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Preparation and Quality Evaluation of Three Kinds of Oleanolic Acid-loaded Nanoparticles

Author: JiangNi
Tutor: TianYan
School: Dalian Medical University
Course: Pharmacology
Keywords: Oleanolic acid Nanoparticles Lactic acid glycolic acid copolymer Lactic acid -glycolic acid - water-soluble vitamin E Polycaprolactone - polylactic acid - water-soluble vitamin E
CLC: R94
Type: Master's thesis
Year: 2010
Downloads: 131
Quote: 0
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Abstract


Objective: To a commercially available in vivo biodegradable medicinal polymer material lactic acid glycolic acid copolymer (PLGA) as a reference, with homemade lactic acid glycolic acid copolymer - the water-soluble vitamin E (PLGA-TPGS), polycaprolactone ester - polylactic acid - water-soluble vitamin E (The PCL-PLA-TPGS) as a carrier material, were prepared oleanolic acid nanoparticles and the encapsulation efficiency, particle size and drug loading indicators evaluate its quality, in order to find out suitable particle size, drug loading reasonable and in vitro drug release ideal nanoparticles, and lay the foundation for the evaluation of liver targeting, better play its hepatoprotective oleanolic acid, the role of anti-hepatitis and anti-liver cancer. Methods: homemade lactic acid glycolic acid copolymer - a water-soluble vitamin E (PLGA-TPGS), poly-caprolactone, - the polylactic acid - water-soluble vitamin E (PCL-PLA-lactic acid-glycolic acid copolymer (PLGA) using a commercially available TPGS) as the carrier material, phacoemulsification - solvent evaporation method three kinds of oleanolic acid nanoparticle encapsulation efficiency, particle size and drug loading indicators optimized by orthogonal design test preparation process. By RP-HPLC column HYPERSIL C18 column (4.6mm × 250mm, 5μm), with methanol: 0.03% aqueous solution of acetic acid (90:10) as the mobile phase, detection wavelength of 210 nm were measured three kinds of oleanolic acid nanoparticle drug loading, encapsulation efficiency and in vitro cumulative release rate. Results: homemade oleanolic acid - lactic acid-glycolic acid copolymer - nanoparticles, oleanolic acid - lactic acid-glycolic acid - water-soluble vitamin E-nanoparticles and oleanolic acid - poly caprolactone - polylactic acid - water soluble Vitamin E-average particle size of the nanoparticles were 227.4nm ± 2.2nm. 192.4nm ± 1.2nm.214.2nm ± 1.6nm, drug loading amount, respectively, 19.9% ??± 1.4%, 21.6% ± 1.0% and 20.2% ± 1.3%, the encapsulation efficiency was 85.6% ± 4.9%, 89.9% ± 4.3%, 87.7% ± 4.5%. The oleanolic acid nanoparticles in vitro release behavior Higuchi equation fitting release kinetics equation: Q = 4.581t1 / 2 7.189 (r = 0.9867) and Q = 4.493t1 / 2 3.856 ( r = 0.9904), Q = 4.358t1 / 2 3.528 (r = 0.9898), in vitro drug release showed a two phase release, release completely. Conclusion: The three kinds of oleanolic acid carrier material prepared nanoparticles particle size in line with the requirements of 10-1000nm nanoparticles and uniform particle size distribution, drug loading, encapsulation efficiency, quality controlled, in vitro release completely in sustained action, targeting the liver to be further studied. If the distribution of the drug in vivo experiments to further validate oleanolic acid - lactic acid-glycolic acid - water-soluble vitamin E-nanoparticles and oleanolic acid - poly caprolactone - polylactic acid - water-soluble vitamin E-liver concentrations of nanoparticles than oleanolic acid - lactic acid and glycolic acid copolymer - liver concentrations of nanoparticles will prove the homemade carrier material prepared two kinds of oleanolic acid nanoparticles inducing drugs liver targeting of oleanolic acid better play its hepatoprotective, anti-hepatitis and anti-hepatoma, and align the research of the OLA new preparations, industrial production and clinical research of nanoparticles has a certain value.

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