Pharmaceutical Development and Technology最新文献_第3页

Cationic nanocrystalline suspensions: a potential approach for nose to brain delivery of L-dopa in Parkinson's therapy. 阳离子纳米晶体悬浮液：在帕金森治疗中左旋多巴鼻到脑输送的一种潜在途径。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-01 Epub Date: 2025-06-16 DOI: 10.1080/10837450.2025.2516237

Chiedza Kakono, Bwalya A Witika, Pedzisai A Makoni, Roderick B Walker

{"title":"Cationic nanocrystalline suspensions: a potential approach for nose to brain delivery of L-dopa in Parkinson's therapy.","authors":"Chiedza Kakono, Bwalya A Witika, Pedzisai A Makoni, Roderick B Walker","doi":"10.1080/10837450.2025.2516237","DOIUrl":"10.1080/10837450.2025.2516237","url":null,"abstract":"Levodopa (L-dopa) an effective treatment for Parkinson's disease, but it exhibits low oral bioavailability. Intranasal L-dopa nanosuspensions were manufactured to improve bioavailability using the olfactory and trigeminal delivery routes for direct brain delivery. The development of L-dopa nanocrystals and in vitro characterization was undertaken. Nanosuspensions were optimized using Design of Experiments. The L-dopa nanosuspension was produced at 50 °C using sonoprecipitation and mechanical stirring. Water and ethanol were solvent and antisolvent, and Tween® 80 and cetyltrimethylammonium bromide, stabilizing agents. The critical quality attributes (CQA) monitored were droplet size (PS), polydispersity index (PDI), Zeta potential (ZP), and percent yield (%), pH and osmolarity of the optimized formulation were monitored. SEM, pXRD, DSC, FTIR, and in vitro release were used for further characterization. Short-term stability testing at 4 °C and 22 °C was evaluated for 28 days. The mean PS, PDI, ZP, and % yield of the optimized nanosuspension were 161.4 ± 20.152 nm, 0.383 ± 0.090, +15.45 ± 1.664 mV, and 72.106 ± 0.023%, respectively. In vitro test results for the optimized formulation show the target CQA, had been met. The system may enhance the bioavailability of L-dopa when administered intranasally. In vivo studies are required to confirm nose-to-brain transport.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"646-665"},"PeriodicalIF":2.6,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144226273","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

Amelioration of Imiquimod-induced Psoriasis in the Mice model by Topical Delivery of Phosphodiesterase 4 Inhibitor Roflumilast Incorporated Nanoemulgel. 局部递送磷酸二酯酶4抑制剂罗氟米司特纳米凝胶改善咪喹莫致小鼠银屑病模型。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-15 DOI: 10.1080/10837450.2025.2505004

Velpula Prasannanjaneyulu, Shweta Nene, Ganesh Vambhurkar, Kamatham Pushpa Tryphena, Dharmendra Kumar Khatri, Saurabh Srivastava

{"title":"Amelioration of Imiquimod-induced Psoriasis in the Mice model by Topical Delivery of Phosphodiesterase 4 Inhibitor Roflumilast Incorporated Nanoemulgel.","authors":"Velpula Prasannanjaneyulu, Shweta Nene, Ganesh Vambhurkar, Kamatham Pushpa Tryphena, Dharmendra Kumar Khatri, Saurabh Srivastava","doi":"10.1080/10837450.2025.2505004","DOIUrl":"https://doi.org/10.1080/10837450.2025.2505004","url":null,"abstract":"Several clinical trials on repurposing of roflumilast are in progress, majorly focused on the potential treatment for psoriasis and atopic dermatitis like inflammatory skin diseases. Therefore, the current research focuses on formulation and in vivo evaluation of repurposed drug roflumilast loaded nanoemulgel for topical management of psoriasis. The roflumilast loaded nanoemulsion was prepared by spontaneous nanoemulsification method. The optimized roflumilast nanoemulsion has shown droplet size of found to be 10.92 ± 0.15 nm, PDI <0.3. The optimized nanoemulsion was further converted into gel referred as nanoemulgel. The prepared nanoemulgel has shown pseudoplastic shear thinning behaviour with pH value ranging between the skin pH while the content of roflumilast (%) was found >95%. Ex vivo permeation study of roflumilast nanoemulgel showed significantly higher skin retention of roflumilast (**p < 0.01) compared to free roflumilast gel. The antipsoriatic potential of roflumilast nanomulgel has been evaluated in psoriasis model of BALB/c mice. The levels of pro-inflammatory cytokines including IL-17, IL-22, IL-23 and TNF-α in skin homogenates of mice group treated with roflumilast nanoemulgel showed significant reduction compared to negative control. Furthermore, the histopathology of mice skin treated with topical roflumilast nanoemulgel showed reduced psoriatic lesions. The study findings clearly demonstrated the effectiveness roflumilast loaded nanoemulgel (0.1% w/w) for the topical management of psoriasis in mice.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-14"},"PeriodicalIF":2.6,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144079544","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

