International Journal of Pharmaceutics: X最新文献

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Design of an innovative nanovehicle to enhance brain permeability of a novel 5-HT6 receptor antagonist 设计创新型纳米载体,提高新型 5-HT6 受体拮抗剂的脑渗透性
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-21 DOI: 10.1016/j.ijpx.2024.100296
María Javiera Alvarez-Figueroa , Francisco Nuñez-Navarro , Gonzalo Recabarren-Gajardo , José Vicente González-Aramundiz
{"title":"Design of an innovative nanovehicle to enhance brain permeability of a novel 5-HT6 receptor antagonist","authors":"María Javiera Alvarez-Figueroa ,&nbsp;Francisco Nuñez-Navarro ,&nbsp;Gonzalo Recabarren-Gajardo ,&nbsp;José Vicente González-Aramundiz","doi":"10.1016/j.ijpx.2024.100296","DOIUrl":"10.1016/j.ijpx.2024.100296","url":null,"abstract":"<div><div>An innovative nanovehicle based on lipid nanocapsules (LNC) was designed to facilitate the passage of a new 5-HT<sub>6</sub> receptor antagonist, namely PUC-10, through the blood-brain barrier. PUC-10 is a new synthetic <em>N</em>-arylsulfonylindole that has demonstrated potent 5-HT<sub>6</sub> receptor antagonist activity, but it exhibits poor solubility in water, which indicates limited absorption. The lipid nanocapsules designed had a nanometric size (53 nm), a monomodal distribution (PI&lt;0.2), a negative Z potential (−17 ± 7 mV) and allowed efficient PUC-10 encapsulation (74 %). Furthermore, the LNC demonstrated to be stable for at least 4 weeks at 4 °C (storage conditions), for at least 4 h in DMEM at pH 7.4, and for 18 h in water with 5 % DMSO, with both latter conditions maintained at 37 °C. They also demonstrated that cell viability was not affected at the different concentrations studied. Finally, <em>in vitro</em> studies that simulate the blood brain barrier (PAMPA-BBB) demonstrated that the nanoencapsulation of PUC-10 promoted their penetration through the blood-brain barrier, with a calculated permeability of 1.3 × 10<sup>−8</sup> cm/s, compared to the null permeability exhibited by non-nanoencapsulated PUC-10.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100296"},"PeriodicalIF":5.2,"publicationDate":"2024-10-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142551881","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
Development of cancer-associated fibroblasts-targeting polymeric nanoparticles loaded with 8-O-methylfusarubin for breast cancer treatment 开发癌症相关成纤维细胞靶向聚合物纳米颗粒,载入 8-O-甲基扶桑黄素用于乳腺癌治疗
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-17 DOI: 10.1016/j.ijpx.2024.100294
Kamonlatth Rodponthukwaji , Suyanee Thongchot , Suttikiat Deureh , Tanva Thongkleang , Mattika Thaweesuvannasak , Kornrawee Srichan , Chatchawan Srisawat , Peti Thuwajit , Kytai T. Nguyen , Kwanruthai Tadpetch , Chanitra Thuwajit , Primana Punnakitikashem
{"title":"Development of cancer-associated fibroblasts-targeting polymeric nanoparticles loaded with 8-O-methylfusarubin for breast cancer treatment","authors":"Kamonlatth Rodponthukwaji ,&nbsp;Suyanee Thongchot ,&nbsp;Suttikiat Deureh ,&nbsp;Tanva Thongkleang ,&nbsp;Mattika Thaweesuvannasak ,&nbsp;Kornrawee Srichan ,&nbsp;Chatchawan Srisawat ,&nbsp;Peti Thuwajit ,&nbsp;Kytai T. Nguyen ,&nbsp;Kwanruthai Tadpetch ,&nbsp;Chanitra Thuwajit ,&nbsp;Primana Punnakitikashem","doi":"10.1016/j.ijpx.2024.100294","DOIUrl":"10.1016/j.ijpx.2024.100294","url":null,"abstract":"<div><div>Cancer-associated fibroblasts (CAFs) are abundant stromal cells residing in a tumor microenvironment (TME) which are associated with the progression of tumor. Herein, we developed novel CAFs-targeting polymeric nanoparticles encapsulating a synthetic 8-<em>O</em>-methylfusarubin (OMF) compound (OMF@NPs-anti-FAP). Anti-FAP/fibroblast activation protein antibody was employed as a CAFs-targeting ligand. The physicochemical properties of the synthesized nanomaterials were firstly