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IMAGE: Vitamin E TPGS Emulsified Vinorelbine Bitartrate Loaded Solid Lipid Nanoparticles (SLN): Formulation Development, Optimization and In vitro Characterization.
Credit: Dr. Sanjay Singh, Bentham Science Publishers
Vinorelbine Bitartrate (VRL), a semi-synthetic vinca alkaloid was approved by the FDA for breast cancer treatment, as it has been proven to be beneficial for first line of defense and subsequent therapies. But its hydrophilic and thermolabile structure causes hindrance to oral clinical translation. The main objective of this research is the development and optimization of a solid lipid nanoparticle (SLN) structure that can encapsulate hydrophilic and thermolabile Vinorelbine bitartrate to maximize the anticancer activity of the drug without compromising its efficacy and integrity. For this purpose, the study is mainly focused on the application of DOE, a modern statistical optimization tool for nanoparticle modification.
To prepare SLNs, a solvent diffusion technique was used employing Taguchi orthogonal array design with process variables and optimized formulation. Glyceryl mono-oleate (GMO) were used for its emulsifying nature and low melting point to enhance entrapment and reducing temperature associated degradation. To prevent infection, two types of surfactants, Vitamin E TPGS, and Poloxamer-188 were used to obtain TPGS-VRL-SLNs and PL-VRL-SLNs.
The results proved the method to be effective. The SLNs were produced spherical in shape with entrapment efficiency (EE) upto 58%. A biphasic release pattern was observed in in vitro release studies followed by the Korsemeyer peppas model with fickian release kinetics. MTT assay results revealed that TPGS-VRL-SLNs and PL-VRL-SLNs were 39.5 and 18.5 time more effective than VRL in its original nature. The DOE method was believed to be a successful approach for development of VRL-SLNs. Enhanced entrapment with anticancer efficacy of TPGS-VRL-SLN was the result of emulsifying nature of GMO and the cytotoxic nature of TPGS which influences VRL effects. Such properties of TPGS-VRL-SLNs may prove them to be a potentially useful carrier in cancer chemotherapeutics.