4.7 Article

Development, characterization and application of in situ gel systems for intranasal delivery of tacrine

期刊

INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 468, 期 1-2, 页码 272-282

出版社

ELSEVIER
DOI: 10.1016/j.ijpharm.2014.04.015

关键词

Tacrine; In situ gel; Intranasal; Pluronic F-127; Pharmacokinetics

资金

  1. General Research Fund [CUHK 480809]

向作者/读者索取更多资源

The present study aimed to develop an in situ gel formulation for intranasal delivery of tacrine (THA), an anti-Alzheimer's drug. Thermosensitive polymer Pluronic F-127 was used to prepare THA in situ gels. Sol-gel transition temperature (Tsol-gel), rheological properties, in vitro release, and in vivo nasal mucociliary transport time were optimized. The pharmacokinetics and brain dispositions of in situ gel were compared with that from THA oral solution in rats. The in situ gel demonstrated a liquid state with Newtonian fluid behavior under 20 degrees C, while it exhibited as non-flowing gel with pseudoplastic fluid behavior beyond its Tsol-gel of 28.5 degrees C. Based on nasal mucociliary transport time, the in situ gel significantly prolonged its retention in nasal cavity compared to solution form. Moreover, the in situ gel achieved 2-3 fold higher peak plasma concentration (C-max) and area under the curve (AUC) of THA in plasma and brain tissue, but lowered Cmax and AUC of the THA metabolites compared to that of oral solution. The enhanced nasal residence time, improved bioavailability, increased brain uptake of parent drug and decreased exposure of metabolites suggested that the in situ gel could be an effective intranasal formulation for THA. (C) 2014 Elsevier B.V. All rights reserved.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.7
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

Article Pharmacology & Pharmacy

Screening of Bioequivalent Extended-Release Formulations for Metformin by Principal Component Analysis and Convolution-Based IVIVC Approach

Yufeng Zhang, Hua Liu, Minghui Johnson Tang, Nicolas James Ho, Tsun Lam Shek, Zhijun Yang, Zhong Zuo

Summary: This study presented a novel approach for the selection of bioequivalence (BE) extended-release (ER) formulations, using dissolution tests, principal component analysis (PCA), IVIVC model development, and in vivo pharmacokinetic data analysis. A pilot BE study in healthy volunteers confirmed the WM formulation as the most suitable for GXR.

AAPS JOURNAL (2021)

Article Plant Sciences

Accumulation of the Major Components from Polygoni Multiflori Radix in Liver and Kidney after Its Long-Term Oral Administrations in Rats

Dan Li, Yuanfeng Lyu, Jiajia Zhao, Xiaoyu Ji, Yufeng Zhang, Zhong Zuo

Summary: The study evaluated the biodistribution of Polygoni Multiflori Radix components in rats, revealing significant accumulation of TSG and EMG in the liver and kidney after multiple oral administrations of PMR. This accumulation was considered to be associated with the toxicity of PMR.

PLANTA MEDICA (2022)

Article Chemistry, Multidisciplinary

Effect of autoinduction and food on the pharmacokinetics of furmonertinib and its active metabolite characterized by a population pharmacokinetic model

Hui-xi Zou, Yu-feng Zhang, Da-fang Zhong, Yong Jiang, Fei Liu, Qian-yu Zhao, Zhong Zuo, Yi-fan Zhang, Xiao-yu Yan

Summary: A population pharmacokinetic model was developed to characterize the nonstationary pharmacokinetics of furmonertinib and its active metabolite AST5902. Model-based simulation showed an increase in furmonertinib clearance during treatment, while the concentration of total active compounds appeared to be stable. Food intake, serum alkaline phosphatase, and body weight were identified as significant covariates affecting pharmacokinetics.

ACTA PHARMACOLOGICA SINICA (2022)

Review Pharmacology & Pharmacy

Overview of Current Herb-Drug Interaction Databases

Yufeng Zhang, Chung Man Ip, Yuen Sze Lai, Zhong Zuo

Summary: This article discusses the significance of HERB-Drug Interaction (HDI) databases and provides an overview of the currently available databases. It suggests using a standardized format and Concept Unique Identifier (CUI) to accelerate structured data collection.

DRUG METABOLISM AND DISPOSITION (2022)

Article Chemistry, Physical

The bending behavior of an l-phenylalanine monohydrate soft crystal via reversible hydrogen bond rupture and remodeling

Yaxiang Gong, Yuanfeng Wei, Yuan Gao, Zunting Pang, Jianjun Zhang, Shuai Qian

Summary: This study reports a novel l-phenylalanine monohydrate (l-Phe·H2O) soft crystal, which has the potential to be developed as a medical microdevice due to its flexibility and biosafety. The study investigates the bending mechanism of the l-Phe·H2O soft crystal by analyzing the variations of hydrogen bonds. In situ micro-Raman and in situ micro-infrared spectra show that the hydrogen bonds rupture and rearrange during the bending process. Energy calculations suggest that the non-directional Coulomb attraction is the major force maintaining the crystal integrity when bent.

