Enhanced oral bioavailability of Coenzyme Q10 by self-emulsifying drug delivery systems.
To enhance the solubility and bioavailability of poorly water-soluble Coenzyme Q(10) (CoQ(10)), self-emulsifying drug delivery system (SEDDS) composed of oil, surfactant and cosurfactant for oral administration of CoQ(10) was formulated. The solubility of CoQ(10) was determined in various oils and surfactants. The formulations were prepared using two oils (Labrafil M 1944 and Labrafil M 2125), surfactant (Labrasol) and cosurfactant (Lauroglycol FCC and Capryol 90). In all the formulations, the level of CoQ(10) was fixed at 6% (w/v) of the vehicle. These formulations were characterized by solubility of the drug in the vehicle, particle size of the dispersed emulsion, zeta potential and drug release profile. Ternary phase diagrams were used to evaluate the emulsification domain. The self-emulsification time following introduction into an aqueous medium under gentle agitation was evaluated. The optimized SEDDS formulation consist of 65% (v/v) Labrasol, 25% (v/v) Labrafil M 1944 CS and 10% (v/v) Capryol 90 of each excipient showed minimum mean droplet size (about 240 nm) and optimal drug release profile in water. The pharmacokinetic study in rats for the optimized formulation was performed and compared to powder formulation. SEDDS have significantly increased the C(max) and area under the curve (AUC) of CoQ(10) compared to powder (P<0.05). Thus, this self-micro emulsifying drug delivery system should be an effective oral dosage form for improving oral bioavailability of lipophilic drug, CoQ(10).
Balakrishnan
Prabagar
P
College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan, South Korea.
Lee
Beom-Jin
BJ
Oh
Dong Hoon
DH
Kim
Jong Oh
JO
Lee
Young-Im
YI
Kim
Dae-Duk
DD
Jee
Jun-Pil
JP
Lee
Yong-Bok
YB
Woo
Jong Soo
JS
Yong
Chul Soon
CS
Choi
Han-Gon
HG
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D016503:Drug Delivery Systems; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry; D008297:Male; D009821:Oils / Q000737:chemistry*; D009930:Organic Chemicals / Q000737:chemistry; D010316:Particle Size; D044367:Phase Transition; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D014451:Ubiquinone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D014815:Vitamins / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
D004655:Emulsions; D005989:Glycerides; C514708:Labrafil M 1944 CS; D009821:Oils; D009930:Organic Chemicals; D013501:Surface-Active Agents; D014815:Vitamins; C440220:Labrasol; D014451:Ubiquinone; D011092:Polyethylene Glycols; C024989:coenzyme Q10