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12:48
PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
Published on: December 27, 2013
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Vitamin E TPGS Emulsified Vinorelbine Bitartrate Loaded Solid Lipid Nanoparticles (SLN): Formulation Development,
Lakshmi Maurya1, Sanjay Singh1, Vijayakumar M Rajamanickam1
1Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (BHU), Varanasi, U.P, India.
Current Drug Delivery
|April 10, 2018
Summary
Solid lipid nanoparticles (SLNs) were developed using a design of experiments (DOE) approach to encapsulate vinorelbine bitartrate (VRL). The resulting TPGS-VRL-SLNs demonstrated significantly enhanced anticancer efficacy compared to VRL alone, showing potential as cancer therapeutics.
Area of Science:
- Nanotechnology
- Materials Science
- Pharmacology
Background:
- Vinorelbine bitartrate (VRL), a vinca alkaloid for breast cancer, faces oral delivery challenges due to its hydrophilic and thermolabile properties.
- Developing effective oral formulations is crucial for improving VRL's therapeutic application.
Purpose of the Study:
- To apply a design of experiments (DOE) approach for developing and optimizing solid lipid nanoparticles (SLNs) for hydrophilic and thermolabile VRL.
- To maximize VRL encapsulation within SLNs without compromising its integrity or anticancer activity.
Main Methods:
- SLNs were prepared using a solvent diffusion technique with Taguchi orthogonal array design.
- Glyceryl mono-oleate (GMO) was used for enhanced entrapment and minimized thermal degradation.
- Vitamin E TPGS (TPGS) and Poloxamer-188 were employed as surfactants to create TPGS-VRL-SLNs and PL-VRL-SLNs.
Main Results:
- SLNs exhibited spherical morphology with up to 58% entrapment efficiency.
- In vitro release studies indicated a biphasic release pattern following the Korsemeyer-Peppas model with Fickian kinetics.
- MTT assays showed TPGS-VRL-SLNs and PL-VRL-SLNs were 39.5 and 18.5 times more effective than pristine VRL, respectively.
Conclusions:
- The DOE approach successfully facilitated VRL-SLN development.
- Enhanced efficacy of TPGS-VRL-SLNs is attributed to GMO's emulsifying properties and TPGS's inherent cytotoxicity, synergizing with VRL.
- TPGS-associated SLNs show promise as carriers for cancer chemotherapy.
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