检索结果-南通市图书馆

Nanoparticles with high payloads of pipemidic acid, a poorly soluble crystalline drug: drug-initiated polymerization and self-assembly approach

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2018年第3期8卷 420-431页

作者： Elisabetta Pancani Mario Menendez-Miranda Alexandra Pastor Francois Brisset Marie-Francoise Bernet-Camard Didier Desmaele ruxandra gref Institut de Sciences Moléculaires d'Orsay(ISMO) Univ.of Paris-SudUniversitéParis-Saclay Institut Galien UMR8612 Univ.of Paris-SudUniversitéParis-Saclay Institut de Chimie Moléculaire et des Matériaux d'Orsay(ICMMO) Univ.of Paris-SudUniversitéParis-Saclay EA4043" UnitéBactéries Pathogènes et Santé"(UBaPS) Univ.of Paris-SudUniversitéParis-Saclay

Nowadays, biodegradable polymers such as poly(lactic acid)(PLA), poly(D,L-lactic-coglycolic acid)(PLGA) and poly(ε-caprolactone)(PCL) remain the most common biomaterials to produce drug-loaded nanoparticles(NPs). Pipemidic acid(PIP) is a poorly soluble antibiotic with a strong tendency to crystallize. PIP incorporation in PLA/PLGA NPs was challenging because of PIP crystals formation and burst release. As PIP had a poor affinity for the NPs, an alternative approach to encapsulation was used, consisting in coupling PIP to PCL. Thus, a PCL–PIP conjugate was successfully synthesized by an original drug-initiated polymerization in a single step without the need of ***–PIP was characterized by NMR, IR, SEC and mass spectrometry. PCL–PIP was used to prepare selfassembled NPs with PIP contents as high as 27%(w/w). The NPs were characterized by microscopy,DLS, NTA and TRPS. This study paves the way towards the production of NPs with high antibiotic payloads by drug-initiated polymerization. Further studies will deal with the synthesis of novel polymer–PIP conjugates with ester bonds between the drug and PCL. PIP can be considered as a model drug and the strategy developed here could be extended to other challenging antibiotics or anticancer drugs and employed to efficiently incorporate them in NPs.

关键词： Pipemidic acid Nanoparticle Antibiotic Nanoprecipitation Crystalline drug Drug-initiated polymerization

Glycoside scutellarin enhanced CD-MOF anchoring for laryngeal delivery

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2020年第9期10卷 1709-1718页

作者： Kena Zhao Tao Guo Caifen Wang Yong Zhou Ting Xiong Li Wub Xue Li Priyanka Mittal Senlin Shi ruxandra gref Jiwen Zhang College of Pharmaceutical Sciences Zhejiang Chinese Medical UniversityHangzhou 311402China Center for Drug Delivery System Shanghai Institute of Materia MedicaState Key Laboratory of Drug ResearchChinese Academy of SciencesShanghai 201203China NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients National Institutes for Food and Drug ControlBeijing 100050China Key Laboratory of Modern Chinese Medicine Preparations Ministry of EducationJiangxi University of Traditional Chinese MedicineNanchang 330004China Universite´Paris-Saclay CNRS 8214Institut des Sciences Mole´culaires d’OrsayOrsay 91405France University of Chinese Academy of Sciences Beijing 100049China

It is essential to develop new carriers for laryngeal drug delivery in light of the lack of therapy in laryngeal related *** the inhalable micron-sized crystals ofγ-cyclodextrin metal-organic framework(CD-MOF)was utilized as dry powder inhalers(DPIs)carrier with high fine particle fraction(FPF),it was found in this research that the encapsulation of a glycoside compound,namely,scutellarin(SCU)in CD-MOF could significantly enhance its laryngeal ***,SCU loading into CD-MOF was optimized by ***,a series of characterizations were carried out to elucidate the mechanisms of drug ***,the laryngeal deposition rate of CD-MOF was 57.72±2.19%improved by SCU,about two times higher than that of CD-MOF,when it was determined by Next Generation Impactor(NGI)at 65 L/*** a proof of concept,pharyngolaryngitis therapeutic agent dexamethasone(DEX)had improved laryngeal deposition after being co-encapsulated with SCU in *** molecular simulation demonstrated the configuration of SCU in CD-MOF and its contribution to the free energy of the SCU@CD-MOF,which defined the enhanced laryngeal *** conclusion,the glycosides-like SCU could effectively enhance the anchoring of CD-MOF particles to the larynx to facilitate the treatment of laryngeal diseases.

