Preparation Of Ledum Volatile Oil Solid Lipid Nanoparticles

Objective:Ledum oil microemulsion method to prepare a colostrum, solidified into solid lipid nanoparticles in ice water (SLN). Establishment of quality evaluation criteria and evaluation methods in vitro percutaneous experiment, and skin penetration enhancing drugs, the influence of the anti-inflammatory effects of Ledum oil SLN in mice, the analgesic.Methods:Preparation of Ledum oil SLN by microemulsion method, were screened by influence factors test pre experiment and single factor preparation technology for SLN system, According to the entrapment efficiency as the evaluation index, the choice of drugs, dosage of emulsifier and co emulsifier, glycerol monostearate were investigated, through the optimization of preparation technology of SLN orthogonal design; Properties and surface morphology of Ledum oil SLN were characterized by particle size analyzer, transmission electron microscopy; Determination of p-cymene of Ledum oil SLN by capillary gas chromatography, and method of inspection; And then the stability experiment of Ledum oil SLN; using TP-6 type transdermal permeation tests in vitro were performed percutaneous permeability diffusion apparatus, the effects of SLN in vitro, the equation fitting on transdermal behavior; Investigation of analgesic effect of Ledum oil SLN by acetic acid writhing, anti-inflammatory effects by xylene induced mouse ear swelling test SLN.Results:Ledum oil SLN the best preparation process:Ledum oil dosage is 0.7G, glycerol monostearate was 1.5g, Twain 80 and poloxamer 188 were 2.0g and 1.0g, Ledum oil SLN using the optimum preparation of the average entrapment efficiency was 82.5%, RSD was 1.39%(n=3); average the particle size of SLN 146.9nm, the dispersion coefficient 0.264, Zeta potential is-23.77mV, transmission electron microscope is spherical, round appearance, uniform distribution. GC gas chromatography results showed that:p-cymene in 0.1006-3.018 mg/mL linear range of concentration of y=1.0413x+0.0167 (r^2=0.9998); The recovery rate is 99.89%, RSD is 0.84%(n=9), Ledum oil SLN three batches of p-cymene was 1.35%,1.41%, 1.37%. The stability test showed that the effect of high temperature on stability, Ledum oil SLN is large, and in high humidity, light stability under the condition of SLN is better, because the stability of Ledum oil SLN liquid, should first freeze drying, freeze dried into powder, then cryopreservation; in vitro evaluation show that: the penetration of Du Xiang oil SLN system promote Ledum oil; Pharmacodynamic test results show that:the writhing of Ledum oil SLN inhibited 0.6% by acetic acid, has certain analgesic effect; Ledum oil SLN in xylene induced mice ear swelling significantly inhibited, has the effect of anti inflammation.Conclusion:Ledum oil SLN has the advantages of simple preparation process, high encapsulation efficiency, quality evaluation meets the requirements, the in vitro transdermal absorption test and drug control of Ledum oil liquid, Ledum oil SLN permeation effect; no skin irritation and sensitization, pharmacodynamics experiment showed that Ledum oil SLN high agent the amount of analgesic and anti-inflammatory effects of group was better than the positive group of Ledum oil raw materials.