Pharmaceutical Development and Technology最新文献

Topical hyalubilosomes of dantrolene sodium as muscle targeted nanocarrier for muscle spasms: fabrication, ex-vivo permeation and behavioral animal model. 作为肌肉痉挛靶向纳米载体的丹曲林钠局部透明体：制备、体外渗透和行为动物模型。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-17 DOI: 10.1080/10837450.2025.2504999

Abdelrahaman M M Othman, Ossama Y Abdallah, Yosra S R Elnaggar

{"title":"Topical hyalubilosomes of dantrolene sodium as muscle targeted nanocarrier for muscle spasms: fabrication, ex-vivo permeation and behavioral animal model.","authors":"Abdelrahaman M M Othman, Ossama Y Abdallah, Yosra S R Elnaggar","doi":"10.1080/10837450.2025.2504999","DOIUrl":"https://doi.org/10.1080/10837450.2025.2504999","url":null,"abstract":"Topical muscle relaxants are gaining interest in pharmaceuticals. Dantrolene sodium (DS), an FDA-approved relaxant targeting ryanodine receptors, is limited in topical use by poor physicochemical properties, delayed onset, and hepatotoxicity. This study introduces the first optimized hyalubilosome-based nanocarrier for non-invasive DS delivery. Two anionic surfactants were used as edge activators to improve drug encapsulation and permeation. The optimized nanocarrier had a spherical shape, 165 nm particle size, -31.2 mV zeta potential, and 97.47% entrapment efficiency. Ex vivo studies showed superior permeation compared to DS suspension (10% in water, pH 6.8), with 30% of the dose permeating within 15 min. In vivo, efficacy was tested in Wistar mice using the Straub tail test with a single 30 mg/kg topical dose. Behavioral analysis showed a fivefold increase in muscle relaxation vs. untreated controls (p < 0.0001). The formulation had an onset within one minute and complete relief within two minutes, unlike the conventional topical DS, which showed no effect for 90 min. This highlights hyaluronic acid-based transbilosomes as a promising nanoplatform for fast, effective topical DS delivery and potential muscle spasm treatment.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-14"},"PeriodicalIF":2.6,"publicationDate":"2025-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144079545","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

Formulation and characterization of transfersomes for ocular delivery of tonabersat. 托那伯沙眼给药转移体的制备与表征。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-15 DOI: 10.1080/10837450.2025.2501991

Santosh Bhujbal, Ilva D Rupenthal, Priyanka Agarwal

{"title":"Formulation and characterization of transfersomes for ocular delivery of tonabersat.","authors":"Santosh Bhujbal, Ilva D Rupenthal, Priyanka Agarwal","doi":"10.1080/10837450.2025.2501991","DOIUrl":"10.1080/10837450.2025.2501991","url":null,"abstract":"Transfersomes (TFS) are deformable vesicles, known for their ability to enhance transdermal drug penetration. This study aimed to evaluate whether TFS can also enhance ocular delivery of poorly soluble tonabersat. TFS were prepared using Phospholipon® 90G with Tween® 80 as the edge activator. The effect of formulation parameters (edge activator and cryoprotectant concentrations) on TFS characteristics were evaluated using a full factorial design. The optimized TFS eyedrop was characterized for particle size, zeta potential, deformability, entrapment efficiency (EE), drug content, pH, osmolality and TFS stability over 3 months at different storage conditions. Furthermore, drug penetration into the cornea, conjunctiva, eyelid, and sclera-choroid after topical application was studied ex vivo using a tonabersat solution in medium chain triglycerides as the control. The optimized TFS formed spherical unilamellar vesicles with a mean diameter <130 nm, EE >80%, and were stable at -20 and 5 ± 3 °C for up to 3 months. The TFS eyedrop resulted in significantly greater ocular penetration than the control without affecting the barrier properties of the tested tissues. Drug penetration into different ocular tissues was compared, shedding light on the penetration mechanism of TFS. Overall, this study demonstrates that TFS provide a promising alternative for the ocular delivery of tonabersat.","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":"144009207","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

Enzyme-sensitive peptide KC26 modifies milk exosomes encapsulating carboplatin for the treatment of retinoblastoma. 酶敏感肽KC26修饰乳外泌体包封卡铂治疗视网膜母细胞瘤。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-13 DOI: 10.1080/10837450.2025.2505005

