Lecithin-based microemulsion of a peptide for oral administration: Preparation, characterization, and physical stability of the formulation

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Cilek A., Celebi N., Tirnaksiz F. F.

DRUG DELIVERY, cilt.13, sa.1, ss.19-24, 2006 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 13 Sayı: 1
  • Basım Tarihi: 2006
  • Doi Numarası: 10.1080/10717540500313109
  • Dergi Adı: DRUG DELIVERY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.19-24
  • Anahtar Kelimeler: lecithin purity, microemulsion, phase diagrams, soybean lecithin, stability, TERNARY PHASE-DIAGRAMS, PHOSPHOLIPID MICROEMULSIONS, ISOPROPYL MYRISTATE, DRUG-DELIVERY, SYSTEMS, OIL, ALCOHOL, ABSORPTION, VISCOSITY, ESTERS
  • Gazi Üniversitesi Adresli: Evet

Özet

The objective of our study was to prepare and characterize a stable microemulsion formulation for oral administration of a peptide, e. g., rh-insulin. The microemulsions were prepared using Labrafil M 1944 CS, Phospholipon 90G (lecithin), absolute alcohol, and bidistilled water. Commercially available soybean lecithins (namely, Phospholipon 80, phosphatidylcholine purity 76 +/- 3%, and Phospholipon 90G, phosphatidylcholine purity 93 +/- 3%) were used in the study. The results showed that the phase diagram obtained using a low purity lecithin was not similar to that obtained with a high purity lecithin. We observed that the microemulsion area was wider at the phase diagram obtained with the higher purity lecithin. We found that the extent of the microemulsion region depended upon both the purity of the lecithin and the surfactant/co-surfactant (s/co-s) mixing ratios (K-m). The rheological studies showed that microemulsions followed a Newtonian behavior. Such physical characteristics as viscosity, turbidity, density, conductivity, refractive index, droplet size, physical appearance, and phase separation of the microemulsion were measured at different temperatures (4 degrees C, 25 degrees C, and 40 degrees C) during 6 months. The results indicated that the physical characteristics of the developed microemulsions did not change under different storage temperatures (p > 0.05).