Sponge like microparticles for drug delivery and cosmeto-textile use: Formulation and human skin penetration

Int J Pharm. 2017 Oct 30;532(1):623-634. doi: 10.1016/j.ijpharm.2017.08.122. Epub 2017 Sep 1.

Abstract

This unique work is targeted to achieve three main goals: i) to enhance the aqueous solubility of three specifically selected hydrophobic active agents, ii) to prepare such polymeric biodegradable microparticles which can encapsulate actives-cyclodextrin complexes and iii) to functionalize a polyamide base textile with active loaded microparticles and active-cyclodextrin loaded microparticles. To achieve this objective, biodegradable cationic microparticles were prepared via double emulsion solvent evaporation process and were loaded with hydroxypropyl-beta-cyclodextrin based complexes of Indomethacin, α-tocopheroland Lauryl Isoquinolinium Bromide during the formulation process. Inclusion complex based particles were evaluated for their morphology, size distribution, zeta potential, skin penetration aptitude and adsorption onto a selected textile. It was observed that active-cyclodextrin complex encapsulation do not affect the morphology, size and zeta potential of the microparticles as well as adsorption of the microparticles onto textile remains unaltered. However such active-cyclodextrin complex encapsulated particles provided the enhancement in the aqueous solubility of hydrophobic agents and also provided prolonged release formulations.

Keywords: Anti-hair growth; Anti-inflammation; Antioxidant; Cosmetology; Double emulsion-solvent evaporation; Eudragit(®) RS100; Hydroxypropyl-beta-cyclodextrin (HPβCD); Indomethacin (IMC); Lauryl Isoquinolinium Bromide (LIB); Zeta CAD; α-tocopherol (Vit. E).

MeSH terms

  • 2-Hydroxypropyl-beta-cyclodextrin
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Drug Delivery Systems*
  • Humans
  • Particle Size
  • Skin Absorption*
  • Solubility
  • Textiles*
  • beta-Cyclodextrins

Substances

  • Delayed-Action Preparations
  • beta-Cyclodextrins
  • 2-Hydroxypropyl-beta-cyclodextrin