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
Abstract:
A novel approach to designing sustained-release preparations of tacrolimus using mesoporous silica as a carrier material is presented in this study. Previous studies focused on solid dispersion techniques, but the use of mesoporous silica for this purpose had not been explored. The aim of this research was to develop an environmentally friendly and straightforward method for loading tacrolimus onto mesoporous silica to create a sustained-release preparation. The process involved dissolving tacrolimus in a molten mixture of Compritol 888 ATO and Gelucire 50/13, forming a drug-loaded lipid-based drug delivery system (LBDDS). The liquid LBDDS was then adsorbed onto mesoporous silica, transforming it into a solid powder known as the tacrolimus sustained release silica-lipid hybrid (SLH). Characterization of the SLH was performed using SEM, CLSM, XRPD, and DSC, while in vitro drug release was evaluated using a paddle method. SEM and CLSM observations demonstrated efficient distribution of the LBDDS within the silica pores. DSC and XRPD results indicated that the lipid existed in an amorphous state inside the silica. The drug-loaded SLH exhibited favorable flowability, compressibility, and compactibility, and displayed a two-phase in vitro drug release process over 24 hours, which remained stable even after storage at 40 °C for 10 days. This study introduces a novel and straightforward method for preparing tacrolimus sustained release powder, offering a viable solution for solidifying liquid LBDDS with extended drug release behavior, improved stability, and desirable micromeritic properties.
Keywords
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
Conclusion
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.
