Pharmaceutical Development and Technology最新文献

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Preparation and evaluation the effects of retinoic acid loaded proliposomal nanofibers on microbial biofilm inhibition. 制备并评估维甲酸负载的脂质体纳米纤维对微生物生物膜的抑制作用。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-07 DOI: 10.1080/10837450.2024.2411034
Serdar Tort, Ziya Canberk Öztürk, Fatma Kaynak-Onurdağ, N Başaran Mutlu-Ağardan
{"title":"Preparation and evaluation the effects of retinoic acid loaded proliposomal nanofibers on microbial biofilm inhibition.","authors":"Serdar Tort, Ziya Canberk Öztürk, Fatma Kaynak-Onurdağ, N Başaran Mutlu-Ağardan","doi":"10.1080/10837450.2024.2411034","DOIUrl":"10.1080/10837450.2024.2411034","url":null,"abstract":"<p><p>The electrospinning method involves the production of different drug delivery systems using various polymers. The production of proliposomes with electrospinning provides the hybridization of two novel drug delivery systems. Retinoic acid, also known as all-trans retinoic acid (ATRA), is a common and effective drug for acne therapy. This study aimed to prepare ATRA-loaded proliposomal nanofibers and evaluate their effectiveness on microbial biofilm inhibition. Blank and ATRA-loaded proliposomal nanofiber formulations were fabricated in various polyvinylpyrrolidone, phosphatidylcholine and cholesterol ratios. TEM images verified the rapid formation of the liposomes after the hydration of nanofibers. The vesicle size, polydispersity index and zeta potential values of self-assembled liposomes were measured. The vesicle size values were found to be 321.9-363.8 nm with PDI values varying between 0.332 and 0.511 and zeta potential values of (-16.8) to (-20.5)mV. ATRA-loaded proliposomal nanofibers provided higher bioadhesion (0.25 mJ/cm<sup>2</sup>) than the commercial cream (0.07 mJ/cm<sup>2</sup>). The short-term stability results showed that the initial characteristics remained for three months at 4 °C. The proposed ATRA-loaded self-assembled proliposomal system provided antibacterial, fungistatic or fungicidal effects superior to retinoic acid itself and inhibited biofilm formation in lower concentrations. This approach can combine the stability advantage of nanofibers in the dry state with the high effectiveness of liposomes in acne treatment presenting antibacterial and anti-biofilm-forming activity against <i>Candida albicans</i> and <i>Cutibacterium acnes</i>.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"955-965"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351888","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
Influence of punch coating surface properties on sticking during the tableting process. 冲头涂层表面特性对压片过程中粘连的影响
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-12 DOI: 10.1080/10837450.2024.2413147
Komlan Koumbogle, François Gitzhofer, Nicolas Abatzoglou
{"title":"Influence of punch coating surface properties on sticking during the tableting process.","authors":"Komlan Koumbogle, François Gitzhofer, Nicolas Abatzoglou","doi":"10.1080/10837450.2024.2413147","DOIUrl":"10.1080/10837450.2024.2413147","url":null,"abstract":"<p><strong>Introduction: </strong>The present study evaluates the sticking propensity of Uncoated steel, and chromium nitride (CrN), zirconium nitride (ZrN), titanium nitride (TiN) and Ultracoat punch coatings during the tableting process of microcrystalline cellulose (MCC) conducted on a Manesty<sup>®</sup> F3 single station tableting press.</p><p><strong>Methods: </strong>Surface properties including surface roughness, surface free energy (SFE) and its components, the atomic percentage of surface polar functional groups and oxides measured with X-ray photoelectron spectroscopy were used to characterize the surface propensity to sticking.</p><p><strong>Results: </strong>After five hours of tablet pressing, MCC powder particles were found to adhere to the TiN coated and the uncoated steel punches. Surface analysis show that surface roughness of all the tested punches was similar. The Lewis base SFE component (LB-comp) was found to govern the acid-base interactions of the tested surfaces, and its value was higher for punch surfaces affected by sticking. The surfaces exhibiting higher LB-comp are more prone to strong acid-base interactions with water molecules that evaporate from the powder bed during compression. Therefore, these surfaces adsorbed water and allow sticking through capillary adhesion force.</p><p><strong>Conclusion: </strong>The total atomic percentage of the surface polar functional groups (PFG) and oxides was also high for the surfaces that stick to MCC during tableting, suggesting that hydrophilic molecules on the punch surface favor sticking.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"987-995"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142372523","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 evaluation of carrier-based dry powders containing budesonide and arformoterol for inhalation therapy. 用于吸入治疗的含布地奈德和阿福莫特罗的载体型干粉的配制和评估。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-23 DOI: 10.1080/10837450.2024.2413145
