AAPS PharmSciTech最新文献_第5页

Freeze-Drying as a Tool for Preparing Porous Materials: From Proof of Concept to Recent Pharmaceutical Applications. 冷冻干燥作为制备多孔材料的工具：从概念证明到最近的制药应用。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-06-03 DOI: 10.1208/s12249-025-03117-4

Kawthar K Abla, Mohammed M Mehanna

{"title":"Freeze-Drying as a Tool for Preparing Porous Materials: From Proof of Concept to Recent Pharmaceutical Applications.","authors":"Kawthar K Abla, Mohammed M Mehanna","doi":"10.1208/s12249-025-03117-4","DOIUrl":"10.1208/s12249-025-03117-4","url":null,"abstract":"Freeze-drying (FD) is the most extensive drying technique in pharmaceutical and biopharmaceutical industries. It relies on three main steps: freezing, primary, and secondary drying, where the sample is frozen and then dried by ice sublimation. FD possesses several features, mainly its suitability for heat-sensitive materials and its ability to produce dry products with improved physicochemical characteristics. Although FD is a gentle drying process, it can cause numerous stresses that induce chemical and physical instabilities. Herein, the addition of suitable excipients along with optimizing the process parameters is critical in attaining lyophilizates with high-quality attributes. Besides, the freeze-drying method has been explored as a unique route to produce porous materials with different applications. This work aims to dismantle the basics of freeze-drying and its role in developing porous materials, mainly amorphous and co-amorphous solid-dispersions, orodispersible tablets and films, as well as porous dressings and 3D scaffolds for effective wound healing and tissue engineering, respectively. The challenges and limitations of lyophilization have also been addressed.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"159"},"PeriodicalIF":3.4,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144214519","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 Characterization of Diclofenac Sodium-Purolite A430MR Complexes for Taste Masking. 双氯芬酸钠- purolite A430MR味掩蔽配合物的制备与表征。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-06-03 DOI: 10.1208/s12249-025-03138-z

Genyang Ye, Qun Wang, Yibo Shang, Yibo Li, Rui Yang, Boyu Jing, Qiang Fu

引用次数: 0

Recent Advances in Development of Buccal Formulations: From Small to Macromolecules. 口腔制剂的最新进展：从小分子到大分子。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-06-03 DOI: 10.1208/s12249-025-03154-z

Vrundakumari R Solanki, Vijaykumar K Parmar

引用次数: 0

The Role of Low Global Warming Potential Propellants on Suspension Metered Dose Inhaler Sprays. 低全球变暖潜势推进剂对悬浮计量吸入器喷雾的作用。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-06-02 DOI: 10.1208/s12249-025-03147-y

Daniel J Duke, Lingzhe Rao, Benjamin Myatt, Phil Cocks, Stephen Stein, Hui Xin Ong, Paul Young

{"title":"The Role of Low Global Warming Potential Propellants on Suspension Metered Dose Inhaler Sprays.","authors":"Daniel J Duke, Lingzhe Rao, Benjamin Myatt, Phil Cocks, Stephen Stein, Hui Xin Ong, Paul Young","doi":"10.1208/s12249-025-03147-y","DOIUrl":"10.1208/s12249-025-03147-y","url":null,"abstract":"The reformulation of suspension-based pressurized metered dose inhalers (pMDI) with low global warming potential (GWP) propellants is challenged by wide-ranging changes to their chemicophysical properties such as vapor pressure, density and latent heat. The effect of low-GWP propellants on spray pattern and plume geometry for suspension pMDIs are not fully understood. There is a lack of data regarding the role of propellant choice and potential interactions with suspended drugs, which may explain performance variations between products and guide development of in-silico models. In this study, high speed imaging was used to measure the plume morphology and optical density of sprays containing HFA134a, HFA152a and HFO1234ze(E) propellants. Propellant-only placebo controls were compared to suspension formulations containing 2 mg/mL salbutamol sulphate. It was found that the presence of suspended particles has a significant effect on plume structure, reducing correlations between propellant thermophysical properties and cone angle, targeting angle, and optical center of mass by 6-7 times. These effects vary depending on propellant type due to variations in flash-evaporation behavior, which is less pronounced in low-GWP propellants compared to HFA134a. HFA152a sprays have a 23% reduction in Jakob number compared to HFA134a; plume width at the mouthpiece exit is commensurately increased by 40%. Equivalent HFO1234ze(E) sprays have less pronounced differences in Jakob number (13% reduced) and plume width (25% increased) compared to equivalent HFA134a sprays. Empirical models and standards which implicitly incorporate the flash-evaporation effects commonly observed in high-GWP HFA propellants may require adjustment to be suitable for use with low-GWP formulations.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"154"},"PeriodicalIF":3.4,"publicationDate":"2025-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144207346","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

