Pharmaceutica Analytica Acta

Preparation and characterization of cholesterol-free liposome nanoparticles for therapeutic drug carriers

2^nd World Congress on Bioavailability & Bioequivalence: Pharmaceutical R & D Summit-2011 and International Conference on Pharmaceutics & Novel Drug Delivery Systems

06-08 June 2011, Las Vegas, USA

Ganesan Krishnamoorthy, Praveen Kumar Sehgal, Asit Baran Mandal and Sayeed Sadulla

Scientific Tracks Abstracts: PAA

Abstract:

Purpose:The cholesterol-free Liposome Nanoparticles (LNP) have been prepared and characterized for use as therapeutic drug carriers. Methods: Th e cholesterol-free LNP composed of diff erent ingredients, with varying molar ratios were prepared by heating under the N 2 atmosphere. Th e particle size, shape, zeta potential, surface morphology, structural elicitation and biocompatibility of cholesterol-free LNP were analyzed by Dynamic Light Scattering (DLS), Diff erential Scanning Calorimetric (DSC) and Th ermo gravimetric (TGA), X-ray Diff raction ( XRD), Fourier Transform Infrared (FT-IR) spectral, Scanning Electron Microscopic (SEM), Atomic Force Microscopic (AFM) analysis and Cell viability assay in order to develop a therapeutic drug carrier. Results: Th e particle size analysis showed that the cholesterol-free LNPs were in the size ranges between 20 -300 nm. Th ey exhibit an increase in the denaturation peak temperature when compared to native liposome. Th e XRD and TGA pattern of the LNP revealed the phase composition of both the phospholipids, cholesterol, withanolides components. FT-IR was used to analyze possible changes in the structure of phospholipids by analyzing the frequency of diff erent functional groups and by investigating the acyl chains and head-group region of the lipid molecule in the presence or absence of withanolides. We considered withanolides eff ectively increases the order of saturated alkyl chains of phospholipids (ordering eff ect) and the membrane surface density (condensing eff ect) and this eff ect essential for withanolides to maintain proper fl uidity , reduce passive permeability and increase the mechanical strength o f the LNP. Th e phospholipids withanolides complex was proposed to be maintained by electrostatic interaction between the zwitterionic polar heads of LNP, the phospholipids, cholesterol and withanolides used for making LNP in various ratios. Th e cell viability assay showed more than 90% fi broblast viability (NIH 3T3) aft er 24 and 48 hours of culture on LNP when compared with native liposome. Conclusion: Th ese carriers expecting a new, non-toxic, scalable and robust, and could be used as targeted and controlled/sustained release of drug. Th e lipases such as phospholipases are generally unable to hydrolyze the LNP and reduce the uptake of liposome by the mononuclear phagocytic system (MPS), resulting in an improved circulation half-life time, while simultaneously get piggybacking specifi city. Th e use of LNP also could have many benefi ts, including improving penetration, diff usion and selective transport of active ingredients, longer release time, greater stability of active, reduction of unwanted side eff ects and high biocompatibility. However, studies on an animal model needs to be carried out before using those devices.