Dong-Won Oh, Ji Hoon Choi, Gweon Hee Yu, Bo Kyung Kim, Sang Min Cho, Youn Woong Choi, Jin-Hyuk Jeong, Ji-Hyun Kang, Dong-Wook Kim, Chun-Woong Park
{"title":"Formulation and evaluation of carrier-based dry powders containing budesonide and arformoterol for inhalation therapy.","authors":"Dong-Won Oh, Ji Hoon Choi, Gweon Hee Yu, Bo Kyung Kim, Sang Min Cho, Youn Woong Choi, Jin-Hyuk Jeong, Ji-Hyun Kang, Dong-Wook Kim, Chun-Woong Park","doi":"10.1080/10837450.2024.2413145","DOIUrl":"10.1080/10837450.2024.2413145","url":null,"abstract":"<p><p>Asthma and Chronic Obstructive Pulmonary Disease (COPD) are major global health concerns, with inhalation therapy being a primary treatment method. Dry powder inhalers (DPIs) often face challenges related to particle aggregation, which can diminish drug delivery efficiency. This study investigates particle aggregation and aims to optimize the cohesion-adhesion balance to improve inhalation efficiency. Advanced techniques like atomic force microscopy and Raman imaging were used to analyze particle interactions, focusing on lactose ratios, particle morphology, and drug-drug interactions. The therapeutic efficacy of optimized formulations containing budesonide (BUD) and Arformoterol (AFT) was assessed using an asthma model, showing significant improvements in sRAW, neutrophil count, and tidal volume compared to the positive control, with <i>p</i>-values below 0.01. AFT exhibited comparable efficacy to Formoterol at half the dose. Additionally, pharmacokinetic studies demonstrated similar in vivo behavior between the drugs, confirming the therapeutic advantage of AFT, with <i>p</i>-values for AUC<sub>0-t</sub> and Cmax of .646 and .153, respectively. The fine particle fractions for AFT and BUD were 39.4% and 50.6%, respectively, indicating improved drug delivery efficiency and potential for better clinical outcomes in asthma and COPD patients.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"966-975"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472336","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
Studies on allantoin topical formulations: in vitro drug release studies and rheological characteristics. 尿囊素局部制剂研究:体外药物释放研究和流变特性。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-18 DOI: 10.1080/10837450.2024.2414938
Alisa Elezović, Amar Elezović, Miroslav Hadnađev, Adna Džemat, Emina Hrnčić, Belma Imamović, Ervina Bečić, Veljko Krstonošić
{"title":"Studies on allantoin topical formulations: in vitro drug release studies and rheological characteristics.","authors":"Alisa Elezović, Amar Elezović, Miroslav Hadnađev, Adna Džemat, Emina Hrnčić, Belma Imamović, Ervina Bečić, Veljko Krstonošić","doi":"10.1080/10837450.2024.2414938","DOIUrl":"10.1080/10837450.2024.2414938","url":null,"abstract":"<p><p>The extent and rate of release of active substances from topical products must be sufficient to ensure their effectiveness, which depends on selecting the most appropriate formulation. This study examined allantoin emulsions and gel formulations. In water-in-oil (W/O) and oil-in-water (O/W) emulsions, the main emulsifier was varied, while the same gelling agent was used in all formulations to test the effects of oil phase presence and emulsifier type on allantoin release, as well as the formulations' rheological and textural characteristics. O/W emulsions exhibited similar release rates and the overall amount released over six hours (11-14.8%), while the highest amount of allantoin (20.9%) was released from the gel formulation. Conversely, the amount of allantoin released from the W/O emulsion (0.77%) was insufficient. Experimental data generally fit best with the Higuchi model kinetics. The formulations demonstrated shear-thinning thixotropic behavior. The greatest deviation from the Newtonian type of flow, with the smallest value of constant n (0.106-0.13) and the largest thixotropic loop area (6602.67-8140 Pas<sup>-1</sup>) were shown by O/W emulsions. The W/O emulsion exhibited the highest constant n (0.70) and smaller hysteresis area (991.23 Pas<sup>-1</sup>). Firmness and consistency values increased in the order: gel < W/O emulsion  < O/W emulsions. The O/W emulsions showed similarity in microstructure and textural characteristics, likely explaining their similar release behavior.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1033-1041"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472339","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