Injectable PLGA-based In Situ Forming Subconjunctival Implant for Sustained Ocular Delivery of Ketotifen Fumarate: Formulation, Drug Release, and Biocompatibility Studies. 可注射的基于plga的原位形成结膜下植入物用于富马酸酮替芬的持续眼部递送：配方、药物释放和生物相容性研究。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-06-02 DOI: 10.1208/s12249-025-03142-3

Nur Mita, Xuejia Kang, Pengyu Chen, Oladiran Fasina, Shenise Howard, Anna-Catherine Bowden, Richard J McMullen, Amol Suryawanshi, R Jayachandra Babu

{"title":"Injectable PLGA-based In Situ Forming Subconjunctival Implant for Sustained Ocular Delivery of Ketotifen Fumarate: Formulation, Drug Release, and Biocompatibility Studies.","authors":"Nur Mita, Xuejia Kang, Pengyu Chen, Oladiran Fasina, Shenise Howard, Anna-Catherine Bowden, Richard J McMullen, Amol Suryawanshi, R Jayachandra Babu","doi":"10.1208/s12249-025-03142-3","DOIUrl":"10.1208/s12249-025-03142-3","url":null,"abstract":"Ketotifen fumarate is very effective in treating ocular conditions like allergic conjunctivitis. However, its clinical effectiveness is limited by rapid washout, frequent dosing, and poor bioavailability. This study developed a ketotifen fumarate-loaded in situ forming subconjunctival injectable implant (ISFSI) for use in large animal species such as horses and alpacas. ISFSIs were formulated by dispersing ketotifen fumarate in polylactide-co-glycolide (PLGA) combined with different release retarders (Kolliphor® RH 40, Labrasol®, and Maisine®), then characterized for visual appearance, viscosity, solidification time, and in vitro drug release. The changes in the release medium pH and the solidified ISFSI wet weight were monitored for up to 4 weeks. The selected ISFSI, KFM5, was further characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and rheological behavior. The injectability of KFM5 was predicted using the power law for five different syringe and needle dimensions. Cytotoxicity was tested using the Alamar Blue assay and Calcein AM/PI staining on a human corneal epithelial cell line (HCE-T). Results showed that all ISFSI formulations were clear yellowish, with drug recoveries exceeding 95%, varying viscosities, and solidified upon contact with the release medium. KFM5 exhibited a triphasic drug release profile with the lowest burst release (4.91 ± 0.55%) and followed Higuchi kinetics. SEM imaging revealed a \"hollow and sponge-like\" structure, while DSC confirmed the crystallinity and thermal transitions of ketotifen fumarate within the solidified implant. Rheological analysis indicated shear-thinning fluid behavior with acceptable injection forces. Cytotoxicity assays confirmed > 90% cell viability, confirming biocompatibility in the ocular tissue.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"153"},"PeriodicalIF":3.4,"publicationDate":"2025-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144207345","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

Antitumor Efficacy of Paclitaxel Injection Concentrate for Nanodispersion in Patient-Derived Breast, Head and Neck, and Non-Small Cell Lung Cancer Mouse Xenografts. 紫杉醇注射浓缩物纳米分散体在患者来源的乳腺癌、头颈癌和非小细胞肺癌小鼠异种移植中的抗肿瘤效果。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-05-30 DOI: 10.1208/s12249-025-03153-0

