Development and Evaluation of Solid Lipid Nanoparticles for Bioavailability Enhancement of Curcumin
CHAPTER 2
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LITERATURE REVIEW
2.2 LITERATURE REVIEWED ON DRUG
Chirio, et.al (2011) formulated Curcumin-loaded solid lipid nanoparticles of fatty acids (FA) via coacervation technique based on FA precipitation from their sodium salt micelles in the presence of polymeric non-ionic surfactants and found higher entrapment efficiency and lowest possible cytotoxicity.
Prashar, et.al (2011) studied the various biological effects and other aspects of the Curcumin, herbal remedy and dietary spice. According to them Curcumin is a lipophilic molecule and rapidly permeate cell membranes and act by inhibiting tumor cell proliferation, induction of analysis, inhibition of transformation of normal cells to tumor cells and inhibition of invasion of metastasis. A number of animal studies have shown that Curcumin has a dose-dependent chemopreventive effect in colon, duodenal, stomach, esophageal and oral carcinogenesis. Curcumin possess various other activities like anti-inflammatory, anti-cancer, anti-coagulant, anti-fibrotic, anti-mutagenic, anti-fertility, anti-bacterial, anti-diabetic, anti-protozoan, anti-viral etc and concluded that Curcumin is an effective bioactive agent. The low water solubility and poor bioavailability of Curcumin can be overcome by various structural modifications. Stability aspect shows better effect and less toxicity offering better pharmacodynamic characteristics.
Choudhary, et.al (2012) studied the various potential therapeutic effects of Curcumin and reported that the research towards nanoparticles encapsulated Curcumin should be strengthened to improve bioavailability and therapeutic efficacy in treatment of various disorders.
Wang, et.al (2012) formulated Curcumin loaded solid lipid nanoparticles via solvent injection method using stearic acid and lecithin as lipid, tween 80 as surfactant and chloroform as cosolvent. The prepared SLNs were evaluated for various parameters like entrapment efficiency, drug loading, zeta potential, particle size, x-ray diffraction, in-vitro(via dialysis bag method) and in-vivo(in Balb/c mice) drug release and it was found that average size of C-SLNs was found to be 190 nm with zeta potential value of -20.7 mV and 75% drug entrapment efficiency. X-ray diffraction analysis revealed the amorphous nature of the encapsulated Curcumin. The release profile of C-SLLNs was an initial burst followed by sustained release and the Curcumin concentration in plasma suspension were significantly higher than those obtained with Curcumin alone, following C-SLNs, all the tissue concentrations of Curcumin increased, especially in lung and liver and it was found that in animal model of asthma, C-SLNs effectively suppressed airway hyperresponsiveness and inflammatory cell infiltration and also significantly inhibited the expression of T-helper-2-type cytokines, such as interleukin-4 and interleukin-13, in bronchoalveolar lavage fluid compared to the asthma group and Curcumin-treated group. These observations implied that C-SLNs could be a promising candidate for asthma therapy.
Zheng, et.al (2013) formulated solid lipid nanoparticles to encapsulate Curcumin, by blending liquid lipids (Sefsol-218®) with various solid lipids (Dynasan 114®, Dynasan 118®, Compritol ATO 888, Precirol 5ATO, Glyceryl monostearate, stearic acid and Hexadecanoid acid, Pluronic F68) via high pressure homogenization technique and found that the particle size decreased during the high shear process, and high pressure homogenization ensured the homogeneity of the nanoparticles. They also found that the Poloxamer 188 played a large role in the small and stable lipid nanoparticle system and contributed to the improved incorporation efficiency of Curcumin and concluded that suitable amount of liquid lipid when blended reduced the particle size of solid lipid nanoparticles and stabilized the system with improved dispensability and chemical stability in aqueous systems and exhibited sustained release and prolonged cell growth inhibition and cellular uptake in cancer cells as compared to unformulated free Curcumin and the relative bioavailability significantly increase after intravenous administration in rats.
Kakkar, et.al (2013) prepared and evaluated Curcumin loaded solid lipid nanoparticles in the experimental paradigm of cerebral ischemia (BCCAO model) in rats and found that there was an improvement of 90% in cognition and 52% inhibition of acetylcholinesterase versus cerebral ischemic group. Neurological scoring improved by 79%. Hence, study indicates protective role of Curcumin against cerebral ischemic insult; provided it is packaged suitably for improved brain delivery.
Sun, et.al (2013) prepared Curcumin loaded solid lipid nanoparticles (C-SLNs) by high-pressure homogenization by blending liquid lipid Sefsol-218® with the solid lipids and found that the high shear process, and high pressure homogenization ensured the homogeneity of the nanoparticles thereby improving the dispersibility and chemical stability of Curcumin, prolonging its antitumor activity and cellular uptake and enhancing its bioavailability. The morphology, sbability and release of Curcumin in the optimized formulation were investigated. The anti-cancer activity of the formulation was evaluated in MCF-7 cells. Fluorescence spectrophotometry was used to quantify cellular uptake of the drug. Blending sefsol-218® into a lipid matrix reduced the particle size without improving drug loading, mean size was found to be 152.8±4.7 nm and a 90% entrapment efficiency. Curcumin displayed a two-phase sustained release profile from C-SLNs with improved chemical stability, compared to the soubilized solution, C-SLNSs exhibited prolonged inhibitory activity in cancer cells, as well as time-dependent increases in intra-cellular uptake. After inravenous administration to rats, the bioavailability of Curcumin was increased by 1.25 fold and it was concluded that C-SLNs with improved dispersibility and chemical stability in an aqueous system have been successfully developed. C-SLNs may represent a potentially useful cancer therapeutic Curcumin delivery system.
Chen, et.al (2014) fabricated Curcumin loaded solid lipid nanoparticles via emulsion-evaporated technique and low temperature-solidification technique using monostearin as lipid, tween 80 as surfactant and methanol as cosolvent. C-SLNs were formed by lipid recrystallisation and the blank SLNs were prepared by the same procedure without adding Curcumin. Prepared C-SLNs were evaluated for various parameters like particle size, zeta potential, differential scanning calorimetry, x-ray diffraction, and in-vitro release and it was found that the particle size is 99.99 nm, polydispersity index of 0.158, zeta potential of -19.9 mV, and entrapment efficiency of 97.86 % and drug loading capacity of 4.35 %. The release kinetics in-vitro demonstrated Curcumin-loaded solid lipid nanoparticles can control drug-release and it was concluded that the Curcumin-loaded solid lipid nanoparticles could be prepared successfully with high drug entrapment efficiency and loading capacity and hence may be a promising drug delivery system to control drug release and improve bioavailability.
