| Most of the fat-soluble drugs have low bioavailability problems,which can be attributed to their low water solubility,poor permeability,and large molecular weight.On the one hand,nanoemulsion can increase the solubility of fat-soluble drugs,on the other hand,it can effectively improve the permeability of fat-soluble drugs,which is a potential drug delivery method.In this paper,fat-soluble drug nanoemulsion was prepared by the high-gravity method.The formulation of nanoemulsion was optimized;the effect of process parameters on the particle size and particle size distribution of nanoemulsion were discussed;the stability of nanoemulsion was investigated,and the cytotoxicity,cell uptake and cell permeability of nanoemulsion were evaluated.The following conclusions can be drawn:By comparing the size of the emulsified region of the pseudo-ternary phase diagram,RH-40 was determined as a surfactant,glycerin was used as a co-surfactant.The formula of nanoemulsion was optimized,and coenzyme Q10 and β-carotene nanoemulsion were prepared by high-gravity technology.The particle size of CoQ10 nanoemulsion was 20.33 nm,PDI was 0.069,the concentration reached 2.3 mg/mL,the particle size of(β-carotene nanoemulsion was 19.81 nm,and PDI was 0.070,the appearance was clear and transparent.The prepared nanoemulsion remained stable after dilution and autoclave sterilization.However,after 14 days of illumination,the content of CoQ10 decreased to 4.66%,and the content of β-carotene decreased to 3.19%,which need to be protected from light.After stored at 40℃,4℃ and room temperature for 90 days in the dark,the particle size,zeta potential,content and appearance of CoQ10 nanoemulsion had no obvious change,and had good storage stability.β-carotene nanoemulsion was easy to oxidize and decompose during storage at 40℃,4℃ and room temperature for 30 days.Adding 0.1%TBHQ,BHA or vitamin E into the β-carotene nanoemulsion as antioxidant can obviously improve the stability.The cell uptake experiments qualitatively indicated that the degree of absorption of nanoemulsion by cells was proportional to time.The cell penetration experiments had quantitatively demonstrated the advantages of nanoemulsion administration:on the A-B side,the cumulative penetration of CoQ10 nanoemulsion was the highest,and its Papp was 1.37 times that of tablet,1.49 times that of soft capsule,1.69 times that of hard capsule,and 1.78 times that of API;while on the B-A side,the nanoemulsion had the lowest external displacement,and its Papp was 58%of the API,74%of the hard capsule,82%of the tablet,and 91%of the soft capsule.The Papp of the β-carotene nanoemulsion was 2.11 times that of API on the A-B side and 65%of the API while on the B-A side.In order to facilitate storage and transportation,CoQ10 was made into microcapsule.CoQ10 microcapsule was prepared with gelatin:maltodextrin=1:2 as the wall material and sodium stearyl lactate(150 mg/g)as the emulsifier.The microcapsule particle was dispersed,and the embedding efficiency was 86.03%.After 14 days of illumination,the residual content of CoQ10 in the microcapsules was 7.03 times that of the nanoemulsion,and the microcapsule remained stable at 40℃,4℃,and room temperature for 30 days.The dissolution experiment in vitro showed that the microcapsule had a sustained-release effect,which can improve the solubility and drug release ability of CoQ10. |
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