The use of nano polymeric self-assemblies based on novel amphiphilic polymers for oral hydrophobic drug delivery

Clare Hoskins, Paul Kong Thoo Lin, Laurence Tetley, Woei Ping Cheng

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Purpose
To investigate the use of nano self-assemblies formed by polyallylamine (PAA) modified with 5 or 10% mole fluorenylmethoxy carbonyl (Fmoc5/10), dimethylamino-1-naphthalenesulfonyl (Dansyl5/10) and 5% mole cholesteryl group (Ch5) for oral hydrophobic drug delivery.

Methods
Propofol, griseofulvin and prednisolone were loaded into amphiphilic PAAs. Particle size and morphology of drug-loaded self-assemblies were determined using photon correlation spectroscopy and transmission electron microscopy. Solubilising capacity, in vitro drug release and formulation stability were analysed by HPLC, and in vitro biocompatibility studies (haemolysis and cytotoxicity) were carried out on bovine erythrocytes and Caco-2 cells, respectively. Dansyl10 and Ch5 griseofulvin formulations were administered intra-gastrically to rats, and drug plasma levels were analysed by HPLC.

Results
Drug-encapsulated self-assemblies typically have hydrodynamic size of 300–400 nm. Dansyl10 exhibited universal drug solubiliser property and had significantly improved prednisolone, griseofulvin and propofol solubility by 145, 557 and 224-fold, respectively. Fmoc polymers resulted in modest drug solubility improvement. These polymers were non-haemolytic, did not enhance cytotoxicity compared to unmodified PAA, and demonstrated significant increase in griseofulvin plasma concentration compared to griseofulvin in water after oral administration.

Conclusions
Ch5 and Dansyl10 showed promising potential as nano-carriers for oral hydrophobic drug delivery.
Original languageEnglish
Pages (from-to)782–794
Number of pages13
JournalPharmaceutical Research
Volume29
Issue number3
Early online date5 Oct 2011
DOIs
Publication statusPublished - 31 Mar 2012

Keywords

  • amphiphilic polymer
  • hydrophobic drug
  • nano polymeric self-assemblies
  • oral delivery
  • solubiliser

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