Advertisement

 

 

Nevirapine-polycaprolactone crystalline inclusion complex as a potential long-acting injectable solid form.

Nevirapine-polycaprolactone crystalline inclusion complex as a potential long-acting injectable solid form.
Author Information (click to view)

Yang X, Yu B, Zhong Z, Guo BH, Huang Y,


Yang X, Yu B, Zhong Z, Guo BH, Huang Y, (click to view)

Yang X, Yu B, Zhong Z, Guo BH, Huang Y,

Advertisement

International journal of pharmaceutics 2018 03 26543(1-2) 121-129 pii 10.1016/j.ijpharm.2018.03.043

Abstract

Nevirapine (NVP) is recommended by WHO as the antiretroviral treatment to prevent HIV passing from mother to child. However, the once-daily oral administration results in poor patient compliance, and a long-acting injectable form of NVP is desirable. Using single-crystal X-ray diffraction and other characterization methods, we demonstrated NVP can form crystalline inclusion complex (IC) with the biodegradable hydrophobic poly(ε-caprolactone) (PCL), and investigated the potential of the NVP-PCL IC microparticles as a long-acting injectable solid form. Compared with pure NVP crystals and NVP/polylactide microparticles, the NVP-PCL IC crystals showed significantly decreased solubility and slower dissolution rate, making it more suitable to be developed to achieve sustained-release profiles. In addition, the NVP-PCL IC microparticles with an average diameter below 10 μm can be conveniently prepared by spray drying and are found to be easily injectable through a 25G needle. These results demonstrated the possibility of using drug-polymer IC microparticles as long-acting injectable forms, providing a new approach to design sustained-release drug products.

Submit a Comment

Your email address will not be published. Required fields are marked *

20 − 12 =

[ HIDE/SHOW ]