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Anti-oxidant Containing Nanostructured Lipid Carriers of Ritonavir: Development, Optimization, and In Vitro and In
Srinivas Reddy Jitta1, Navya Ajitkumar Bhaskaran1, Salwa1
1Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education (MAHE), Manipal, Udupi, Karnataka, 576 104, India.
AAPS Pharmscitech
|March 17, 2022
Summary
This study developed nanostructured lipid carriers (NLCs) for ritonavir, enhancing its oral bioavailability and reducing side effects. The optimized NLC formulation significantly improved pharmacokinetic parameters compared to the pure drug.
Area of Science:
- Pharmaceutical Nanotechnology
- Drug Delivery Systems
- Pharmacology
Background:
- Human immunodeficiency virus (HIV) infection is managed with highly active anti-retroviral therapy (HAART).
- Ritonavir, a protease inhibitor, has limitations including low bioavailability and side effects, restricting its use as a primary treatment.
- Despite limitations, ritonavir is used at lower doses as a pharmacokinetic booster for other protease inhibitors.
Purpose of the Study:
- To develop and characterize nanostructured lipid carriers (NLCs) encapsulating ritonavir.
- To improve ritonavir's oral bioavailability and mitigate its adverse effects through nanoencapsulation.
- To evaluate the in vitro and in vivo performance of ritonavir-loaded NLCs.
Main Methods:
- Ritonavir-loaded NLCs were prepared using a hot-emulsion and ultrasonication method with solid and liquid lipids (alpha-tocopherol).
- Quality by Design (QbD) approach was employed for optimization of formulation variables.
- Characterization included particle size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), in vitro drug release, and in vivo pharmacokinetic studies.
Main Results:
- Optimized NLCs exhibited particle sizes between 273.9–458.7 nm, PDI of 0.314–0.480, ZP of -52.2 to -40.9 mV, and entrapment efficiency of 47.37–74.51%.
- In vitro studies showed higher ritonavir release in acidic medium compared to pH 6.8 phosphate buffer.
- In vivo studies demonstrated a 7-fold increase in AUC and over 10-fold higher Cmax for the optimized NLC formulation versus pure ritonavir suspension.
Conclusions:
- Nanostructured lipid carriers effectively encapsulate ritonavir, enhancing its oral bioavailability.
- The developed NLC formulation significantly improves ritonavir's pharmacokinetic profile, offering a promising approach for HIV treatment.
- This nanoformulation strategy holds potential for reducing ritonavir's side effects and improving therapeutic outcomes.
