuous manufacturing. 在高密度聚乙烯连续生产过程中,表面活性剂原料的变化对挤出物清澈外观(透明度)的影响。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-07-13 DOI: 10.1080/10837450.2024.2378333
Claudia A Lohmann, Esther Bochmann, Samuel O Kyeremateng
{"title":"Impact of surfactant raw material variability on extrudate clarity appearance (transparency) in HME continuous manufacturing.","authors":"Claudia A Lohmann, Esther Bochmann, Samuel O Kyeremateng","doi":"10.1080/10837450.2024.2378333","DOIUrl":"10.1080/10837450.2024.2378333","url":null,"abstract":"<p><p>The appearance of an extrudate formulation was monitored during hot-melt extrusion (HME) continuous manufacturing over 3 days. The formulation matrix consisted of a polymeric component, copovidone, and a low molecular weight surfactant, polysorbate 80. Based on studies prior to the continuous manufacturing, the desired appearance of the target extrudate is translucent. Although process parameters such as feed rate and screw speed were fixed during the continuous manufacturing, the extrudate appearance changed over time from turbid to translucent. For root-cause investigation, the extrudates were analyzed offline by differential scanning calorimetry (DSC) and advanced polymer chromatography (APC<sup>™</sup>). Although the polysorbate 80 content of both turbid and translucent extrudates was within target, the glass transition temperature of the turbid extrudate was 2 °C above expected value. The observed turbidity was traced to lot-to-lot variability of the polysorbate 80 used in the continuous manufacturing, where APC<sup>™</sup> analysis revealed that the relative content of the low molecular weight component varied from 23% to 27% in correlation with the evolution from turbid to translucent extrudates. This work stresses the importance of taking feeding material variability into account during continuous manufacturing.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"684-690"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141591015","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation and statistical optimization of letrozole loaded nanotransferosomal gel for tumor targeting. 用于肿瘤靶向的来曲唑负载纳米转运体凝胶的配方和统计优化。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-07-26 DOI: 10.1080/10837450.2024.2382437
Sara Imtiaz, Saba Sohail, Fakhar Ud Din, Zakir Ali, Sibgha Batool, Maimoona Malik, Asif Nawaz, Ali H Alamri, Ahmed A Lahiq, Shaker T Alsharif, Abdullah Asiri
{"title":"Formulation and statistical optimization of letrozole loaded nanotransferosomal gel for tumor targeting.","authors":"Sara Imtiaz, Saba Sohail, Fakhar Ud Din, Zakir Ali, Sibgha Batool, Maimoona Malik, Asif Nawaz, Ali H Alamri, Ahmed A Lahiq, Shaker T Alsharif, Abdullah Asiri","doi":"10.1080/10837450.2024.2382437","DOIUrl":"10.1080/10837450.2024.2382437","url":null,"abstract":"<p><p>Letrozole (LTZ) is used as first-line treatment for hormone-positive breast cancer (BC) in postmenopausal women. However, its poor aqueous solubility and permeability have reduced its clinical efficacy. Herein, we developed LTZ-nanotransferosomes (LTZ-NT) to address above mentioned issues. The LTZ-NT were optimized statistically using Design Expert<sup>®</sup> followed by their characterization <i>via</i> dynamic light scattering (DLS), Transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and Differential scanning calorimetry (DSC). The optimized LTZ-NT was incorporated into 1% chitosan-gel to develop LTZ-NTG. Moreover, <i>in vitro</i> drug release and <i>ex vivo</i> permeation of LTZ-NTG were performed and compared with LTZ-dispersion and LTZ-NT. Additionally, skin irritability and histopathology of LTZ-NTG were investigated. Furthermore, <i>in vitro</i> antitumor study of LTZ-NTG was investigated in BC cell lines. The optimized LTZ-NT showed suitable zeta potential (30.4 mV), spherical size (162.5 nm), and excellent entrapment efficiency (88.04%). Moreover, LTZ-NT exhibited suitable thermal behavior and no interactions among its excipients. In addition, LTZ-NTG had an optimal pH (5.6) and a suitable viscosity. A meaningfully sustained release and improved permeation of LTZ was observed from LTZ-NTG. Additionally, LTZ-NTG showed significantly enhanced cell death of MCF-7 and MCC-7 cells. It can be concluded that LTZ-NTG has the potential to deliver chemotherapeutic agents for possible treatment of BC.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"703-718"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141634207","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quercetin nanocrystals for bioavailability enhancement: impact of different functional stabilizers on in vitro/in vivo drug performances. 用于提高生物利用度的槲皮素纳米晶体:不同功能稳定剂对体外/体内药物性能的影响
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-07-01 Epub Date: 2024-06-05 DOI: 10.1080/10837450.2024.2361654
Yuwen Zhu, Fei Hu, Chengying Shen, Baode Shen, Hailong Yuan
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