investigated with various techniques. The cytocompatibility of polymeric nanoparticles (NPs) was elicited through cell viability of CAFs and human breast epithelial cells, MCF-10A. Additionally, the anti-FAP-conjugated NPs displayed different degrees of cellular internalization regarding the FAP expression level on the CAFs' surface. However, CAFs exposed to NPs containing OMF demonstrated significant cell death which were associated with the apoptotic pathway as confirmed by caspase-3/7 activity. Upon OMF@NPs-anti-FAP treatment, an enhanced toxicity was clearly observed in 3D spheroid models. High FAP-expressed PC-B-132CAFs demonstrated a high percentage of cell death compared to other cells with a low level of FAP expression analyzed by flow cytometry (e.g. MCF-10A, HDFa, and PC-B-142CAFs). This result emphasized the importance of anti-FAP antibody as a targeting ligand. These findings suggest that the fabricated nanosystem of OMF-loaded polymeric NPs with CAFs' high specificity holds a potential NP-based platform for improvement in breast cancer treatment.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100294"},"PeriodicalIF":5.2,"publicationDate":"2024-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534422","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
Effect of wound dressing porosity and exudate viscosity on the exudate absorption: In vitro and in silico tests with 3D printed hydrogels 伤口敷料孔隙率和渗出物粘度对渗出物吸收的影响:三维打印水凝胶的体外和体内测试
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-16 DOI: 10.1016/j.ijpx.2024.100288
Alejandro Seijo-Rabina , Santiago Paramés-Estevez , Angel Concheiro , Alberto Pérez-Muñuzuri , Carmen Alvarez-Lorenzo
{"title":"Effect of wound dressing porosity and exudate viscosity on the exudate absorption: In vitro and in silico tests with 3D printed hydrogels","authors":"Alejandro Seijo-Rabina ,&nbsp;Santiago Paramés-Estevez ,&nbsp;Angel Concheiro ,&nbsp;Alberto Pérez-Muñuzuri ,&nbsp;Carmen Alvarez-Lorenzo","doi":"10.1016/j.ijpx.2024.100288","DOIUrl":"10.1016/j.ijpx.2024.100288","url":null,"abstract":"<div><div>Exudate absorption is a key parameter for proper wound dressing performance. Unlike standardized tests that consider exudate viscosity close to that of water, patients' exudates vary greatly in composition and, therefore, viscosity. This work aimed to investigate the effects of exudate viscosity and pore size of hydrogel-like dressings on the exudate absorption rate to establish rational criteria for the design of dressings that can meet the personalized needs of wound treatment. Computer-aided design (CAD) was used for Digital Light Processing (DLP) 3D printing of hydrogels with 0%, 30% and 60% porosity. The hydrogels were characterized in detail, and the absorption of two simulated exudate fluids (SEFs) was video-recorded. The same CAD files were used to develop <em>in silico</em> models to simulate exudate uptake rate. Both <em>in vitro</em> data and <em>in silico</em> modeling revealed that low-viscosity SEF penetrates faster through relatively small hydrogel pores (approx. 400 μm) compared to larger pores (approx. 1100 μm) due to capillary forces. However, <em>in vitro</em> vertical uptake took longer than when simulated using CAD design due to lateral fluid absorption through the pore walls in the hydrogel bulk. Distortions of hydrogel channels (micro-CT images) and lateral fluid absorption should be both considered for <em>in silico</em> simulation of SEF penetration. Overall, the results evidenced that porous hydrogel dressings allow rapid penetration (within a few seconds) and hosting of exudates, especially for pore size &lt;1 mm. This information may be useful for design criteria of wound dressings with adequate fluid handling and drug release rate.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100288"},"PeriodicalIF":5.2,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142444682","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
