Abstract
Curcumin (C), a natural anticancer agent suffers extremely low aqueous solubility and rapid systemic elimination, therefore, the aim from the present study was to develop and optimize biocompatible, biodegradable solid lipid nanoparticles containing curcumin (CSLNs) using Solvent Injection Method. The components selected to develop the SLNs were Glycerol MonoStearate (GMS; the lipidic carrier), Poloxamer 407 (P407; Surfactant) and Ethanol (solvent for the drug and the lipidic carrier). The combination and ratios for the optimization process were carried out using 23 full-factorial designs. The experimental design runs (8 formulations H1–H8) were prepared and the design dependent responses (assessment of particle size, Entrapment Efficiency % and the in vitro release study) were characterized. The developed formulae showed a nanometric particle size range (203.0–345.0nm), high Entrapment Efficiency % (62.77–87.42 %) and prolonged release over 24 hr periods (55.97–89.64 %). These results were analyzed using JMP® 10 software and its analytical tools were used to draw Pareto charts and the interactions plots. On the basis of the software analysis, formulation H9 with a desirability factor of 0.582 was selected as the optimized formulation and was evaluated for the dependent responses. Formulation H9 showed a particle size of 249.1 nm, 74.51 % Entrapment efficiency, 85.72 % in vitro release over 24 hr and these results suggested that the solid lipid nanoparticles formulations could be a promising method to sustain the release of curcumin.
Highlights
The cumulative curcumin percent released (CDR %) was determined as described earlier by (Nayak et al, 2010; Bisht et al, 2007) with a suitable modification where known amount of lyophilized Curcumin Solid Lipid Nanoparticles (C-SLNs) formulations (100 mg) were dispersed in Phosphate Bufferd Saline (PBS) pH 7.4 and the dispersion was divided into 8 aliquots (1 ml each) in microfuge tubes which were kept in a thermo stable water bath at 37◦C ± 0.5◦C
C-SLNs formulations were successfully prepared by Solvent Injection Method which gave a yellowish sponge product after the freeze-drying process
Another factor should be considered for the relatively high EE % of curcumin in Glycerol MonoStearate (GMS)-based SLNs formulations which is the effect of Poloxamer 407 (P407)
Summary
Traditional medicine is known to be fertile ground for the source of modern medicines (Corson and Crews, 2007; Aggarwal and Sung, 2008; Wu et al, 2011) as Nature’s chemical diversity and complexity form a unique source of molecules for a wide range of therapeutic targets (Balunas and Kinghorn, 2005; Coimbra et al, 2011). SLNs as drug delivery systems have a well known advantages such as good tolerability, lower cytotoxicity, higher bioavailability by oral administration, increase in the drug stability as well as other advantages provided by lipid excipients, such as biodegradability and cost effectiveness that promote their use as novel drug carriers (Mehnert and Mader, 2001; Mukherjee et al, 2007) Since they are consisting of physiological and biodegradable lipids, lipid nanoparticles are suitable for the incorporation of lipophilic, hydrophilic, and poorly water-soluble drugs within the lipid matrix in considerable amounts (Bunjes et al, 2001). Many researchers have optimized nanoparticulate formulations using 23 full-factorial design (Bozkir and Saka, 2005; Bhavsar et al, 2006; Derakhshandeh et al, 2007; Shah and Pathak, 2010)
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