High-throughput formulation screening system for self-microemulsifying drug delivery.
OBJECTIVE
To develop a high-throughput formulation screening (HTFS) system for self-microemulsifying drug delivery system (SMEDDS) formulations.


METHODS
Formulations were prepared by dispensing surfactants and a model compound (Nilvadipine) dissolved in ethanol and oil with a robotic liquid dispenser. Screenings of emulsion particle size and phase stability were conducted for selecting SMEDDS formulations by a turbidity assay.


RESULTS
Formulations were prepared at 40 minute/96-formulation. Both the screenings were conducted at 1 minute/96-formulation. SMEDDS formulations and the most suitable hydrophilic surfactant (HS)/lipophilic surfactant (LS) combination, which formed the largest SMEDDS area on its corresponding phase diagram, were selected by SMEDDS-HTFS system with minimal manpower (one person) and compound consumption (0.2 mg/formulation).


CONCLUSIONS
SMEDDS-HTFS system enabled rapid and efficient selections of SMEDDS formulations and the most suitable HS/LS combination for SMEDDS.
Sakai
Kenichi
K
Formulation Technology Research Department, Chugai Pharmaceutical Co., Ltd., Kita-Ku, Tokyo, Japan. sakaikni@chugai-pharm.co.jp
Maeda
Hiroyuki
H
Yoshimori
Takayuki
T
Obata
Kouki
K
Ogawa
Yutaka
Y
D016503:Drug Delivery Systems; D004355:Drug Stability; D004655:Emulsions; D000431:Ethanol / Q000737:chemistry; D057166:High-Throughput Screening Assays / Q000379:methods*; D009391:Nephelometry and Turbidimetry; D009543:Nifedipine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D012371:Robotics; D013501:Surface-Active Agents / Q000737:chemistry*; D013997:Time Factors
D004655:Emulsions; D009821:Oils; D013501:Surface-Active Agents; C035100:nilvadipine; D000431:Ethanol; D009543:Nifedipine