In vitro and in vivo evaluation of self-microemulsifying drug delivery system of buparvaquone.
OBJECTIVE
The aim of this study was to prepare a lipid-based self-microemulsifying drug delivery system (SMEDDS) to increase the solubility and oral bioavailability of a poorly water-soluble compound, buparvaquone (BPQ).


METHODS
The solubility of BPQ was determined in various vehicles, and pseudo-ternary phase diagrams were constructed to determine the microemulsion region. A series of formulations with different compositions were selected in the microemulsion region for assessment of self-emulsification time and droplet size. The optimized SMEDDS formulation was used for in vitro dissolution and pharmacokinetic studies in rabbits.


RESULTS
The optimum formulation of SMEDDS consisted of Capryol 90 (9.82%), Cremophor EL (70.72%), Labrasol (17.68%), and BPQ (1.78%). Emulsification time and the mean droplet size were found to be 1 minute and 18.0 +/- 0.25 nm, respectively, for the optimum formulation. The cumulative percentage of drug released in 90 minutes was 100% in both SGF and SIF. The calculated absolute oral bioavailability for BPQ was found to be 40.10%.


CONCLUSIONS
The optimum SMEDDS formulation was increased the rate and extent of absorption of BPQ. The formulation is suitable for oral administration of BPQ. It would be useful to conduct efficacy studies of BPQ in diseased animal models and subsequently for toxicokinetics studies.
Venkatesh
Gantala
G
Centre for Drug Research, Universiti Sains Malaysia, Penang, Malaysia. venku16@yahoo.com
Majid
M I A
MI
Mansor
S M
SM
Nair
N K
NK
Croft
Simon L
SL
Navaratnam
V
V
D000818:Animals; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry*; D008297:Male; D009285:Naphthoquinones / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry*; D011817:Rabbits
D045703:Emulsifying Agents; D009285:Naphthoquinones; C046326:buparvaquone