Abstract

curcumin is poorly water soluble drug with low bioavailability. Use of lipid systems in lipophilic substances increases solubility and bioavailability of poorly soluble drugs. The aim of this study was to prepare curcumin loaded Solid Lipid Nanoparticles (SLNs) with high loading efficiency, small particle size and prolonged release profile with enhanced antibacterial efficacy. to synthesize stable SLNs, freeze- Drying was done using mannitol as cryoprotectant. Cholesterol was used as carrier because of good tolerability and biocompatibility. SLNs were prepared using high pressure homogenization method. optimized SLNs had 112 and 163 nm particle size before and after freeze drying, respectively. The prepared SLNs had 71% loading efficiency. 90% of loaded curcumin was released after 48 hours. Morphologic study for formulation was done by taking SEM pictures of curcumin SLNs. RESULTS show the spherical shape of curcumin SLNs. DSC studies were performed to determine prolonged release mechanism. Antimicrobial studies were done to compare the antimicrobial efficacy of curcumin SLNs with free curcumin. DSC studies showed probability of formation of hydrogen bonds between cholesterol and curcumin which resulted in prolonged release of curcumin. Lipid structure of cholesterol could cause enhanced permeability in studied bacteria to increase antibacterial characteristics of curcumin. the designed curcumin SLNs could be candidate for formulation of different dosage forms or cosmeceutical products.

Highlights

  • Phytotherapeutics were prepared in nano size to improve pharmacokinetic and pharmacodynamics characteristics.[1]

  • Since most of the components involved in formulation of solid lipid nanoparticles are of natural origin, they are compatible with components of biological membrane, and generally less toxicological risk is experienced.[8]

  • Preparation of Curcumin Solid Lipid Nanoparticles (SLNs) Curcumin loaded SLNs were prepared using high pressure homogenization. 0.1 g tween 80 and 600 mg curcumin were added to 10 ml of purified water at room temperature, 600 mg of cholesterol was dissolved in mixture of ethanol and acetone on 3-1 ratio at 75-80 °C, the hot oily phase was added to aqueous phase under homogenization at 11000 rpm and the mixture was homogenized for 7 minutes

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Summary

Introduction

Phytotherapeutics were prepared in nano size to improve pharmacokinetic and pharmacodynamics characteristics.[1]. Since most of the components involved in formulation of solid lipid nanoparticles are of natural origin, they are compatible with components of biological membrane, and generally less toxicological risk is experienced.[8] Nanoparticles (NPs) are colloidal particles in which the active ingredients are dissolved, entrapped in and/or is adsorbed or attached on to the particle.[9] Some advantages of nanotechnology in phytoceuticals include: the probability of designing sustained release systems, enhanced physicochemical stability, enhanced permeability, improves tissue distribution and enhanced solubility and bioavailability.[1] Many novel drug delivery strategies such as liposomes, nano- or micro- emulsions, polymeric NPs and solid lipid NPs, polymer conjugates, polymeric micelles, nanocrystals, nanogels, self-assemblies and cyclodextrin inclusion complexes have been described to increase solubility, bioavailability and delivery of curcumin.[10] Solid lipid nanoparticles (SLNs) as colloidal carrier systems combine the advantages of traditional systems but avoid some of their major disadvantages. Curcumin SLNs were designed for treatment of lung cancer by Wang et al 2013.16 As curcumin has been used widely in Iran, in the present study, curcumin loaded SLNs were synthesized to prolong drug release and enhance antibacterial effects

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