Controlled anti-solvent precipitation for enhanced dissolution rate and antiplatelet activity of ticagrelor. 控制抗溶剂沉淀，提高替格瑞洛的溶出率和抗血小板活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-25 DOI: 10.1080/10837450.2025.2489744

Asmaa M Eldeeb, Dalia H Abdelkader, Gamal M El Maghraby

{"title":"Controlled anti-solvent precipitation for enhanced dissolution rate and antiplatelet activity of ticagrelor.","authors":"Asmaa M Eldeeb, Dalia H Abdelkader, Gamal M El Maghraby","doi":"10.1080/10837450.2025.2489744","DOIUrl":"10.1080/10837450.2025.2489744","url":null,"abstract":"The goal of our study is to augment ticagrelor (TC)'s dissolution rate and antiplatelet activity via controlled antisolvent precipitation. A saturated ethanolic solution of TC was prepared in the absence and presence of poloxamer 188 or gelucire 44/14. Aerosil 200 was added before controlled precipitation using water or water-containing poloxamer (1% w/v). The resulting precipitate was dried and characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and in vitro dissolution. FTIR showed hydrogen bonding after the processing of TC. DSC and PXRD reflected partial amorphization. A significant enhancement (p < 0.05) in dissolution efficiency and TC amount released after five minutes was also shown. The most effective composition was F6, which comprised TC, poloxamer, and Aerosil (5:5:2.5), or F9, utilizing gelucire instead of poloxamer at a similar ratio. Assessment of tail bleeding time (min) exhibited a significant (p < 0.05) prolongation for rat groups treated with F6 (24.71 ± 5.46) and F9 (30.06 ± 1.63) compared with negative control (3.43 ± 0.46) and unprocessed TC (5.78 ± 2.18). These results suggest an enhancement of TC's pharmacological activity probably due to enhanced bioavailability imparted with an enhanced dissolution rate. The study introduced controlled antisolvent precipitation as a simple tool for hastened TC's dissolution.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"463-473"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144030976","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

Enhancing ocular drug delivery: development and in vivo evaluation of mucoadhesive nanostructured lipid carriers for terbinafine. 增强眼部药物传递：特比萘芬黏附纳米结构脂质载体的开发和体内评价。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-08 DOI: 10.1080/10837450.2025.2488999

