Preparation and Quality Evaluation of Everolimus Self-Microemulsifying Drug Delivery System
10.3870/j.issn.1004-0781.2017.05.019
- VernacularTitle:依维莫司自微乳化释药系统的制备及质量评价
- Author:
Hou CHEN
- Keywords:
Everolimus;
Self-microemulsifying drug delivery systems;
Pseudo-ternary phase diagram;
Dissolution
- From:
Herald of Medicine
2017;36(5):544-548
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare everolimus self-microemulsifying drug delivery systems (Everolimus-SMEDDS) and evaluate its physicochemical properties.Methods Everolimus-SMEDDS were developed by using rational blends of components with good solubilizing ability for everolimus which were selected based on solubility investigation.Then, pseudo-ternary phase diagram was constructed to determine the self-emulsifying region.The appearance, morphology, particle size distribution, Zeta potential and in vitro drug release behavior of Everolimus-SMEDDS were investigated after being diluted by water.Results An optimal Everolimus-SMEDDS consisting of ethylis oleas, Solutol HS 15 and propylene glycol were identified, and the optimum proportion was 8∶1∶1.Upon mixing with water, Everolimus-SMEDDS formed a clear and transparent microemulsion solution with homogeneous small spherical as seen in transmission electron microscopy.Particle size and Zeta potential of Everolimus-SMEDDS were found to be (48.7±25.1) nm and (-14.2±2.5) mV, respectively.The in vitro release profile indicated that the accumulated release of everolimus in SMEDDS reached up to nearly 100% within 30 min.Conclusion The in vitro dissolution of everolimus was remarkably improved by SMEDDS.It can provide reference for the new dosage form of everolimus.