Hetong Wang, Wei Wang, Qin Tang, Xun Liu, Limin Zhu, Di Sun, Tingting Lin

{"title":"Enzyme-sensitive peptide KC26 modifies milk exosomes encapsulating carboplatin for the treatment of retinoblastoma.","authors":"Hetong Wang, Wei Wang, Qin Tang, Xun Liu, Limin Zhu, Di Sun, Tingting Lin","doi":"10.1080/10837450.2025.2505005","DOIUrl":"https://doi.org/10.1080/10837450.2025.2505005","url":null,"abstract":"Milk exosomes have also been widely used as emerging delivery vehicles for various therapeutic cargoes. Retinoblastoma (RB) is the most common primary intraocular malignancy of childhood. However, the therapeutic efficacy is severely hampered by the presence of blood-retinal barrier (BRB) and systemic side effects. Legumain (LGMN) can be used as a target for tumor microenvironment responsive delivery design and therapeutic applications. Here, a LGMN-sensitive peptide KC26-modified milk exosomes loaded with carboplatin (CBP-KC26-MExos). The system enables milk exosomes loaded with carboplatin (CBP) to reach the target cells by binding to LGMN, improves tumor targeting,enhances cellular uptake and apoptosis, inhibits cell proliferation, invasion and migration. Intravenous injection of CBP-KC26-MExos cross the BRB significantly inhibited intraocular tumor progression and reduced CBP toxicity. We have developed a \"drug-target-carrier\" approach and proposed an enzyme sensitive peptide (KC26) modified milk exosomes loaded with CBP, providing a perspective for exploring targeted therapy of tumor cells and tumor microenvironment, and offering a promising clinical strategy for the treatment of retinoblastoma.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-19"},"PeriodicalIF":2.6,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144026693","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

Solid Supersaturated Self-Nanoemulsifying Drug Delivery System for Abiraterone Acetate: Improved Drug loading, Dissolution, Cellular Uptake and Anticancer Activity. 醋酸阿比特龙固体过饱和自纳米乳化给药系统：改善药物负载、溶出、细胞摄取和抗癌活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-13 DOI: 10.1080/10837450.2025.2505003

Ayush Nair, Mayur Aalhate, Srushti Mahajan, Ujala Gupta, Indrani Maji, Pankaj Kumar Singh

{"title":"Solid Supersaturated Self-Nanoemulsifying Drug Delivery System for Abiraterone Acetate: Improved Drug loading, Dissolution, Cellular Uptake and Anticancer Activity.","authors":"Ayush Nair, Mayur Aalhate, Srushti Mahajan, Ujala Gupta, Indrani Maji, Pankaj Kumar Singh","doi":"10.1080/10837450.2025.2505003","DOIUrl":"https://doi.org/10.1080/10837450.2025.2505003","url":null,"abstract":"Abiraterone acetate (ABT) is an androgen biosynthesis inhibitor approved for the treatment of prostate cancer. However, the treatment course of ABT is constrained by its high dose, poor solubility and permeability issues. A solid supersaturated self-nanoemulsifying drug delivery system (ssSNEDDS) is an excellent approach for improving drug loading. The aim was to increase the solubility and drug loading of ABT in SNEDDS via supersaturation by using a polymeric precipitation inhibitor (HPMC E5). Liquid SNEDDS were thoroughly optimized with a mixture design followed by solidification with Aerosil® 200 by the adsorption method. The developed ABT-ssSNEDDS showed a nano-ranged particle size of 106.23 ± 4.15 nm and PDI of 0.234 ± 0.0069. Further, the powder showed an angle of repose of 34.86 ± 0.30° indicating good flow properties with smooth morphology under SEM analysis. DSC and PXRD studies revealed amorphization of ABT in the ABT-ssSNEDDS group. Further, the dissolution study demonstrated significantly higher ABT release from ABT-ssSNEDDS in comparison to free ABT after 2 h in pH 1.2 and 6.8 pH buffer. In-vitro cell culture studies in the PC-3 cell line denoted significantly enhanced anticancer activity and cellular uptake. Thus, ABT-ssSNEDDS could be an encouraging approach for improved oral therapy and enhanced drug loading of ABT.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-23"},"PeriodicalIF":2.6,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015402","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

An insight into Cell-Penetrating Peptides: Perspectives on Design, Optimization, and Targeting in Drug Delivery Systems. 洞察细胞穿透肽：在药物输送系统的设计，优化和靶向的观点。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-13 DOI: 10.1080/10837450.2025.2505000

Ali Asghar Khakshur, Elham Khodaverdi, Hossein Kamali, Ali Nokhodchi

{"title":"An insight into Cell-Penetrating Peptides: Perspectives on Design, Optimization, and Targeting in Drug Delivery Systems.","authors":"Ali Asghar Khakshur, Elham Khodaverdi, Hossein Kamali, Ali Nokhodchi","doi":"10.1080/10837450.2025.2505000","DOIUrl":"https://doi.org/10.1080/10837450.2025.2505000","url":null,"abstract":"Objective: The authors carried out a comprehensive review of the application of peptides known as cell-penetrating peptides (CPPs) in various drug delivery systems (DDS), with the prospect of achieving novel solutions and ideas to overcome the challenges of DDS, by making them more able to penetrate cells and biological membranes.Methods: A conceptual search was conducted in relevant literature databases (Scopus, PubMed, Web of Science, and Google Scholar) up to 1 April 2025 using keywords such as drug delivery systems, cell-penetrating peptides, CPPs, complexes, conjugates, nanoparticles, dendrimers, exosomes, liquid crystalline, liposomes, micelles, nanospheres and lipid nanoparticles.Results: The studies demonstrate that the antimicrobial effect of drugs, including curcumin, gentamicin, and antifungal drugs like imidazoacridinone derivatives, can be enhanced when they are conjugated or complexed with CPPs. CPPs possess positive charges, which make them suitable for gene therapy applications by facilitating the delivery of plasmids and siRNAs with negative charges in modern delivery systems. Medicinal formulations containing CPPs in combination with liquid crystals or nanostructured lipid carriers (NLCs) increase drugs penetration to the skin. Additionally, several investigations showed that CPPs could have a positive impact on the pharmacokinetic and pharmacodynamic of chemotherapy agents, reducing their side effects.Conclusion: CPPs have significant potential in enhancing penetration, bioavailability, targeting, and optimization of DDS. By using computer modeling and designing CPPs with more desirable features and conducting more clinical studies, new methods for treating diseases and better formulations can be achieved.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-34"},"PeriodicalIF":2.6,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015380","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