Ocular mucoadhesive and biodegradable spanlastics loaded cationic spongy insert for enhancing and sustaining the anti-inflammatory effect of prednisolone Na phosphate; Preparation, I-optimal optimization, and In-vivo evaluation 用于增强和维持泼尼松龙磷酸钠抗炎效果的眼部粘液粘附性和可生物降解的含阳离子海绵插件;制备、I-优化和体内评估
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-16 DOI: 10.1016/j.ijpx.2024.100293
Mayada Said , Khaled M. Ali , Munerah M. Alfadhel , Obaid Afzal , Basmah Nasser Aldosari , Maha Alsunbul , Rawan Bafail , Randa Mohammed Zaki
{"title":"Ocular mucoadhesive and biodegradable spanlastics loaded cationic spongy insert for enhancing and sustaining the anti-inflammatory effect of prednisolone Na phosphate; Preparation, I-optimal optimization, and In-vivo evaluation","authors":"Mayada Said ,&nbsp;Khaled M. Ali ,&nbsp;Munerah M. Alfadhel ,&nbsp;Obaid Afzal ,&nbsp;Basmah Nasser Aldosari ,&nbsp;Maha Alsunbul ,&nbsp;Rawan Bafail ,&nbsp;Randa Mohammed Zaki","doi":"10.1016/j.ijpx.2024.100293","DOIUrl":"10.1016/j.ijpx.2024.100293","url":null,"abstract":"<div><div>This study aimed to formulate and statistically optimize spanlastics loaded spongy insert (SPLs-SI) of prednisolone Na phosphate (PRED) to enhance and sustain its anti-inflammatory effect in a controlled manner. An I-optimal optimization was employed using Design-Expert® software. The formulation variables were sonication time, the Span 60: EA ratio and type of edge activator (Tween 80 or PVA) while Entrapment efficiency (EE%), Vesicles' size (VS) and Zeta potential (ZP) were set as the dependent responses. This resulted in an optimum spanlastics (SPLs) formulation with a desirability of 0.919. It had a Span60:Tween80 ratio of 6:1 with a sonication time of 9.5 min. It was evaluated in terms of its EE%, VS, ZP, release behavior in comparison to drug solution in addition to the effect of aging on its characteristics. It had EE% of 87.56, VS of 152.2 nm and ZP of −37.38 Mv. It showed sustained release behavior of PRED in comparison to drug solution with good stability for thirty days. TEM images of the optimized PRED SPLs formulation showed spherical non-aggregated nanovesicles. Then it was loaded into chitosan spongy insert and evaluated in terms of its visual appearance, pH and mucoadhesion properties. It showed good mucoadhesive properties and pH in the safe ocular region. The FTIR, DSC and XRD spectra showed that PRED was successfully entrapped inside the SPLs vesicles. It was then exposed to an in-vivo studies where it was capable of enhancing the anti-inflammatory effect of PRED in a sustained manner with once daily application compared to commercial PRED solution. The spongy insert has the potential to be a promising carrier for the ocular delivery of PRED.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100293"},"PeriodicalIF":5.2,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534420","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
Multifunctional poloxamer-based thermo-responsive hydrogel loaded with human lactoferricin niosomes: In vitro study on anti-bacterial activity, accelerate wound healing, and anti-inflammation 以聚氧乙烯醚为基础的多功能热响应水凝胶载入人乳铁蛋白纳米体:关于抗菌活性、加速伤口愈合和抗炎的体外研究
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-11 DOI: 10.1016/j.ijpx.2024.100291
Sirikwan Sangboonruang , Natthawat Semakul , Kiattikhun Manokruang , Nuttawut Khammata , Kanyaluck Jantakee , Katanchalee Mai-Ngam , Satrawut Charoenla , Phadungkiat Khamnoi , Kanokwan Saengsawang , Usanee Wattananandkul , Sorasak Intorasoot , Khajornsak Tragoolpua
