ABSTRACT
Objective To enhance the solubility and bioavailability of curcumin (CUR).Methods A novel curcumin nanoparticles were prepared.The CUR-PGD nanoparticles were prepared by the method of ultrasound precipitation combined with high-pressure homogenization using codendrimer PAMAM-co-0.25OEG (PGD) as stabilizer.The stability of CUR-PGD nanoparticles was measured in 0.9% sodium chloride solution,5% glucose, PBS and plasma.Results The drug loading capacity (DL%) of CUR-PGD nanoparticles was 41.2%, the solubility of CUR was increased to 1.5 mg·mL-1 (50 times of CUR bulk powder).The mean diameter of the nanoparticles was 438.0 nm with spherical morphology and the zeta potential was 41.4 mV.The nanoparticles was stable in 0.9% sodium chloride solution,5% glucose, PBS and plasma and there was no hemolytic phenomenon, which meant they were suitable for intravenous administration.The DSC and XRD spectra of CUR-PGD nanoparticles showed that the CUR was presented as crystal morphology in the nanoparticles.The CUR released from nanoparticles was detected in different releasing medium and presented obvious controlled release behavior.Conclusion PGD may be an effective stabilizer for the preparation of CUR-PGD nanoparticles and CUR-PGD nanoparticles are a promising drug delivery system for CUR application in clinic.
ABSTRACT
To prepare and evaluate in vitro the 20 (S) -Protopanaxadiol (Ppd) pharmacosome. The Ppd pharmacosome was successfully prepared by thin film-dispersion and its stability in vitro was studied. The particle size of pharmacosome was evaluated by dynamic scattering (DLS) and the encapsulation efficiency was determined by using centrifugal ultra-filtration. The encapsulation efficiency of Ppd pharmacosome was (80.84 +/- 0.53)% with the diameter of 100. 1 nm; While the encapsulation efficiency of Ppd pharmacosome that added Brij 78 added was (72.76 +/- 0.63)% with the diameter of 117. 3 nm. In addition, the effect of some factors on the encapsulation efficiency and the particles size, such as temperature, alcohol, pH and artificial gastrointestinal fluids, were investigated respectively. The selected formulation and technology are simple and practical to prepare Ppd pharmacosome and preparation properties are more stable.
Subject(s)
Chemistry, Pharmaceutical , Drug Stability , Ethanol , Chemistry , Gastric Acid , Metabolism , Hydrogen-Ion Concentration , Light , Particle Size , Sapogenins , Chemistry , Metabolism , Scattering, Radiation , TemperatureABSTRACT
<p><b>OBJECTIVE</b>To establish a RP-HPLC method for content and entrapment efficiency of 20 (S)-protopanaxadiol in pharmacosomes.</p><p><b>METHOD</b>The separation was performed with a COSMOSIL 5 C18-MS-II column (4.6 mm x 250 mm, 5 mmicrom) using methanol-water (95:5) as the mobile phase and detected at 203 nm. The flow rate was 1.0 mL x min(-1) and 50 microL sample solution was injected for each time.</p><p><b>RESULT</b>The calibration curve was linear within the range 0.1-0.5 mg x mL(-1) (r = 0. 9999) , the intra-day RSD and inter-day RSD were less than 2% and the average recovery was between 101.44%-103.11% (n = 3).</p><p><b>CONCLUSION</b>The method is simple, accurate, sensitive and applicable for determination of content and entrapment efficiency of 20 (S)-protopanaxadiol pharmacosomes.</p>
