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Preparation of PLGA Non-spherical Particles and the Study of Their Potential as Novel Carriers of All-trans-retinoic Acid

Author: LiRuiFeng
Tutor: ZhangQiQing
School: Beijing Union Medical College
Course: Biomedical Engineering
Keywords: Polylactic acid - glycolic acid copolymer Non- spherical micro- structure High yield Drug delivery systems Emulsion Pharmacokinetics
CLC: R943
Type: Master's thesis
Year: 2011
Downloads: 35
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Abstract

The shape and size of the drug carrier, in recent years, more and more people pay attention. It has been realized that the shape and size of the drug carrier particles is closely related to the clinical effect of the pharmaceutical preparations. In this study of polylactic acid - glycolic acid copolymer (PLGA) as a carrier material, the use of the emulsion - solvent evaporation were prepared by non-spherical microparticles of the high yield of the PLGA, application transmission electron microscopy (TEM), scanning electron microscope (SEM) observation The particle shape and application software to measure the particle size and distribution; by adjusting the experimental parameters, such as the viscosity of the reaction system, the content of sodium polyphosphate (STP), the stirring rate, the polymer molecular weight, etc., to achieve the control of the particle shape and size. The characterization of the mechanism of the formation of the non-spherical micro-structure of the prepared particles the PVA residue detection and infrared spectroscopy. Believe that the formation mechanism is the viscosity of the reaction system, and small molecule crosslinker play a synergistic role in the preparation process of the non-spherical microparticles. Hydrophobic drug ATRA as a model drug, the the physical embedding method - emulsification prepared package containing all-trans retinoic acid (ATRA) PLGA spherical and non-spherical particles (NSP / ATRA, SP / ATRA), and The drug loading and encapsulation efficiency were determined also investigated PLGA molecular weight carrier particle shape, drug / carrier ratio of drug loading and encapsulation efficiency, the results show that the non-spherical drug-loaded particles drug loading, encapsulation rates are higher than the drug-loaded microspheres; as a drug carrier particles of the carrier material was prepared using a smaller molecular weight of PLGA is higher than the encapsulation efficiency of a large molecular weight experimental group; appropriate to increase the proportion added of drug entrapment efficiency can be improved, and the drug / ratio of the carrier is too high, it is difficult to further improve the encapsulation efficiency of. Effects of drug-loaded particles release behavior in PBS / ethanol, 50% of the plasma found NSP / of ATRA drug-loaded particles in vitro release uniform gentle, long duration, in sustained release manner NSP / of ATRA the dissolving and diffusion of the drug found Ficks Law, plasma proteins have a significant effect on its release, and there are statistically significant. The The NSP / ATRA.SP / ATRA and free drug ATRA Wister rats in vivo pharmacokinetic experiments results show that in rats, NSP / ATRA can play the role of long-cycle and slow release, both to reduce the side effects of the drug, also can extend the duration of action of the drug; of PLGA non-spherical particles containing drug properties and biological effects, good potential clinical application as a drug carrier.

Preparation of PLGA Non-spherical Particles and the Study of Their Potential as Novel Carriers of All-trans-retinoic Acid

Abstract

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