Preparation and in vitro release of Mestinon-poly(lactic acid) nanoparticles

doi:10.3969/j.issn.2095-4344.2013.08.010

Abstract

Abstract:

BACKGROUND: Mestinon has been used for the symptomatic treatment of myasthenia gravis. It is very soluble in water, which may be responsible for the short half-life and poor bioavailability. The high dosing frequency may cause poor patient compliance. It is of great clinical significance to develop a Mestinon sustained release delivery system.
OBJECTIVE: To prepare a Mestinon-poly(lactic acid) nanoparticle and to assess its in vitro release characteristics.
METHODS: Mestinon-poly(lactic acid) nanoparticle was prepared by a double emulsion-solvent evaporation method. Poly(lactic acid) was used as the carrier material. The single factor experiment was carried out to properly formulate Mestinon-poly(lactic acid) nanoparticle. The in vitro release test was investigated by a dialysis method.
RESULTS AND CONCLUSION: The optimized conditions to prepare Mestinon-poly(lactic acid) nanoparticle were listed as follows: Dichloromethane was used as oil phase, the ratio between inner water phase and oil phase was 1:10, the poly(cactic acid) concentration was 6%, the polyvinyl alcohol concentration was 3%, and the amount of Mestinon was 40 mg. Mestinon-poly(lactic acid) nanoparticle prepared under the optimized conditions had an average particle size of 937 nm, an encapsulation efficiency of (67.59±1.46)% and a drug loading rate of (4.31±0.17)%. Mestinon-poly(lactic acid) nanoparticle displayed spherical shape with smooth surface and no aggregation was observed. Compared with free Mestinon, Mestinon-poly(lactic acid) nanoparticle had an initial burst release and subsequently a very slow release. The accumulated release rate of Mestinon-poly(lactic acid) nanoparticle was 57.03% at 72 hours. Mestinon-poly(lactic acid) nanoparticle with the good sustained-release characteristics could be successfully prepared.

Key words: biomaterials, nanobiomaterials, biomaterials and drug release, nanoparticles, Mestinon, poly(lactic acid), in vitro drug release, single factor trial, sustained release, biomaterial photographs-containing paper

CLC Number:

R318

Xu Mei-ling, Yang Lin, Liao Hong, Hu Xue-yuan, Zhang Jing-qing. Preparation and in vitro release of Mestinon-poly(lactic acid) nanoparticles[J]. Chinese Journal of Tissue Engineering Research, 2013, 17(8): 1384-1389.

Figures/Tables 9

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