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Emodin nanostructured lipid carriers(ED-NLC) were prepared and their quality was evaluated in vitro. Based on the results of single-factor experiments, the ED-NLC formulation was optimized by Box-Behnken response surface method with the dosages of emodin, isopropyl myristate and poloxamer 188 as factors and the nanoparticle size, encapsulation efficiency and drug loading as evaluation indexes. Then the evaluation was performed on the morphology, size and in vitro release of the nanoparticles prepared by emulsification-ultrasonic dispersion method in line with the optimal formulation, i.e., 3.27 mg emodin, 148.68 mg isopropyl myristate and 173.48 mg poloxamer 188. Under a transmission electron microscope(TEM), ED-NLC were spherical and their particle size distribution was uniform. The particle size of ED-NLC was(97.02±1.55) nm, the polymer dispersion index 0.21±0.01, the zeta potential(-38.96±0.65) mV, the encapsulation efficiency 90.41%±0.56% and the drug loading 1.55%±0.01%. The results of differential scanning calorimeter(DSC) indicated that emodin may be encapsulated into the nanostructured lipid carriers in molecular or amorphous form. In vitro drug release had obvious characteristics of slow release, which accorded with the first-order drug release equation. The fitting model of Box-Behnken response surface methodology was proved accurate and reliable. The optimal formulation-based ED-NLC featured concentrated particle size distribution and high encapsulation efficiency, which laid a foundation for the follow-up study of ED-NLC in vivo.
Subject(s)
Drug Carriers , Emodin , Follow-Up Studies , Lipids , NanostructuresABSTRACT
Objective: To prepare plumbagin transfersomal (PBG-T) gel and investigate its transdermal penetration characteristics in vitro. Methods: Plumbagin transfersomes were prepared by film-ultrasonic dispersion method. The optimal prescription condition of PBG-T was selected by central composite design and response surface method. The formula of PBG-T gel was optimized by orthogonal test. The Franz diffusion cell was used to investigate transdermal penetration characteristics of PBG-T gel in vitro. Results: The optimal prescription condition of transfersomes was determined as drug 10.0 mg, phospholipids 700.0 mg, Tween-80 91.5 mg, ultrasonication time 13 min. The optimal prescription condition of transfersomal gel was 1% carbomer 940 as gel matrix, and 5% glycerol as the humectant. According to the optimized prescription, the entrapment efficiency, the mean particle size, and Zeta potential of PBG-T were (79.88 ± 2.26)%, (125.64 ± 4.54) nm, and (-30.97 ± 1.13) mV. The cumulative penetration rate of PBG-T gel was 70.0% at 12 h. Conclusion: The optimal preparation technique is stable and feasible. Transfersomal gel features a sustained release in vitro, the transfersomal gel can increase penetration rate of plumbagin through the skin of rats.
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AIM To prepare nanostructured lipid carriers for volatile oils from Artemisiae argyi Folium.METHODS Heated melting-ultrasonic dispersion method was applied to preparing lipid carriers.Taking solid/liquid lipid ratio,amounts of lipid,emulsifier and volatile oils as influencing factors,and average paticle size as an evaluation index,the formulation was optimized by orthogonal test.With cineole,camphor and borneol as indices,GC-MS was adopted in the content determination of volatile oils.RESULTS The optimal formulation was determined to be 5 ∶ 5 for solid/liquid lipid ratio,1％,3％ and 0.5％ for amounts of lipid,emulsifier and volatile oils,respectively.The obtained clear and transparent lipid carriers demonstrated the average particle size of (72.33 ±1.93) nm,PDI of 0.273 ± 0.004 5,and Zeta potential of (-30.59 ± 1.42) mV,whose in vitro release rate was lower than that of raw medicine within 120 h,along with a higher stability under 4 ℃ than that under 25 ℃.The entrapment efficiencies of cineole,camphor and borneol were 87.49％,86.45％ and 92.12％ with the drug loadings of 8.25％,2.00％ and 3.38％,respectively.CONCLUSION It is suggested that nanostructured lipid carriers for volatile oils from Artemisiae argyi Folium should be stored under 4 ℃ with the features of sustainedrelease and stable physicochemical properties.
