Advertisement

 

 

Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation().

Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation().
Author Information (click to view)

Zainuddin R, Zaheer Z, Sangshetti JN, Momin M,


Zainuddin R, Zaheer Z, Sangshetti JN, Momin M, (click to view)

Zainuddin R, Zaheer Z, Sangshetti JN, Momin M,

Advertisement
Share on FacebookTweet about this on TwitterShare on LinkedIn

Drug development and industrial pharmacy 2017 09 13() 1-9 doi 10.1080/03639045.2017.1371732

Abstract
OBJECTIVE
To synthesize β cyclodextrin nanosponges using a novel and efficient microwave mediated method for enhancing bioavailability of Rilpivirine HCl (RLP).

SIGNIFICANCE
Belonging to BCS class II RLP has pH dependent solubility and poor oral bioavailability. However, a fatty meal enhances its absorption hence the therapy indicates that the dosage form be consumed with a meal. But then it becomes tedious and inconvenient to continue the therapy for years with having to face the associated gastric side effects such as nausea.

METHOD
Microwave synthesizer was used to mediate the poly-condensation reaction between β-cyclodextrin and cross-linker diphenylcarbonate. Critical parameters selected were polymer to cross-linker ratio, Watt power, reaction time and solvent volume. Characterization studies were performed using FTIR, DSC, SEM, (1)H-NMR and PXRD. Molecular modeling was applied to confirm the possibility of drug entrapment. In vitro drug dissolution followed by oral bioavailability studies was performed in Sprawley rats. Samples were analyzed using HPLC.

RESULTS
Microwave synthesis yields para-crystalline, porous nanosponges (∼205 nm). Drug entrapment led to enhancement of solubility and a two-fold increase in drug dissolution (P < 0.001) following Higuchi release model. Enhanced oral bioavailability was observed in fasted Sprawley rats where Cmax and AUC0-∞ increases significantly (Cmax of NS∼ 586 ± 5.91 ng/mL; plain RLP ∼310 ± 5. 74 ng/mL). CONCLUSION
The approach offers a comfortable dosing zone for AIDs patients, negating the requirement of consuming the formulation in a fed state due to enhancement in drugs’ oral bioavailability.

Submit a Comment

Your email address will not be published.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

nine − three =

[ HIDE/SHOW ]