Ajay J Khopade, Malay D Shah, Bhushan S Borole, Vinod Burade

{"title":"Antitumor Efficacy of Paclitaxel Injection Concentrate for Nanodispersion in Patient-Derived Breast, Head and Neck, and Non-Small Cell Lung Cancer Mouse Xenografts.","authors":"Ajay J Khopade, Malay D Shah, Bhushan S Borole, Vinod Burade","doi":"10.1208/s12249-025-03153-0","DOIUrl":"10.1208/s12249-025-03153-0","url":null,"abstract":"Paclitaxel Injection Concentrate for Injection (PICN) is a novel nanoparticle formulation designed to overcome the limitations associated with the administration of marketed Cremophor and albumin based (nab) paclitaxel formulations. This study compared the in vivo antitumor efficacy of PICN with that of solvent-based paclitaxel and nab-paclitaxel in a murine NMRI nu/nu athymic nude mouse model bearing various human tumor xenotransplants: head and neck cancer (HNXF 1838 and HNXF 1842), lung cancer xenografts (LXFA 1584), and breast cancer xenografts (MAXF 574 and MAXF 1384). PICN displayed good to excellent antitumor activity. Moreover, PICN inhibited tumor growth more than solvent based paclitaxel formulation when compared at comparable tolerated dose levels. The higher antitumor efficacy of PICN compared to paclitaxel at lower dose levels of half the maximum tolerated dose (1/2MTD) was significant (P < 0.05) in three of the tumor models, i.e. HNXF 1842, MAXF 574, and MAXF 1384. The higher efficacy of PICN compared to paclitaxel was also evident at the MTD, but somewhat less pronounced, and was significant (P < 0.05) in one tumor model (HNXF 1838). The antitumor activity of PICN was similar to that of nab-paclitaxel. However, in one tumor model (HNXF 1838) PICN 50 mg/kg (1/2 MTD) showed a slight benefit over the same dose of nab-paclitaxel. The nanoparticulate nature of PICN and nab-paclitaxel therefore seems to enhance tumor cell penetration compared to conventional paclitaxel, resulting in better antitumor efficacy.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"150"},"PeriodicalIF":3.4,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144186233","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 Study of Erythromycin Dry Powder Inhaler Based on Ternary Complex Structure. 基于三元配合物结构的红霉素干粉吸入剂的制备与研究。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-05-30 DOI: 10.1208/s12249-025-03140-5

Hongyu Yang, Jianpeng Qin, Yuou Wang, Ji Li, Dongkai Wang

{"title":"Preparation and Study of Erythromycin Dry Powder Inhaler Based on Ternary Complex Structure.","authors":"Hongyu Yang, Jianpeng Qin, Yuou Wang, Ji Li, Dongkai Wang","doi":"10.1208/s12249-025-03140-5","DOIUrl":"10.1208/s12249-025-03140-5","url":null,"abstract":"Pulmonary bacterial infections are a common disease, with erythromycin being a first-line treatment. However, conventional erythromycin tablets and injectables exhibit limited therapeutic efficacy and are associated with severe gastrointestinal side effects. Additionally, injectable formulations suffer from poor patient compliance. Dry powder inhaler (DPI) offers superior pulmonary targeting, circumvent first-pass metabolism, and are portable, enhancing patient adherence. In this study, we successfully developed a ternary inhalable erythromycin dry powder formulation (Ery-DPI). The Quality by Design (QbD) approach was employed to establish a design space for erythromycin micronization and to optimize the formulation. The physicochemical properties and fine particle fraction of the erythromycin DPI were evaluated through in vitro experiments. The final formulation, composed of α-lactose, mannitol, and erythromycin in a ratio of 1:0.2:2 (v/v/v), exhibited an FPF of 70 ± 3%. In vivo studies demonstrated that, compared to intravenous administration, Ery-DPI achieved higher and more stable local drug exposure in the lungs. Overall, our study provides new insights into pulmonary drug delivery strategies for treating bacterial infections.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"151"},"PeriodicalIF":3.4,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144186237","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

Correction: Stability Evaluation of Lyotropic Liquid Crystalline Precursor for the Co-delivery of Chlorhexidine and Silver Nanoparticles. 修正：溶变液晶前驱体对氯己定和纳米银共递送的稳定性评价。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-05-30 DOI: 10.1208/s12249-025-03150-3

Fangqin Fu, Xin Li, Tengyi Zheng, Xiao Xia, Minqun Du, Zhengwei Huang, Ying Huang, Xin Pan, Chuanbin Wu

引用次数: 0

Grape Seed Oil Microemulsion for Improved Skin Delivery of Resveratrol. 葡萄籽油微乳液用于改善白藜芦醇的皮肤输送。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-05-30 DOI: 10.1208/s12249-025-03146-z