Tarek A Samra, Ibrahim A Elbahwy, Hammam A Mowafy, Mohsen I Afouna

{"title":"Enhancing ocular drug delivery: development and in vivo evaluation of mucoadhesive nanostructured lipid carriers for terbinafine.","authors":"Tarek A Samra, Ibrahim A Elbahwy, Hammam A Mowafy, Mohsen I Afouna","doi":"10.1080/10837450.2025.2488999","DOIUrl":"10.1080/10837450.2025.2488999","url":null,"abstract":"This study investigated incorporating Terbinafine Hydrochloride (TH) into chitosan-coated nanostructured lipid carrier (NLCs) to improve ocular treatment for fungal keratitis. Solubility studies were conducted to determine the most suitable lipids for NLCs formulation. TH-loaded NLCs were prepared via emulsification followed by ultrasonication. The impact of various lipids and surfactants on the formulation was investigated. The optimal formulation (TH-NLC10) was coated with chitosan (0.5% w/v), resulting in the coated TH-NLC10-CS 0.05% formulation. This formulation was evaluated for physicochemical properties, morphology, in-vitro release, mucoadhesion, permeation, and in vivo efficacy in treating ocular fungal keratitis in rabbits. Results revealed variations in lipids and surfactants significantly affected particle size. All prepared TH-NLCs formulations within the nanometer range. Physicochemical characterizations of the coated TH-NLC10-CS 0.05% showed 88.37 ± 2.41 nm size, 20.2 ± 1.4 mV zeta potential, 93.3 ± 1.5% w/w entrapment efficiency, and spherical morphology. TH-NLC10-CS 0.05% exhibited sustained TH release (66.65 ± 4.3% over 8 h) and strong mucoadhesion as indicated by a decrease in zeta potential from +20.2 ± 1.4 mV to +2.9 ± 0.7 mV. TH-NLC10-CS 0.05% demonstrated a 2.4-fold increase in TH permeation compared to plain TH, along with effective in vivo antifungal activity. This study confirms that mucoadhesive NLCs with TH are promising for the treatment of ocular fungal keratitis.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"417-429"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143784453","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

Lessons learned from the COVID-19 pandemic: the intranasal administration as a route for treatment - a patent review. 从COVID-19大流行中吸取的教训：鼻内给药作为一种治疗途径-专利审查。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-09 DOI: 10.1080/10837450.2025.2487575

Nicole Menezes Pinto, Marcos Rafael das Chagas Mendonça, Jeferson da Silva Santos, Camilla Martins Dos Santos Ferraz, Daniela Santos Oliveira, Lívia Vilas Boas Dos Santos, Adriano Antunes de Souza Araújo, Lucindo José Quintans Júnior, Divaldo Pereira Lyra Júnior, Alfredo Dias de Oliveira Filho, Ana Amélia Moreira Lira, Mairim Russo Serafini, Rogéria de Souza Nunes

{"title":"Lessons learned from the COVID-19 pandemic: the intranasal administration as a route for treatment - a patent review.","authors":"Nicole Menezes Pinto, Marcos Rafael das Chagas Mendonça, Jeferson da Silva Santos, Camilla Martins Dos Santos Ferraz, Daniela Santos Oliveira, Lívia Vilas Boas Dos Santos, Adriano Antunes de Souza Araújo, Lucindo José Quintans Júnior, Divaldo Pereira Lyra Júnior, Alfredo Dias de Oliveira Filho, Ana Amélia Moreira Lira, Mairim Russo Serafini, Rogéria de Souza Nunes","doi":"10.1080/10837450.2025.2487575","DOIUrl":"10.1080/10837450.2025.2487575","url":null,"abstract":"The COVID-19 pandemic exposed the fragility of today's marketed treatments for respiratory infections. As a primary site of infection, the upper airways may represent a key access route for the control and treatment for these conditions. The present study aims to explore and identify, through a patent review, the novelty of therapies for COVID-19 that use the intranasal route for drug administration. A search was carried out in Wipo and Espacenet, using the descriptors 'COVID-19 OR SARS-CoV 2' AND 'treatment OR therapy' AND NOT 'vaccine OR immunizing' and the classification 'A61K9/0043'. Of the 151 patents identified, we excluded 73 duplicates, and 36 documents that meet the criteria adopted for exclusion (not nasally administered formulations, vaccines, post COVID-19 treatments, uncertain route of administration or form). We identified 78 unique patents on patent databases, of which 42 were selected for this review. The documents revealed the use of the intranasal pathway not only for drug repositioning but also for using plant-derived and biological molecules. Overall, the new formulations explore a variety of known drugs and natural products incorporated in drug carrier systems and devices for drug delivery and administration. Thus, the intranasal route remains a promising strategy for drug delivery, offering direct access to the primary infection site and warranting further exploration.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"400-416"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143788754","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

