Mucoadhesive tetrahydrocannabinol-loaded NLC - Formulation optimization and long-term physicochemical stability

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Drug Delivery

Background:

• Oral Tetrahydrocannabinol (THC) formulations are common for cancer pain.
• A need exists for faster-acting, easily administered formulations, especially for breakthrough pain.
• Nasal delivery offers potential for rapid absorption and localized effects.

Purpose of the Study:

• To develop an aqueous nasal spray formulation of Tetrahydrocannabinol (THC).
• To utilize nanostructured lipid carriers (NLC) for improved stability and mucoadhesion.
• To assess the physical stability, mucoadhesive properties, and drug retention of the NLC formulation.

Main Methods:

• Nanostructured lipid carriers (NLC) were prepared using cetyl palmitate and Tetrahydrocannabinol (THC).
• NLCs were characterized for particle size, zeta potential, and mucoadhesion using mucin.
• Physical stability of THC within NLCs was evaluated under various storage conditions.

Main Results:

• NLCs with approximately 200nm diameter and positive surface charge were produced.
• Optimal formulations showed good miscibility with THC and 1-year physical stability.
• NLCs demonstrated strong mucoadhesion and maintained particle size upon spraying.
• High Tetrahydrocannabinol (THC) retention was observed: 91% after 6 months at 4°C and 79% at 40°C.

Conclusions:

• Aqueous Tetrahydrocannabinol (THC) nasal spray using nanostructured lipid carriers (NLC) is a feasible formulation.
• The NLC system enhances drug stability and mucoadhesion for effective nasal delivery.
• This formulation shows promise for managing cancer pain, particularly breakthrough pain.