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Loading of tacrolimus containing lipid based drug delivery systems into mesoporous silica for extended release

Asian Journal of Pharmaceutical Sciences 2016年第6期11卷 751-759页

作者： Li Liu Jia Li Mei-hui Zhao Hui Xu Lin-sen Li Shao-ning Wang School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China Department of Biochemistry Shenyang Medical CollegeShenyang 110034China School of Pharmaceutical Engineering Shenyang Pharmaceutical UniversityShenyang 110016China

Many studies had been focused on designing tacrolimus sustained release preparations based on solid dispersion technique, but no one had tried to employ mesoporous silica as the carrier material to realize this goal. The purpose of this study was to develop a novel, simple and environmental friendly drug loading method with mesoporous silica to obtain tacrolimus sustained-release preparation. Tacrolimus was firstly dissolved in the molten mixed lipid composed of Compritol 888 ATO and Gelucire 50/13 to prepare a drug loaded lipid-based drug delivery systems(LBDDS), then the liquid LBDDS was adsorbed by mesoporous silica to transfer the liquid into solid powder, ie. the tacrolimus sustained release silica-lipid hybrid(SLH). The SLH was characterized by SEM, CLSM, XRPD and DSC, and the in vitro drug release was tested using a paddle method. SEM and CLSM observation showed that the LBDDS was efficiently distributed throughout the pores of the silica. The results of DSC and XRPD illustrated that the lipid existed inside the silica at amorphous state. The drug-loaded SLH showed good flowability, compressibility, compactibilty and two-phase in vitro drug release process within 24 hours, which did not change obviously even after storage at 40 °C for 10 *** present study provided a novel and simple method to prepare tacrolimus sustained release powder, which provided a feasible solution to solidify the liquid LBDDS of not only extended drug release behavior, but also improved stability and micromeritic properties.

关键词： Tacrolimus lipid-based drug delivery system Mesoporous silica Silica-lipid hybrid Sustained-release

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Flavonoids Loaded in Nanocarriers: An Opportunity to Increase Oral Bioavailability and Bioefficacy

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Food and Nutrition Sciences 2014年第13期5卷 1212-1327页

作者： Anna Rita Bilia Benedetta Isacchi Chiara Righeschi Clizia Guccione Maria Camilla Bergonzi Department of Chemistry University of Florence Florence Italy

Flavonoids are among the biggest group of polyphenols, widely distributed in plant-based foods. A plethora of evidence supports the health benefits and value of flavonoids can play in the physiological function treatment and in the prevention of disease particularly in the prevention of degenerative conditions including cancers, cardiovascular and neurodegenerative diseases. Hence, flavonoids represent the active constituents of many dietary supplements and herbal remedies, as well as there is an increasing interest in this class of polyphenols as functional ingredients of beverages, food grains and dairy products. Conversely, various studies have also shown that flavonoids have some drawbacks after oral administration such as stability, bioavailability and bioefficacy. This article reviews the current status of novel nanodelivery systems including nanospheres, nanocaspsules, micro- and nanoemulsions, micelles, solid lipid nanoparticles and nanostructured lipid capsules, successfully developed for overcoming the delivery challenges of flavonoids.

关键词： Flavonoids Nanodelivery Systems lipid-based Nanocarriers Polymer-based Nanocarriers Improved Stability Bioavailability and Bioefficacy

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