Anti-PDGF receptor β antibody-conjugated squarticles loaded with minoxidil for alopecia treatment by targeting hair follicles and dermal papilla cells

Nanomedicine. 2015 Aug;11(6):1321-30. doi: 10.1016/j.nano.2015.04.009. Epub 2015 Apr 29.

Abstract

This study developed lipid nanocarriers, called squarticles, conjugated with anti-platelet-derived growth factor (PDGF)-receptor β antibody to determine whether targeted Minoxidil (MXD) delivery to the follicles and dermal papilla cells (DPCs) could be achieved. Squalene and hexadecyl palmitate (HP) were used as the matrix of the squarticles. The PDGF-squarticles showed a mean diameter and zeta potential of 195 nm and -46 mV, respectively. Nanoparticle encapsulation enhanced MXD porcine skin deposition from 0.11 to 0.23 μg/mg. The antibody-conjugated nanoparticles ameliorated follicular uptake of MXD by 3-fold compared to that of the control solution in the in vivo mouse model. Both vertical and horizontal skin sections exhibited a wide distribution of nanoparticles in the follicles, epidermis, and deeper skin strata. The encapsulated MXD moderately elicited proliferation of DPCs and vascular endothelial growth factor (VEGF) expression. The active targeting of PDGF-squarticles may be advantageous to improving the limited success of alopecia therapy.

From the clinical editor: Topical use of minoxidil is only one of the very few treatment options for alopecia. Nonetheless, the current delivery method is far from ideal. In this article, the authors developed lipid nanocarriers with anti-platelet-derived growth factor receptor ? antibody to target dermal papilla cells, and showed enhanced uptake of minoxidil.

Keywords: Alopecia; Dermal papilla cells; Hair follicle; Minoxidil; Squarticles.

MeSH terms

  • Alopecia / therapy*
  • Animals
  • Antibodies / immunology*
  • Calorimetry, Differential Scanning
  • Hair Follicle / drug effects*
  • Mice
  • Mice, Nude
  • Microscopy, Atomic Force
  • Microscopy, Electron, Scanning
  • Minoxidil / administration & dosage*
  • Minoxidil / pharmacology
  • Minoxidil / therapeutic use
  • Receptor, Platelet-Derived Growth Factor beta / immunology*
  • Skin / drug effects*

Substances

  • Antibodies
  • Minoxidil
  • Receptor, Platelet-Derived Growth Factor beta