ABSTRACT
Flexible liposomes are an excellent drug delivery nanocarrier, however, the leakage of drugs from liposomes has become common technical obstacle in the industry and also hindered its further application seriously. It is very urgent and necessary to avoid or reduce the leakage of drugs from liposomes. In this work, five kinds of essential oils such as Folium Artemisiae Argyi oil (FA), Folium Eucalypti oil (FE), Arabian Jasmine oil (AJ), Syzygium Aromaticum oil (SA) and Fructus Forsythiae oil (FF) were encapsulated in the lipid bilayer of palmatine chloride (PC) loaded flexible nano-liposomes (PFL), then the optimal essential oil and its dosage level were determined by the external leakage curve of PC. The female Japanese white rabbits were used to evaluate the vaginal irritancy potential of liposomes samples. The pharmaceutical properties such as encapsulation efficiency, particle size, zeta potential, deformability and structure of liposomes samples were evaluated. In order to investigate the permeability of liposomes samples to deliver PC across skin and mucous membrane in vitro, the side-by-side diffusion cells were used. The results showed that the leakage of hydrosoluble PC from PFL was reduced at different degrees by the essential oils in the lipid bilayer of PFL, however, the reduction in leakage degree was obviously higher for FA than thoses of FE, AJ, SA and FF (P < 0.05), and the highest reduction in leakage degree was obtained when the FA and lipid mass ratio was 1:6. The encapsulation efficiency, particle size, zeta potential and deformability of PFL were not significantly changed after FA was encapsulated in the lipid bilayer of the PFL (P > 0.05), so did the lamellar structure of PFL. In addition, the transdermal and transmucosal permeability of PC were also enhanced obviously by encapsulating FA in the lipid bilayer of PFL, and there was no vaginal/vulvar irritation observed in the rabbits. In summary, the drug leakage was reduced by encapsulating suitable essential oil (such as FA) in the lipid bilayer of flexible liposomes, and the vaginal mucosa permeability were improved for the drug. These results provide a novel technique in the improvement of flexible nano-liposomes for drug delivery.
ABSTRACT
AIM To establish an HPLC method for the simultaneous content determination of six constituents in Jiaotai Pills (Coptidis Rhizoma and Cinnamomi Cortex).METHODS The analysis of 30％ methanol of this drug was performed on a 30 ℃ Agilent ZORBAX SB-C1s column (4.6 mm ×250 mm,5 μm),with the mobile phase comprising of acetonitrile-KH2PO4flowing at 0.8 mL/min in a gradient elution manner,and the detection wavelength was set at 276 nm.RESULTS Epiberberine,jatrorrhizine hydrochloride,coptisine hydrochloride,palmatine chloride,berberine hydrochloride and cinnamaldehyde showed good linear relationships within the ranges of 0.64-41.24 μg/mL (R2 =0.999 9),0.65-43.76 μg/mL (R2 =1.000 0),0.82-52.65 μg/mL (R2 =0.999 9),0.79-50.70 μg/mL (R2 =0.999 9),3.08-197.20 μg/mL (R2=0.999 8) and 0.65-41.65 μg/mL (R2 =0.999 9),whose average recoveries were 98.06％,102.76％,99.27％,99.75％,96.74％ and 101.33％ with the RSDs of 0.56％,0.54％,0.39％,0.55％,0.48％ and 2.14％,respectively.CONCLUSION This accurate,sensitive,stable and reproducible method can be used for the quality control of Jiaotai Pills.
ABSTRACT
AIM To establish an HPLC method for the simultaneous content determination of four constituents in Xiaojie'an Capsules (Forsythiae Fructus,Leonuri Herba,Spatholobi Caulis,etc.).METHODS The analysis of chloroform extract of this drug was carried out on a 30 ℃ thermostatic Diamond C1scolumn(250 mm ×4.6 mm,5 μm),with the mobile phase comprising of acetonitrile (A)-0.05 mol/L monosodium phosphate (B) flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 278 nm.RESULTS Berberine hydrochloride,palmatine chloride,phillyrin and rutin showed good linear relationships within the ranges of 0.033 7-0.337 2 μg (r =0.999 1),0.054 8-0.548 3 μg (r =0.999 0),0.025 9-0.258 8 μg (r=0.999 2) and 0.008 4-0.084 2 μg (r =0.999 6),whose average recoveries were 98.8％ (RSD =1.3％),99.8％ (RSD =0.7％),98.8％ (RSD =1.3％) and 96.8％ (RSD =1.0％),respectively.CONCLUSION This sensitive and accurate method can be used for the quality control of Xiaojie'an Capsules.