Preparation and evaluation of shikonin nanostructured lipid carriers
Objective To prepare and optimize the formulation of shikonin nanostructured lipid carrier(NLC)and to evaluate its characterization,wound irritation testing and anti-inflammatory activity.Methods The prescriptions of shikonin NLC were screened by saturated solubility,lipid compatibility and emulsification ability.With particle size and polymer dispersity index(PDI)as indexes,the preparation method of shikonin NLC was examined.The ranges of solid-liquid lipid ratio,total lipid dosage,emulsifier dosage and drug dosage were investigated by single factor method.Effects of solid-liquid lipid ratio,total lipid dosage and drug dosage on PDI and drug loading were determined by orthogonal experiment,and the optimal prescription was verified.The characterization of shikonin NLC was completed.The wound irritation of shikonin NLC was tested by continuous administration after damage causing to the dorsal epidermis of rats.Lipopolysaccharide induced RAW264.7 cell inflammation model was used to evaluate the in vitro anti-inflammation activity of shikonin NLCs with nitric oxide release rate as the indicator.Results Transcutol P was used as a liquid lipid,the solid lipid was glyceryl distearate,and the emulsifier was BRIJ®O20.The optimal prescription of shikonin NLC prepared by film-dispersion and hydration method was as follows:emulsifier dosage of 6％,solid-liquid lipid ratio of 4∶6,the total lipid dosage at 6％,and drug dosage at 20 mg.No erythema or edema was seen on the damaged skin on the rats'back,and the skin tissue structure was basically normal.At the same dose,shikonin NLC better inhibited the release of nitric oxide from RAW264.7 than shikonin alone.Conclusion Nanoparticles with high drug loading and uniform particle size are obtained.Shikonin NLC do not irritate the wound surface,with decreased cytotoxicity and good anti-inflammation activity.
shikoninnanostructured lipid carrierorthogonal test designcharacterizationirritation evaluation
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