{"title":"Multifunctional poloxamer-based thermo-responsive hydrogel loaded with human lactoferricin niosomes: In vitro study on anti-bacterial activity, accelerate wound healing, and anti-inflammation","authors":"Sirikwan Sangboonruang ,&nbsp;Natthawat Semakul ,&nbsp;Kiattikhun Manokruang ,&nbsp;Nuttawut Khammata ,&nbsp;Kanyaluck Jantakee ,&nbsp;Katanchalee Mai-Ngam ,&nbsp;Satrawut Charoenla ,&nbsp;Phadungkiat Khamnoi ,&nbsp;Kanokwan Saengsawang ,&nbsp;Usanee Wattananandkul ,&nbsp;Sorasak Intorasoot ,&nbsp;Khajornsak Tragoolpua","doi":"10.1016/j.ijpx.2024.100291","DOIUrl":"10.1016/j.ijpx.2024.100291","url":null,"abstract":"<div><div>Chronic wound infections are attributed to delayed tissue repair, which remains a major clinical challenge in long-term health care. Particularly, infections with antibiotic resistance have more serious effects on health, often resulting in unsuccessful treatments. Thus, antimicrobial peptide (AMP)-based therapy holds promise as a potential therapeutic approach to overcoming drug resistance. Conventional wound dressing is a passive strategy for wound care that is not capable of eradicating pathogens and promoting tissue repair. In this study, we aim to construct an advanced wound dressing; a thermo-responsive hydrogel incorporated with lactoferricin (Lfcin) niosome (Lfcin-Nio/hydrogel) for bacterial pathogen treatment. The Lfcin-loaded niosome (Lfcin-Nio) has a particle size of 396.91 ± 20.96 nm, 0.38 ± 0.01 of PdI, −10.5 ± 0.3 mV of ζ potential, and 72.30 ± 7.05 % Lfcin entrapment efficiency. Lfcin-Nio exhibited broad antibacterial activity on both drug-susceptible and drug-resistant strains, and also on bacteria residing in the biofilm matrix. The Lfcin-Nio/hydrogel was fabricated from 0.5 % <em>w</em>/<em>v</em> poloxamer 188–20 % w/v poloxamer 407, and supplemented with Lfcin-Nio and epidermal growth factor (EGF). The physical properties of Lfcin-Nio/hydrogels showed elasticity, swelling ability, and strong injectability with responsiveness to 33–37 °C temperatures. The biological properties of Lfcin-Nio/hydrogels exhibited a bactericidal effect against drug-resistant strains of <em>S. aureus</em> and <em>P. aeruginosa,</em> and showed less toxicity to the human skin fibroblast. It also promoted the healing of scratches by 55 % within 6 h, compared to the wound closure rate of 20 % in the cell control. The inflammatory response of the Lfcin-Nio/hydrogel-treated cells was reduced <em>via</em> suppression of <em>IL-1β</em> and <em>COX-2</em> mRNA expressions. From this study, Lfcin-Nio/hydrogels can be suggested as a modern wound dressing that possesses multifunctional and beneficial properties for the management of chronic wound infections.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100291"},"PeriodicalIF":5.2,"publicationDate":"2024-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142441265","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
Study on the preparation of stabilizer-free silymarin nanocrystals and its oral absorption mechanisms 无稳定剂水飞蓟素纳米晶体的制备及其口服吸收机制研究
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-10 DOI: 10.1016/j.ijpx.2024.100292
Liangxing Tu , Ping Han , Yongbing Sun , Yi Jin , Kaili Hu , Meng Cheng , Yisen Shao , Jianfang Feng , Fangying Yuan
{"title":"Study on the preparation of stabilizer-free silymarin nanocrystals and its oral absorption mechanisms","authors":"Liangxing Tu ,&nbsp;Ping Han ,&nbsp;Yongbing Sun ,&nbsp;Yi Jin ,&nbsp;Kaili Hu ,&nbsp;Meng Cheng ,&nbsp;Yisen Shao ,&nbsp;Jianfang Feng ,&nbsp;Fangying Yuan","doi":"10.1016/j.ijpx.2024.100292","DOIUrl":"10.1016/j.ijpx.2024.100292","url":null,"abstract":"<div><div>Many researchers have studied the oral absorption mechanisms yet, however, considering stabilizers often participate in the absorption process of nanocrystals, these known mechanisms may be incorrect. Hence in this study, we aimed to explore the correct absorption mechanism of nanocrystals by performing related studies on stabilizer-free nanocrystals. We firstly prepared stabilizer-free silymarin nanocrystals by high-pressure