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Objective To prepare asiatic acid (AA) loaded chitosan-deoxycholic acid self-assembled micelles (AA-CS-DCA PMs) adopting chitosan-deoxycholic acid (CS-DCA) as carriers and investigate its pharmacokinetic characteristics in rats. Methods AA-CS-DCA PMs were prepared by ultrasonic dispersion method. The characteristics of micelles were evaluated by the distribution of particle size, Zeta potential, drug loading, encapsulation efficiency, and in vitro release. Model of bile drainage was established in conscious rats and pre-column derivatization HPLC method was used to determine the concentration of AA in bile. Moreover, the pharmacokinetics characteristics of AA-CS-DCA PMs in vivo was evaluated by tmax, Cmax and AUC0-t. Results The particle size was (70.5 ± 9.8) nm, the Zeta potential was (38.4 ± 0.8) mV, and encapsulation efficiency and drug loading were (77.8 ± 1.2)% and (11.7 ± 0.2)%, respectively. The in vitro release profile showed a sustained release property. In vivo study showed that Cmax of AA-CS-DCA group (26.05 ± 3.04) μg/h was 2.8 times higher than that of the control group (9.19 ± 1.12) μg/h; The tmax of AA-CS-DCA PMs group prolonged significantly (P < 0.05) in biliary excretion (2 h vs 1 h) and the elimination half-life t1/2 was 1.8 times of the control group [(2.68 ± 1.71) h vs (1.49 ± 0.38 h)]. In addition, the AUC0-24 h which reflected the degree of drug absorption increased by 200% compared with the control group [(99.05 ± 12.83) μg vs (33.56 ± 8.33) μg]. Conclusion The chitosan- deoxycholic acid self-assembled micelles can raise the concentration of AA and prolong the retention time in vivo, which effectively improve the oral bioavailability of AA.
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Objective: To prepare hydrogel matrix sustained-release tablets of resveratrol solid lipid nanoparticles, and the factors that might influence drug release and in vitro release models were also investigated in present study. Methods: The resveratrol-solid lipid nanoparticles (Res-SLN) were prepared by thin-film ultrasonic dispersion method, and then the hydrogel matrix was prepared by dispersed in excipients of hydrogel matrix sustained-release tablets. Single factor analysis was used to study the effects of varieties of adhesives, PEG, HPMC, and the amounts of HPMC K15 on drug release. Then the orthogonal design was used to gain the optimum formulation. Zero-order, first-order, Higuchi, and Ritger-Pappas models were used for the model fitting of drug release. Results: Hydrogel matrix sustained-release tablet of Res-SLN was better accorded with Zero-order kinetics model. The equation was Mt/M∞ = 0.078 7 t + 0.003 6 (r = 0.998 0). In vitro release behavior was in line with Ritger-Peppas equation, and the drug release from the tablets was controlled by degradation of the matrix. Conclusion: Prescription of hydrogel matrix sustained-release tablet of Res-SLN is reasonable; The preparation technology is feasible and exhibits perfect sustained-release characteristics in vitro in 12 h.
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Objective To prepared the docetaxel nano liposome (L-DOC) for the therapy of liver cancer HepG2 cells in vitro and in vivo. Methods The film-ultrasonic dispersion method was used to prepare the L-DOC.The diameter and Zeta potential of L-DOC were determined by Nanosizer and the encapsulation efficiency was further measured.CCK-8 method was used to determine the cell viability of HepG2 cell after treating with various concentration of DOC and L-DOC respectively and the cell death type was detected by Flow cytometer.Next, we have studied the relative tumor volume change of tumor-bearing mice and the toxicity in vivo.Results The average diameter of L-DOC was 104 nm and the Zeta potential was about -35.1 mV.The Zeta potential of L-DOC was almost unchanged after standing for 96 hours.The encapsulation efficiency of L-DOC was ( 71.2 ±1.6 )%.The CCK-8 results showed that the cell viability was decreased after treating with various concentration of DOC and L-DOC, but the inhibition effect of L-DOC was better than that of DOC after treating with the same dose, especially for 20μg/mL.It was found that the cell death was induced by apoptosis.The in vivo study results showed that 6mg/kg L-DOC could inhibit the tumor volume better than that of same dose of DOC.In addition, 6mg/kg L-DOC and DOC didn’ t induce in vivo toxicity.Conclusion The L-DOC is prepared by film-ultrasonic dispersion method which has small diameter, great biocompatibility.And it could inhibit the HepG2 cells in vitro and in vivo, especially for no in vivo toxicity.
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Objective: To establish a method for the preparation of chrysophanol freeze-dried liposomes. Methods: The liposome suspension was prepared by film-ultrasonic dispersion method. The entrapment efficiency (EE) was determined by low-speed centrifugation and the influences of pre-freezing time, drying time, and type, dosage, and adding methods of the protective agents on EE of the freeze-dried liposome were studied. Results: The pre-freezing time was 24 h, the drying time was 24 h, mannitol-sucrose (mass ratio 1:1) as protective agent was externally added to get uniform particle with good redissolution and the EE was (61.30 ± 2.2)%. Conclusion: The liposome prepared by film-ultrasonic dispersion method is protected by mannitol-sucrose to get uniform particle size with the excellent redissolution and high EE.