Release kinetics of hydrophobic and hydrophilic model drugs from pluronic F127/poly(lactic acid) nanoparticles

J Control Release. 2005 Mar 2;103(1):73-82. doi: 10.1016/j.jconrel.2004.11.018. Epub 2004 Dec 20.

Abstract

Poly(lactic acid) (PLA) was successfully grafted to both ends of Pluronic F127 block copolymers (PEO-PPO-PEO) to obtain amphiphilic PLA-F127-PLA block copolymers. The block composition and structure of PLA-F127-PLA block copolymers were studied by nuclear magnetic resonance (NMR), gel permeation chromatography (GPC), differential scanning calorimetric (DSC) and wide angle X-ray diffraction (WXRD) techniques. Data from DSC and WXRD measurements indicated that Tg and Tm of PLA blocks in PLA-F127-PLA block polymers are lower than those of PLA homopolymer. Furthermore, Tm and crystallinity of PLA blocks decrease with decreasing PLA block length in PLA-F127-PLA block copolymers. The release behaviors of both hydrophobic 9-(methylaminomethyl)anthracene (MAMA) and hydrophilic procaine hydrochloride (PrHy) model drugs from PLA-F127-PLA nanoparticles with vesicular structure in PBS solution at 37 degrees C were examined by UV spectroscopy. The release kinetics of both MAMA and PrHy model drugs from PLA-F127-PLA nanoparticles exhibit burst release characteristics, which are believed to be controlled by concentration gradient resulting from the slow hydrolytic degradation of PLA segments.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Hydrophobic and Hydrophilic Interactions*
  • Lactic Acid / pharmacokinetics*
  • Models, Chemical*
  • Nanostructures*
  • Pharmaceutical Preparations / metabolism*
  • Poloxamer / pharmacokinetics*
  • Polyesters
  • Polymers / pharmacokinetics*

Substances

  • Pharmaceutical Preparations
  • Polyesters
  • Polymers
  • Poloxamer
  • Lactic Acid
  • poly(lactide)