Long chain lipid based tamoxifen NLC. Part I: preformulation studies, formulation development and physicochemical...

Area of Science:

• Pharmaceutical Nanotechnology
• Drug Delivery Systems
• Lipid Nanoparticles

Background:

• Tamoxifen citrate (Tmx) exhibits limited bioavailability and associated toxicity.
• Targeting the lymphatic system is a strategy to enhance Tmx efficacy at metastasis sites.
• Nanostructured lipid carriers (NLC) offer a promising platform for improved drug delivery.

Purpose of the Study:

• To formulate and characterize Tamoxifen citrate-loaded nanostructured lipid carriers (Tmx-NLC).
• To evaluate the potential of Tmx-NLC for lymphatic targeting and improved bioavailability.
• To assess the stability and drug release profile of Tmx-NLC in simulated gastrointestinal conditions.

Main Methods:

• Solvent diffusion technique was employed for Tmx-NLC formulation.
• Physicochemical characterization included TEM, DSC, XRD, and FTIR.
• Entrapment efficiency, particle size, and stability studies were conducted.

Main Results:

• Tmx-NLC achieved >90% entrapment efficiency with a particle size of 215.60 ± 7.98 nm.
• Freeze-dried Tmx-NLC demonstrated stability in various gastrointestinal pH media.
• Sustained drug release pattern was observed irrespective of the medium's pH.

Conclusions:

• Tmx-NLC formulation is a viable approach for enhancing tamoxifen delivery.
• The NLC system shows potential for improved lymphatic targeting and reduced toxicity.
• Tmx-NLC exhibits favorable stability and sustained release characteristics for oral administration.