homogenization, and then performed absorption-related studies, such as solubility, dissolution rate, pharmacokinetic study, cellular uptake and intracellular transport. Results showed the stabilizer-free silymarin nanocrystals had an average particle size of (450.2 ± 4.46) nm, with PDI of 0.280 ± 0.021 and Zeta potential of −26.9 ± 2.4 mV. The conversion of silymarin crude drug to stabilizer-free silymarin nanocrystals increased the compound's solubility by 1.41 times, with a dissolution rate of 92.2 % in water within 30 min compared to 38.5 % for crude drugs. Pharmacokinetic studies showed the oral bioavailability of stabilizer-free silymarin nanocrystals was found to be 1.48 times greater than that of the crude drugs. The cell experimentation results demonstrated that the stabilizer-silymarin nanocrystals can improve uptake but have poor transmembrane transport properties. Most researchers believe that nanocrystals can enhance transmembrane transport of drugs via an endocytosis-mediated pathway. In fact, nanocrystals are indeed endocytosed more by the cells, but this transport pathway is poor because the cells lack the intracellular transport pathway to transport nanocrystals from the AP side to the BP side. Therefore, we believe that the intracellular transport of nanocrystals can be enhanced by modifications and other carriers if needed to improve nanocrystals' ability to promote oral absorption.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100292"},"PeriodicalIF":5.2,"publicationDate":"2024-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534421","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
Investigating the effect of whey and casein proteins on drug solubility from a paediatric drug absorption perspective 从儿科药物吸收角度研究乳清蛋白和酪蛋白对药物溶解度的影响
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-09 DOI: 10.1016/j.ijpx.2024.100290
Matthias Van der Veken , Joachim Brouwers , Neil Parrott , Patrick Augustijns , Cordula Stillhart
{"title":"Investigating the effect of whey and casein proteins on drug solubility from a paediatric drug absorption perspective","authors":"Matthias Van der Veken ,&nbsp;Joachim Brouwers ,&nbsp;Neil Parrott ,&nbsp;Patrick Augustijns ,&nbsp;Cordula Stillhart","doi":"10.1016/j.ijpx.2024.100290","DOIUrl":"10.1016/j.ijpx.2024.100290","url":null,"abstract":"<div><div>Considering the predominantly milk-based diet of neonates and infants and their immature gastrointestinal digestion, milk proteins may affect drug behaviour and absorption in this population. Using in vitro models, this study investigated the impact of the representative milk proteins, whey and casein, on the solubility and permeation of the lipophilic model drugs spironolactone, clopidogrel and ritonavir. Drug solubility experiments revealed that the presence of milk proteins increased drug solubility. Next, permeation studies demonstrated that the same milk proteins reduced drug permeation across an artificial membrane. These results highlight the importance of the solubility-permeability interplay and indicate the effect of these proteins may be considered during (paediatric) drug development. Lastly, the findings underscore the importance of considering milk protein-drug interactions to optimize drug delivery strategies during (paediatric) drug development and especially for the youngest and most vulnerable part of this population.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100290"},"PeriodicalIF":5.2,"publicationDate":"2024-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142420374","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
Antiaging synergistic effect in noninvasive transdermal delivery of peptide loaded liposomes by low energy/frequency radiofrequency 低能量/高频射频非侵入性透皮给药多肽脂质体的抗衰老协同效应
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-10-05 DOI: 10.1016/j.ijpx.2024.100289