Lycopene-Carrier Solid Dispersion loaded Lipid Liquid Crystal Nanoparticle: in vitro Evaluation and in vivo Wound Healing Effects. 番茄红素载体固体分散脂质液晶纳米颗粒：体外评价和体内伤口愈合效果。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-13 DOI: 10.1080/10837450.2025.2504998

Farhad Shahverdi, Elham Khodaverdi, Jebrail Movaffagh, Soheil Tafazzoli Mehrjardi, Hossein Kamali, Ali Nokhodchi

{"title":"Lycopene-Carrier Solid Dispersion loaded Lipid Liquid Crystal Nanoparticle: in vitro Evaluation and in vivo Wound Healing Effects.","authors":"Farhad Shahverdi, Elham Khodaverdi, Jebrail Movaffagh, Soheil Tafazzoli Mehrjardi, Hossein Kamali, Ali Nokhodchi","doi":"10.1080/10837450.2025.2504998","DOIUrl":"https://doi.org/10.1080/10837450.2025.2504998","url":null,"abstract":"This study was conducted to develop a lycopene-carrier solid dispersion-loaded lipid liquid crystal nanoparticle (LLC) formulation aimed at enhancing aqueous solubility, bioavailability, and wound healing efficacy. Lycopene was extracted from tomato paste using the Soxhlet method and was formulated into solid dispersions with polyvinylpyrrolidone (PVP) and Poloxamer (Plx) to enhance the solubility of lycopene. The physicochemical properties of the solid dispersion products were characterized. Cytotoxicity on human fibroblast cells, cell migration, and wound healing treatment in the mice were also assessed. PVP demonstrated greater efficacy in enhancing the aqueous solubility of lycopene than Plx. The results indicated that the morphology of the LLC was cubosome, achieving a high encapsulation efficiency of 71.57 ± 2.1%. The LLC formulations demonstrated significantly enhanced release rates of 68.18 ± 1.78% and improved skin permeation compared to the lycopene solid dispersion solution. The results of the cell culture demonstrated the safety of the formulation, and the in vitro scratch test showed the migration of fibroblast cells in the presence of the lycopene-PVP solid dispersion loaded LLC compared to lycopene alone. Based on the obtained results, it can be concluded that the proposed formulation (lycopene-PVP solid dispersion loaded LLC) could be a suitable option for wound healing.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-19"},"PeriodicalIF":2.6,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144023279","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 stabilized by glycyrrhizic acid for liver targeted drug delivery: impact of glycyrrhizic acid concentrations. 甘草酸稳定的槲皮素纳米晶体用于肝脏靶向药物递送：甘草酸浓度的影响。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-01 DOI: 10.1080/10837450.2025.2498370

Fengxia Wang, Chengying Shen, Fangwen Chen, Jinyun Cao, Pengfei Yue, Baode Shen

{"title":"Quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery: impact of glycyrrhizic acid concentrations.","authors":"Fengxia Wang, Chengying Shen, Fangwen Chen, Jinyun Cao, Pengfei Yue, Baode Shen","doi":"10.1080/10837450.2025.2498370","DOIUrl":"https://doi.org/10.1080/10837450.2025.2498370","url":null,"abstract":"The purpose of this study was to investigate the impact of glycyrrhizic acid (GL) concentrations on in vitro and in vivo behavior of quercetin (QT) nanocrystals stabilized by GL (QT-NCs/GL), with a particular focus on its influence on liver targeted drug delivery. QT-NCs/GL with similar particle size around 200 nm were successfully prepared by media milling technique using different concentrations of GL, which were 10%, 20% and 40% (w/w) of the QT. All QT-NCs/GL showed oval and rod shapes, and remained in crystalline state with a reduced crystallinity as GL concentrations increased. All QT-NCs/GL exhibited significant solubility increase and drug release improvement of QT as compared to raw QT. Pharmacokinetics revealed similar plasma concentration-time profiles of QT after intravenous of all QT-NCs/GL. All QT-NCs/GL exhibited rapidly distribution of QT to liver with the maximum QT concentration more than 750 μg/g at 5 min after intravenous administration, and the AUC0∼t of QT for three formulations in liver were significant difference with the following order: QT-NCs/GL-40% > QT-NCs/GL-20% > QT-NCs/GL-10%. These results suggested that different GL concentrations exhibited significant influence on liver targeted delivery of QT-NCs/GL, and more GL used in QT-NCs/GL may contribute more liver distribution of QT.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-10"},"PeriodicalIF":2.6,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144017644","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