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Archives of Pharmacal Research

, Volume 28, Issue 8, pp 988–994 | Cite as

Multivesicular liposomes for oral delivery of recombinant human epidermal growth factor

  • Hong Li
  • Jun Hee An
  • Jeong-Sook Park
  • Kun Han
Articles Drug Efficacy

Abstract

The purpose of the present study was to prepare multivesicular liposomes with a high drug loading capacity and to investigate its potential applicability in the oral delivery of a peptide, human epidermal growth factor (rhEGF). The multivesicular liposomes containing rhEGF was prepared by a two-step water-in-oil-in-water double emulsification process. The loading efficiency was increased as rhEGF concentration increased from 1 to 5 mg/mL, reaching approximately 60% at 5 mg/mL. Approximately 47% and 35% of rhEGF was released from the multivesicular liposomes within 6 h in simulated intra-gastric fluid (pH 1.2) and intra-intestinal fluid (pH 7.4), respectively. rhEGF-loaded multivesicular liposomes markedly suppressed the enzymatic degradation of the peptide in an incubation with the Caco-2 cell homogenate. However, the transport of rhEGF from the multivesicular liposomes to the basolateral side of Caco-2 cells was two times lower than that of the rhEGF in aqueous solution. The gastric ulcer healing effect of rhEGF-loaded multivesicular liposomes was significantly enhanced compared with that of rhEGF in aqueous solution; the healing effect of the liposomes was comparable to that of the cimetidine in rats. Collectively, these results indicate that rhEGF-loaded multivesicular liposomes may be used as a new strategy for the development of an oral delivery system in the treatment of peptic ulcer diseases.

Key words

rhEGF Multivesicular liposomes Loading efficiency Oral delivery Peptide 

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Copyright information

© The Pharmaceutical Society of Korea 2005

Authors and Affiliations

  • Hong Li
    • 1
  • Jun Hee An
    • 1
  • Jeong-Sook Park
    • 1
  • Kun Han
    • 1
  1. 1.College of PharmacyChungbuk National UniversityCheongju, ChungbukKorea

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