Enhancing Oral Bioavailability and Brain Biodistribution of Perillyl Alcohol Using Nanostructured Lipid Carriers

Area of Science:

• * Pharmaceutical Nanotechnology
• * Cancer Therapeutics
• * Drug Delivery Systems

Background:

• * Perillyl alcohol (POH), a limonene-derived monoterpenoid, exhibits antitumor potential for brain tumors.
• * Limited oral bioavailability and poor brain penetration of POH restrict its clinical efficacy.
• * Nanostructured lipid carriers (NLCs) offer a strategy to overcome these delivery challenges.

Purpose of the Study:

• * To develop and characterize POH-loaded NLCs for improved brain biodistribution.
• * To evaluate the in vitro and in vivo performance of POH-loaded NLCs.

Main Methods:

• * NLCs were prepared using hot homogenization.
• * Physicochemical properties (size, morphology, encapsulation efficiency, crystallinity) were analyzed.
• * In vitro release, stability, pharmacokinetic, and biodistribution studies were conducted in rats.

Main Results:

• * POH-loaded NLCs exhibited a mean diameter of 287 nm, spherical morphology, and 99.68% encapsulation efficiency.
• * NLCs demonstrated biphasic in vitro release and stability in simulated gastrointestinal fluids.
• * In vivo studies showed enhanced oral bioavailability and significantly increased POH brain concentration with NLCs compared to free POH.

Conclusions:

• * NLCs effectively enhance the oral bioavailability and brain biodistribution of perillyl alcohol.
• * This NLC-based delivery system presents a promising strategy for brain tumor treatment.