ROS-responsive glycol chitosan-linked prodrug nanoparticle as a nanoplatform for tumor chemo-photodynamic therapy. 响应 ROS 的乙二醇壳聚糖连接原药纳米粒子作为肿瘤化疗光动力疗法的纳米平台。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-09-30 DOI: 10.1080/10837450.2024.2411027
Jingmou Yu, Mengqi Liu, Chao Zhang, Lizhen Cheng, Changchun Peng, Dengzhao Jiang, Wenbo Liu, Hongguang Jin, Jin Ren
{"title":"ROS-responsive glycol chitosan-linked prodrug nanoparticle as a nanoplatform for tumor chemo-photodynamic therapy.","authors":"Jingmou Yu, Mengqi Liu, Chao Zhang, Lizhen Cheng, Changchun Peng, Dengzhao Jiang, Wenbo Liu, Hongguang Jin, Jin Ren","doi":"10.1080/10837450.2024.2411027","DOIUrl":"10.1080/10837450.2024.2411027","url":null,"abstract":"<p><p>Herein, we designed and synthesized novel reactive oxygen species (ROS)-responsive glycol chitosan-doxorubicin (DOX) prodrug <i>via</i> a ROS-cleavable thioketal (TK) linker. The obtained GC-TK-DOX formed self-assembled nanoparticles of 312 nm in aqueous media. Photosensitizers zinc phthalocyanine (ZnPc)-loaded GC-TK-DOX (GC-TK-DOX/ZnPc) nanoparticles were fabricated by using a dialysis approach. The GC-TK-DOX and GC-TK-DOX/ZnPc nanoparticles were nearly spherical by transmission electron microscopy (TEM) observation. Under 660-nm laser irradiation, GC-TK-DOX/ZnPc could generate singlet oxygen. Further, GC-TK-DOX/ZnPc nanoparticles exhibited ROS-sensitive release of DOX and ZnPc <i>in vitro</i>. GC-TK-DOX/ZnPc with laser irradiation showed more drug uptake and higher cytotoxic effects than GC-TK-DOX/ZnPc without irradiation, free DOX and GC-TK-DOX in HeLa tumor cells. Overall, these findings suggested that GC-TK-DOX/ZnPc could be a promising nanoarchitecture for synergetic chemo-photodynamic therapy against tumors.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"945-954"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351890","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
Facile fabrication of degradable, serrated polyethylene diacrylate microneedles using stereolithography. 利用立体光刻技术轻松制作可降解的锯齿状聚乙烯二丙烯酸酯微针。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-10 DOI: 10.1080/10837450.2024.2413146
Vedant Joshi, Nidhi Singh, Pallab Datta
{"title":"Facile fabrication of degradable, serrated polyethylene diacrylate microneedles using stereolithography.","authors":"Vedant Joshi, Nidhi Singh, Pallab Datta","doi":"10.1080/10837450.2024.2413146","DOIUrl":"10.1080/10837450.2024.2413146","url":null,"abstract":"<p><p>Microneedles have the potential for minimally invasive drug delivery. However, they are constrained by absence of rapid, scalable fabrication methods to produce intricate arrays and serrations for enhanced adhesion. 3D printing techniques like stereolithography (SLA) are fast, scalable modalities but SLAs require non-degradable and stiff resins. This work attempts to overcome this limitation by utilizing a poly (ethylene glycol diacrylate) (PEGDA, F3) resin and demonstrating its compatibility with a commercial SLA printer. FESEM images showed high printing efficiency of customized bioinks (F3) similar to commercial resins using SLA 3D printer. Mechanical endurance tests of whole MNA showed that MNs array printed from F3 resin (485 ± 5.73 N) required considerably less force than commercial F1 resin (880 ± 32.4 N). Penetration performance of F1 and F3 was found to be 10.8 ± 2.06 N and 0.705 ± 0.03 N. In-vitro degradation study in PBS showed that MNs fabricated from F3 resin exhibited degradation after 7 days, which was not observed with the commercial F1 resin provided by the manufacturer. The histology of porcine skin exhibited formation of triangular pores with pore length of 548 μm and efficient penetration into the deeper dermal layer. In conclusion, PEGDA can be used as for fabricating degradable, serrated solid MNs over commercial resin.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"976-986"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142372522","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
Recent progress in nanoparticulate-based intranasal delivery for treating of different central nervous system diseases. 基于纳米微粒的鼻内给药治疗不同中枢神经系统疾病的最新进展。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-11 DOI: 10.1080/10837450.2024.2409807
