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| 1 | Drug nanoclusters formed in confined nano-cages of CD-MOF: dramatic enhancement of solubility and bioavailability of azilsartan显示文摘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. | 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 | 2019 | Acta Pharmaceutica Sinica B2019，9，1： | 13 |
| 2 | Poly(β-cyclodextrin)-mediated Polylactide-cholesterol Stereocomplex Micelles for Controlled Drug Delivery显示文摘A series of host-guest interaction-adjusted polylactide stereocomplex micelles was prepared via the self-assembly of 4-armed poly(ethylene glycol)-block-poly(L-lactide/D-lactide)-cholesterol(4-armed PEG-b-PLLA/PDLA-CHOL) and poly(β-cyclodextrin)(PCD) with the molar ratios of CHOL/β-CD at 1:0.5, 1:1, and 1:2 in an aqueous environment. The hydrodynamic diameters of the micelles ranged from 84.1 nm to 107 nm depending on the molar ratio of CHOL/β-CD. It was shown that the micelle with the largest proportion of PCD possessed excellent abilities in drug release, cell internalization as well as proliferation inhibitory effect toward human A549 lung cancer cells. The results demonstrated that the stereocomplex and host-guest interactions-mediated PLA micelles exhibited great potential in sustained drug delivery. | Xiang-ru Feng 丁建勋 Ruxandra Gref Xue-si Chen | 2017 | Chinese Journal of Polymer Science2017，35，6： | 6 |
| 3 | Study of emulsion stabilization by graft copolymers using the optical analyzer Turbiscan显示文摘 | Caroline Lemarchand Patrick Couvreur Christine Vauthier Dominique Costantini Ruxandra Gref | 2002 | International Journal of Pharmaceutics2002，，1： | 1 |
| 4 | Biodegradable long-circulating polymeric nanospHeres显示文摘 | Ruxandra Gref Yoshiharu Minam it ake Maria Teress Peracchia | 1994 | Science1994，263，： | 1 |
| 5 | 显示文摘 | Ruxandra Gref Jaqueline Rodrigues Patrick Couvreur | 2002 | Macromolecule2002，35，： | 1 |
| 6 | Biodegradable long-circulating polymeric nanospHeres显示文摘 | Ruxandra Gref Yoshiharu Minamitake Maria Teress Peracchia | 1994 | Science1994，263，： | 1 |
| 7 | Biodegradable long-circulating polymeric nanospheres显示文摘 | Ruxandra Gref Yoshiharu Minamitake Maria Teresa Peracchia | 1994 | Science1994，263，5153： | 1 |
| 8 | Nanoparticles with high payloads of pipemidic acid, a poorly soluble crystalline drug: drug-initiated polymerization and self-assembly approach显示文摘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 catalyst.PCL–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. | Elisabetta Pancani Mario Menendez-Miranda Alexandra Pastor Francois Brisset Marie-Francoise Bernet-Camard Didier Desmaele Ruxandra Gref | 2018 | Acta Pharmaceutica Sinica B2018，8，3： | 0 |
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