关键词： Laryngeal delivery g-Cyclodextrin metalorganic framework Scutellarin Dexamethasone Molecular simulation

Metal-organic frameworks for advanced drug delivery

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2021年第8期11卷 2362-2395页

作者： Siyu He Li Wu Xue Li Hongyu Sun Ting Xiong Jie Liu Chengxi Huang Huipeng Xu Huimin Sun Weidong Chen ruxandra gref Jiwen Zhang Center for Drug Delivery Systems Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences Beijing 100049China Institut de Sciences Moléculaires D'Orsay UniversitéParis-SaclayOrsay Cedex 91400France Key Laboratory of Modern Chinese Medicine Preparations Ministry of EducationJiangxi University of Traditional Chinese MedicineNanchang 330004China School of Pharmaceutical Sciences Anhui University of Chinese MedicineHefei 230012China NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients National Institutes for Food and Drug ControlBeijing 100050China

Metal-organic frameworks(MOFs),comprised of organic ligands and metal ions/metal clusters via coordinative bonds are highly porous,crystalline *** tunable porosity,chemical composition,size and shape,and easy surface functionalization make this large family more and more popular for drug *** is a growing interest over the last decades in the design of engineered MOFs with controlled sizes for a variety of biomedical *** article presents an overall review and perspectives of MOFs-based drug delivery systems(DDSs),starting with the MOFs classification adapted for DDSs based on the types of constituting metals and ***,the synthesis and characterization of MOFs for DDSs are developed,followed by the drug loading strategies,applications,biopharmaceutics and quality ***,a variety of representative applications of MOFs are detailed from a point of view of applications in pharmaceutics,diseases therapy and advanced *** particular,the biopharmaceutics and quality control of MOFs-based DDSs are summarized with critical issues to be ***,challenges in MOFs development for DDSs are discussed,such as biostability,biosafety,biopharmaceutics and nomenclature.

关键词： Metal-organic frameworks Drug loading Drug delivery systems Synthesis and characterization Diseases therapy Pharmaceutics Biopharmaceutics Biosafety

Drug nanoclusters formed in confined nano-cages of CD-MOF: dramatic enhancement of solubility and bioavailability of azilsartan

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2019年第1期9卷 97-106页

作者： Yuanzhi He Wei Zhang Tao Guo Guoqing Zhang Wei Qin Liu Zhang Caifen Wang Weifeng Zhu Ming Yang Xiaoxiao Hu Vikramjeet Singh Li Wu ruxandra gref Jiwen Zhang Key Laboratory of Modern Preparation of TCM Ministry of Education Jiangxi University of Traditional Chinese Medicine Center for Drug Delivery Systems Shanghai Institute of Materia Medica Chinese Academy of Sciences School of Chemistry and Environmental Engineering Shanghai Institute of Technology Institut des Sciences Moléculaires d'Orsay UMR 8214 CNRS Université Paris-Sud Université Paris-Saclay School of Pharmacy Key Laboratory of Molecular Pharmacology and Drug Evaluation Ministry of Education Yantai University

Tremendous efforts have been devoted to the enhancement of drug solubility using nanotechnologies, but few of them are capable to produce drug particles with sizes less than a few nanometers. This challenge has been addressed here by using biocompatible versatile γ-cyclodextrin(γ-CD) metal-organic framework(CD-MOF) large molecular cages in which azilsartan(AZL) was successfully confined producing clusters in the nanometer range. This strategy allowed to improve the bioavailability of AZL in Sprague–Dawley rats by 9.7-fold after loading into CD-MOF. The apparent solubility of AZL/CD-MOF was enhanced by 340-fold when compared to the pure drug. Based on molecular modeling, a dual molecular mechanism of nanoclusterization and complexation of AZL inside the CD-MOF cages was proposed, which was confirmed by small angle X-ray scattering(SAXS) and synchrotron radiation-Fourier transform infrared spectroscopy(SR-FTIR) techniques. In a typical cage-like unit of CD-MOF, three molecules of AZL were included by the γ-CD pairs, whilst other three AZL molecules formed a nanocluster inside the 1.7 nm sized cavity surrounded by six γ-CDs. This research demonstrates a dual molecular mechanism of complexation and nanoclusterization in CD-MOF leading to significant improvement in the bioavailability of insoluble drugs.

关键词： γ-Cyclodextrin metal-organic framework Nanoclusterization Azilsartan Mechanism Solubility Bioavailability Molecular modeling