Black seed oil boosts antidiabetic activity of glibenclamide: development of solidified self nanoemulsifying drug delivery system and evaluation in Streptozotocin-Induced diabetic rat model. 黑籽油增强格列本脲抗糖尿病活性：固化自纳米乳化给药系统的研制及链脲佐菌素诱导糖尿病大鼠模型的评价。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-11 DOI: 10.1080/10837450.2025.2489004

Abdelrahman Y Sherif, Doaa Hasan Alshora, Ahlam Alhusaini, Mohamed Abbas Ibrahim, Abdullah Ahmed Alghannam

{"title":"Black seed oil boosts antidiabetic activity of glibenclamide: development of solidified self nanoemulsifying drug delivery system and evaluation in Streptozotocin-Induced diabetic rat model.","authors":"Abdelrahman Y Sherif, Doaa Hasan Alshora, Ahlam Alhusaini, Mohamed Abbas Ibrahim, Abdullah Ahmed Alghannam","doi":"10.1080/10837450.2025.2489004","DOIUrl":"10.1080/10837450.2025.2489004","url":null,"abstract":"Self nano-emulsifying drug delivery system (SNEDDS) has been widely used to enhance dissolution and bioavailability of glibenclamide (GB). In addition, black seed oil, containing bioactive thymoquinone (TQ), showed promising antihyperglycemic effect. Therefore, this work aims to design solid SNEDDS formulation loaded with Black seed oil and GB. SNEDDS formulations were prepared and characterized for miscibility, dispersibility, droplet size, zeta potential, and in-vitro dissolution. Moreover, antidiabetic activity of prepared formulation against pure drug was evaluated using streptozotocin-induced diabetic rat model. The selected liquid SNEDDS (F7) formulation consisted of Kolliphor EL: Caproyl 90: BSO that produced nanoemulsion particles (24.9 ± 0.2 nm). Different solidified formulations were prepared from F7, and the solidified (S4) formulation was selected as optimum formulation that showed GB and TQ had a DE% value of 73.16 ± 0.59 and 70.9%, respectively. Overall, both pure GB and GB-SNEDDS formulations significantly reduced blood glucose levels compared to the control diabetic group. The GB-SNEDDS showing superior efficacy (67% reduction, p = 5.5 × 10-5) compared to pure GB (52% reduction, p = 1.5 × 10-4). Moreover, the GB-SNEDDS formulation has a significant (p = 0.0363) reducing action on blood glucose levels compared with the pure GB group. Present results showed that the prepared formulation boosted the antidiabetic activity of GB.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"430-440"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143780824","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

Design, fabrication, and in vitro-in vivo evaluation of surface-engineered pyrazinamide-loaded lipid nanoparticles for tuberculosis therapy. 设计，制造和体外体内评估表面工程吡嗪酰胺负载脂质纳米颗粒结核病治疗。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-22 DOI: 10.1080/10837450.2025.2492136

Nimitt V Chokshi, Preksha Vinchhi, Shreyansh Chauhan, Vivek Bora, Bhoomika M Patel, Mayur M Patel

