Abstract
Objective: The present study was aimed at preparing stable lyophilized curcumin loaded nanostructured lipid carriers (NLCs). The optimized lyophilized curcumin loaded NLCs were characterized and evaluated for various quality control parameters. Methods: The optimized curcumin loaded NLCs were prepared by modified hot emulsification using precirol ATO 5 (PRE), capmul MCM C8 EP (CAP) as solid and liquid lipids, respectively. The combination of tween 80 (T80) and solutol HS 15 (SHS) were used as an emulsifier. The NLCs dispersion was lyophilized into powder form to improve the thermodynamic stability of the formulation. The lyophilized curcumin loaded NLCs were evaluated for particle size, size distribution, zeta potential, entrapment efficiency (EE), drug loading, assay, in vitro drug release, crystallinity and surface morphology studies. Results: The optimized lyophilized curcumin loaded NLCs have a mean particle size of 286.2±11.5 nm with a size distribution of 0.288±0.011, a zeta potential of 0.247±0.025 mV with high entrapment of 98.20±1.53 % and drug loading of 2.50±0.21 %. The X-ray diffraction and endothermic peaks confirmed the maximum encapsulation of curcumin in lipid matrices. The particles were spherical with smooth surface morphology. In vitro release studies showed sustained release for up to 24 h. The cytotoxicity against human lung cancer line A-549 for curcumin-loaded NLCs was confirmed with positive control adriamycin (ADR). Conclusion: Curcumin-loaded NLCs prepared had a nanosize particle distribution with maximum entrapment efficiency. Dispersion stability was increased by the lyophilisation process. The solid lyophilized powder is reconstituted for oral delivery.
Highlights
A polyphenolic compound, curcumin, targets various signalling compounds at the cellular level [1]
The solubility of curcumin in solid lipids is in the order of precirol ATO 5 (PRE)>Dynasan 116 (D116)>GLE>Dynasan 114 (D114)>Dynasan 118 (D118)
The optimized curcumin loaded nanostructured lipid carriers (NLCs) were developed by a modified hot melt emulsification with maximum entrapment efficiency, drug loading, nano particle size distribution and zeta potential
Summary
A polyphenolic compound, curcumin, targets various signalling compounds at the cellular level [1]. Curcumin potently effects intracellularly by altering important processes like modulation of the genome, cell invasion and death. This shows curcumin as a promising candidate for cytostatic and cytotoxic activity. Low plasma levels of curcumin are due to poor solubility and high first-pass metabolism and intestinal metabolism including glucuronidation and sulfation on oral administration [8]. The cytotoxic activity of curcumin loaded NLCs were previously reported against human HepG2 cells [22], astrocytoma–glioblastoma cell line (U373MG) [23], Caco-2 cell [24], brain cancer [25, 26], HeLa cells [27], human lung adenocarcinoma A549 cells [28]. We evaluated in vitro cytotoxic activity against cell lines of non-small cell lung cancer for optimized curcumin NLC formulation
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