Marianne A P C Nogueira, Camila O Cardoso, Lucas F F Albuquerque, Marcilio Cunha-Filho, Tais Gratieri, Guilherme M Gelfuso

{"title":"Grape Seed Oil Microemulsion for Improved Skin Delivery of Resveratrol.","authors":"Marianne A P C Nogueira, Camila O Cardoso, Lucas F F Albuquerque, Marcilio Cunha-Filho, Tais Gratieri, Guilherme M Gelfuso","doi":"10.1208/s12249-025-03146-z","DOIUrl":"10.1208/s12249-025-03146-z","url":null,"abstract":"Given the anti-inflammatory properties of Resveratrol, this paper proposes developing a grape seed oil-in-water microemulsion (ME) for topical administration to treat inflammatory skin pathological conditions. Thermal analyses confirmed compatibility between Resveratrol, grape seed oil, Tween 80, and Span 80 used in the formulations. Two compositions (ME1 and ME2) were selected from a pseudo-ternary diagram prepared by components titration. ME1 (50% water, 35% surfactant, 15% oil) and ME2 (60% water, 30% surfactant, 10% oil) showed mean droplet sizes of 23.1 ± 0.7 nm and 24.9 ± 1.7 nm (PdI = 0.34 and 0.47), zeta potential between -11.7 ± 0.5 and -13.6 ± 0.9 mV, and pH values of 6.2 ± 0.5 and 7.1 ± 1.1, respectively. Rheological analyses revealed Newtonian behavior and low viscosity, with physical stability for 60 days at room temperature. In vitro drug permeation studies using porcine skin demonstrated that ME increased Resveratrol penetration into deeper skin layers by fourfold (p < 0.001) compared to the control solution (ME1: 2.9 ± 0.1 μg/cm2, ME2: 2.4 ± 0.1 μg/cm2), while reducing retention in the stratum corneum. HET-CAM experiments indicated safety for topical application. In conclusion, the ME was a promising alternative for future clinical investigations to treat inflammatory skin conditions.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"148"},"PeriodicalIF":3.4,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144186236","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

Combination Drug Product of Amorphous Solid Dispersion Show Extended Supersaturation and Enhanced Dissolution. 非晶态固体分散体的组合药物表现出过饱和延长和溶解增强。

IF 3.4 4区医学

AAPS PharmSciTech Pub Date : 2025-05-30 DOI: 10.1208/s12249-025-03126-3

Prachi Joshi, Abhay T Sangamwar

{"title":"Combination Drug Product of Amorphous Solid Dispersion Show Extended Supersaturation and Enhanced Dissolution.","authors":"Prachi Joshi, Abhay T Sangamwar","doi":"10.1208/s12249-025-03126-3","DOIUrl":"10.1208/s12249-025-03126-3","url":null,"abstract":"Investigation on multidrug formulations is increasing, because of enhanced efficacy and patient compliance. The two antiparasitic drugs Albendazole (ABZ) and mebendazole (MBZ) combination is well reported in the clinical research. However, ABZ-MBZ drug combination do not progressed well due to in vivo drug-drug interaction of precipitation of either drug leading to sub-therapeutic concentration in systemic circulation. Herein, we studied the effect of various cellulosic polymers on the supersaturation behaviour of ABZ and MBZ in combination. We screened a large group of cellulosic polymers and selected HPMCAS on the basis of supersaturation behaviour, drug-polymer solubility, and drug particle size. An amorphous solid dispersion was developed comprising ABZ-MBZ and HPMCAS. Drug amorphization was confirmed using thermal and crystallographic technique. In kinetic solubility, the ternary ASD enhanced the solubility of ABZ/MBZ by 1.88/3.52-fold (pH 1.2), 146.08/201.38-fold (pH 6.8) and 182.47/50.38-fold (water) as compared to crystalline ABZ and MBZ. In vitro release study supports kinetic solubility data as in ternary ASD the fraction drug release of ABZ/MBZ was increased by 2.22/2.55-fold (pH 1.2), 22.82/25.98-fold (pH 6.8) and 18.5/12-fold (water) in comparison to crystalline drugs. AUC0-120 min displayed significant enhancement in drug solubility with ternary ASD.","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"152"},"PeriodicalIF":3.4,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144186234","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