Nanxi Xiang , Zeting Huang , Chunqiao Zhang , Jiahong Huang , Zhenyuan Wang , Jichuan Zhang , Chengyu Wu , Weihua Peng , Jiaheng Zhang
{"title":"Antiaging synergistic effect in noninvasive transdermal delivery of peptide loaded liposomes by low energy/frequency radiofrequency","authors":"Nanxi Xiang ,&nbsp;Zeting Huang ,&nbsp;Chunqiao Zhang ,&nbsp;Jiahong Huang ,&nbsp;Zhenyuan Wang ,&nbsp;Jichuan Zhang ,&nbsp;Chengyu Wu ,&nbsp;Weihua Peng ,&nbsp;Jiaheng Zhang","doi":"10.1016/j.ijpx.2024.100289","DOIUrl":"10.1016/j.ijpx.2024.100289","url":null,"abstract":"<div><div>Low energy/frequency radiofrequency (LRF) combined with the transdermal delivery of liposome (L) encapsulated antiaging peptides technology is a remarkable, newly developed physical noninvasive transdermal penetration technique; it is considered a highly efficient, comprehensive and safe technology. In this study, our objective was to evaluate the physical and chemical mechanisms underlying the efficacy of this innovative technique involving a combination of LRF and L, termed LLRF, that exerts a synergistic anti-aging effect on human skin, via an animal experiment. Physical and chemical analyses indicated that a relatively stable liposome with a uniform nano-size, which was formed, possessed good transdermal permeability that was 2.74 folds higher than that of the free peptide (F). LLRF exhibited a higher transdermal permeation performance that was of 3.65 folds higher than that of the free one, which was substantiated via confocal laser scanning fluorescence microscopy. The mouse UVB photoaging model trial confirmed that the LLRF technology exerted a significant synergistic effect compared to liposome technology, or free peptide, by downregulating inflammatory factors (IL-6, TNF-α), inhibiting the mRNA and protein expression of matrix metalloproteinases (MMP1, MMP3), promoting the mRNA and protein expression of related collagens (Procollagen, Col1α1 and Col3α1), and repairing the stratum corneum barrier function, as evidenced by trans-epidermal water loss (TEWL), skin cuticle hydration (SCH), and decreased expression of β-gal, an aging marker. These findings indicated that photoaging skin can be effectively and comprehensively rejuvenated, and that even photodamage can be reversed, thereby restoring the original physiological characteristics of healthy skin. Clinical tests have confirmed that although liposome technology is an effective antiaging method which helps exert tightening and anti-wrinkle effects on human skin, LLRF is an even more effective anti-aging technique. This study reveals a highly effective technique involving a combination physical and chemical therapy that may be utilized for antiaging purposes as well as repairing lightly damaged skin, and can be made readily available in the future.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100289"},"PeriodicalIF":5.2,"publicationDate":"2024-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142420373","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
Autoencoder-based inverse design and surrogate-based optimization of an integrated wet granulation manufacturing process 基于自动编码器的湿法造粒集成制造工艺的逆向设计和代用优化
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-09-26 DOI: 10.1016/j.ijpx.2024.100287
Ashley Dan, Rohit Ramachandran
