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Loading Of Tacrolimus Containing Lipid Based Drug Delivery Systems Into Mesoporous Silica For Extended Release

Authors: Li Liu, Jia Li, Mei-hui Zhao, Hui Xu, Lin-sen Li, Shao-ning Wang


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 d. The 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.


Tacrolimus; Lipid-based drug delivery system; Mesoporous silica; Silica-lipid hybrid; Sustained-release

Citation: Li Liu, Jia Li, Mei-hui Zhao, Hui Xu, Lin-sen Li, Shao-ning Wang Loading of tacrolimus containing lipid based drug delivery systems into mesoporous silica for extended release doi:10.1016/j.ajps.2016.07.005

Received: 15 April 2016, Revised: 22 June 2016, Accepted: 20 July 2016, Available online: 4 August 2016

Copyright: © 2016 Elsevier B.V. or its licensors or contributors. Open Access funded by Shenyang Pharmaceutical University


In this study, we provided a novel method to prepare a sustained release powder containing tacrolimus by employing mesoporous silica as the carrier to adsorb drug-loaded LBDDS. Using this method, the low melting-point, wax-like LBDDS could be transformed to a rigid solid powder with good flowability, compressibility and compactibility. By the combination of lipids and mesoporous silica, we successfully obtained a kind of sustained-release powder, and the stability of LBDDS under challenge condition could also be obviously improved. Such organic solvent-free technique supplied a novel, simple, low cost, ecologically friendly and easy to obtain at industrial scale method to prepare tacrolimus solid sustained-release powder, the powder we obtained had a better stability and micromeritic properties, which could be made into dry suspension, granules, capsules, and tablets according to the clinical requirements.

Declaration of interest

The authors report no declarations of interest.

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