Eman A Bseiso, Nermin M Sheta, Khaled M Abdel-Haleem
{"title":"Recent progress in nanoparticulate-based intranasal delivery for treating of different central nervous system diseases.","authors":"Eman A Bseiso, Nermin M Sheta, Khaled M Abdel-Haleem","doi":"10.1080/10837450.2024.2409807","DOIUrl":"10.1080/10837450.2024.2409807","url":null,"abstract":"<p><p>Drug administration to the central nervous system (CNS) has become a great obstacle because of several biological barriers, such as the blood-brain barrier, therefore, brain targeting insights are a light for scientists to move forward for treating neurogenerative diseases using advanced non-invasive methods. The current demand is to use a potential direct route as the nasal administration to transport drugs into the brain enhancing the BBB permeability and hence, increasing the bioavailability. Interestingly, recent techniques have been implanted in formulating nanocarriers-based therapeutics for targeting and treating ischemic stroke using lipid or polymeric-based materials. Nanoparticulate delivery systems are set as an effective platform for brain targeting as polymeric nanoparticles and polymeric micelles or nanocarriers based on lipids for preventing drug efflux to promote optimal therapeutic medication concentration in the brain-diseased site. In recent years, there has been a notable increase in research publications and ongoing investigations on the utilization of drug-loading nanocarriers for the treatment of diverse CNS diseases. This review comprehensively depicts these dangerous neurological disorders, drug targeting challenges to CNS, and potential contributions as novel intranasal nano-formulations are being used to treat and regulate a variety of neurological diseases.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"913-929"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351889","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
Development of gallic acid loaded composite nanovesicles for the topical treatment of acne: optimization, characterization, and clinical investigation. 用于痤疮局部治疗的没食子酸负载复合纳米颗粒的开发:优化、表征和临床研究。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-10-02 DOI: 10.1080/10837450.2024.2409812
Shymaa Hatem, Noha H Moftah, Maha H Ragai, Enas El-Maghawry
{"title":"Development of gallic acid loaded composite nanovesicles for the topical treatment of acne: optimization, characterization, and clinical investigation.","authors":"Shymaa Hatem, Noha H Moftah, Maha H Ragai, Enas El-Maghawry","doi":"10.1080/10837450.2024.2409812","DOIUrl":"10.1080/10837450.2024.2409812","url":null,"abstract":"<p><p>Gallic acid (GA) proved to produce desired effects topically in the treatment of acne, through its antibacterial, anti-inflammatory and antioxidant characteristics. In the current work, nanovesicular systems; aspasomes loaded with GA were prepared, and evaluated on <i>in-vitro</i> and <i>ex-vivo</i> levels. Formulations were coated with chitosan due to its mucoadhesive properties. Results indicated that the size of the formulations ranged between 273.20 and 855.00 nm, with positively charged zeta potential ranging between 30.60 and 34.40 mV, EE% ranging between 57.651% and 95.20% and good stability after 3-months storage. The formulae provided a sustained drug release of 98.22% over 24 h, 5.4-fold higher <i>ex-vivo</i> skin deposition compared to GA solution, and powerful antioxidant potential compared to the control solution and appeared as spherical bilayer vesicles on being examined using transmission electron microscope. A clinical study was carried out on patients suffering from acne, where the reduction percent of comedones, inflammatory, total acne lesions and infiltrate was calculated. Results revealed that aspasomes exhibited reduction percentages of 72.35%, 80.33%, 77.95% and 90.01% ± for comedones, inflammatory lesions, total lesions, and infiltrate, respectively compared to control solution providing an effective topical delivery system for the management of acne.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"899-911"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351887","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
Sustained linagliptin administration: superior glycemic control and less pancreatic injury in diabetic rats. 持续服用利拉利汀:糖尿病大鼠的血糖控制更佳,胰腺损伤更少。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-09-30 DOI: 10.1080/10837450.2024.2407852