PHYSICAL CHEMISTRY CHEMICAL PHYSICS (2022)

Article Chemistry, Multidisciplinary

Orally administered bismuth drug together with N-acetyl cysteine as a broad-spectrum anti-coronavirus cocktail therapy

Runming Wang, Jasper Fuk-Woo Chan, Suyu Wang, Hongyan Li, Jiajia Zhao, Tiffany Ka-Yan Ip, Zhong Zuo, Kwok-Yung Yuen, Shuofeng Yuan, Hongzhe Sun

Summary: The emergence of SARS-CoV-2 variants impacts vaccine efficacy, highlighting the importance of further developing orally administered anti-SARS-CoV-2 therapies. A cocktail therapy combining colloidal bismuth subcitrate or bismuth subsalicylate with N-acetyl-l-cysteine shows potent preclinical anti-SARS-CoV-2 efficacy, offering a potential at-home treatment for combating SARS-CoV-2 and future coronavirus infections.

CHEMICAL SCIENCE (2022)

Review Chemistry, Multidisciplinary

Insights into Cocrystallization and Coamorphization Engineering Techniques in the Delivery of Traditional Chinese Medicine: Formation Mechanism, Solid-State Characterization, and Improved Pharmaceutical Properties

Weili Heng, Xiaoshuang He, Yutong Song, Jiawei Han, Zunting Pang, Shuai Qian, Jianjun Zhang, Yuan Gao, Yuanfeng Wei

Summary: This review highlights the potential of cocrystals and coamorphous systems in improving the pharmaceutical properties of traditional Chinese medicine (TCM). It provides an overview of the definition, preparation methods, characterization techniques, and pharmaceutical properties of these systems. The formation mechanisms and intermolecular interactions are discussed, along with recent research on drug delivery using cocrystallization and coamorphization technologies.

CRYSTAL GROWTH & DESIGN (2022)

Review Pharmacology & Pharmacy

Recent advances on small molecular gels: formation mechanism and their application in pharmaceutical fields

Meiling Su, Jingwen Zhang, Zudi Li, Yuanfeng Wei, Jianjun Zhang, Zunting Pang, Yuan Gao, Shuai Qian, Weili Heng

Summary: Small molecular gels based on non-covalent interactions are attracting research interest for their potential advantages in terms of high structural functionality, lower biological toxicity, and reversible stimulus-response. This review provides an overview of recent advances in small molecular gels, including their gelation mechanism, gel properties, and physicochemical characterizations. It also discusses the effects of drug-based small molecular gels on drug development and their potential applications in the pharmaceutical fields.

EXPERT OPINION ON DRUG DELIVERY (2022)

Article Chemistry, Medicinal

Mechanistic Study on Transformation of Coamorphous Baicalein- Nicotinamide to Its Cocrystal Form

Fei Ding, Wei Cao, Runze Wang, Ningning Wang, Anran Li, Yuanfeng Wei, Shuai Qian, Jianjun Zhang, Yuan Gao, Zunting Pang

Summary: Coamorphization and cocrystal technologies have gained significant attention in the pharmaceutical industry for their ability to improve solubility, dissolution, and bioavailability of poorly water-soluble drugs. This study prepared a single homogeneous coamorphous system of BCS II drug bai-calein (BAI) and nicotinamide (NIC) with a single transition temperature. Interestingly, the coamorphous BAI-NIC transformed into its cocrystal form under the influence of temperature and humidity stress, instead of forming a physical mixture of crystalline BAI and NIC. The transformation rate was temperature-dependent and the crystallinity of the cocrystal increased with increasing temperature. Water vapor sorption tests indicated that the transformation was faster under higher humidity conditions, attributed to the accelerated nucleation process of cocrystal BAI-NIC.

JOURNAL OF PHARMACEUTICAL SCIENCES (2023)

Article Medicine, Research & Experimental

Switch between Cocrystal and Coamorphous Forms Depending on Thermal Modulation of Hot-Melt Extrusion

Peiya Shen, Chunfeng Zhang, Enshi Hu, Yuan Gao, Yuanfeng Wei, Jianjun Zhang, Shuai Qian, Weili Heng

Summary: Cocrystal (CC) and coamorphous (CM) formulations of indomethacin (IMC) and nicotinamide (NIC) were produced using hot-melt extrusion (HME) technique. Different formulations were selectively obtained by adjusting the barrel temperature of HME. The CC and CM formulations showed enhanced dissolution and stability compared to crystalline/amorphous IMC. This study provides an environmentally friendly strategy for the flexible regulation of CC and CM formulations.

