Purpose: Oil/PEG creams have advantages over creams which consist of water in terms of drug loading in case of hydrophobic drugs, longer duration of action due to no or lesser metamorphosis and stability for water degradable drugs. Conventional techniques involve high shear homogenizers to prepare heterogenous semi-solids which could have batch to batch variations. The purpose of this study was to develop and optimize Oil/PEG creams suitable for hydrophobic and water sensitive drugs by hot melt extrusion technology.
Methods: Oil/PEG creams were prepared using hydrocortisone as active ingredient and by qualitatively and qualitatively varying different grades of PEGs, light mineral oil, Labrafil M1944 CS, Tefose 63 and Tween 80. Shaft with a diameter ratio (Do/Di) of 1.71 was used for the preparation of cream by injecting the drug and surfactant dissolved in oil phase and combination of PEGs with the help of two peristaltic pumps. Different shaft speeds (50 rpm, 100 rpm, 150 rpm and 200 rpm) were also used to optimize the formulation. The creams were characterized for content uniformity, globule size distribution, water activity and in-vitro drug release studies. The final formulation was also characterized for in-vitro permeation testing (IVPT) was performed using 1.64 cm2 Franz diffusion cells (n=4) in addition to aforementioned tests.
Results: The optimized formulation was prepared using PEG 2000, PEG 400, Tefose 63, Labrafil M1944 CS. The content uniformity of the Oil/PEG cream was found to be 96.2 ± 0.4% with globule size distribution of d10-10.10 µm, d50-16.48 µm, d90- 29.45 µm. The solvent activity of the cream was 0.93 ± 0.0. The area under the curve (AUC) and maximum flux (Jmax) of the optimized formulation were 0.47 µg/cm2/h and 1.43 µg/cm2 respectively.
Conclusion: Hot melt extrusion technology can be used as a continuous manufacturing process to prepare stable Oil/PEG creams suitable for hydrophobic and water sensitive drugs.
Shivakumar H. Nanjappa– KLE University, Karnataka
Srinath Rangappa– Post Doctoral Research Associate, University of Mississippi, Mississippi
Vijay Kulkarni– STEERLife India Pvt. Ltd., Karnataka
Narasimha Murthy– Professor-Pharmaceutics and Drug Delivery, University of Mississippi, University, Mississippi