{"title":"Design, fabrication, and in vitro-in vivo evaluation of surface-engineered pyrazinamide-loaded lipid nanoparticles for tuberculosis therapy.","authors":"Nimitt V Chokshi, Preksha Vinchhi, Shreyansh Chauhan, Vivek Bora, Bhoomika M Patel, Mayur M Patel","doi":"10.1080/10837450.2025.2492136","DOIUrl":"10.1080/10837450.2025.2492136","url":null,"abstract":"Pyrazinamide (PYZ), a nicotinamide derivative, is an essential first-line anti-TB drug. However, its dose-dependent hepatotoxicity poses a considerable challenge, accentuating the need for improved delivery approaches. The key objective of the research work was to develop mannose-appended pyrazinamide-containing solid-lipid nanoparticles (Mn-PYZ-SNs) for the targeted management of TB. The developed Mn-PYZ-SNs depicted a particle size of 422±09 nm, which was slightly higher than that of unconjugated PYZ-SNs (Un-PYZ-SNs)(401±08 nm), with a minimal reduction in entrapment efficiency(83.64±1.42%). The in vitro drug release studies demonstrated comparable sustained release patterns for both formulations, with a similarity factor (f2) of 77.33, indicating that the structural integrity of PYZ-SNs was maintained during mannose conjugation. Fluorescence imaging and flow cytometric analysis revealed significantly enhanced cellular uptake of Mn-C6-SNs, with a 1.60-fold increase compared to Un-C6-SNs. The in vivo pharmacokinetic studies conducted on Sprague-Dawley rats showed a 4.7-fold improvement in relative bioavailability for Mn-PYZ-SNs. Biodistribution studies demonstrated significantly higher lung accumulation of Mn-PYZ-SNs (1.93-fold) compared to Un-PYZ-SNs at 24 hours. The aforementioned results imply that the developed Mn-PYZ-SNs could be a promising carrier for the treatment of TB. via the oral intestinal lymphatic pathway, circumventing its hepatic first-pass metabolism, and thereby preventing hepatic adverse effects.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"474-487"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015397","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

Nanoparticles co-loaded with sorafenib and emodin: preparation and efficacy against liver cancer in vitro and in vivo. 索拉非尼和大黄素共载纳米颗粒：体外和体内抗肝癌的制备和疗效。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-21 DOI: 10.1080/10837450.2025.2489743

Yichun Jiang, Qiulan Li, Yan Chen, Xiaoshi Zhou, Yunzhong Luo, Tong Qiu, Zhen Meng, Xue Ying, Min Wu

{"title":"Nanoparticles co-loaded with sorafenib and emodin: preparation and efficacy against liver cancer in vitro and in vivo.","authors":"Yichun Jiang, Qiulan Li, Yan Chen, Xiaoshi Zhou, Yunzhong Luo, Tong Qiu, Zhen Meng, Xue Ying, Min Wu","doi":"10.1080/10837450.2025.2489743","DOIUrl":"10.1080/10837450.2025.2489743","url":null,"abstract":"Liver cancer is common worldwide and associated with relatively high mortality. Sorafenib is a first-line treatment for advanced liver cancer, but its efficacy is limited by its high toxicity, wide distribution in the body and low water solubility. Combination therapy with multiple drugs can lead to greater therapeutic efficacy, and nano-delivery systems can facilitate such therapy by solubilizing drugs and thereby increasing their bioavailability. Here nanoparticles of sorafenib and emodin encapsulated in the copolymer PEG-PLGA were constructed for liver therapy. Nanoparticles carrying sorafenib and emodin were prepared using a double emulsion method, and showed a diameter around 290 nm and uniform morphology. The encapsulation rates of sorafenib and emodin were 77.4 ± 0.71% and 80.78 ± 0.05%, the drug loading rates were 12.0 ± 0.1% and 13.0 ± 0.21%, and the cumulative drug release rates in pH 5.0 medium were 83.6% and 80.2%. The dual-loaded nanoparticles demonstrated significantly suppressed cellular proliferation and markedly enhanced apoptotic induction compared to free drug formulations or monotherapy nanoparticles. In murine xenograft models, the nanoparticles achieved superior tumor growth suppression (p < 0.01 vs free drugs). These findings collectively indicate that the sorafenib-emodin co-encapsulated PEG-PLGA nanoparticles represent a promising therapeutic platform for hepatocellular carcinoma intervention and may provide more therapeutic options against advanced liver cancer.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"450-462"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144049779","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

Enhanced skin penetration and clinical antifungal activity of eugenol encapsulated in aspasomes. 丁香酚包封在Aspasomes中增强皮肤渗透和临床抗真菌活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-07 DOI: 10.1080/10837450.2025.2486808

Muhammad Salah Eleleemy, Maha H Ragaie, Basma Hamdy Amin, Maha Nasr, Omaima A Sammour