MOLECULAR PHARMACEUTICS (2023)

Article Chemistry, Multidisciplinary

Structural Self-Destruction of Deep Eutectic Solvents Induced the Formation of Unusual Diamond-Shaped Crystals of Honokiol and Its Mechanistic Study

Meiling Su, Maoli Huang, Yuanfeng Wei, Yuan Gao, Jianjun Zhang, Shuai Qian, Weili Heng

Summary: A highly unusual diamond-shaped habit of honokiol was obtained from volatile DESs due to the formation of the hole and molecular cluster environments and the preferential adsorption of DESs on the (010) face.

CRYSTAL GROWTH & DESIGN (2023)

Article Pharmacology & Pharmacy

Functional in situ formed deep eutectic solvents improving mechanical properties of powders by enhancing interfacial interactions

Meiling Su, Maoli Huang, Zunting Pang, Yuanfeng Wei, Yuan Gao, Jianjun Zhang, Shuai Qian, Weili Heng

Summary: This study firstly utilized deep eutectic solvent (DES) to improve the powder mechanical properties and tabletability of drugs, and explored the interfacial interaction mechanism. The results showed that DES could form solid-liquid interfaces in the drug powders and enhance the interparticulate interactions, leading to improved tabletability.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2023)

Article Chemistry, Physical

Specific separation of flavonoids isomers by defect modulated metal-organic framework HKUST-1: Experiment and density functional theory analysis

Zezhi Lin, Wei Cao, Jianjun Zhang, Yuanfeng Wei, Shuai Qian, Yuan Gao, Weili Heng

Summary: For the first time, a simple and efficient approach to separate active monomers with larger diameters from structurally similar natural compounds has been proposed. The defective MOF, with hierarchical microporous/mesoporous structures and Cu1+/Cu2+ mixed-valence sites, demonstrated specific loading of silibinin A&B with high separation capacity. This separation technique offers advantages of high specificity, efficiency, and ease of operation.

APPLIED SURFACE SCIENCE (2023)

Review Materials Science, Biomaterials

Metal-organic gels: recent advances in their classification, characterization, and application in the pharmaceutical field

Wei Cao, Zezhi Lin, Daoyi Zheng, Jianjun Zhang, Weili Heng, Yuanfeng Wei, Yuan Gao, Shuai Qian

Summary: Metal-organic gels (MOGs) are functional soft substances with a 3D network structure and solid-like behavior. They have potential advantages of high porosity, flexible structure, and adjustable mechanical properties. In the pharmaceutical field, MOGs are extensively researched for intelligent drug delivery, programmable drug release, tissue repair, drug detection, etc.

JOURNAL OF MATERIALS CHEMISTRY B (2023)

Article Chemistry, Multidisciplinary

Self-gelation involved in the transformation of resveratrol and piperine from a co-amorphous system into a co-crystal system

Jiawei Han, Luyuan Li, Qian Yu, Daoyi Zheng, Yutong Song, Jianjun Zhang, Yuan Gao, Weili Heng, Shuai Qian, Zunting Pang

Summary: The study focused on improving drug solubility and investigating the potential transformation between co-amorphous and co-crystal systems. The co-crystal system showed enhanced dissolution and maintained supersaturation, while the co-amorphous system exhibited reduced dissolution due to gel formation. The stronger intermolecular interactions between the components led to directional rearrangement and transformation from co-amorphous to co-crystal.

CRYSTENGCOMM (2022)

Article Pharmacology & Pharmacy

3D human foreskin model for testing topical formulations of sildenafil citrate

Greta Camilla Magnano, Marika Quadri, Elisabetta Palazzo, Roberta Lotti, Francesca Loschi, Stefano Dall'Acqua, Michela Abrami, Francesca Larese Filon, Alessandra Marconi, Dritan Hasa

Summary: This study aimed to investigate the loading of sildenafil citrate in three commercial transdermal vehicles using 3D full-thickness skin equivalent and compare the results with permeability experiments using porcine skin. The results showed that the results obtained using the 3D skin equivalent were comparable to those obtained using porcine skin, suggesting that the 3D skin model can be a valid alternative for ex-vivo skin absorption experiments.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2024)

Article Pharmacology & Pharmacy

Large volume subcutaneous delivery using multi-orifice jet injection

James W. Mckeage, Andrew Z. H. Tan, Andrew J. Taberner

Summary: Needle-free jet injection is a promising alternative drug delivery technique that offers rapid, non-invasive, and large-volume injections. The study presents a prototype multi-orifice nozzle and a computational fluid dynamic model to demonstrate the feasibility and effectiveness of this technology.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2024)