Incorporation of Lamotrigine Drug in the PEO–PPO–PEO Triblock Copolymer (Pluronic F127) Micelles: Effect of Hydrophilic Polymers

Abstract

AbstractThe hydrophobic drug Lamotrigine (LTG) shows low bioavailability after oral administration. Work has been performed to improve the aqueous solubility of LTG using the micelles of amphiphilic block copolymers. Polyethylene oxide‐ polypropylene oxide‐ polyethylene oxide triblock copolymers (PEO–PPO–PEO), known as Pluronic®, have been the subject of current interest due to the versatile structural possibilities of varying PEO/PPO ratios. Incorporation of LTG in the aqueous micellar solutions of Pluronic® F127 was investigated using UV–visible spectroscopy. The shapes and size of the micelles with and without LTG have been ascertained using dynamic light scattering and small angle neutron scattering experiments. Results show increase in the Pluronic® micellar size with hard sphere radius with the incorporation of LTG. The effect of hydrophilic polymers (PEG1500 and F68) on the LTG‐incorporated Pluronic® F127 micelles was also studied and found inefficient for enhancement of the solubility of LTG. Solid forms of LTG‐incorporated Pluronic® F127 micelles with and without hydrophilic polymers, coded as LPMs, were successfully prepared through the thin‐film hydration method. Fourier transform infrared spectroscopy, X‐ray diffraction spectroscopy and thermogravimetric analysis have been used to ensure the compatibility of the LTG with Pluronic® F127 micelles in prepared LPMs. All the LPMs showed good incorporation efficiency, loading capacity and the sustained release profile of LTG. Results showed no specific improvement with the addition of hydrophilic polymers in the studied concentration range.