{"title":"Enhanced skin penetration and clinical antifungal activity of eugenol encapsulated in aspasomes.","authors":"Muhammad Salah Eleleemy, Maha H Ragaie, Basma Hamdy Amin, Maha Nasr, Omaima A Sammour","doi":"10.1080/10837450.2025.2486808","DOIUrl":"10.1080/10837450.2025.2486808","url":null,"abstract":"Fungal infections are among the common diseases affecting the skin, which necessitate either topical or systemic delivery of antifungal agents. Eugenol was reported to exhibit antifungal properties, but owing to its poor skin-penetration ability, it requires encapsulation within delivery carriers. This study aimed to enhance the skin penetration and antifungal efficacy of eugenol through encapsulation in novel aspasomal formulations. Cationic and anionic aspasomes were prepared using ascorbyl palmitate, transcutol, and charge inducers, achieving high encapsulation efficiencies (90.55% for cationic, 63.32% for anionic) and stable formulations. Ex-vivo skin deposition studies showed significant eugenol retention in deeper skin layers, with 82.2% (cationic) and 77.2% (anionic) total skin deposition. Both formulations demonstrated superior antifungal activity compared to eugenol solution, with larger zones of inhibition against Candida albicans and Trichophyton rubrum. Clinical trials in patients with candidiasis and dermatophytosis revealed complete resolution of symptoms in 100% of patients treated with aspasomes, while eugenol solution showed partial improvement. These findings suggest that aspasomal encapsulation significantly enhances eugenol's therapeutic potential, offering a promising strategy for improving the treatment of fungal skin infections.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"372-384"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143753850","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

Chitosan nanoparticle encapsulation of thymus capitatus essential oil: in vitro release, antioxidant, antibacterial activity and cytotoxicity in MDA-MB-231 cells. 壳聚糖纳米颗粒包封胸腺精油：体外释放、抗氧化、抗菌活性及MDA-MB-231细胞毒性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-04-01 Epub Date: 2025-04-08 DOI: 10.1080/10837450.2025.2487255

Huseyin Beyaz, Doga Kavaz, Nahit Rizaner

{"title":"Chitosan nanoparticle encapsulation of thymus capitatus essential oil: in vitro release, antioxidant, antibacterial activity and cytotoxicity in MDA-MB-231 cells.","authors":"Huseyin Beyaz, Doga Kavaz, Nahit Rizaner","doi":"10.1080/10837450.2025.2487255","DOIUrl":"10.1080/10837450.2025.2487255","url":null,"abstract":"Thymus capitatus (Th. Ca) is known to treat mouth ulcers and respiratory infections in Cyprus. However, antioxidant, antibacterial, and cytotoxic potential of Th. Ca. EO on MDA-MB-231 cells and its' encapsulation into nanoparticles has not been well studied. Therefore, we aimed to analyze the antioxidant, antibacterial, cytotoxic potential, loading efficiency, and in vitro release profile of both Th. Ca. EO and Chitosan Nanoparticle (Ch. Np) - Th. Ca. EO. GC-MS analysis revealed 53.97% carvacrol, 14.53% borneol, and 12.09% sabinene presence in EO. The loading efficiency of Th. Ca. EO into Ch. Np. was calculated as 35.27% and the in vitro release profile reached a maximum of 68% in pH 7 for two weeks. The Minimum Inhibitory Concentration (MIC) assay showed that E. coli had an MIC50 of 0.3215 mg/ml while B. subtilis had an MIC50 of 0.5304 mg/ml. The antioxidant activity of the EO was assessed by performing a DPPH assay with an IC50 = 440 μg/ml. Trypan Blue Assay revealed that 60 µg/ml Th. Ca. EO significantly reduced the cell viability of MDA-MB-231 cells by 10.7% at 48h and 20.06% at 72h. Overall, Ch. Np. - Th. Ca. EO has shown a promising formulation for the pharmaceutical industry.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"385-399"},"PeriodicalIF":2.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143753920","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}

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