Journal Title
Title of Journal: Drug Deliv and Transl Res
|
Abbravation: Drug Delivery and Translational Research
|
|
|
|
|
|
|
|
Authors: Anna C Pham TriHung Nguyen Cameron J Nowell Bim Graham Ben J Boyd
Publish Date: 2015/09/02
Volume: 5, Issue: 6, Pages: 566-574
Abstract
Lipidbased liquid crystalline LC systems have the potential to sustain the oral absorption of poorly watersoluble drugs in vivo facilitating slow drug release from their complex internal structure To further evaluate the dynamic relationship between gastric retention and sustained drug absorption for these systems this study aimed to explore noninvasive Xray microCT imaging as an approach to assess gastric retention Pharmacokinetic studies were also conducted with cinnarizineloaded LC formulations to correlate gastric retention of the formulation to drug absorption The in vivo studies demonstrated the interplay between gastric retention and drug absorption based on the digestibility of the LC structures An increase in nondigestible phytantriol PHY composition in the formulation relative to digestible glyceryl monooleate GMO increased the gastric retention with 68 ± 4 of formulation intensity remaining at 8 h for 85 w/w PHY and 26 ± 9 for 60 w/w PHY Interestingly it was found that PHY 30 w/w in GMO provided the highest bioavailability for cinnarizine CZ amongst the other combinations including GMO alone The studies demonstrated that combining digestible and nondigestible lipids into LC systems allowed for an optimal balance between sustaining drug absorption whilst increasing plasma concentration C max over time leading to enhanced oral bioavailability The results demonstrate the potential for utilising noninvasive Xray microCT imaging to dynamically assess the GI transit of orally administered liquid crystalforming formulationsFunding is acknowledged from the Australian Research Council under the Discovery Projects scheme DP120104032 BJB is a recipient of an Australian Research Council Future Fellowship FT120100697 We acknowledge Tanmay Joshi and Olga Gazukin for transmission electron microscopy TEM images Bim Graham and Raymond Lam for GNP synthesis Joanne Du and Linda Hong for SAXS analysis and Orlagh Feeney for assistance with UPLC We also acknowledge the MBI Facility for provision of instrumentation training and general support SAXS measurements were performed on the SAXS/WAXS beamline at the Australian Synchrotron facility
Keywords:
.
|
Other Papers In This Journal:
|