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AAPS PharmSciTech

, 20:102 | Cite as

Effects of Polymer/Surfactant as Carriers on the Solubility and Dissolution of Fenofibrate Solid Dispersion

  • Baixue Yang
  • Lulu Wu
  • Jia Ke
  • Liuchenzi Zhou
  • Meixu Chen
  • Sanming LiEmail author
  • Xuesong FengEmail author
Research Article
  • 13 Downloads

Abstract

The purpose of this work is to investigate the effects of polymer/surfactant as carriers on the solubility and dissolution of fenofibrate solid dispersions (FF SDs) with the aid of systematic research on the physicochemical properties of the polymer/surfactant system and further highlight the importance of studying polymer/surfactant interaction in the preformulation. The critical micelle concentration (CMC) of sodium lauryl sulfate (SLS) and critical aggregation concentration (CAC) of polymer/SLS solutions were obtained through conductivity measurement. Meanwhile, surface tension, viscosity, morphology, and wettability of polymer/SLS with different weight ratios of SLS were analyzed to screen out the suitable content of SLS (weight%, 5% in carriers) incorporated in SDs. Polymer/SLS coprecipitate and FF SDs were prepared by the solvent evaporation method. The results from differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis showed that FF was molecularly dispersed in SDs. Compared to the solubility of FF in povidone/SLS (PVP/SLS) solutions, the increment of FF solubility in copovidone/SLS (VA64/SLS) solutions was due to the formation of free SLS micelles, which have been confirmed by transmission electron microscopy (TEM). Particularly, the wettability of FF SDs and physical mixtures (PMs) was also determined by the sessile drop technique. A linear relationship between the wettability of carriers and that of FF SDs was found, which revealed the significant role of carriers on the surface composition of FF SDs. As the molecular weight of PVP increased, the wettability of carriers decreased, thus leading to the reduction of the dissolution rate of SDs. Although the presence of SLS did not enhance the dissolution of FF SDs, it increased the amount of drug released at the initial stage. All these results indicated that the polymer/SLS interaction would affect the performance of SDs; hence, it was necessary to study their properties in the preformulation.

KEY WORDS

polymer/surfactant interaction solubility dissolution solid dispersion 

Notes

Acknowledgments

This work was financially supported by the National Natural Science Foundation of China (No.81473161) and National Science and Technology Major Project (No. 2017ZX09101001-006-012).

Compliance with Ethical Standards

Conflict of Interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  1. 1.Faculty of PharmacyShenyang Pharmaceutical UniversityBenxiChina
  2. 2.School of PharmacyChina Medical UniversityShenyangChina

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