The enhancement of the aqueous solubility of Albendazole employing polymeric amorphous solid dispersion (ASD) as an approach

PURPOSE

Poor aqueous solubility is a significant issue in the current pharmaceutical industry with approximately 90% of new chemical entities in the development pipeline characterised as poorly watersoluble.
Amongst various means to address the solubility issue, the amorphous solid dispersion (ASD) approach is highly attractive but associated with high risks, due to the inherent instability of the amorphous drug forms. ASDs often contain the drugs in a high energy form but offer increased stability due to significant interaction with the polymeric carrier in which they are embedded.
Hot melt extrusion has been extensively researched to show significant promise in continuous manufacturing of ASDs.
In this study, we examine a model BCS class II drug Albendazole (ABZ), which has been initially utilized as an anti-parasite drug to act in the intestinal lumen, but recently shown anti-cancer effects.

OBJECTIVES

Adopting a range of pre-screening tools as a means of identifying polymers suitable for the formulation of ASDs
to manufacture those polymeric ASDs using HME
to examine the potential of this process to produce suitable drug formulation to enable the performance of ABZ

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CONCLUSIONS

In this study, we have manufactured amorphous solid dispersions of ABZ and shown that the drug release performance can be improved.
A range of pre-screening tools was investigated, and it was shown that a combination of methods can be employed to help identify appropriate polymer systems and drug loadings and this a formulation design space for effective manufacture of drug enabled formulations.

Authors: J. Yang, V. Mohylyuk, S. Li, D. S. Jones, G. P. Andrews.
Excipients: Kollidon VA64, PEG 6000, Soluplus