Esraa M Zakaria, Shrouk Fayrouz El-Gamal, Samar Mortada Mahmoud, Hanan M El-Nahas, Hany M El-Bassossy
{"title":"Sustained linagliptin administration: superior glycemic control and less pancreatic injury in diabetic rats.","authors":"Esraa M Zakaria, Shrouk Fayrouz El-Gamal, Samar Mortada Mahmoud, Hanan M El-Nahas, Hany M El-Bassossy","doi":"10.1080/10837450.2024.2407852","DOIUrl":"10.1080/10837450.2024.2407852","url":null,"abstract":"<p><p>While linagliptin is the most potent dipeptidyl peptidase 4 inhibitor, its use is limited due to poor bioavailability and the potential risk of pancreatic injury. Here, we investigated whether the sustained weekly administration of linagliptin could provide better effect compared to frequent daily oral administration. Type 2 diabetes was induced by feeding rats a high fructose/fat/salt diet followed by STZ injection. Compared to the partial glycemic control achieved with daily oral linagliptin, a weekly subcutaneous injection containing about one-fourth of the oral dose produced superior glycemic control, as evidenced by the 4-week postprandial glucose follow-up and oral glucose tolerance test. This was confirmed by the significant increase in serum insulin in the case of the sustained linagliptin administration. Higher levels of the anti-inflammatory cytokine adiponectin and lower triglyceride levels were observed after sustained linagliptin administration compared with daily oral linagliptin. In addition, sustained linagliptin displayed a significant increase in β-cells' insulin immunoreactivity when compared with daily linagliptin. More reduction in collagen deposition and caspase-3 immunoreactivity in pancreatic tissue were observed in sustained linagliptin compared with oral linagliptin. In conclusion, sustained linagliptin administration provided superior glycemic control, which seems to be mediated by more reduction in pancreatic injury.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"874-885"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142293123","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
Preparation and characterisation of esculetin-loaded nanostructured lipid carriers gels for topical treatment of UV-induced psoriasis. 用于局部治疗紫外线诱发的银屑病的埃克替林负载纳米结构脂质载体凝胶的制备和表征。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-10-01 DOI: 10.1080/10837450.2024.2407854
Rawia M Khalil, Mohamed F Abdelhameed, Sally Abou Taleb, Mohamed A El-Saied, Eman Samy Shalaby
{"title":"Preparation and characterisation of esculetin-loaded nanostructured lipid carriers gels for topical treatment of UV-induced psoriasis.","authors":"Rawia M Khalil, Mohamed F Abdelhameed, Sally Abou Taleb, Mohamed A El-Saied, Eman Samy Shalaby","doi":"10.1080/10837450.2024.2407854","DOIUrl":"10.1080/10837450.2024.2407854","url":null,"abstract":"<p><strong>Significance: </strong>As an inflammatory and autoimmune skin condition, psoriasis affects 2-3% of people worldwide. Psoriasis requires prolonged treatments with immunosuppressive medications which have severe adverse effects. Esculetin (Esc) is a natural medication that has been utilised to treat psoriasis.</p><p><strong>Objective: </strong>The goal of this work is to improve Esc's solubility by developing novel Esc nanostructured lipid carriers (NLCs) for treating psoriasis and increasing the residence time on the skin which infers better skin absorption.</p><p><strong>Methods: </strong>The particle size, zeta potential and entrapment efficiency (EE) of Esc NLCs were assessed. Incorporating NLCs into gum Arabic gel preparation enhances their industrial applicability, absorption and residence time on the skin. Esc NLC gels were evaluated by <i>in vitro</i> release and <i>in vivo</i> effectiveness on a rat model of UV-induced psoriasis.</p><p><strong>Results: </strong>Esc NLCs showed high EE reaching more than 95% and reasonable particle size ranging between (53.86 ± 0.38 to 236.3 ± 0.11 nm) and were spherical. The release study of Esc NLCs gel demonstrated a fast release of Esc denoting enhanced bioavailability. Compared to free Esc, Esc NLCs gel (F2) could considerably lower the level of CD34 and TNF-α in the skin. The results were validated through histopathological analysis.</p><p><strong>Conclusion: </strong>As Esc NLCs gel (F2) has strong anti-inflammatory properties, our results showed that it presented a significant potential for healing psoriasis.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"886-898"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142308279","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
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