Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Preparation of Dexamethasone-21-palmitate Incorporated Lipid Nanosphere: Physical Properties by Varying Components and Ratio of Lipid

팔미틴산덱사메타손이 봉입된 지질나노입자의 제조: 지질종류와 함량에 따른 물리적 특성

  • Jung, Suk-Hyun (Bioactive Molecules Delivery & Control Team, Korea Research Institute of Chemical Technology) ;
  • Lee, Jung-Eun (Bioactive Molecules Delivery & Control Team, Korea Research Institute of Chemical Technology) ;
  • Seong, Ha-Soo (Bioactive Molecules Delivery & Control Team, Korea Research Institute of Chemical Technology) ;
  • Shin, Byung-Cheol (Bioactive Molecules Delivery & Control Team, Korea Research Institute of Chemical Technology)
  • 정석현 (한국화학연구원 생체분자전달제어팀) ;
  • 이정은 (한국화학연구원 생체분자전달제어팀) ;
  • 성하수 (한국화학연구원 생체분자전달제어팀) ;
  • 신병철 (한국화학연구원 생체분자전달제어팀)
  • Published : 2006.12.21
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Abstract

Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.

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References

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