{"title":"Autoencoder-based inverse design and surrogate-based optimization of an integrated wet granulation manufacturing process","authors":"Ashley Dan,&nbsp;Rohit Ramachandran","doi":"10.1016/j.ijpx.2024.100287","DOIUrl":"10.1016/j.ijpx.2024.100287","url":null,"abstract":"<div><div>In pharmaceutical manufacturing, integrating model-based design and optimization can be beneficial for accelerating process development. This study explores the utilization of Machine Learning (ML) techniques as a surrogate model for the optimization of a three-unit wet-granulation based flowsheet model for solid dosage form manufacturing. First, a reduced representation of a wet granulation flowsheet model is developed, incorporating a granulation and milling process, along with a novel dissolution model that accounts for the effect of particle size, porosity, and microstructure on dissolution rate. Two optimization approaches are compared, including an autoencoder-based inverse design and a surrogate-based forward optimization. Both methods address the bi-objective problem of maximizing dissolution time and product yield by identifying the optimal granulation and mill process parameters. For this case study, both approaches were effective and incurred a similar computational cost, averaging under 4 s. However, the autoencoder approach offers an advantage through dimensionality reduction, a feature not available in surrogate-based optimization. Dimensional reduction is particularly beneficial for complex process designs with numerous inputs and outputs. The lower dimensional representation helps improve process understanding through enhanced visualization of the process design space and facilitates feasibility studies involving multiple constraints. The autoencoder-based inverse design introduced in this work showcases an implementation of AI and ML in pharmaceutical process development, demonstrating the potential to enhance process efficiency and product quality in complex manufacturing scenarios.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100287"},"PeriodicalIF":5.2,"publicationDate":"2024-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142420610","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
Multifunctional Bi2S3-Au nanoclusters for fluorescence/infrared thermal imaging guided photothermal therapy 用于荧光/红外热成像引导光热疗法的多功能 Bi2S3-Au 纳米团簇
IF 5.2 2区 医学
International Journal of Pharmaceutics: X Pub Date : 2024-09-17 DOI: 10.1016/j.ijpx.2024.100286
Hongmei Sun , Yuyu Cao , Beibei Zhai , Xiaoshuang Zhao , Xuejun Zhang , Jiangtao Su
{"title":"Multifunctional Bi2S3-Au nanoclusters for fluorescence/infrared thermal imaging guided photothermal therapy","authors":"Hongmei Sun ,&nbsp;Yuyu Cao ,&nbsp;Beibei Zhai ,&nbsp;Xiaoshuang Zhao ,&nbsp;Xuejun Zhang ,&nbsp;Jiangtao Su","doi":"10.1016/j.ijpx.2024.100286","DOIUrl":"10.1016/j.ijpx.2024.100286","url":null,"abstract":"<div><div>Nanotechnology has attracted extensive attention in the diagnosis and treatment of cancer. Therefore, the research aimed at developing new nanomaterials and exploring their applications in biomedicine has attracted more attention. In this study, Bi<sub>2</sub>S<sub>3</sub>-Au nanoclusters (Bi<sub>2</sub>S<sub>3</sub>-AuNCs) as fluorescence/infrared thermal imaging-guided photothermal therapy (PTT) was prepared for the first time. It was achieved in a facile and mild way by optimizing the amount of Bi<sup>3+</sup> and Au<sup>3+</sup> using bovine serum albumin (BSA) as reducer and stabilizer. The as-prepared Bi<sub>2</sub>S<sub>3</sub>-AuNCs with special morphology showed high stability, excellent biocompatibility and good photostability. Apart from these, it also can accumulate at tumor sites and exhibit considerable fluorescence/infrared thermal imaging-guided PTT. Bi<sub>2</sub>S<sub>3</sub>-AuNCs nanoparticles integrate imaging and therapeutic functions into an advanced application platform, which provides the possibility to build a novel nano-cancer diagnosis and treatment platform.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"8 ","pages":"Article 100286"},"PeriodicalIF":5.2,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000586/pdfft?md5=70c1d210ccb12e79699cce62e385f85d&pid=1-s2.0-S2590156724000586-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142310406","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
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