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The nanostructure of rod-like ascorbyl dipalmitate nanoparticles stabilized by a small amount of DSPE-PEG

  • Ziqiao Chen
  • , Kenjirou Higashi
  • , Ryuhei Shidara
  • , Keisuke Ueda
  • , Takeshi Morita
  • , Waree Limwikrant
  • , Keiji Yamamoto
  • , Kunikazu Moribe
  • Chiba University

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

Previously, we reported the formation of 100–200 nm disk- and tube-like nanoparticles by hydration of L-ascorbyl 2,6-dipalmitate (ASC-DP) and distearoylphosphatidylethanolamine polyethylene glycol 2000 (DSPE-PEG) films prepared at an initial molar ratio of 2:1. This study investigated the feasibility of nanoparticle formation with higher ASC-DP loading. Although particle size distribution determined by dynamic light scattering showed a multimodal pattern including micro-sized particles at a molar ratio of 3:1, the mean particle size gradually decreased with a further increased molar ratio. Homogeneous ca. 240 nm nanoparticles with a unimodal size distribution were obtained at a molar ratio of 10:1. FE-TEM showed that the nanoparticles at a molar ratio of 10:1 were rod-shaped with a diameter of ca. 100 nm and a length of ca. 300 nm. After centrifugation, X-ray analysis of the nanoparticle precipitates showed that these rod-like nanoparticles were composed of a series of lamellar structures with 3.7 nm repeated units. The molar ratio of ASC-DP/DSPE-PEG in the nanoparticle precipitates determined by 1H NMR measurements was 68.8:1. The rod-like nanoparticles should be composed of a core–shell structure, where a small amount of DSPE-PEG covers the lamellar structure of ASC-DP. Further increase in the ASC-DP/DSPE-PEG molar ratio over 33:1 no longer provided nanoparticles. Hence, to prepare a stable ASC-DP nanoparticle suspension, it is necessary to prepare ASC-DP/DSPE-PEG films containing at least 3 mol% DSPE-PEG.

Original languageEnglish
Article number120599
JournalInternational Journal of Pharmaceutics
Volume602
DOIs
Publication statusPublished - 1 Jun 2021

Keywords

  • Ascorbyl dipalmitate
  • DSPE-PEG
  • Lamellar structure
  • Rod-like nanoparticles
  • SAXS

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